Drug Communities - di Bernardo Lab

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					DRUG COMMUNITIES
                                                                      Biochemica      CB
                                                                           l      Therapeuti Therapeuti                             Pharmacol
Community                 Members             ATC-Codes   D-Targets
                                                                      Interaction      c       c Uses
                                                                                                                       MOA
                                                                                                                                       ogy
                                                                           s      Indications
                                                                                       Herpes
            2-deoxy-D-glucose                                                                       anti-viral
                                                                                      Genitalis

                                                                        acts as an
                                                                       inhibitor of
            arachidonyltrifluoromethane                               proteins with
                                                                      phospholipas
                                                                      e A2 activity

                                          C
                                          0                             acts as an
                                          4                            inhibitor of
            fasudil                       A                           proteins with
                                          X                               kinase
                                          3                              activity
                                          2
                                                                                                                     Novobiocin
                                                                                                                         is an       Novobiocin
                                                                                                                   aminocouma             is an
                                                                                                                          rin.      aminocouma
                                                                                                                   Aminocouma       rin antibiotic
                                                                                                                   rins are very       that was
                                                                                                                        potent      produced by
                                                                                                                    inhibitors of          the
                                                                                                                       bacterial    actinomycet
                                                                                                                    DNA gyrase              e
                                                                                                                   and work by       <i>Strepto
                                                                        acts as an
                                                                                                                   targeting the         myces
                                                                       inhibitor of     Gram-
                                                                                                                   GyrB subunit     niveus</i>.
                                                                      protein DNA      Positive
                                                                                                                        of the       Novobiocin
                                                                         gyrase B      Bacterial
                                                                                                                       enzyme       binds to DNA
                                                                       subunitacts    Infections      anti-
            novobiocin                                    gyrB                                                       involved in     gyrase, and
                                                                          as an         Gram-       bacterial
                                                                                                                        energy           blocks
                                                                       inhibitor of    Negative
                                                                                                                    tranduction.      adenosine
                                                                      protein DNA      Bacterial
                                                                                                                     Novobiocin     triphosphata
                                                                      topoisomera     Infections
                                                                                                                      as well as    se (ATPase)
                                                                           se II
                                                                                                                      the other        activity.
                                                                                                                   aminocouma            Other
                                                                                                                          rin       antibiotics in
                                                                                                                      antibiotics          the
                                                                                                                        act as      aminocouma
                                                                                                                    competitive        rin class

   1
                                                                                                                    inhibitors of       include
                                                                                                                     the ATPase     coumermyci
                                                                                                                       reaction        n A1 and
                                                                                                                   catalysed by      clorobiocin.
                                                                                                                         GyrB.
                                          A
                                          1                             acts as an
                                          6                            inhibitor of
            sodium_phenylbutyrate         A                           proteins with
                                          X                           deacetylase
                                          0                              activity
                                          3
                                                                                                                     Tamoxifen
                                                                                                                        binds to     Tamoxifen
                                                                                                                       estrogen     belongs to a
                                                                                                                      receptors         class of
                                                                                                                         (ER),      drugs called
                                                                                                                     inducing a       selective
                                                                                                                    conformatio       estrogen
                                                                                                                    nal change         receptor
                                                                                                                         in the      modulators
                                                                                                                       receptor.      (SERMs),
                                                                                                                    This results     which have
                                                                       acts as an
                                                                                                                          in a            both
                                                                     antagonist of
                                                                                                                    blockage or      estrogenic
                                                                     proteins with
                                          L                                                                           change in           and
                                                                        estrogen
                                          0                                                                                the      antiestrogeni
                                                                        receptor
                                          2               ABCB1                                                      expression       c effects.
                                                                      activityacts      Breast      hormone
            tamoxifen                     B               ECGF1 ESR1                                                                 Tamoxifen
                                                                          as an       Neoplasms    antagonist       of estrogen
                                          A               EPHX2 ESR2                                                                    has the
                                                                     antagonist of                                   dependent
                                          0                                                                                              same
                                                                         protein                                    genes. The
                                          1                                                                                          nucleus as
                                                                        estrogen                                      prolonged
                                                                                                                      binding of    diethylstilbe
                                                                      receptor 2
                                                                                                                   tamoxifen to       strol but
                                                                       (ER beta)
                                                                                                                    the nuclear     possesses an
                                                                                                                   chromatin of      additional
                                                                                                                   these results     side chain
                                                                                                                     in reduced     (<i>trans</i
                                                                                                                          DNA        > isomer)
                                                                                                                    polymerase           which
                                                                                                                        activity,   accounts for
                                                                                                                       impaired            its
                                                                                                                      thymidine     antiestrogeni
                                                                                                                     utilization,    c activity.

                                                                                                       anti-        blockade of
            3-aminobenzamide
                                                                                                   proliferative
            4-hydroxyphenazone
                   C
                   0
                   1                                              cardiovascul
    bucladesine    C
                                                                    ar agent
                   E
                   0
                   4
                                                                                   Probucol
                                                                                    lowers
                                                                                    serum
                                                                                cholesterol
                                                                                       by
                                                                                 increasing
                                                                                      the
                                                                                  fractional
                                                                               rate of low-
                                                                                    density
                                                                                lipoprotein Probucol is a
2                                                                                    (LDL)
                                                                                catabolism
                                                                                               powerful
                                                                                             antioxidant
                   C                                                            in the final     drug
                   1                                                             metabolic     normally
                                                                  anti-oxidant
                   0                                                           pathway for      used to
                                                     Hypercholest     anti-
    probucol       A                                                                           prevent
                                                       erolemia   hyperlipidem cholesterol
                   X                                                                           vascular
                                                                       ic       elimination
                   0                                                                            disease
                                                                                  from the
                   2                                                                          caused by
                                                                                     body.
                                                                               Additionally,   the free
                                                                                   probucol  radicals in
                                                                               may inhibit    the body.
                                                                               early stages
                                                                                       of
                                                                                cholesterol
                                                                               biosynthesis
                                                                               and slightly
                                                                                    inhibit
                                                                                    dietary
                                                                                cholesterol
                                                                               absorption.
    5109870                                                                         Recent
    5182598
    5211181
    5248896
    5255229
    5279552
                                                                                  The precise
                                                                                  mechanism
                                                                                                  Apomorphin
                                                                                  of action of
                                                                                                  e is a type of
                                                                                 apomorphin
                                                                                                  dopaminergi
                                                                                      e as a
                                                                                                   c agonist, a
                                                                                   treatment
                                                                                                     morphine
                                                                                        for
                                                                                                    derivative
                                                                                  Parkinson's
                                                                                                       which
                                                                                   disease is
                                                                                                     primarily
                                                                                   unknown,
                                                                                                    affects the
                                                                                 although it is
                                                                                                  hypothalami
                                                                                  believed to
                                                                                                    c region of
                                                                                   be due to
                   G   N                                                                            the brain.
                                                                                  stimulation
                   0   0                acts as an                                                     Drugs
                           DRD2 DRD1                                                 of post-
                   4   4                agonist of                                                  containing
                           DRD4 DRD3                  Parkinson                     synaptic
    apomorphine    B   B                 protein                     emetic                             this
                           DRD5                        Disease                     dopamine
                   E   C                dopamine                                                    substance
                           DRD1IP                                                   D2-type
                   0   0               receptor D2                                                      are
                   7   7
                                                                                   receptors
                                                                                                   sometimes
                                                                                   within the
                                                                                                   used in the
                                                                                      brain.
                                                                                                  treatment of
                                                                                 Apomorphin
                                                                                                   Parkinson's
                                                                                  e has been
                                                                                                    disease or
                                                                                    shown to
                                                                                                      erectile
                                                                                    improve
                                                                                                  dysfunction.
                                                                                      motor
                                                                                                     In higher
                                                                                  function in
                                                                                                   doses it is a
                                                                                   an animal
                                                                                                       highly
                                                                                    model of
                                                                                                     effective
                                                                                  Parkinson's
                                                                                                      emetic.
                                                                                  disease. In
                                                                                   particular,
    blebbistatin                                                                 apomorphin
                                                                                    Unlike       Ciclopirox is
                                                                                antifungals         a broad-
                                                                                   such as         spectrum
                                                                               itraconazole       antifungal
                                                                                     and          medication
                                                                                terbinafine,    that also has
                                                                               which affect      antibacterial
                                                                                    sterol         and anti-
                                                                                 synthesis,      inflammator
                                                                               ciclopirox is    y properties.
                                                                                 thought to         Its main
                                                                                act through         mode of
                                                                              the chelation         action is
                   D   G                                                      of polyvalent       thought to
                   0   0                                                            metal         be its high
                   1   1   ALOX15
                                                                              cations, such       affinity for
    ciclopirox     A   A   PTGS1                   Mycoses      anti-fungal
                                                                                      as            trivalent
                   E   X   PTGS2
                                                                               Fe<sup>3+            cations,
                   1   1
                   4   2
                                                                               </sup> and       which inhibit
                                                                                Al<sup>3+       essential co-
                                                                                  </sup>.          factors in
                                                                                    These          enzymes.
                                                                                   cations         Ciclopirox
                                                                              inhibit many          exhibits
                                                                                  enzymes,            either
                                                                                  including     fungistatic or
                                                                              cytochromes          fungicidal
                                                                                    , thus         activity in
                                                                                 disrupting     vitro against
                                                                                   cellular         a broad
                                                                                  activities     spectrum of
                                                                                   such as           fungal
                                                                              mitochondria        organisms,
                                      acts as an
                                     activator of
                                    proteins with Hypertensio
    colforsin                                                   vasodilator
                                      adenylate       n
                                       cyclase
                                       activity
                                                                              Deferoxamin       Deferoxamin
                                                                                 e works in     e, otherwise
                                                                              treating iron        known as
                                                                                 toxicity by    desferrioxam
                                                                                    binding          ine or
                                                                                   trivalent    desferal, is a
                                                                                (ferric) iron      chelating
                                                                               (for which it     agent used
                                                                              has a strong        to remove
                                                                                   affinity),    excess iron
                                                                                   forming      or aluminum
                                                                              ferrioxamine         from the
                                                                                  , a stable    body. It acts
                   V                                                               complex        by binding
                   0                                                               which is      free iron or
                   3
                                                                                 eliminated     aluminum in
    deferoxamine   A
                                                                                    via the            the
                   C
                                                                              kidneys. 100      bloodstream
                   0
                   1
                                                                                     mg of            and
                                                                              deferoxamin         enhancing
                                                                               e is capable             its
                                                                                 of binding      elimination
                                                                              approximate       in the urine.
                                                                               ly 8.5 mg of     By removing
                                                                                   trivalent     excess iron
                                                                              (ferric) iron.            or
                                                                              Deferoxamin         aluminum,
                                                                                 e works in       the agent
                                                                                   treating      reduces the
                                                                                 aluminum           damage
                                                                                 toxicity by        done to
                                                                                 binding to         various
                                                                              tissue-bound       organs and




3
                                                                                               Etoposide is
                                                                                                      an
                                                                                               antineoplasti
                                                                                               c agent and
                                                                                                      an
                                                                                Etoposide      epipodophyll
                                                                              inhibits DNA        otoxin (a
                                                                              topoisomera      semisyntheti
                                                                                   se II,       c derivative
                                                                                 thereby            of the
                                                                                inhibiting     podophylloto
                                                                                   DNA            xins). It
                                                                              synthesis at     inhibits DNA
                  L                                                                 the        topoisomera
                  0                acts as an
                                                                               premitotic           se II,
                  1               inhibitor of
                      TOP2A                                       anti-       stage of cell        thereby
    etoposide     C              protein DNA      Neoplasms
                      MAP2K7                                    neoplastic       division.       inhibiting
                  B              topoisomera
                                                                              Etoposide is           DNA
                  0                   se II
                  1                                                             cell cycle       synthesis.
                                                                               dependent       Etoposide is
                                                                               and phase          cell cycle
                                                                                 specific,      dependent
                                                                                 affecting       and phase
                                                                              mainly the S        specific,
                                                                                  and G2          affecting
                                                                                phases of      mainly the S
                                                                              cell division.       and G2
                                                                                               phases. Two
                                                                                                  different
                                                                                                    dose-
                                                                                                dependent
3                                                                           Guaifenesin
                                                                                                 responses
                                                                                               are seen. At
                                                                                                Guaifenesin
                                                                            may act as               is an
                                                                           an irritant to       expectorant
                                                                           gastric vagal             which
                                                                             receptors,           increases
                                                                            and recruit        the output of
                                                                               efferent             phlegm
                                                                           parasympath            (sputum)
                                                                           etic reflexes              and
                                                                             that cause            bronchial
                                                                              glandular           secretions
                                                                           exocytosis of        by reducing
                                                                                a less         adhesivenes
                  R                                                            viscous               s and
                  0                                                             mucus               surface
                                                                  anti-
                  5                              Xerophthalm
                                                               asthmatic      mixture.         tension. The
    guaifenesin   C                                ia Cough
                                                              expectorant Cough may               increased
                  A                                 Asthma
                                                              anti-tussive        be             flow of less
                  0
                  3
                                                                             provoked.              viscous
                                                                                 This             secretions
                                                                           combination            promotes
                                                                             may flush         ciliary action
                                                                             tenacious,        and changes
                                                                             congealed               a dry,
                                                                           mucopurulen         unproductive
                                                                             t material        cough to one
                                                                                 from           that is more
                                                                             obstructed          productive
                                                                                small              and less
                                                                            airways and        frequent. By
                                                                              lead to a        reducing the
                                                                             temporary         viscosity and
                                                 Schistosomia     anti-    improvemen          adhesivenes
    hycanthone
                                                      sis       parasitic
                                   acts as an
                                  inhibitor of
    kaempferol                      protein
                                 topoisomera
                                  se (DNA) I
                                                                  anti-
                                                  Neoplasms inflammator
                      LDOX HCK
    quercetin                                    Inflammatio yvitamin anti-
                      PIK3CG
                                                      n       neoplastic
                                                               flavonoid
                                                                                     Resveratrol,
                                                                                             a
                                                                                     phytoalexin,
                                                                                        has been
                                                                                        found to
                                                                       Resveratrol
                               acts as an                                                 inhibit
                                                                        suppresses
                              inhibitor of                                               herpes
                                                                        NF-kappaB
                                protein                                                  simplex
                                                                      (NF-kappaB)
                             ribonucleotid                                           virus types 1
                                                                       activation in
                              e reductase                                            and 2 (HSV-
                                                                      HSV infected
                                   M1                                                 1 and HSV-
                                                                            cells.
                              polypeptide                                                    2)
                                                                          Reports
                               acts as an                                            replication in
                                                                            have
                              inhibitor of                                               a dose-
                                                                         indicated
                  TTR NQO2      protein                                               dependent,
                                                                         that HSV
                  PTGS1          casein                                                reversible
resveratrol                                                            activates NF-
                  CSNK2A1      kinase 2,                                                manner,
                                                                          kappaB
                  PTGS2 CHS2    alpha 1                                              although this
                                                                           during
                              polypeptide                                             is only one
                                                                        productive
                               acts as an                                             of its many
                                                                      infection and
                              inhibitor of                                           pharmaceuti
                                                                       this may be
                             proteins with                                                  cal
                                                                       an essential
                             prostaglandi                                             properties.
                                                                       aspect of its
                                   n-                                                   In some
                                                                        replication
                             endoperoxid                                                countries
                                                                          scheme
                              e synthase                                             where there
                                                                          [PMID:
                                activity                                                is higher
                                                                        9705914].
                                                                                     consumption
                                                                                      of red wine,
                                                                                           there
                                                                                       appears to
                                                                                       be a lower
                                                                       Triamterene incidence of
                                                                         interferes
                                                                      with sodium
                                                                      reabsorption
                                                                       in the distal   Triamterene,
                                                                      renal tubule      a relatively
                                                                      by inhibiting          weak,
                                                                           sodium       potassium-
                                                                         transport          sparing
                                                                      mechanisms       distal tubule
                                                                          directly.    diuretic and
                                                                        Specifically   antihyperten
                                                                         it inhibits   sive, is used
              C                                                              the             in the
              0                                                       Na<sup>+<
                  SCNN1G                                                               managemen
              3
                  SCNN1A                               diuretic anti- /sup>/K<su              t of
triamterene   D                              Malaria
                  SCNN1B                                 malarial     p>+</sup>/       hypokalemia
              B
                  SCNN1D                                                2Cl<sup>-               .
              0
              2
                                                                       </sup> co-      Triamterene
                                                                      transporter.      is similar in
                                                                      The result is        action to
                                                                      an electrical-      amiloride
                                                                          potential      but, unlike
                                                                         difference      amiloride,
                                                                        across the        increases
                                                                        membrane        the urinary
                                                                        that blocks    excretion of
                                                                       the passive     magnesium.
                                                                            distal
                                                                           tubular
                                                                       secretion of
                                                                        potassium.
                                                                        Relative to
                                                                            Trifluridine   Trifluridine is
                                                                            interferes     a fluorinated
                                                                             with DNA        pyrimidine
                                                                           synthesis in      nucleoside
                                                                              cultured     with in vitro
                                                                           mammalian        and in vivo
                                                                                cells.         activity
                                                                            Trifluridine       against
                                                                           presumably          herpes
                                                                                stops          simplex
                                                                          replication of    virus, types
                                                                           herpes viral    1 and 2 and
                                                                             DNA in 3      vacciniavirus
                 S                                                           ways: 1)          . Some
                 0                                                         competitive        strains of
                 1                                                         inhibition of    adenovirus
                     UL30 TK
trifluridine     A
                     TYMS                                                    viral DNA         are also
                 D
                                                                          polymerase,       inhibited in
                 0
                                                                                  2)            vitro.
                 2
                                                                           incorporatio    Trifluridine is
                                                                            n into and           also
                                                                           termination      effective in
                                                                               of the             the
                                                                          growing viral    treatment of
                                                                            DNA chain,        epithelial
                                                                               and 3)      keratitis that
                                                                           inactivation        has not
                                                                            of the viral     responded
                                                                                DNA         clinically to
                                                                          polymerase.        the topical
                                                                            Trifluridine   administrati
                                                                           targets HSV           on of
5114445                                                                      and VSV        idoxuridine
5286656
                 P               acts as an
                 0              inhibitor of
                 1                protein
artemisinin      B             dihydroorota    Malaria    anti-malarial
                 E                   te
                 0             dehydrogena
                 1                   se
                                 acts as an
                                inhibitor of
                               proteins with
                               cholinesteras
                                 e activity
                                 acts as an                  anti-            Not              Not
berberine            qacR                    Arrhythmia
                                 agonist of               arrhythmic        Available        Available
                               proteins with
                                  alpha2-
                                adrenergic
                                  receptor
                                   activity
                 N
                 0
                 5
bromperidol      A
                 D
                 0
                 6
butacaine                                                  anesthetic
canrenoic_acid
                                                                          Carbamazepi
                                                                            ne inhibits
                                                                                         Carbamazepi
                                                                            sustained
                                                                                               ne, an
                                                                            repetitive
                                                                                         anticonvulsa
                                                                             firing by
                                                                                                  nt
                                                                          blocking use-
                                                                                          structurally
                                                                            dependent
                                                                                            similar to
                                                                              sodium
                                                                                              tricyclic
                                                                            channels.
                                                                                         antidepressa
                                                                          Pain relief is
                                                                                          nts, is used
                                                                           believed to
                                                                                              to treat
                                                                                 be
                                                                                               partial
                                                                            associated
                 N                                                                           seizures,
                                                                                with
                 0                                                                        tonic-clonic
                                                                           blockade of
                 3                                                                           seizures,
                                                              anti-          synaptic
carbamazepine    A   SCN5A                     Seizures                                       pain of
                                                           convulsant     transmission
                 F                                                                         neurologic
                                                                               in the
                 0                                                                        origin such
                 1
                                                                            trigeminal
                                                                                         as trigeminal
                                                                          nucleus and
                                                                                           neuralgia,
                                                                              seizure
                                                                                                 and
                                                                           control with
                                                                                          psychiatric
                                                                          reduction of
                                                                                            disorders
                                                                          post-tetanic
                                                                                            including
                                                                          potentiation
                                                                                              manic-
                                                                           of synaptic
                                                                                          depressive
                                                                          transmission
                                                                                           illness and
                                                                          in the spinal
                                                                                          aggression
                                                                                cord.
                                                                                               due to
                                                                          Carbamazepi
                                                                                           dementia.
                                                                              ne also
                                                                            possesses
                                                                          anticholinerg
                                                                                     Decitabine is
                                                                                      believed to
                                                                                        exert its
                                                                                     antineoplasti
                                                                                        c effects
                                                                                           after
                                                                                     phosphorylat
                                                                                         ion and
                                                                                          direct
                                                                                     incorporatio
                                                                                      n into DNA      Decitabine is
                                                                                           and        an analogue
                                                                                     inhibition of       of the
                                                                                           DNA          natural
                                                                                     methyltransf      nucleoside
                                                                                          erase,        2    -
    decitabine               DNMT1
                                                                                         causing      deoxycytidin
                                                                                     hypomethyla          e. It
                                                                                      tion of DNA     functions in
                                                                                      and cellular     the same
                                                                                     differentiatio    way as 5-
                                                                                           n or       Azacytidine.
                                                                                       apoptosis.
                                                                                       Decitabine
                                                                                     inhibits DNA
                                                                                     methylation
                                                                                        in vitro,
                                                                                        which is
                                                                                      achieved at
                                                                                     concentratio
                                                                                       ns that do
                                                                                       not cause
                                                                                          major
                                            acts as an
                                           inhibitor of
    depudecin                             proteins with
                                          deacetylase
                                             activity
                                                                                            As a      Hydroflumet
                                                                                         diuretic,    hiazide is an
                                                                                     Hydroflumet      oral thiazide
                                                                                          hiazide     used to treat
                                                                                         inhibits     hypertension
                                                                                          active       and edema.
                                                                                         chloride       High blood
4                                                                                    reabsorption
                                                                                      at the early
                                                                                                         pressure
                                                                                                       adds to the
                                                                                     distal tubule     workload of
                                                                                     via the Na-Cl       the heart
                                                                                     cotransporte     and arteries.
                                                                                       r, resulting          If it
                         C                                                                 in an      continues for
                         0                                                             increase in     a long time,
                             SLC12A1
                         3
                             ATP1A1 CA4                               diuretic anti-        the          the heart
    hydroflumethiazide   A
                             KCNMA1                                   hypertensive excretion of        and arteries
                         A
                             CA2 CA1                                                     sodium,          may not
                         0
                         2
                                                                                     chloride, and        function
                                                                                          water.         properly.
                                                                                        Thiazides         This can
                                                                                            like       damage the
                                                                                     Hydroflumet            blood
                                                                                      hiazide also      vessels of
                                                                                          inhibit       the brain,
                                                                                       sodium ion       heart, and
                                                                                        transport         kidneys,
                                                                                        across the    resulting in a
                                                                                     renal tubular    stroke, heart
                                                                                       epithelium       failure, or
                                                                                         through           kidney
                                                                                        binding to    failure. High
    ikarugamycin                                                                      the thiazide          blood
    metanephrine
                         C
                         0                                  Angina
                         1                                            anti-anginal
                                                            Pectoris
    molsidomine          D                                                anti-
                                                          Hypertensio
                         X                                            hypertensive
                                                               n
                         1
                         2
                                                                         anti-
    monocrotaline                                         Neoplasms
                                                                       neoplastic
                         C                  acts as an
                         0
                                           activator of
                         2
                                          proteins with Hypertensio    anti-
    pinacidil            D
                                           potassium        n       hypertensive
                         G
                         0                   channel
                         1                   activity
                                                 Vitamin B6    Vitamin B6
                                                    is the    (pyridoxine)
                                                  collective   is a water-
                                                 term for a        soluble
                                                  group of   vitamin used
                                               three related        in the
                                                compounds, prophylaxis
                                                 pyridoxine          and
                                                    (PN),     treatment of
                                                  pyridoxal    vitamin B6
                                                  (PL) and      deficiency
                                               pyridoxamin           and
                                                e (PM), and     peripheral
                                                     their     neuropathy
                    PDXP PDXK                  phosphorylat       in those
                    CBS PSAT1                         ed         receiving
pyridoxine
                    ALB                         derivatives,     isoniazid
                    ALDH7A1                    pyridoxine 5'- (isonicotinic
                                                 phosphate           acid
                                                   (PNP),       hydrazide,
                                               pyridoxal 5'-        INH).
                                                 phosphate     Vitamin B6
                                                 (PLP) and       has been
                                               pyridoxamin       found to
                                                     e 5'-          lower
                                                 phosphate     systolic and
                                                   (PMP).         diastolic
                                                Although all        blood
                                                six of these pressure in a
                                                compounds small group
                                                   should      of subjects
                                                 technically         with
quinostatin                                     be referred      essential
syrosingopine
                                                                Thiamine is
                                                                  a vitamin
                                                                     with
                                                                antioxidant,
                                                               erythropoieti
                                                               c, cognition-
                                                                and mood-
                                                                modulatory,
                                               It is thought   antiatheroscl
                                                  that the          erotic,
                                  acts as a                        putative
                                                mechanism
                                  binder of                      ergogenic,
                                                of action of
                                   protein                           and
                                               thiamine on
                A               transketolas                   detoxificatio
                                                endothelial
                1               e (Wernicke-                    n activities.
                                                   cells is
                1                 Korsakoff                       Thiamine
                    TPK1                       related to a
thiamine        D               syndrome)ac
                    SLC19A3                    reduction in       has been
                A                   ts as a
                                               intracellular      found to
                0                 binder of
                                                   protein         protect
                1                  protein
                                               glycation by    against lead-
                                   thiamin                     induced lipid
                                                redirecting
                                pyrophospho                    peroxidation
                                                     the
                                  kinase 1                       in rat liver
                                                 glycolytic
                                                    flux.       and kidney.
                                                                  Thiamine
                                                                 deficiency
                                                                  results in
                                                                  selective
                                                                  neuronal
                                                                   death in
                                                                    animal
                                                               models. The
5140203                                                           neuronal
AG-028671
                                                                            Aminoglutet
                                                                                himide
                                                                            reduces the
                                                                             production
                                                                                of D5-
                                                                           pregnenolon     Aminoglutet
                                                                           e and blocks        himide
                                                                               several      inhibits the
                                                                            other steps      enzymatic
                                                                              in steroid    conversion
                                                                             synthesis,           of
                                                                           including the    cholesterol
                                                                            C-11, C-18,        to D5-
                                                                              and C-21     pregnenolon
                                       acts as an Hyperaldost
                                                                            hydroxylatio   e, resulting
                                      inhibitor of eronismBrea
                                                                             ns and the          in a
aminoglutethimide       CYP19A1      proteins with      st
                                                                            hydroxylatio   decrease in
                                      aromatase     Neoplasms
                                                                            ns required          the
                                        activity      Edema
                                                                                for the      production
                                                                           aromatizatio      of adrenal
                                                                                  n of     glucocorticoi
                                                                             androgens            ds,
                                                                                   to      mineralocort
                                                                             estrogens,        icoids,
                                                                              mediated       estrogens,
                                                                            through the          and
                                                                             binding of    androgens.
                                                                            aminoglutet
                                                                              himide to
                                                                            cytochrome
                                                                                 P-450
                                                                            complexes.
                                                                             A decrease    Azathioprine
                                                                                                  is a
                                                                         Azathioprine
                                                                                            chemothera
                                                                          antagonizes
                                                                                               py drug,
                                                                              purine
                                                                                              now rarely
                                                                          metabolism
                                                                                               used for
                                                                            and may
                                                                                            chemothera
                                                                              inhibit
                                                                                            py but more
                                                                          synthesis of
                                                                                                   for
                                                                           DNA, RNA,
                                                                                           immunosupp
                                                                                and
                                                                                              ression in
                                                                           proteins. It
                                                                                                organ
                                                                            may also
                                                                                           transplantati
                    L   IMPDH1                                              interfere
                                                                                                on and
                    0   IMPDH2                                            with cellular
                                                                                           autoimmune
                    4   GMPS GMPR                             immunosupp metabolism
                                                   Arthritis,                              disease such
azathioprine        A   GMPR2 ADSL                              ressive    and inhibit
                                                  Rheumatoid                                       as
                    X   ADSS                                     agent    mitosis. The
                                                                                             rheumatoid
                    0   AMPD1                                             mechanism
                    1
                                                                                              arthritis or
                        AMPD2                                              of action of
                                                                                            inflammator
                                                                          azathioprine
                                                                                               y bowel
                                                                                 in
                                                                                              disease or
                                                                          rheumatoid
                                                                                               Crohn's
                                                                           arthritis is
                                                                                           disease. It is
                                                                           not known
                                                                                             a pro-drug,
                                                                           but is most
                                                                                            converted in
                                                                         likely related
                                                                                             the body to
                                                                               to its
                                                                                              the active
                                                                         immunosupp
                                                                                           metabolite 6-
                                                                              resive
                                                                                           mercaptopur
                                                                             action.
                                                                                                 ine.
                                                                                           Azathioprine
                                                                                                acts to
                                                                                          By binding        Azlocillin,
                                                                                          to specific       similar to
                                                                                           penicillin-     mezlocillin
                                                                                             binding            and
                                                                                             proteins     piperacillin,
                                                                                              (PBPs)           is an
                                                                                             located     acylampicilli
                                                                                           inside the       n with an
                                                                                        bacterial cell      extended
                                                                                               wall,      spectrum of
                                                                                            azlocillin    activity and
                                                                                         inhibits the      greater in
                                                                                            third and    vitro potency
                J                                                                       last stage of        than the
                0                                                                       bacterial cell       carboxy
                1
                                                                Bacterial     anti-            wall        penicillins.
azlocillin      C                                     pbpA
                                                               Infections   bacterial     synthesis.        Azlocillin
                A
                                                                                         Cell lysis is   demonstrate
                0
                9
                                                                                               then              s
                                                                                        mediated by      antibacterial
                                                                                        bacterial cell        activity
                                                                                               wall         against a
                                                                                            autolytic          broad
                                                                                            enzymes       spectrum of
                                                                                             such as        bacteria,
                                                                                        autolysins; it      including
                                                                                          is possible    <i>Pseudom
                                                                                               that            onas
                                                                                            azlocillin   aeruginosa<
                                                                                           interferes     /i>, and, in
                                                                                             with an       contrast to
                                                                                            autolysin          most
bergenin                                                                                    inhibitor.   cephalospori
                                                                                         Betamethas       Betamethas
                                                                                             one is a      one and its
                                                                                        glucocorticoi      derivatives,
                                                                                           d receptor    betamethaso
                                                                                         agonist. The       ne sodium
                                                                                         antiinflamm        phosphate
                                                                                        atory actions          and
                                                                                                 of      betamethaso
                                                                                         corticosteroi     ne acetate,
                                                                                              ds are     are synthetic
                                                                                           thought to    glucocorticoi
                                                                                             involve      ds. Used for
                                                                                          lipocortins,          its
                A   C   D   D   H   R   R   S   S   SS                                  phospholipas      antiinflamm
                0   0   0   0   0   0   0   0   0   00                                         e A2          atory or
                7   5   7   7   2   1   3   1   1   23
                                                       NR3C1                                inhibitory   immunosupp
betamethasone   E   A   A   X   A   A   B   B   C   BB
                                                       ANXA1                                 proteins        ressive
                A   A   C   C   B   D   A   A   B   AA
                                                                                              which,       properties,
                0   0   0   0   0   0   0   0   0   00
                4   5   1   1   1   6   4   6   4   73
                                                                                             through     betamethaso
                                                                                            inhibition         ne is
                                                                                         arachidonic        combined
                                                                                         acid, control        with a
                                                                                                the      mineralocort
                                                                                         biosynthesis        icoid to
                                                                                                 of          manage
                                                                                         prostaglandi        adrenal
                                                                                              ns and      insufficiency
                                                                                        leukotrienes.      and is used
                                                                                        The immune         in the form
                                                                                            system is           of
                                                                                         suppressed      betamethaso
                                                                                                 by      ne benzoate,
                                                                                         corticosteroi   betamethaso
                                                                        Bisoprolol        Bisoprolol is
                                                                        selectively                a
                                                                           blocks         competitive,
                                                                      catecholami             beta(1)-
                                                                              ne              selective
                                                                       stimulation        (cardioselect
                                                                       of beta(1)-               ive)
                                                                        adrenergic          adrenergic
                                                                       receptors in        antagonist.
                                                                         the heart        Bisoprolol is
                                                                      and vascular        used to treat
                                                                          smooth          hypertension
                                                                      muscle. This                 ,
               C                 acts as an                            results in a       arrhythmias,
               0                                                      reduction of            coronary
                               antagonist of
               7
                   ADRB1           protein   Hypertensio    anti-       heart rate,             heart
bisoprolol     A
                   ADRB2        adrenergic,      n       hypertensive      cardiac            disease,
               B
                                  beta-1-,                                output,           glaucoma,
               0
               7                  receptor                             systolic and         and is also
                                                                          diastolic            used to
                                                                            blood         reduce non-
                                                                         pressure,        fatal cardiac
                                                                      and possibly           events in
                                                                            reflex        patients with
                                                                        orthostatic       heart failure.
                                                                      hypotension.        Activation of
                                                                        Bisoprolol            beta(1)-
                                                                          can also           receptors
                                                                      competitivel            (located
                                                                           y block        mainly in the
                                                                         beta(2)-            heart) by
                                                                        adrenergic         epinephrine
                                                                      responses in
                                                                      In vitro tests         increases
                                                                         demonstrate
                                                                             that the
                                                                          bactericidal       Cefazolin
                                                                            action of     (also known
                                                                         cephalospori     as cefazoline
                                                                           ns results            or
                                                                               from        cephazolin)
                                                                         inhibition of      is a semi-
                                                                             cell wall       synthetic
                                                                           synthesis.     cephalospori
                                                                           By binding           n for
                                                Gram-                      to specific      parenteral
               J                               Positive                    penicillin-     administrati
               0                                                             binding
                                               Bacterial                                  on. Cefazolin
               1
                   ABCC4 ALB                  Infections       anti-         proteins       has broad-
cefazolin      D
                   PON1 pbpA                    Gram-        bacterial        (PBPs)         spectrum
               B
                                               Negative                      located         antibiotic
               0
               4                               Bacterial                   inside the     action due to
                                              Infections                 bacterial cell    inhibition of
                                                                              wall, it    bacterial cell
                                                                          inhibits the          wall
                                                                            third and     synthesis. It
                                                                         last stage of     attains high
                                                                         bacterial cell   serum levels
                                                                                wall           and is
                                                                           synthesis.        excreted
                                                                          Cell lysis is     quickly via
                                                                               then         the urine.
                                                                         mediated by
                                                                         bacterial cell
                                                                                wall
cinchonidine                                   Malaria     anti-malarial    autolytic
                                                                                                            Ciprofloxacin
                                                                                                              is a broad-
                                                                                                               spectrum
                                                                                                             antiinfective
                                                                                                             agent of the
                                                                                                            fluoroquinolo
                                                                                                 The            ne class.
                                                                                            bactericidal    Ciprofloxacin
                                                                                              action of        has <i>in
                                                                                           ciprofloxacin       vitro</i>
                                                  acts as an
                                                                                            results from         activity
                                                 inhibitor of
                                                                                            inhibition of      against a
                                                   protein
                                                                                           the enzymes        wide range
                    S   J   S   S                cytochrome
                                                                                           topoisomera          of gram-
                    0   0   0   0                P45, family
                                                                                             se II (DNA     negative and
                    2   1   1   3   gyrA parC   1, subfamily                  antiseptic
                                                                 Bacterial                  gyrase) and           gram-
    ciprofloxacin   A   M   A   A   ALB TOP2A         A,                        anti-
                                                                Infections                 topoisomera           positive
                    A   A   X   A   acrB        polypeptide                   bacterial
                                                                                           se IV, which     microorganis
                    1   0   1   0                2acts as an
                    5   2   3   7                                                          are required         ms. The
                                                 inhibitor of
                                                                                            for bacterial     mechanism
                                                protein DNA
                                                                                                DNA           of action of
                                                topoisomera
                                                                                             replication,     quinolones,
                                                     se II
                                                                                           transcription       including
                                                                                           , repair, and    ciprofloxacin
                                                                                           recombinatio      , is different
                                                                                                  n.         from that of
                                                                                                                  other
                                                                                                            antimicrobial
                                                                                                             agents such
                                                                                                                as beta-
                                                                                                                lactams,
                                                                                                             macrolides,
    convolamine                                                                                             tetracyclines
                                                                                                             Haloperidol
                                                                                            The precise
                                                                                                                   is a
                                                                                            mechanism
                                                                                                            psychotropic
                                                   acts as a                               whereby the
                                                                                                                  agent
                                                  blocker of                                therapeutic
                                                                                                            indicated for
                                                    protein                                   effects of
                                                                                                                   the
                                                  Potassium                                 haloperidol
                                                                                                            treatment of
                                                channel acts                                       are
                                                                                                            schizophreni
                                                     as an                                 produced is
                                                                                                              a. It also
                                                antagonist of                               not known.
                                                                                                                 exerts
                                                    protein                                Its effect on
                                                                                                            sedative and
                                                  glutamate                                 the central
                                                                                                             antiemetic
                                                  receptor,                                    nervous
                                                                                                                activity.
                    N                           ionotropic, N-                                system is
                                                                                                             Haloperidol
                    0                             methyl D-                                  thought to
                                                                              tranquilizer                   has actions
                    5               DRD2        aspartate 2B                                       be
                                                               Psychotic         anti-                       at all levels
    haloperidol
5
                    A               GRIN2B        acts as an                                 associated
                                                               Disorders       psychotic                         of the
                    D               DRD1        antagonist of                                  with the
                                                                             (neuroleptic)                       central
                    0                               protein                                competitive
                    1
                                                                                                                nervous
                                                  dopamine                                  blockade of
                                                                                                                system-
                                                 receptor D2                               postsynaptic
                                                                                                             primarily at
                                                  acts as an                                 dopamine
                                                                                                             subcortical
                                                antagonist of                              D2 receptors
                                                                                                               levels-as
                                                proteins with                                    in the
                                                                                                              well as on
                                                N-methyl-D-                                 mesolimbic
                                                                                                                multiple
                                                  aspartate                                dopaminergi
                                                                                                                  organ
                                                   selective                                   c system
                                                                                                               systems.
                                                  glutamate                                     and an
                                                                                                             Haloperidol
                                                   receptor                                   increased
                                                                                                             has strong
                                                    activity                                   turnover
                                                                                                            antiadrenerg
                                                                                           rate of brain
                                                                                                                 ic and
                                                                                            dopamine.
                                                                                                                weaker
                                                                                                              peripheral
                                                                           Isocarboxazi    Isocarboxazi
                                                                             d works by      d is a non-
                                                                            irreversibly       selective
                                                                           blocking the       hydrazine
                                                                             action of a    monoamine
                                                                               chemical         oxidase
                                                                              substance          (MAO)
                                                                              known as         inhibitor
                                                                            monoamine      used to treat
                                                                                oxidase     depression.
                                                                           (MAO) in the      In vivo and
                                                                               nervous          in vitro
                                                                               system.          studies
                       N                                                         MAO       demonstrate
                       0                acts as an
                                                                            subtypes A       d inhibition
                       6               inhibitor of
                                                                              and B are       of MAO in
isocarboxazid          A   MAOA MAOB     protein
                                                                             involved in      the brain,
                       F               monoamine
                                                                                  the        heart, and
                       0                oxidase A
                       1
                                                                            metabolism            liver.
                                                                            of serotonin     Depression
                                                                                  and              is a
                                                                            catecholami     complicated
                                                                                   ne       disease that
                                                                           neurotransm       is not fully
                                                                             itters such    understood.
                                                                                   as      It is thought
                                                                           epinephrine,            that
                                                                           norepinephri      depression
                                                                                ne, and         may be
                                                                             dopamine.      linked to an
                                                                           Isocarboxazi    imbalance of
                                                                                d, as a       chemicals
                       H                                                   nonselective       within the
                       0
                       3
levothyroxine_sodium   A
                       A
                       0
                       1
                                                                                            Methocarba
                                                                                              mol is a
                                                                                               central
                                                                                               muscle
                                                                                The         relaxant for
                                                                           mechanism          skeletal
                                                                           of action of       muscles,
                                                                           methocarba      used to treat
                                                                               mol in      spasms. It is
                                                                           humans has       structurally
                                                                             not been        related to
                                                                           established,     guaifenesin.
                                                                           but may be       Methocarba
                       M                                                       due to       mol's exact
                       0                                                                    mechanism
                                                                 muscle       central
                       3
                                                                relaxant      nervous        of causing
methocarbamol          B                              Spasm
                                                              (spasmolytic    system          skeletal
                       A
                                                                    )      depression.         muscle
                       0
                       3                                                     It has no     relaxation is
                                                                           direct action    unknown. It
                                                                               on the      is thought to
                                                                            contractile         work
                                                                           mechanism         centrally,
                                                                            of striated     perhaps by
                                                                           muscle, the        general
                                                                            motor end       depressant
                                                                           plate or the      effects. It
                                                                           nerve fiber.    has no direct
                                                                                              relaxant
                                                                                             effects on
                                                                                              striated
                                                                                              muscle,
                                                                                           nerve fibers,
                                                                                              Minocycline,
                                                                                                 the most
                                                                             Minocycline      lipid soluble
                                                                                 passes          and most
                                                                                 directly           active
                                                                             through the       tetracycline
                                                                             lipid bilayer    antibiotic, is,
                                                                            or passively             like
                                                                                diffuses      doxycycline,
                                                                                through            a long-
                                                                                  porin             acting
                                                                             channels in      tetracycline.
                                                                            the bacterial     Minocycline's
                           A   J                                             membrane.          effects are
                           0   0   rpsD rpsI
                                                                            Tetracyclines       related to
                           1   1   IL1B ALOX5
                                                 Bacterial      anti-              like              the
minocycline                A   A   MMP9 VEGF
                                                Infections    bacterial      minocycline      inhibition of
                           B   A   CASP1
                                                                              bind to the          protein
                           2   0   CASP3
                           3   8                                                   30S          synthesis.
                                                                               ribosomal         Although
                                                                                subunit,      minocycline'
                                                                              preventing         s broader
                                                                             the binding      spectrum of
                                                                              of tRNA to          activity,
                                                                              the mRNA-       compared to
                                                                               ribosome             other
                                                                            complex and       members of
                                                                              interfering       the group,
                                                                            with protein          includes
                                                                               synthesis.          activity
                                                                                                   against
                                                                                              <i>Neisseria
N-acetyl-L-aspartic_acid                                                                      meningitidis
                                                             contraceptiv
noretynodrel
                                                                  e
                           P
                           0
                           2
oxantel                    C
                           C
                           0
                           2
                                                                                               Pivmecillina
                                                                                                   m is a
                                                                                              pivaloyloxym
                                                                                               ethyl ester
                                                                             Pivmecillina
                                                                                                      of
                                                                            m interferes
                                                                                              amdinocillin
                                                                               with the
                                                                                               that is well
                                                                            biosynthesis
                                                                                                absorbed
                                                                                 of the
                           J                                                                    orally, but
                                                                            bacterial cell
                           0                                                                  broken down
                                                                            wall however
                           1                                                                          to
                                                                            its activity is
pivmecillinam              C       pbpA                                                       amdinocillin
                                                                                slightly
                           A                                                                       in the
                           0                                                   different
                                                                                                intestinal
                           8                                                 from that of
                                                                                              mucosa. It is
                                                                                 other
                                                                                                   active
                                                                              penicillins
                                                                                                  against
                                                                                  and
                                                                                                  gram-
                                                                            cephalospori
                                                                                                 negative
                                                                                   ns
                                                                                                organisms
                                                                                              and used as
                                                                                                     for
                                                                                              amdinocillin.
                                                                            Quinidine, a
                                                                              hydantoin
                                                                            anticonvulsa
                                                              Quinidine       nt, is used
                                                                acts on     alone or with
                                                                sodium      phenobarbit
                                                            channels on       al or other
                                                           the neuronal     anticonvulsa
                                                                  cell            nts to
                                                            membrane,           manage
                                                            limiting the     tonic-clonic
                                                              spread of        seizures,
               C                                                seizure     psychomotor
                       SCN5A
               0                                            activity and       seizures,
                       ORM1
               1                                               reducing      neuropathic
                       ABCB1                     anti-
quinidine      B               Arrhythmia                       seizure            pain
                       KCNH2                  arrhythmic
               A                                           propagation.      syndromes
               0       KCNK1
                                                                  The          including
               1       KCNK6
                                                           antiarrhythm         diabetic
                                                              ic actions    neuropathy,
                                                                  are          digitalis-
                                                              mediated          induced
                                                               through           cardiac
                                                              effects on    arrhythmias,
                                                                sodium       and cardiac
                                                            channels in     arrhythmias
                                                               Purkinje       associated
                                                                fibers.        with QT-
                                                                                interval
                                                                            prolongation
                                                                                    .

                                                           Aminoglycosi     Streptomyci
                                                               des like          n is an
                                                            Streptomyci     aminoglycosi
                                                                   n        de antibiotic.
                                                           "irreversibly"   Aminoglycosi
                                                               bind to      des work by
                                                           specific 30S-      binding to
                                                               subunit      the bacterial
                                                           proteins and            30S
                                                             16S rRNA.        ribosomal
                                                            Specifically        subunit,
                                                            Streptomyci         causing
                                                             n binds to      misreading
               A   J                                             four          of t-RNA,
               0   0                                        nucleotides      leaving the
               7   1           Tuberculosis
                                                 anti-     of 16S rRNA        bacterium
streptomycin   A   G   rpsL      Bacterial
                                               bacterial   and a single        unable to
               A   A            Infections
                                                            amino acid        synthesize
               0   0
               4   1
                                                             of protein     proteins vital
                                                             S12. This            to its
                                                             interferes         growth.
                                                                 with       Aminoglycosi
                                                              decoding          des are
                                                             site in the         useful
                                                             vicinity of     primarily in
                                                             nucleotide       infections
                                                            1400 in 16S        involving
                                                           rRNA of 30S          aerobic,
                                                           subunit. This         Gram-
                                                                region         negative
                                                              interacts        bacteria,
                                                              with the          such as
                                                           wobble base      Pseudomona
                                                                                           The precise      Topiramate
                                                                                           mechanism              is an
                                                                                           of action of    anticonvulsa
                                                                                           topiramate       nt indicated
                                                                                               is not            in the
                                                                                             known.        treatment of
                                                                                            However,       epilepsy and
                                                                                          studies have       migraine.
                                                                                           shown that       Topiramate
                                                                                           topiramate        enhances
                                                                                            blocks the          GABA-
                                                                                              action          activated
                                                                                            potentials         chloride
                          N                     acts as an                                   elicited      channels. In
                          0                                                                repetitively       addition,
                                                agonist of
                          3       GABRA1                                                        by a        topiramate
                                                  protein
topiramate                A       SCN1A CA2                      Seizures     cns agent
                                                 Gamma-                                     sustained          inhibits
                          X       CA4 GRIK1
                                               aminobutyric                               depolarizatio      excitatory
                          1
                                               acid receptor                                 n of the      neurotransm
                          1
                                                                                          neurons in a          ission,
                                                                                               time-           through
                                                                                           dependent         actions on
                                                                                             manner,        kainate and
                                                                                          suggesting a           AMPA
                                                                                              state-         receptors.
                                                                                           dependent           There is
                                                                                             sodium           evidence
                                                                                             channel               that
                                                                                             blocking       topiramate
                                                                                              action.            has a
                                                                                           Topiramate          specific
                                                                                                also          effect on
5149715                                                                                     augments            GluR5
5152487
5186223
                          M   M
                          0   0
                          2   1
aceclofenac               A   A
                          A   B
                          2   1
                          5   6
AR-A014418
calycanthine
corticosterone
                          C
                          0
                          2
debrisoquine              C
                          C
                          0
                          4
                          A
                          0
                          3
diphemanil_metilsulfate   A
                          B
                          1
                          5
                                                                                             Estradiol
                                                                                          enters target
                                                                                            cells freely
                                                                                          (e.g., female
                                                                                              organs,
                                                                                              breasts,
                                                                                          hypothalamu
                                                                                           s, pituitary)
                                                                                          and interacts
                                                                                          with a target
                                                                                                             Estradiol,
                                                                                          cell receptor.
                                                                                                           the principal
                                                                                             When the
                                                                                                           intracellular
                                                                                             estrogen
                          G                                                                                   human
                                                                                          receptor has
                          0                                                                                estrogen, is
                                                                                             bound its
                          3                                                                                substantially
                                  ESR1 NR1I2                   Osteoporosis               ligand it can
estradiol                 C                                                                                more active
                                  SHBG ESR2                     Menopause                    enter the
                          A                                                                                   than its
                                                                                            nucleus of
                          0                                                                                metabolites,
                          3
                                                                                            the target
                                                                                                           estrone and
                                                                                             cell, and
                                                                                                             estriol, at
                                                                                             regulate
                                                                                                            the cellular
                                                                                               gene
                                                                                                               level.
                                                                                          transcription
                                                                                           which leads
                                                                                          to formation
                                                                                                 of
                                                                                           messenger
                                                                                             RNA. The
                                                                                               mRNA
                                                                                             interacts
                                                                                                with
                                                                                          ribosomes to
                                                                                              produce
                                                                             The
                                                                       antiinflamm
                                                                      atory effects
                                                                        of etodolac
                                                                        may result
                                                                          from the
                                                                       inhibition of
                                                                       the enzyme
                                                                      cycooxygena
                                                                        se and the
                                   acts as an                                          Etodolac, an
                                                                       subsequent
                                  inhibitor of                                         antiinflamm
                                                                        peripheral
                                     protein                                            atory agent
                                                                       inhibition of
                 M               prostaglandi                                               with
                                                                      prostaglandi
                 0                      n-                                               analgesic
                                                                       n synthesis.
                 1               endoperoxid       Pain        anti-                         and
                     PTGS1                                                    As
    etodolac     A               e synthase 2 Inflammatio inflammator                   antipyretic
                     PTGS2 ALB                                        prostaglandi
                 B               (prostagland       n      yanalgesic                   properties,
                                                                       ns sensitize
                 0                   in G/H                                              is used to
                 8
                                                                             pain
                                    synthase                                                treat
                                                                        receptors,
                                       and                                             osteoarthriti
                                                                            their
                                 cyclooxygen                                           s and control
                                                                         inhibition
                                      ase)                                              acute pain.
                                                                      accounts for
                                                                             the
                                                                        peripheral
                                                                         analgesic
                                                                         effects of
                                                                         etodolac.
                                                                        Antipyresis
                                                                        may occur
                                                                        by central
                                                                      action on the
                                                                      hypothalamu
                                                                       Hexyl caine
                                                                         acts mainly
                                                                       by inhibiting
                                                                            sodium
                                                                                       Hexylcaine is
                                                                             influx
                                                                                       a local ester-
                                                                           through
                                                                                              class
                                                                            voltage
                                                                                        anesthetic.
                                                                             gated
                                                                                              Local
                                                                            sodium
                                                                                        anesthetics
                                                                         channels in
                                                                                          produce a
                                                                       the neuronal
                                                                                           transient
                                                                               cell
                                                                                            block of
                                                                         membrane
                                                                                             nerve
                                                                       of peripheral
                                                                                        conduction
                                                                            nerves.
                                                                                                by
                     SCN5A                                                When the
    hexylcaine                                                                           interfering
                     SCN10A                                                influx of
                                                                                       with sodium
                                                                          sodium is
                                                                                          channels.
                                                                        interrupted,
                                                                                       This effect of
                                                                          an action
                                                                                               the
                                                                           potential
                                                                                         anesthetic
                                                                       cannot arise
                                                                                          interferes
                                                                          and signal
                                                                                           with the
                                                                       conduction is
                                                                                       development
                                                                              thus
                                                                                        of an action
                                                                          inhibited.
                                                                                           potential
                                                                       The receptor
                                                                                         across the
                                                                             site is
                                                                                             nerve.
                                                                         thought to
                                                                       be located at
                                                                               the
                                                                        cytoplasmic
                                                                            (inner)




6
                                           Hydroxyzine      Hydroxyzine,
                                              competes      a piperazine
                                                  with      antihistamin
                                              histamine             e
                                            for binding      structurally
                                                   at         related to
                                           H<sub>1</s         buclizine,
                                                 ub>-          cyclizine,
                                               receptor            and
                                            sites on the    meclizine, is
                                            effector cell   used to treat
                                               surface,      histamine-
                                            resulting in       mediated
                  N                        suppression       pruritus or
                  0                        of histaminic    pruritus due
                  5
                                                edema,        to allergy,
    hydroxyzine   B   HRH1
                                              flare, and     nausea and
                  B
                                           pruritus. The      vomiting,
                  0
                  1
                                               sedative         and, in
                                           properties of    combination

6                                          hydroxyzine
                                           occur at the
                                                                with an
                                                                 opiate
                                             subcortical        agonist,
                                            level of the      anxiolytic
                                                 CNS.             pain.
                                             Secondary      Hydroxyzine
                                           to its central   is also used
                                           anticholinerg          as a
                                             ic actions,    perioperativ
                                           hydroxyzine       e sedative
                                                may be             and
                                            effective as      anxiolytic
                                                   an            and to
                                                            Metformin is
                                            Metformin's
                                                                    an
                                           pharmacolog
                                                            antihypergly
                                                   ic
                                                            cemic agent,
                                           mechanisms
                                                                  which
                                           of action are
                                                               improves
                                               different
                                                                 glucose
                                             from other
                                                             tolerance in
                                              classes of
                                                            patients with
                                                  oral
                                                                 type 2
                                           antihypergly
                                                               diabetes,
                                                 cemic
                                                                lowering
                                                agents.
                                                              both basal
                  A                          Metformin
                                                                   and
                  1                          decreases
                                                            postprandial
                  0            Diabetes         hepatic
                                                                 plasma
    metformin     B   PRKAB1   Mellitus,        glucose
                                                                glucose.
                  A             Type 2      production,
                                                            Metformin is
                  0                          decreases
                  2
                                                                   not
                                              intestinal
                                                              chemically
                                             absorption
                                                                    or
                                            of glucose,
                                                            pharmacolog
                                                  and
                                                            ically related
                                              improves
                                                             to any other
                                                insulin
                                                              classes of
                                             sensitivity
                                                                   oral
                                                   by
                                                            antihypergly
                                             increasing
                                                                  cemic
                                             peripheral
                                                                 agents.
                                                glucose
                                                                  Unlike
                                            uptake and
                                                             sulfonylurea
                                             utilization.
                                                            s, metformin
                                                                does not
                                                                                Naltrexone      Naltrexone,
                                                                               binds to the        a pure
                                                                                 opioid mu          opioid
                                                                                  receptor      antagonist,
                                                                               antagonistic          is a
                                                                              ally, thereby       synthetic
                                                                                preventing      congener of
                                                                              conventional     oxymorphon
                                      acts as an
                                                                                   opiate         e with no
                                    antagonist of
                                                                                  (heroin,          opioid
                                       protein
                                                                                 morphine)         agonist
                                        opioid
                                                                                drugs from      properties.
                                      receptor,
                                                                                binding and     Naltrexone
                N                    kappa 1acts
                                                                                  inducing      is indicated
                0                        as an
                                                                              opioid neural         in the
                7       OPRM1 TNF     agonist of
                                                                                responses.     treatment of
naltrexone      B       OPRK1          protein
                                                                                     The           alcohol
                B       OPRD1           opioid
                                                                                mechanism      dependence
                0                   receptor, mu
                4
                                                                                of action of    and for the
                                     1 acts as an
                                                                                naltrexone      blockade of
                                    antagonist of
                                                                              in alcoholism      the effects
                                       protein
                                                                                    is not             of
                                        opioid
                                                                               understood;     exogenously
                                      receptor,
                                                                                 however,      administered
                                        delta 1
                                                                               involvement       opioids. It
                                                                                    of the        markedly
                                                                               endogenous        attenuates
                                                                                    opioid             or
                                                                                 system is      completely
                                                                                 suggested         blocks,
                                                                              by preclinical     reversibly,
                                                                                    data.             the
                                                                                Naltrexone
                                                                                Prednisone       subjective
                                                                                     is a
                                                                            glucocorticoi
                                                                             d agonist. It
                                                                                   is first
                                                                                               Prednisone,
                                                                             metabolized
                                                                                                 the most
                                                                               in the liver
                                                                                                commonly-
                                                                              to its active
                                                                                                prescribed
                                                                                    form,
                                                                                               corticosteroi
                                                                            prednisolone
                                                                                               d, is used to
                                                                                       .
                                                                                                    treat
                                                                            Prednisolone
                                                                                                  allograft
                                                                              crosses cell
                A   H                                                                            rejection,
                                                                             membranes
                0   0                                                                             asthma,
                                                                                and binds
                7   2                                                anti-                       systemic
                        NR3C1                       Inflammatio                  with high
prednisone      E   A                                           inflammator                         lupus
                        ANXA1                            n                      affinity to
                A   B                                                 y                        erythematos
                                                                                  specific
                0   0                                                                             us, and
                3   7
                                                                             cytoplasmic
                                                                                                many other
                                                                                receptors.
                                                                                               inflammator
                                                                                The result
                                                                                                 y states.
                                                                                 includes
                                                                                                Prednisone
                                                                             inhibition of
                                                                                                  has very
                                                                                leukocyte
                                                                                                     little
                                                                            infiltration at
                                                                                               mineralocort
                                                                                the site of
                                                                                                     icoid
                                                                             inflammatio
                                                                                                  activity.
                                                                                      n,
                                                                             interference
                                                                                   in the
                                                                               function of
                                                                            mediators of
Prestwick-675                                                                inflammator
                                                                                                Tacrine is a
                                                                                               parasympath
                                                                                                 omimetic,
                                                                                                specifically,
                                                                                                a reversible
                                                                                               cholinesteras
                                                                              Tacrine acts      e inhibitor.
                                                                              by elevating        Tacrine is
                                                                              acetylcholine    indicated for
                                                                              concentratio           the
                                                     acts as a                   ns in the     treatment of
                                                    blocker of                    cerebral         mild to
                                                  proteins with                  cortex by        moderate
                      N                               calcium                  slowing the      dementia of
                      0                                                                              the
                                                     channel                  degradation
                      6
                                                  activity acts                       of        Alzheimer's
tacrine               D               ACHE
                                                       as an                  acetylcholine         type.
                      A
                                                   inhibitor of                released by        Tacrine is
                      0
                      1                           proteins with                 still intact     postulated
                                                    potassium                   cholinergic     to exert its
                                                     channel                   neurons. It      therapeutic
                                                      activity                  does so by        effect by
                                                                                reversibly       enhancing
                                                                                  binding        cholinergic
                                                                              acetylcholine       function.
                                                                                  sterase.         This is
                                                                                               accomplishe
                                                                                                     d by
                                                                                                 increasing
                                                                                                     the
                                                                                               concentratio
                                                                                                     n of
tetrahydroalstonine                                                                            acetylcholine
5151277
5162773
5186324
5213008

                                                                              Amrinone is
                                                                                      a         Amrinone is
                                                                              phosphodies        a positive
                                                    acts as an
                                                                                   terase          inotropic
                                                   inhibitor of
                                                                                 inhibitor,     cardiotonic
                                                     protein
                                                                               resulting in           with
                                                  Phosphodies
                      C                                                         increased       vasodilator
                                                   terase acts
                      0                                                         cAMP and        properties,
                                                      as an
                      1                                                       therefore an     phosphodies
                                      PDE4B TNF    inhibitor of    cardiac
amrinone              C                                                        increase in           terase
                                      PDE3A          protein      stimulant
                      E                                                        the calcium        inhibitory
                      0                           ectonucleoti
                                                                                influx like    activity, and
                      1                                 de
                                                                              that caused      the ability to
                                                  pyrophospha
                                                                                 by beta-         stimulate
                                                  tase/phosph
                                                                                  agonists      calcium ion
                                                   odiesterase
                                                                               resulting in      influx into
                                                         3
                                                                                increased       the cardiac
                                                                                 inotropic            cell.
                                                                                   effect.
BAS-012416453
                      A   G   M   M
                      0   0   0   0
                      1   2   1   2
benzydamine           A   C   A   A
                      D   C   X   A
                      0   0   0   0
                      2   3   7   5
                                                                       Buspirone    Buspirone is
                                                                       binds to 5-   used in the
                                                                       HT type 1A treatment of
                                                                        serotonin    generalized
                                                                     receptors on       anxiety
                                                                      presynaptic where it has
                                                                       neurons in    advantages
                                                                       the dorsal     over other
                                                                       raphe and     antianxiety
                             acts as a
                                                                             on          drugs
                               partial
                                                                     postsynaptic because it
                             agonist of
                                                                       neurons in      does not
                             protein 5-
                                                                            the          cause
            N              hydroxytrypt
                                                                      hippocampu       sedation
            0                  amine                    tranquilizer
                                                                          s, thus   (drowsiness)
            5               (serotonin)                     anti-
                                                                        inhibiting and does not
buspirone   B   HTR1A DRD2    receptor     Anxiety       psychotic
                                                                        the firing       cause
            E               1Aacts as a                (neuroleptic)
                                                                      rate of 5-HT- tolerance or
            0                binder of                  anti-anxiety
            1
                                                                       containing      physical
                             protein 5-
                                                                       neurons in dependence.
                           hydroxytrypt
                                                                       the dorsal     Buspirone
                               amine
                                                                          raphe.     differs from
                            (serotonin)
                                                                       Buspirone        typical
                           receptor 1A
                                                                     also binds at benzodiazepi
                                                                       dopamine           ne
                                                                     type 2 (DA2) anxiolytics in
                                                                       receptors,    that it does
                                                                         blocking      not exert
                                                                      presynaptic anticonvulsa
                                                                       dopamine nt or muscle
                                                                       receptors.      relaxant
                                                                       Buspirone      effects. It
            J                                                           increases     also lacks
            0
            1                              Bacterial       anti-
cefapirin   D
                                          Infections     bacterial
            B
            0
            8

                                                                                    Cefotetan is
                                                                                            a
                                                                                   semisyntheti
                                                                                            c
                                                                                    cephamycin
                                                                                      antibiotic
                                                                                         that is
                                                                                   administered
                                                                                    intravenousl
                                                                                           y or
                                                                                   intramuscula
                                                                          The      rly. The drug
            J                                                        bactericidal      is highly
            0
                                                                       action of     resistant to
            1
                                                                       cefotetan        a broad
cefotetan   D
                                                                     results from spectrum of
            C
            0                                                        inhibition of        beta-
            5                                                           cell wall    lactamases
                                                                      synthesis. and is active
                                                                                      against a
                                                                                     wide range
                                                                                        of both
                                                                                     aerobic and
                                                                                      anaerobic
                                                                                         gram-
                                                                                    positive and
                                                                                         gram-
                                                                                       negative
                                                                                   microorganis
                                                                                           ms.
                                                                                          Cinnarizine
                                                                                               is an
                                                                                         antihistamin
                                                                                             e and a
                                                                         Binds to the
                                                                                             calcium
                                                                          Histamine
                                                                                             channel
                                                                         H1 receptor
                                                                                             blocker.
                                                                             and to
                                                                                          Histamines
                                                                          muscarinic
                                                                                            mediate a
                                                                        acetylcholine
                                                                                           number of
                                                                          receptors.
                                                                                            activities
                                                                         Cinnarizine
                                                                                             such as
                                                                         also inhibits
                                                                                          contraction
              N                                                          contractions
                                                                                            of smooth
              0                   acts as an                              of vascular
                                                                                            muscle of
              7       HRH1      antagonist of                               smooth
                                                                                          the airways
cinnarizine   C       CACNA1A      protein                               muscle cells
                                                                                                and
              A       DRD2        histamine                              by blocking
                                                                                         gastrointesti
              0                  receptor H1                                 L type
              2
                                                                                            nal tract,
                                                                            calcium
                                                                                         vasodilatatio
                                                                           channels.
                                                                                            n, cardiac
                                                                         Cinnarizine
                                                                                         stimulation,
                                                                            has also
                                                                                         secretion of
                                                                              been
                                                                                         gastric acid,
                                                                        implicated in
                                                                                         promotion of
                                                                          binding to
                                                                                           interleukin
                                                                          dopamine
                                                                                         release and
                                                                               D2
                                                                                          chemotaxis
                                                                          receptors.
                                                                                                 of
                                                                                          eosinophils
                                                                                            and mast
                                                                                               cells.
                                                                               As a      Competitive
                                                                            diuretic,
                                                                           diazoxide
                                                                             inhibits
                                                                              active      Diazoxide is
                                                                            chloride      a potassium
                                                                        reabsorption         channel
                                                                         at the early       activator,
                                                                        distal tubule    which causes
                                                                        via the Na-Cl          local
                                                                        cotransporte     relaxation in
                                                                          r, resulting        smooth
                                                                              in an        muscle by
              C   V   SLC12A3     acts as an                              increase in      increasing
              0   0                                                            the
                      CA1 CA2    activator of                                              membrane
              2   3
                      CA4       proteins with Hypertensio                excretion of    permeability
diazoxide     D   A                                         vasodilator
                      KCNMA1     potassium        n                         sodium,      to potassium
              A   H
                      ATP1A1       channel                              chloride, and       ions. This
              0   0
              1   1   KCNJ11       activity                                   water.      switches off
                                                                           Thiazides         voltage-
                                                                               like            gated
                                                                           diazoxide      calcium ion
                                                                          also inhibit       channels
                                                                          sodium ion           which
                                                                           transport      inhibits the
                                                                           across the      generation
                                                                        renal tubular     of an action
                                                                          epithelium        potential.
                                                                            through
                                                                           binding to
                                                                         the thiazide
                                                                            sensitive
                                                                            sodium-
                                                                            The precise       Diflunisal is
                                                                            mechanism                a
                                                                                of the       nonsteroidal
                                                                             analgesic         drug with
                                                                             and anti-         analgesic,
                                                                           inflammator             anti-
                                                                            y actions of     inflammator
                                                                            diflunisal is         y and
                                                                            not known.        antipyretic
                                                                            Diflunisal is     properties.
                                                                                   a              It is a
                                       acts as an                          prostaglandi      peripherally-
                                      inhibitor of                         n synthetase       acting non-
                 N                       protein                           inhibitor. In        narcotic
                 0                                               analgesic
                                         acetyl-                              animals,         analgesic
                 2       PTGS1                          Pain        anti-
                                     Coenzyme A                            prostaglandi           drug.
    diflunisal   B       PTGS2 TTR                 Inflammatio inflammator
                                     acetyltransfe                          ns sensitize     Habituation,
                 A       ALB                         n Fever       y anti-
                                         rase 1                               afferent         tolerance
                 1                                                pyretic
                 1                   (acetoacetyl                           nerves and             and
                                     Coenzyme A                              potentiate        addiction
                                        thiolase)                          the action of        have not
                                                                           bradykinin in          been
                                                                              inducing         reported.
                                                                            pain. Since       Diflunisal is
                                                                           prostaglandi              a
                                                                               ns are        difluorophen
                                                                           known to be       yl derivative
                                                                            among the          of salicylic
                                                                           mediators of            acid.
                                                                              pain and        Chemically,
                                                                           inflammatio          diflunisal
                                                                           n, the mode        differs from
                                                                            of action of
                                                                             The exact           aspirin
                                                                                              Droperidol
                                                                              mechanism         produces
                                                                              of action is       marked
                                                                               unknown,      tranquilizatio
                                                                                however,          n and
                                                                               droperidol     sedation. It
                                                                                 causes a         allays
                                                                                   CNS        apprehensio
                                                                              depression          n and
                                                                                     at        provides a
                                                                              subcortical        state of
                                                                             levels of the        mental
                                                                                  brain,      detachment
                 N   N                                                          midbrain,           and
                 0   0                                                             and        indifference
                 1   5
                                                               sedative anti- brainstem            while
    droperidol   A   A   DRD2                       Vomiting
                                                                  emetic         reticular    maintaining
                 X   D
                                                                               formation,       a state of
                 0   0
                 1   8
                                                                                   may            reflex
                                                                              antagonize        alertness.
                                                                              the actions      Droperidol
                                                                              of glutamic     produces an
                                                                              acid within      antiemetic
                                                                                    the          effect as
                                                                             extrapyrami       evidenced
                                                                              dal system,         by the
                                                                              may inhibit     antagonism
                                                                             cathecolami             of
                                                                             ne receptors     apomorphin
                                                                                 and the      e in dogs. It
                                                                              reuptake of      lowers the
                                                                             neurotransm      incidence of
                                                                                iters, has    nausea and




7
                                                                                             Mecamylami
                                                                               Mecamylami         ne is a
                                      acts as an
                                                                                   ne is a    potent, oral
                                    antagonist of
                                                                                 ganglionic  antihyperten
7                                       protein
                                      cholinergic
                                                                                   blocker
                                                                                    which
                                                                                               sive agent
                                                                                             and ganglion
                                       receptor,
                                                                                  prevents   blocker, and
                                       nicotinic,
                                                                                stimulation         is a
                                     alpha 7 acts
                                                                                      of       secondary
                                         as an
                                                                               postsynaptic       amine.
                                    antagonist of
                                                                               receptors by  Mecamylami
                                        protein
                                                                               acetylcholine       ne is
                                      cholinergic
                                                                                  released   indicated for
                   C                   receptor,
                                                                                    from            the
                   0                   nicotinic,
                                                                                presynaptic  managemen
                   2                    beta 2
                                                                                    nerve           t of
    mecamylamine   B   CHRNA2         (neuronal)
                                                                               endings. The   moderately
                   B                  acts as an
                                                                               hypotensive      severe to
                   0                antagonist of
                   1                                                              effect of       severe
                                        protein
                                                                               Mecamylami       essential
                                       Nicotinic
                                                                                    ne is    hypertension
                                    acetylcholine
                                                                               attributed to      and in
                                    receptor acts
                                                                               reduction in   uncomplicat
                                         as an
                                                                               sympathetic    ed cases of
                                    antagonist of
                                                                                    tone,      malignant
                                        protein
                                                                               vasodilation, hypertension
                                      cholinergic
                                                                               and reduced            .
                                       receptor,
                                                                                   cardiac   Mecamylami
                                       nicotinic,
                                                                                output, and   ne reduces
                                        alpha 2
                                                                                is primarily       blood
                                      (neuronal)
                                                                                  postural.   pressure in
                                                                                                   both
                                                                               Melatonin is normotensiv
                                                                                              Melatonin is
                                                                               a derivative a hormone
                                                                                       of       normally
                                                                                tryptophan. produced in
                                                                                 It binds to   the pineal
                                                                                 melatonin     gland and
                                                                                  receptor   released into
                                                                                  type 1A,     the blood.
                                                                                 which then         The
                                                                                   acts on      essential
                                                                                 adenylate amino acid L-
                                                                                cylcase and tryptophan
                                                                                      the           is a
                   N                                                           inhibition of precursor in
                   0                                                                                the
                       MTNR1A                                                      a cAMP
                   5
                       ESR1 BCL2                                  anti-             signal    synthesis of
    melatonin      C                                Neoplasms
                       SNCA CASP3                               neoplastic     transduction melatonin. It
                   H
                       CYCS                                                       pathway.         helps
                   0
                   1                                                             Melatonin      regulate
                                                                                  not only    sleep-wake
                                                                                   inhibits  cycles or the
                                                                                 adenylate      circadian
                                                                               cyclase, but      rhythm.
                                                                                    it also    Production
                                                                                  activates  of melatonin
                                                                               phosphilpase is stimulated
                                                                                   C. This    by darkness
                                                                                potentiates and inhibited
                                                                                the release     by light.
                                                                                       of     High levels
                                                                               arachidonate of melatonin
                                                                                        .    induce sleep
                   R                                                                              and so
                   0
                   5
    noscapine      D                                 Cough      anti-tussive
                   A
                   0
                   7
                                                                          Antiinflamm
                                                                          atory effects
                                                                          of Oxaprozin
                                                                          are believed
                                                                                            Oxaprozin is
                                                                          to be due to
                                                                                                   a
                                                                           inhibition of
                                                                                            nonsteroidal
                                                                          cylooxygena
                                                                                            antiinflamm
                                                                                se in
                                                                                              atory drug
                                                                              platelets
                                                                                               (NSAID)
                                                                           which leads
                                                                                                  with
                                                                               to the
                                       acts as an                                              analgesic
                 M                                                         blockage of
                                      inhibitor of                                                and
                 0                                 Inflammatio            prostaglandi
                                     proteins with                                           antipyretic
                 1                                  n Arthritis,   anti-   n synthesis.
                                     prostaglandi                                            properties.
oxaprozin        A           PTGS2                 Rheumatoid inflammator Antipyretic
                                           n-                                               Oxaprozin is
                 E                                 Osteoarthriti    y      effects may
                 1                   endoperoxid                                            used to treat
                                                         s                   be due to
                 2                    e synthase                                             rheumatoid
                                                                          action on the
                                        activity                                               arthritis,
                                                                          hypothalamu
                                                                                            osteoarthriti
                                                                            s, resulting
                                                                                                   s,
                                                                                in an
                                                                                            dysmenorrh
                                                                             increased
                                                                                              ea, and to
                                                                            peripheral
                                                                                               alleviate
                                                                            blood flow,
                                                                                              moderate
                                                                          vasodilation,
                                                                                                 pain.
                                                                                 and
                                                                           subsequent
                                                                                 heat
                                                                           dissipation.


                                                                                  The
                                                                            antiinflamm
                                                                            atory effect    Piroxicam is
                                                                            of Piroxicam     in a class of
                                                                             may result     drugs called
                                                                               from the     nonsteroidal
                                                                              reversible          anti-
                                                                            inhibition of   inflammator
                                                                            cyclooxygen          y drugs
                                                                            ase, causing      (NSAIDs).
                                                                                   the         Piroxicam
                                                                             peripheral        works by
                                                                            inhibition of       reducing
                 M   M   S                                                  prostaglandi      hormones
                 0   0   0                                                  n synthesis.      that cause
                 1   2   1
                                                  Inflammatio                     The       inflammatio
piroxicam        A   A   B   PTGS1
                                                       n                    prostaglandi    n and pain in
                 C   A   C
                                                                                 ns are        the body.
                 0   0   0
                 1   7   6
                                                                            produced by     Piroxicam is
                                                                             an enzyme           used to
                                                                             called Cox-      reduce the
                                                                            1. Piroxicam          pain,
                                                                             blocks the     inflammatio
                                                                                 Cox-1           n, and
                                                                               enzyme,          stiffness
                                                                               resulting      caused by
                                                                                into the     rheumatoid
                                                                            disruption of   arthritis and
                                                                             production     osteoarthriti
                                                                                    of              s.
                                                                            prostaglandi
                                                                                   ns.
Prestwick-1082                                                                Piroxicam
ricinine
                 D   H
                 1   0
                 1   3
tiratricol       A   A
                 X   A
                 0   0
                 8   4
                                                                                                      The
                                                                                                antiinflamm
                                                                                               atory actions
                                                                                                        of
                                                                                                corticosteroi
                                                                                                     ds are
                                                                                                  thought to
                                                                                                    involve
                                                                                                 lipocortins,
                                                                                               phospholipas
                                                                                                                  Triamcinolon
                                                                                                      e A2
                                                                                                                    e and its
                                                                                                   inhibitory
                                                                                                                   derivatives
                                                                                                    proteins
                A   D   D   H   R   R   S                                                                         are synthetic
                                                                                                     which,
                0   0   0   0   0   0   0                                                                         glucocorticoi
                                                                                                    through
                1   7   7   2   1   3   1                                               anti-                      ds that are
                                            SERPINA6                   Inflammatio              inhibition of
triamcinolone   A   A   X   A   A   B   B                                          inflammator                       used for
                                            ANXA1                           n                   arachidonic
                C   B   B   B   D   A   A                                                y                             their
                                                                                                acid, control
                0   0   0   0   1   0   0                                                                          antiinflamm
                1   9   2   8   1   6   5
                                                                                                       the
                                                                                                                     atory or
                                                                                                biosynthesis
                                                                                                                  immunosupp
                                                                                                        of
                                                                                                                     ressive
                                                                                                prostaglandi
                                                                                                                   properties.
                                                                                                     ns and
                                                                                               leukotrienes.
                                                                                               The immune
                                                                                                   system is
                                                                                                 suppressed
                                                                                                        by
                                                                                                corticosteroi
                                                                                                 ds due to a
                                                                                                decrease in
                                                                                                the function
                                                                                                     of the          In allergic
                                                                                                                   reactions an
                                                                                                                       allergen
                                                                                                                      interacts
                                                                                                                      with and
                                                                                                                    cross-links
                                                                                                                    surface IgE
                                                                                                  Triprolidine      antibodies
                                                                                                 binds to the          on mast
                                                                                                   histamine          cells and
                                                                                                 H1 receptor.        basophils.
                                                                                                  This blocks         Once the
                                                                                                 the action of       mast cell-
                R                                                                                endogenous          antibody-
                0                                        acts as an
                                                                                                   histamine,          antigen
                6                                      antagonist of
                                                                                        anti-         which         complex is
triprolidine    A                           HRH1          protein
                                                                                     histamine   subsequentl         formed, a
                X                                        histamine
                                                                                                   y leads to         complex
                0                                       receptor H1
                7                                                                                  temporary          series of
                                                                                                  relief of the         events
                                                                                                    negative        occurs that
                                                                                                   symptoms         eventually
                                                                                                  brought on      leads to cell-
                                                                                                       by         degranulatio
                                                                                                   histamine.        n and the
                                                                                                                     release of
                                                                                                                     histamine
                                                                                                                    (and other
                                                                                                                      chemical
                                                                                                                    mediators)
                                                                                                                      from the
                                                                                                                   mast cell or
                                                                                                                      basophil.
                                                                              Zidovudine
                                                                                  is a
                                                                              nucleoside
                                                                                reverse
                                                                            transcriptase
                                                                               inhibitor
                                                                             (NRTI) with
                                                            Zidovudine,         activity
                                                            a structural        against
                                                               analog of        Human
                                                             thymidine,      Immunodefi
                                                             inhibits the    ciency Virus
                                                              activity of   Type 1 (HIV-
               J                                                 HIV-1             1).
               0                                                reverse       Zidovudine
               5                                           transcriptase            is
                               Retroviridae
zidovudine     A   gag                        anti-viral   (RT) both by
                                Infections                                  phosphorylat
               F                                              competing      ed to active
               0                                                with the     metabolites
               1                                                natural           that
                                                               substrate     compete for
                                                           dGTP and by       incorporatio
                                                                   its        n into viral
                                                            incorporatio      DNA. They
                                                             n into viral     inhibit the
                                                                 DNA.        HIV reverse
                                                                            transcriptase
                                                                                enzyme
                                                                            competitivel
                                                                            y and act as
                                                                                a chain
                                                                              terminator
6-azathymine                                                                    of DNA
                                                                          Ethambutol
                                                                           is an oral
                                                                         chemothera
                                                                         peutic agent
                                                                            which is
                                                                          specifically
                                                                            effective
                                                                             against
                                                                            actively
                                                                            growing
                                                                         microorganis
                                                                           ms of the
                                                                              genus
               J                                            Ethambutol
                                                                         Mycobacteri
               0                                              inhibits
                                                                               um,
               4                                             arabinosyl
                   embB embA     Bacterial      anti-                      including
ethambutol     A                                           transferases
                   embC         Infections    bacterial                      <i>M.
               K                                            involved in
                                                                         tuberculosis
               0                                              cell wall
               2
                                                                              </i>.
                                                           biosynthesis.
                                                                          Ethambutol
                                                                         inhibits RNA
                                                                           synthesis
                                                                               and
                                                                           decreases
                                                                            tubercle
                                                                              bacilli
                                                                          replication.
                                                                           Nearly all
                                                                           strains of
                                                                             <i>M.
                                                                         tuberculosis
                                                                           </i> and
etifenin                                                                     <i>M.
fusaric_acid
                                                                       Nafcillin is a
                                                                       semisyntheti
                                                                         c antibiotic
                                                                         substance
                                                                       derived from
                                                                          6-amino-
                                                      Penicillinase-
                                                                         penicillanic
                                                         resistant
                                                                          acid. The
                                                        penicillins
                                                                       drugs in this
                                                          exert a
                                                                          class are
                                                       bactericidal
                                                                            highly
                                                           action
                                                                        resistant to
                                                          against
                                                                        inactivation
                                                        penicillin-
                                                                              by
                                                       susceptible
                                                                       staphylococc
                                                      microorganis
                              Bacterial     anti-                             al
    nafcillin         pbpA                              ms during
                             Infections   bacterial                    penicillinase
                                                       the state of
                                                                           and are
                                                           active
                                                                            active
                                                      multiplicatio
                                                                           against
                                                           n. All
                                                                       penicillinase-
                                                        penicillins
                                                                         producing
                                                        inhibit the
                                                                           and non
                                                      biosynthesis
                                                                       penicillinase-
                                                           of the
                                                                         producing
                                                      bacterial cell
                                                                          strains of
                                                            wall.
                                                                       Staphylococc
                                                                         us aureus.
                                                                             The
                                                                       penicillinase-
                                                                          resistant
                                                                          penicillins
                                                       Oxamniquin      are active in
                                                                       Oxamniquin
                                                            e may          e is an
                                                         associates    anthelmintic
                                                           with an           with
                                                        irreversible   schistosomic
                                                       inhibition of    idal activity
                                                        the nucleic        against
                                                             acid      <i>Schistos
                                                       metabolism            oma
                                                            of the      mansoni</i
                                                       parasites. A      >, but not
                                                         hypothesis        against
                                                      has been put           other
                  P                                      forth that    Schistosoma
                  0                                     the drug is          spp.
                  2
                                                      activated by     Oxamniquin
    oxamniquine   B
                                                          a single        e causes
                  A
                                                           step, in       worms to
                  0
                  2
                                                           which a        shift from
                                                      schistosome             the
                                                          enzyme        mesenteric
                                                          converts      veins to the
                                                      oxamniquine       liver where
                                                      into an ester       the male
                                                         (probably       worms are
                                                          acetate,        retained;
                                                        phosphate,       the female
                                                        or sulfate).       worms
                                                      Subsequentl      return to the
                                                       y, the ester     mesentery,
                                                      spontaneous        but can no
                                                              ly            longer
                                                       dissociates,    release egg.




8
                                                                                               Phenacetin
                                                                                             was the first
                                                                                               NSAID and
                                                                                                   fever

8
                                                                                                reducer to
                                                                                                go on the
                                                                                              market. Its
                                                                                                 analgesic
                                                                                               effects are
                                                                                                due to its
                                                                                                actions on
                                                                                              the sensory
                                                                                             tracts of the
                 N                                                                            spinal cord.
                 0                                                                            In addition,
                 2
                                                  Fever                         Not            phenacetin
    phenacetin   B   PTGS1                                    anti-pyretic
                                                 Neuralgia                    Available            has a
                 E
                                                                                               depressant
                 0
                 3
                                                                                             action of the
                                                                                             heart, where
                                                                                               it acts as a
                                                                                                 negative
                                                                                              inotrope. It
                                                                                                    is an
                                                                                              antipyretic,
                                                                                                 acting on
                                                                                              the brain to
                                                                                             decrease the
                                                                                             temperature
                                                                                             set point. It
                                                                                              is also used
                                                                                                  to treat
                                                                                              rheumatoid
                                                                                               Probenecid
                                                                                                     is a
                                                                                                uricosuric
                                                                                                and renal
                                                                                                 tubular
                                                                                                 blocking
                                                                                             agent and is
                                                                                                 used in
                                                                                             combination
                                                                                                    with
                                                                              Probenecid
                                                                                             colchicine to
                                                                              inhibits the
                                                                                             treat chronic
                                                                                 tubular
                                                                                                   gouty
                 M                                                           reabsorption
                                  acts as an                                                     arthritis
                 0                                                              of urate,
                                  inducer of                                                       when
                 4   SLC22A8                                                       thus
                                 proteins with                                               complicated
    probenecid   A   ALB ABCC1                                                 increasing
                                     GABA                                                    by frequent,
                 B   SLC22A11                                                 the urinary
                                   receptor                                                     recurrent
                 0                                                           excretion of
                 1                  activity                                                       acute
                                                                             uric acid and
                                                                                               attacks of
                                                                              decreasing
                                                                                                 gout. It
                                                                             serum urate
                                                                                              inhibits the
                                                                                 levels.
                                                                                                 tubular
                                                                                             reabsorption
                                                                                                of urate,
                                                                                                    thus
                                                                                               increasing
                                                                                              the urinary
                                                                                              excretion of
                                                                                             uric acid and
                                                                                              decreasing
                                                                                             serum urate
                                   acts as a                                                      levels.
                                  blocker of
                                 proteins with
    pronetalol                       beta-
                                  adrenergic
                                   receptor
                                    activity
                 J
                 0
                 1                                Bacterial      anti-
    sisomicin    G
                                                 Infections    bacterial
                 B
                 0
                 8
                                                                                      Sulfonylurea      Tolazamide
                                                                                      s likely bind       is an oral
                                                                                           to ATP-           blood
                                                                                          sensitive         glucose
                                                                                        potassium-         lowering
                                                                                          channel       drug of the
                                                                                      receptors on     sulfonylurea
                                                                                             the             class.
                                                                                         pancreatic     Tolazamide
                                                                                      cell surface,      appears to
                                                                                          reducing        lower the
                                                                                         potassium           blood
                                                                                      conductance           glucose
                                               A                                      and causing        acutely by
                                               1                                      depolarizatio     stimulating
                                               0              Glucose                     n of the      the release
     tolazamide                                B   KCNJ1    Metabolism                 membrane.          of insulin
                                               B             Disorders                Depolarizati         from the
                                               0
                                                                                              on       pancreas, an
                                               5
                                                                                         stimulates          effect
                                                                                        calcium ion      dependent
                                                                                            influx           upon
                                                                                          through       functioning
                                                                                          voltage-      beta cells in
                                                                                          sensitive           the
                                                                                           calcium       pancreatic
                                                                                         channels,       islets. The
                                                                                           raising      mechanism
                                                                                       intracellular       by which
                                                                                      concentratio      tolazamide
                                                                                      ns of calcium    lowers blood
                                                                                        ions, which         glucose
     11-deoxy-16,16-dimethylprostaglandin_E2                                           induces the     during long-
     16-phenyltetranorprostaglandin_E2
9    BCB000038
     CP-944629
     IC-86621
     15(S)-15-methylprostaglandin_E2

10   BCB000039
     BCB000040
     CP-319743
     alpha-ergocryptine
                                                                                            The          Citalopram
                                                                                      antidepressa       is one of a
                                                                                            nt,            class of
                                                                                      antiobsessiv     antidepressa
                                                                                             e-          nts known
                                                                                      compulsive,       as selective
                                                                                            and           serotonin
                                                                                       antibulimic        reuptake
                                                                                        actions of        inhibitors
                                                                                       Citalopram      (SSRIs). It is
                                                                                            are        used to treat
                                                                                      presumed to             the
                                                                                      be linked to       depression
                                               N                                      its inhibition     associated
                                               0                                          of CNS         with mood
                                               6
                                                                            anti-        neuronal       disorders. It
     citalopram                                A   SLC6A4   Depression
                                                                         depressant     uptake of       is also used
                                               B
                                                                                        serotonin.     on occassion
                                               0
                                               4
                                                                                       Citalopram           in the
                                                                                        blocks the     treatment of
11                                                                                     reuptake of
                                                                                      serotonin at
                                                                                                             body
                                                                                                        dysmorphic
                                                                                            the        disorder and
                                                                                        serotonin      anxiety. The
                                                                                         reuptake      antidepressa
                                                                                      pump of the             nt,
                                                                                         neuronal       antiobsessiv
                                                                                       membrane,               e-
                                                                                        enhancing       compulsive,
                                                                                       the actions           and
                                                                                      of serotonin       antibulimic
                                                                                             on           actions of
     CP-320650-01                                                                     5HT<sub>1          Citalopram
     CP-690334-01
                                               C
                                               0
                                               1
     dilazep                                   D
                                               X
                                               1
                                               0
     PHA-00745360
     spiradoline
                                                                                   Bromphenira      Bromphenira
                                                                                    mine works       mine is an
                                                                                    by acting as    antihistamin
                                                                                            an            ergic
                                                                                   antagonist of     medication
                                                                                         the H1          of the
                                                                                      histamine     propylamine
                                                                                   receptors. It    class. It is a
                                                                                           also           first-
                                                                                    functions as     generation
                                                                                             a      antihistamin
                                                                                    moderately      e. In allergic
                                                                                       effective    reactions an
                           R                                                       anticholinger        allergen
                           0                                                           ic agent,       interacts
                           6
                                                                                       likely an       with and
     brompheniramine       A   HRH1
                                                                                   antimuscarin      cross-links
                           B
                                                                                        ic agent     surface IgE
                           0
                           1
                                                                                      similar to     antibodies
                                                                                          other         on mast
                                                                                       common          cells and
                                                                                   antihistamin       basophils.
                                                                                     es such as        Once the
                                                                                   diphenhydra        mast cell-
                                                                                       mine. Its      antibody-
                                                                                      effects on        antigen
                                                                                           the       complex is
                                                                                     cholinergic      formed, a
                                                                                    system may         complex
                                                                                   include side-       series of
                                                                                    effects such         events
                                                                                            as       occurs that
                                                                                    drowsiness,      eventually
                                                                                           The
                                                                                    mechanism
                                                                                     of action is
                                                                                     not known.
                                                                                    Rather than
                                                                                         acting
                                                                                                    Carisoprodol
                                                                                     directly on
                                                                                                    is used as a
                                                                                        skeletal
                                                                                                       skeletal
                           M                                                            muscle,
                                                                                                       muscle
                           0                                                        carisoprodol
                                                                       analgesic                      relaxant.
                           3                                                          interrupts
                                                                        smooth                       One of its
     carisoprodol          B                               Pain                        neuronal
                                                                        muscle                      metabolites,
                           A                                                       communicati
                           0                                           relaxant                     meprobamat
                                                                                   on within the
                           2                                                                             e, is
                                                                                       reticular
                                                                                                    available as
                                                                                      formation
                                                                                                    an anxiolytic
                                                                                      and spinal
                                                                                                        agent.
                                                                                          cord,
12                                                                                   resulting in
                                                                                   sedation and
                                                                                    alteration in
                                                                                          pain
                                                                                    perception.
     Chicago_Sky_Blue_6B
                                                                                          As a        Thiazides
                                                                                       diuretic,        such as
                                                                                   hydrochlorot     hydrochlorot
                                                                                        hiazide         hiazide
                                                                                       inhibits        promote
                                                                                        active        water loss
                                                                                       chloride        from the
                                                                                   reabsorption          body
                                            acts as an                              at the early     (diuretics).
                                           inhibitor of                            distal tubule     They inhibit
                                         proteins with                             via the Na-Cl    Na<sup>+<
                                            carbonate                              cotransporte     /sup>/Cl<su
                                         dehydratase                                 r, resulting    p>-</sup>
                           C              activity acts                                  in an      reabsorption
                           0                                                         increase in       from the
                               SLC12A3         as an
                           3
                               CA1 CA2     inhibitor of Hypertensio diuretic anti-        the            distal
     hydrochlorothiazide   A
                               CA4           protein        n       hypertensive excretion of        convoluted
                           A
                               KCNMA1         solute                                   sodium,        tubules in
                           0
                           3                  carrier                              chloride, and    the kidneys.
                                            family 12                                   water.        Thiazides
                                         (sodium/chlo                                 Thiazides       also cause
                                                ride                                      like          loss of
                                          transporters                             hydrochlorot       potassium
                                         ), member 3                                hiazide also        and an
                                                                                        inhibit      increase in
                                                                                     sodium ion      serum uric
                                                                                      transport          acid.
                                                                                      across the      Thiazides
                                                                                   renal tubular       are often
                                                                                     epithelium     used to treat
                                                                                       through      hypertension
                                                                                      binding to      , but their
                           D                                                        the thiazide    hypotensive
                           1
                           0                             Bacterial       anti-
     meclocycline          A
                                                        Infections     bacterial
                           F
                           0
                           4
                  R
                  0
                  5
oxolamine         D
                  B
                  0
                  7
SR-95639A
                                    acts as an
                                  antagonist of
                                  proteins with
                                      alpha2-
                                    adrenergic
                                     receptor
                                   activity acts
                                   as a partial
                                    agonist of
                                    protein 5-
                                  hydroxytrypt
                                       amine
                                   (serotonin)
                                     receptor
                                  1Aacts as an
                                  antagonist of
alpha-yohimbine
                                      protein
                                   adrenergic,
                                    alpha-2A-,
                                  receptor acts
                                       as an
                                  antagonist of
                                      protein
                                   adrenergic,
                                    alpha-2C-,
                                  receptor acts
                                       as an
                                  antagonist of
                                      protein
                                   adrenergic,
                                    alpha-2B-,
                                  receptor acts
                                       as an                                               Atropine, a
                                                                          Generally,          naturally
                                                                            atropine         occurring
                                                                          lowers the       belladonna
                                                                           "rest and      alkaloid, is a
                                                                             digest"          racemic
                                                                        activity of all     mixture of
                                                                        muscles and        equal parts
                                                                             glands        of d- and l-
                                                                        regulated by      hyoscyamine
                                                                               the            , whose
                                                                        parasympath         activity is
                                                              muscle    etic nervous       due almost
                  A   S            acts as an
                          CHRM2                              relaxant   system. This        entirely to
                  0   0           antagonist of
                          CHRM1                            (spasmolytic      occurs           the levo
                  3   1           proteins with
                          CHRM4                              )smooth        because          isomer of
atropine          B   F            muscarinic      Spasm
                          CHRM5                               muscle    atropine is a        the drug.
                  A   A           acetylcholine
                          CHRM3                              relaxant    competitive        Atropine is
                  0   0             receptor
                  1   1   ACHE                               mydriatic   inhibitor of       commonly
                                     activity
                                                             antidote          the         classified as
                                                                          muscarinic             an
                                                                        acetylcholine     anticholinerg
                                                                           receptors            ic or
                                                                        (acetylcholin     antiparasym
                                                                            e is the          pathetic
                                                                        neurotransm       (parasympat
                                                                        itter used by          holytic)
                                                                               the         drug. More
                                                                        parasympath         precisely,
                                                                        etic nervous       however, it
                                                                           system).       is termed an
                                                                                          antimuscarin
                                                                                              ic agent
                                                      Bupropion         Bupropion,
                                                      selectively             an
                                                     inhibits the     antidepressa
                                                       neuronal           nt of the
                                                     reuptake of      aminoketone
                                                      dopamine,         class and a
                                                    norepinephri      non-nicotine
                                                        ne, and             aid to
                                                      serotonin;          smoking
                                                      actions on      cessation, is
                                                    dopaminergi         chemically
                                                      c systems       unrelated to
                                                       are more           tricyclic,
             N                                        significant       tetracyclic,
             0                                            than            selective
             7
                 SLC6A3                   anti-      imipramine       serotonin re-
bupropion    B            Depression
                 SLC6A2                depressant           or             uptake
             A
                                                    amitriptyline      inhibitor, or
             0
             2
                                                    whereas the       other known
                                                     blockade of      antidepressa
                                                    norepinephri         nt agents.
                                                         ne and       Compared to
                                                       serotonin          classical
                                                     reuptake at           tricyclic
                                                    the neuronal      antidepressa
                                                    membrane is              nts,
                                                      weaker for      Bupropion is
                                                      bupropion         a relatively
                                                        than for            weak
                                                        tricyclic       inhibitor of
                                                    antidepressa      the neuronal
                                                        nts. The         uptake of
                                                     increase in
                                                    Cefuroxime,       norepinephri
                                                                       Cefuroxime
                                                         like the      is a &beta;-
                                                    penicillins, is    lactam type
                                                         a beta-         antibiotic.
                                                          lactam              More
                                                    antibiotic. By     specifically,
                                                      binding to             it is a
                                                         specific           second-
                                                       penicillin-      generation
                                                         binding      cephalospori
                                                         proteins               n.
                                                          (PBPs)      Cephalospori
                                                         located       ns work the
             J                                         inside the     same way as
             0                                      bacterial cell      penicillins:
             1
                           Bacterial      anti-           wall, it            they
cefuroxime   D   pbpA
                          Infections    bacterial    inhibits the          interfere
             C
                                                        third and          with the
             0
             2
                                                    last stage of     peptidoglyca
                                                    bacterial cell      n synthesis
                                                            wall             of the
                                                      synthesis.           bacterial
                                                     Cell lysis is          wall by
                                                           then           inhibiting
                                                    mediated by            the final
                                                    bacterial cell    transpeptida
                                                            wall       tion needed
                                                        autolytic     for the cross-
                                                        enzymes          links. This
                                                         such as            effect is
                                                    autolysins; it    bactericidal.
                                                      is possible      Cefuroxime
                                                            that        is effective
                                                                                   Clonidine       Clonidine is
                                                                                  acts as an            an
                                                                                  agonist at      antihyperten
                                                                                 presynaptic       sive agent
                                                                                   alpha(2)-          and an
                                                                                receptors in         epidural
                                                                                 the nucleus        agent for
                                                                                     tractus        refractory
                                                                                 solitarius of    cancer pain.
                                                                                the medulla         Similar to
                                                                                  oblongata.       guanabenz
                                                                                 Stimulation             in
                                                                                    of these       mechanism
                 C   N   S                acts as an
                                                                                   receptors        of action,
                 0   0   0                agonist of
                                                                               results in the      clonidine is
                 2   2   1               proteins with
                             ADRA2A                    Hypertensio    anti-       supression       used in the
clonidine        A   C   E                 alpha2-
                             TACR2                         n       hypertensive of efferent       treatment of
                 C   X   A                adrenergic
                                                                                sympathetic       hypertension
                 0   0   0                 receptor
                 1   2   4
                                                                                   pathways       , opiate and
                                            activity
                                                                                    and the          nicotine
                                                                                 subsequent        withdrawal,
                                                                                 decrease in         vascular
                                                                                      blood        headaches,
                                                                               pressure and          diabetic
                                                                                    vascular        diarrhea,
                                                                                 tone in the       glaucoma,
                                                                                      heart,        ulcerative
                                                                                kidneys, and      colitis, Gilles
                                                                                  peripheral           de la
                                                                                vasculature.        Tourette's
                                                                                 Clonidine is      syndrome,
                                                                               also a partial      menopause
                                                                                  agonist at
                                                                               Demeclocycli        symptoms,
                                                                                                  Demeclocycli
                                                                                    ne inhibits        ne is a
                                                                                   cell growth     tetracycline
                                                                                  by inhibiting     antibiotic
                                                                                   translation.         active
                                                                                      It binds     against the
                                                                                  (reversibly)       following
                                                                                    to the 30S    microorganis
                                                                                     and 50S             ms:
                                                                                    ribosomal     <i>Rickettsi
                                                                                  subunit and         ae</i>
                                                                                  prevents the         (Rocky
                                                                                   amino-acyl       Mountain
                 D   J                                                              tRNA from         spotted
                 0   0                                                              binding to          fever,
                 6   1
                                                         Bacterial      anti-     the A site of   typhus fever
demeclocycline   A   A       rpsD rpsI
                                                        Infections    bacterial          the          and the
                 A   A
                                                                                    ribosome,          typhus
                 0   0
                 1   1
                                                                                       which         group, Q
                                                                                      impairs           fever,
                                                                                      protein       rickettsial
                                                                                  synthesis by       pox, tick
                                                                                     bacteria.        fevers),
                                                                                  The binding     <i>Mycoplas
                                                                                  is reversible           ma
                                                                                    in nature.    pneumoniae
                                                                                    The use in    </i> (PPLO,
                                                                                       SIADH            Eaton
                                                                                      actually        agent),
                                                                                    relies on a     agents of
                                                                                    side-effect     psittacosis
                                                                                          of             and
                                                                                  tetracycline      ornithosis,
                                                                                              The
                                                                                       antiinflamm
                                                                                       atory effects
                                                                                                            Diclofenac is
                                                                                       of diclofenac
                                                                                                               an acetic
                                                                                       are believed
                                                                                                                 acid
                                                                                       to be due to
                                                                                                            nonsteroidal
                                                                                       inhibition of
                                                                                                            antiinflamm
                                                                                             both
                                                                                                              atory drug
                                                                                         leukocyte
                                                                                                               (NSAID)
                                                                                         migration
                                                                                                                 with
                                                                                           and the
                                                                                                               analgesic
                                                                                           enzyme
                                                                                                                  and
                                                                                       cylooxygena
                                D   M   M   S                                                                antipyretic
                                                               Arthritis,                se (COX-1
                                1   0   0   0                                                                properties.
                                                             Rheumatoid                and COX-2),
                                1   1   2   1                                   anti-                       Diclofenac is
                                                PTGS1        Inflammatio                 leading to
     diclofenac                 A   A   A   B                              inflammator                      used to treat
                                                PTGS2 TTR          n                          the
                                X   B   A   C                                    y                               pain,
                                                             Osteoarthriti               peripheral
                                1   0   1   0                                                               dysmenorrh
                                8   5   5   3                      s                   inhibition of
                                                                                                              ea, ocular
                                                                                       prostaglandi
                                                                                                            inflammatio
                                                                                       n synthesis.
                                                                                                                   n,
                                                                                               As
                                                                                                            osteoarthriti
                                                                                       prostaglandi
                                                                                                                   s,
                                                                                       ns sensitize
                                                                                                             rheumatoid
                                                                                             pain
                                                                                                               arthritis,
                                                                                         receptors,
                                                                                                             ankylosing
                                                                                       inhibition of
                                                                                                             spondylitis,
                                                                                             their
                                                                                                             and actinic
                                                                                       synthesis is
                                                                                                               keratosis
                                                                                        responsible
                                                                                            for the
                                                                                          analgesic
     DL-thiorphan                                                                         effects of
                                M
                                0                                               anti-
                                1                                          proliferative
                                                             Inflammatio                       Not             Not
     flufenamic_acid            A               AKR1C3 TTR                      anti-
                                                                 nPain                       Available       Available
                                G                                          inflammator
                                0                                           y analgesic
                                3
     gramine
     hydrastine_hydrochloride
     hydroxyachillin

                                                                                                 After        Ifosfamide
                                                                                             metabolic        selectively
                                                                                             activation,     inhibits the
                                                                                                active      synthesis of
                                                                                            metabolites     deoxyribonu
                                                                                           of ifosfamide       cleic acid
                                                                                             alkylate or    (DNA). The
                                                                                              bind with     guanine and
                                                                                                 many           cytosine
                                                                                            intracellular       content
                                L                                                            molecular        correlates
                                0
                                                                                             structures,        with the
                                1                            Neoplasms
                                                                              anti-           including        degree of
     ifosfamide                 A               DNMT1        Testicular
                                                                            neoplastic          nucleic     ifosfamide-
13
                                A                            Neoplasms
                                0                                                            acids. The         induced
                                6                                                             cytotoxic          cross-
                                                                                               action is      linking. At
                                                                                              primarily           high
                                                                                           due to cross-    concentratio
                                                                                              linking of       ns of the
                                                                                             strands of           drug,
                                                                                              DNA and       cellular RNA
                                                                                           RNA, as well     and protein
                                                                                           as inhibition       synthesis
                                                                                             of protein         are also
                                                                                             synthesis.     suppressed.
                                                                                   Labetalol
                                                                                    has two
                                                                                 asymmetric
                                                                                 centers and
                                                                                  therefore,       Labetalol is
                                                                                  exists as a      an alpha-1
                                                                                  molecular          and beta
                                                                                 complex of        adrenergic
                                                                                       two        blocker used
                                                                                diastereoiso      to treat high
                                           acts as a
                                                                                 meric pairs.          blood
                                           blocker of
                                                                                   Dilevalol,      pressure. It
                                         proteins with
                                                                                    the R,R'         works by
                        C                    alpha-
                                                                                stereoisomer         blocking
                        0                 adrenergic
                                ADRA1A                                           , makes up            these
                        7                   receptor
                                ADRA1B                 Hypertensio    anti-          25% of        adrenergic
labetalol               A                 activityacts
                                ADRB1                      n       hypertensive     racemic         receptors,
                        G                as a blocker
                                ADRB2                                              labetalol.     which slows
                        0                 of proteins
                        1
                                                                                   Labetalol       sinus heart
                                          with beta-
                                                                                       HCl             rate,
                                          adrenergic
                                                                                   combines         decreases
                                            receptor
                                                                                      both          peripheral
                                             activity
                                                                                   selective,        vascular
                                                                                competitive,       resistance,
                                                                                    alpha-1-            and
                                                                                  adrenergic        decreases
                                                                                blocking and          cardiac
                                                                                nonselective          output.
                                                                                        ,
                                                                                competitive,
                                                                                      beta-
                                                                                  adrenergic
                        C                                                           blocking
                        0
                        8
lidoflazine             E
                        X
                        0
                        1
                                                                     diagnostic
methacholine_chloride
                                                                       agent
                                                                                   Perhaps by      Papaverine
                                                                                     its direct          is a
                                                                                   vasodilating   nonxanthine
                                                                                    action on     phosphodies
                                                                                      cerebral         terase
                                                                                        blood     inhibitor for
                                                                                      vessels,     the relief of
                                                                                   Papaverine     cerebral and
                                                                                    increases       peripheral
                                                                                      cerebral       ischemia
                                                                                    blood flow      associated
                                                                                         and      with arterial
                                                                        anti-       decreases      spasm and
                        A   G                                        asthmatic        cerebral     myocardial
                        0   0                            Virus
                                                                       smooth        vascular        ischemia
                        3   4                          Diseases
                                                                       muscle     resistance in   complicated
papaverine              A   B   PDE4B                   Angina
                                                                   relaxantvaso        normal             by
                        D   E                         PectorisAsth
                                                                    dilator anti-   subjects;     arrhythmias.
                        0   0                             ma
                        1   2                                        viral anti-      oxygen         The main
                                                                       anginal    consumption        actions of
                                                                                  is unaltered.    Papaverine
                                                                                       These       are exerted
                                                                                   effects may      on cardiac
                                                                                   explain the    and smooth
                                                                                       benefit    muscle. Like
                                                                                     reported       qathidine,
                                                                                     from the      Papaverine
                                                                                      drug in     acts directly
                                                                                      cerebral    on the heart
                                                                                     vascular        muscle to
                                                                                  encephalopa         depress
                                                                                         thy.       conduction
                                                                                                  and prolong
                                                                                              Physostigmi
                                                                                                   ne is a
                                                                                             parasympath
                                                                                               omimetic,
                                                                                              specifically,
                                                                                              a reversible
                                                                                             cholinesteras
                                                                                               e inhibitor
                                                                                                   which
                                                                                  By           effectively
                                                                              interfering       increases
                                                                               with the              the
                                                                              metabolism     concentratio
                   S   V                                                           of                n of
                   0   0                                                                     acetylcholine
                                                                             acetylcholine
                   1   3
                                                                                   ,          at the sites
physostigmine      E   A   ACHE                    Glaucoma        miotic
                                                                             physostigmi              of
                   B   B
                                                                             ne indirectly     cholinergic
                   0   1
                   5   9                                                      stimulates     transmission
                                                                                 both                 .
                                                                             nicotinic and    Physostigmi
                                                                              muscarinic     ne is used to
                                                                              receptors.            treat
                                                                                               glaucoma.
                                                                                               Because it
                                                                                              crosses the
                                                                                              blood-brain
                                                                                              barrier, it is
                                                                                             also used to
                                                                                                 treat the
                                                                                                  central
                                                                                                  nervous
                                                                                                  system
                                                  Hypertensio    anti-
protoveratrine_A
                                                      n       hypertensive
                                                                             Ramiprilat,      Ramipril is
                                                                              the active              an
                                                                             metabolite,     angiotensin-
                                                                              competes        converting
                                                                                  with          enzyme
                                                                            angiotensin I          (ACE)
                                                                             for binding        inhibitor
                                                                                 at the        similar to
                                                                            angiotensin-      benazepril,
                                                                             converting        fosinopril,
                                                                               enzyme,               and
                                                                            blocking the     quinapril. An
                                                                             conversion          inactive
                   C                   acts as an                                  of           prodrug,
                   0                                                        angiotensin I     ramipril is
                                      inhibitor of
                   9
                                        protein    Cerebrovasc cardiovascul        to        converted to
ramipril           A       ACE ACE
                                     acetylcholine ular Accident ar agent    angiotensin     ramiprilat in
                   A
                                      sterase (Yt                                II. As      the liver and
                   0
                   5                 blood group)                            angiotensin       is used to
                                                                                 II is a            treat
                                                                            vasoconstrict    hypertension
                                                                               or and a        and heart
                                                                              negative-        failure, to
                                                                               feedback           reduce
                                                                            mediator for      proteinuria
                                                                                 renin         and renal
                                                                                activity,     disease in
                                                                                 lower       patients with
                                                                            concentratio     nephropathi
                                                                            ns result in a    es, and to
                                                                             decrease in         prevent
                                                                                 blood            stroke,
                                                                            pressure and      myocardial
                                                                             Scopolamine
                                                                                    is a
                                                                               muscarinic
                                                                               antagonist
                                                                              structurally
                                                                                similar to
                                                                                    the
                                                                             neurotransm
                                                                                   itter
                                                            Scopolamine
                                                                             acetylcholine
                                                                acts by
                                                                              and acts by
                                                              interfering
                                                                              blocking the
                                                               with the
                                                                               muscarinic
               A   N   S                                    transmission
                                                                             acetylcholine
               0   0   0                                       of nerve
                                                                                receptors
               4   5   1                                    impulses by
                                                                              and is thus
scopolamine    A   C   F   CHRM1                mydriatic   acetylcholine
                                                                              classified as
               D   M   A                                         in the
                                                                                     an
               0   0   0                                    parasympath
               1   5   2
                                                                             anticholinerg
                                                            etic nervous
                                                                                     ic.
                                                                system
                                                                             Scopolamine
                                                             (specifically
                                                                               has many
                                                            the vomiting
                                                                                  uses
                                                                center).
                                                                             including the
                                                                               prevention
                                                                               of motion
                                                                              sickness. It
                                                                              is not clear
                                                                                   how
                                                                             Scopolamine
                                                                                prevents
                                                                              nausea and
                                                                             vomiting due
                                                                              Sulfadiazine
                                                                                    is a
                                                                             sulfonamide
                                                                               antibiotic.
                                                                                    The
                                                            Sulfadiazine     sulfonamide
                                                                   is a            s are
                                                             competitive        synthetic
                                                              inhibitor of   bacteriostati
                                                                bacterial    c antibiotics
                                                                  para-       with a wide
                                                            aminobenzoi        spectrum
                                                                  c acid     against most
               J                                               (PABA), a          gram-
               0                                                             positive and
                                                            substrate of
               1
                                    Bacterial     anti-      the enzyme      many gram-
sulfadiazine   E
                                   Infections   bacterial   dihydroptero        negative
               C
                                                                   ate        organisms.
               0
               2                                             synthetase.       However,
                                                            The inhibited    many strains
                                                               reaction is         of an
                                                            necessary in       individual
                                                                  these      species may
                                                               organisms     be resistant.
                                                                 for the     Sulfonamide
                                                            synthesis of         s inhibit
                                                               folic acid.   multiplicatio
                                                                             n of bacteria
                                                                             by acting as
                                                                              competitive
                                                                             inhibitors of
                                                                              <i>p</i>-
                                                                             aminobenzoi
                                                                                 The effects    Testosterone
                                                                                         of      is a steroid
                                                                                testosterone       hormone
                                                                                  in humans        from the
                                                                                   and other       androgen
                                                                                 vertebrates          group.
                                                                                occur by way    Testosterone
                                                                                 of two main     is primarily
                                                                                mechanisms       secreted in
                                                                                       : by     the testes of
                                                                                activation of     males and
                                                                                        the      the ovaries
                                                                                   androgen       of females
                 G                                                                  receptor       although
                 0                                                               (directly or         small
                 3
                     AR ALB                      Hypogonadis     hormone           as DHT),     amounts are
testosterone     B
                     SHBG NPPB                       m           therapy             and by      secreted by
                 A
                                                                                  conversion     the adrenal
                 0
                 3
                                                                                 to estradiol   glands. It is
                                                                                       and      the principal
                                                                                activation of      male sex
                                                                                     certain       hormone
                                                                                   estrogen          and an
                                                                                  receptors.        anabolic
                                                                                       Free       steroid. In
                                                                                testosterone     both males
                                                                                      (T) is    and females,
                                                                                 transported     it plays key
                                                                                    into the        roles in
                                                                                cytoplasm of      health and
                                                                                target tissue    well-being.
                                                                                cells, where      Examples
tomatidine                                                                        it can bind        include
tremorine

                                   acts as an
                                  inhibitor of
                                     protein
                                     cyclin-
                                  dependent
                                kinase 2 acts
                                 as a binder
                     GSK3B CDK5 of protein
                                                                   anti-            Not             Not
alsterpaullone       CDC2        cell division
                                                               proliferative      Available       Available
                     CDK2deltaT  cycle 2, G1
                                 to S and G2
                                 to Macts as
                                 an inhibitor
                                   of protein
                                     cyclin-
                                  dependent
                                    kinase 5

                                                                                   Azacitidine Azacitidine is
                                                                                       (5-       believed to
                                                                                 azacytidine)      exert its
                                                                                     causes     antineoplasti
                                                                                hypomethyla c effects by
                                                                                  tion of DNA       causing
                                                                                   and direct hypomethyla
                                                                                  cytotoxicity tion of DNA
                                                                                 in abnormal      and direct
                                                                                hematopoiet cytotoxicity
                                                                                ic cells in the on abnormal
                                                                                      bone      hematopoiet
                                                                                    marrow,     ic cells in the
                                                                                  resulting in       bone
                                                                   anti-
                                                                                 cell death. 5- marrow. The
                                                                neoplastic
                                                                                  azacytidine concentratio
azacitidine          DNMT1                        Infection        anti-
                                                                                is a chemical         n of
                                                                 infective
                                                                                  analogue of azacitidine
                                                                   agent
                                                                                 the cytosine required for
                                                                                   nucleoside     maximum
                                                                                 used in DNA inhibition of
                                                                                    and RNA.         DNA
                                                                                  Cells in the methylation
                                                                                  presence of in vitro does
                                                                                        5-        not cause
                                                                                  azacytidine        major
                                                                                  incorporate suppression
                                                                                  it into DNA       of DNA
                                                                                     during       synthesis.
                                                                                 transcription Hypomethyl
                                                                                    and RNA       ation may
                                                                                     during         restore
                 A                                                                translation.      normal
                 0                 acts as an
                 3               antagonist of
                                                               sedative anti-
bromopride       F                  protein       Vomiting
                                                                  emetic
                 A                 dopamine
                 0                receptor D2
                 4
                                                                                              Camptotheci
                                                                            Camptotheci                n
                                                                              n binds to      demonstrate
                                                                                   the            d strong
                                                                            topoisomera        anticancer
                                                                               se I and         activity in
                                                                                  DNA          preliminary
                                                                               complex        clinical trials
                                                                                  (the        but also low
                                  acts as an
                                                                               covalent          solubility
                                enhancer of
                                                                              complex)        and adverse
                                   protein                       anti-
                                              Gastrointesti                 resulting in a           drug
                                topoisomera                   neoplastic
                                                   nal                          ternary          reaction.
                                 se (DNA) I                      anti-
     camptothecin       TOP1                  NeoplasmsH                       complex,       Camptotheci
                                  acts as an                   protozoal
                                              IV Infections                  and thereby      n is believed
                                 inhibitor of                  anti-viral
                                               Neoplasms                    stabilizing it.        to be a
                                   protein                    insecticide
                                                                                  This             potent
                                topoisomera
                                                                               prevents       topoisomera
                                 se (DNA) I
                                                                                  DNA          se inhibitor
                                                                              relegation             that
                                                                                  and           interferes
                                                                              therefore           with the
                                                                             causes DNA          essential
                                                                               damage          function of
                                                                            which results     topoisomera
                                                                            in apoptosis.       se in DNA
                                                                                               replication.
                                                                             Daunorubici      Daunorubici
                                                                                 n has             n is an
                                                                             antimitotic      antineoplasti
                                                                                  and              c in the
                                                                               cytotoxic      anthracyclin
                                                                                activity           e class.
                                                                              through a           General
                                                                              number of       properties of
                                                                              proposed        drugs in this
                                                                            mechanisms              class
                                                                              of action:          include:
                                                                             Daunorubici       interaction
                                                                                n forms        with DNA in
                    L             acts as an                                 complexes         a variety of
                    0                                                       with DNA by          different
                                 intercalator
                    1
                        ABCB1     of proteins                   anti-       intercalation           ways
     daunorubicin   D                            Neoplasms
                        ABCC1         with                    neoplastic       between           including
                    B
                                oxidoreducta                                 base pairs,      intercalation
                    0
                    2             se activity                                    and it        (squeezing
                                                                                inhibits      between the
                                                                            topoisomera       base pairs),
                                                                            se II activity     DNA strand
                                                                                    by          breakage
                                                                              stabilizing            and
                                                                              the DNA-          inhibition
                                                                            topoisomera           with the
                                                                                  se II           enzyme
                                                                              complex,        topoisomera
                                                                             preventing        se II. Most
                                                                                   the            of these
                                                                              religation       compounds
                                                                              portion of       have been
                                                                            the ligation-
                                                                             Doxorubicin          isolated
                                                                                               Doxorubicin
                                                                                   has              is an
                                                                             antimitotic      antineoplasti
                                                                                  and             c in the
                                                                               cytotoxic      anthracyclin
                                                                                activity          e class.
                                                                              through a          General
                                                                             number of        properties of
                                                                              proposed        drugs in this
                                                                            mechanisms             class
                                   acts as an                                 of action:         include:
                                 intercalator                                Doxorubicin       interaction
                                  of proteins                                    forms         with DNA in
                    L                 with                                   complexes         a variety of
                    0                                                       with DNA by          different
                                oxidoreducta
                    1
                                       se                                   intercalation          ways
     doxorubicin    D   TOP2A
                                 activityacts                                  between          including
                    B
                                     as an                                   base pairs,      intercalation
                    0
                    1             inhibitor of                                   and it        (squeezing
                                protein DNA                                     inhibits      between the

14                              topoisomera
                                      se II
                                                                            topoisomera
                                                                            se II activity
                                                                                              base pairs),
                                                                                               DNA strand
                                                                                    by          breakage
                                                                              stabilizing            and
                                                                              the DNA-          inhibition
                                                                            topoisomera          with the
                                                                                  se II          enzyme
                                                                              complex,        topoisomera
                                                                             preventing        se II. Most
                                                                                   the           of these
                                                                              religation       compounds
                                                                              portion of       have been
                                                                            the ligation-        isolated
14




                                             acts as an
                                            inhibitor of
     ellipticine                           protein DNA
                                           topoisomera
                                                se II
     fisetin
                                                                                                        Gallamine
                                                                                     It competes
                                                                                                      Triethiodide
                                                                                           with
                                                                                                            is a
                                                                                     acetylcholine
                                                                                                      nondepolariz
                                                                                          (ACh)
                                                                                                             ing
                                                                                       molecules
                                                                                                      neuromuscul
                                                                                     and binds to
                                                                                                       ar blocking
                                                                                      muscarinic
                                                                                                            drug
                                                                                     acetylcholine
                                                                                                         (NDMRD)
                                                                                     receptors on
                                             acts as an                                                used as an
                                                                                        the post-
                                           antagonist of                                                adjunct to
                                                                                         synaptic
                                           proteins with                                                anesthesia
                                                                                      membrane
                                            muscarinic                                                   to induce
                                                                                     of the motor
                                           acetylcholine                                                  skeletal
                                                                                      endplate. It
                                              receptor                     muscle                         muscle
                                  CHRNA2                                               blocks the
                                            activityacts                  relaxant                      relaxation.
     gallamine_triethiodide       CHRM2                                                 action of
                                           as a blocker                 (spasmolytic                   The actions
                                  ACHE                                                  ACh and
                                            of proteins                       )                       of gallamine
                                                                                        prevents
                                           with calcium-                                               triethiodide
                                                                                     activation of
                                             activated                                                  are similar
                                                                                      the muscle
                                            potassium                                                  to those of
                                                                                      contraction
                                              channel                                                 tubocurarine
                                                                                       process. It
                                               activity                                                  , but this
                                                                                     can also act
                                                                                                      agent blocks
                                                                                      on nicotinic
                                                                                                       the cardiac
                                                                                      presynaptic
                                                                                                        vagus and
                                                                                     acetylcholine
                                                                                                        may cause
                                                                                       receptors
                                                                                                           sinus
                                                                                          which
                                                                                                       tachycardia
                                                                                      inhibits the
                                                                                                            and,
                                                                                       release of
                                                                                                      occasionally,
                                                                                           ACh.
                                                                                                      hypertension
                                             acts as an                                                     and
                                            inhibitor of
                                               protein
     GW-8510
                                               cyclin-
                                            dependent
                                              kinase 2
                                             acts as an
                                            inhibitor of
                                           proteins with
                                               protein
                                              kinase C
                                            activityacts
     H-7
                                                as an
                                            inhibitor of
                                           proteins with
                                               protein
                                              kinase C
                                               activity
                                                                                      Mitoxantrone
                                                                                         , a DNA-
                                                                                          reactive
                                                                                        agent that
                                                                                      intercalates
                                                                                            into
                                                                                      deoxyribonu
                                                                                         cleic acid
                                                                                                      Mitoxantrone
                                                                                           (DNA)
                                                                                                         has been
                                                                                          through
                                                                                                         shown in
                                                                                        hydrogen
                                                                                                          vitro to
                                                                                         bonding,
                                                                                                      inhibit B cell,
                                                           Prostatic                       causes
                              L                                                                         T cell, and
                                             acts as an   Neoplasms                     crosslinks
                              0                                                                        macrophage
                                            intercalator Neoplasms                     and strand
                              1                                                                        proliferation
                                  TOP2A      of proteins  Leukemia,        anti-          breaks.
     mitoxantrone             D                                                                         and impair
                                  ABCG2          with    Nonlymphoc      neoplastic   Mitoxantrone
                              B                                                                           antigen
                                           oxidoreducta      ytic,                          also
                              0                                                                       presentation
                              7              se activity AcuteMultipl                   interferes
                                                                                                       , as well as
                                                          e Sclerosis                       with
                                                                                                      the secretion
                                                                                       ribonucleic
                                                                                                       of interferon
                                                                                       acid (RNA)
                                                                                                         gamma,
                                                                                          and is a
                                                                                                      TNFa, and IL-
                                                                                           potent
                                                                                                             2.
                                                                                       inhibitor of
                                                                                      topoisomera
                                                                                         se II, an
                                                                                          enzyme
                                                                                       responsible
                                                                                      for uncoiling
                                                                                            and
                                                                                         repairing
                                                                                        damaged
                                             acts as an
                                            inhibitor of
     MS-275                                proteins with
                                           deacetylase
                                              activity
                                               acts as an
                                              inhibitor of
                                             protein v-src
                                                sarcoma
                                               (Schmidt-
                                 LCK PIM1    Ruppin A-2)
                                 ITK SYK          viral
                                 MAPKAPK2      oncogene                                     Not              Not
     staurosporine
                                 GSK3B CSK      homolog                                   Available        Available
                                 CDK2         (avian)acts
                                 PIK3CG           as an
                                              inhibitor of
                                             proteins with
                                                 protein
                                                kinase C
                                                 activity
                                               acts as an
                                              inhibitor of
                                               protein v-
                                                 erb-b2
                                             erythroblasti
                                              c leukemia
                                                  viral
     tyrphostin_AG-825                         oncogene
                                              homolog 2,
                                             neuro/gliobl
                                                astoma
                                                derived
                                               oncogene
                                                homolog
                                                 (avian)
                         S
                         0
                         1
     diclofenamide       E
                         C
                         0
                         2
     Gly-His-Lys
                                                                                                         Pilocarpine is
                                                                                                            a choline
                                                                                                          ester miotic
                                                                                                              and a
                                                                                                           positively
                                                                                        Pilocarpine is
                                                                                                             charged
                                                                                        a cholinergic
                                                                                                          quaternary
                                               acts as an                               parasympath
                                                                                                          ammonium
                                               agonist of                                 omimetic
                                                                                                          compound.
                                             proteins with                                 agent. It
                                                                                                          Pilocarpine,
                                              muscarinic                                   increase
                                                                                                                in
                                             acetylcholine                              secretion by
                                                                                                          appropriate
                                                receptor                                the exocrine
15                       N   S                activityacts
                                                  as an
                                                                                         glands, and
                                                                                           produces
                                                                                                         dosage, can
                                                                                                            increase
                         0   0                                                                           secretion by
                         7   1                 agonist of                                contraction
                                 CHRM1                                                                   the exocrine
     pilocarpine         A   E                   protein                    miotic        of the iris
                                 CHRM2                                                                    glands. The
                         X   B                cholinergic                                  sphincter
                                                                                                              sweat,
                         0   0                 receptor,                                 muscle and
                         1   1
                                                                                                            salivary,
                                             muscarinic 2                                    ciliary
                                                                                                            lacrimal,
                                               acts as an                                   muscle
                                                                                                             gastric,
                                               agonist of                               (when given
                                                                                                          pancreatic,
                                             proteins with                               topically to
                                                                                                               and
                                             acetylcholine                              the eyes) by
                                                                                                           intestinal
                                                receptor                                    mainly
                                                                                                          glands and
                                                 activity                                stimulating
                                                                                                          the mucous
                                                                                         muscarinic
                                                                                                          cells of the
                                                                                          receptors.
                                                                                                          respiratory
                                                                                                         tract may be
                                                                                                          stimulated.
                                                                                                              When
                                                                                                             applied
     STOCK1N-35874                                                                                        topically to
                         M   M                acts as an
                         0   0
                                             antagonist of               analgesic
                         1   2
                                             proteins with Inflammatio      anti-
     bufexamac           A   A
                                             prostaglandi      nPain   inflammator
                         B   A
                         1   0                n receptor                     y
                         7   9                  activity
                         R
                         0                     acts as an
                         3                    inhibitor of
                                                             Bronchial   bronchodilat
     diprophylline       D                   protein cAMP-
                                                             Diseases         or
                         A                   phosphodies
                         0                       terase
                         1
                                                                                        Fusidic acid
                                                                                          works by
                                                                                                        Fusidic acid
                                                                                         interfering
                                                                                                             is a
                                                                                             with
                                                                                                       bacteriostati
                                                                                          bacterial
                                                                                                        c antibiotic
               D   D   J   S                                                               protein
                                                                                                       that is often
               0   0   0   0                                                             synthesis,
                                                            Gram-                                           used
               6   9   1   1                                               anti-        specifically
                                                           Positive                                     topically in
fusidic_acid   A   A   X   A   cat3 cat                                bacterial anti-        by
                                                           Bacterial                                    creams and
               X   A   C   A                                               viral        preventing
               0   0   0   1                              Infections                                     eyedrops,
                                                                                             the
               1   2   1   3                                                                           but may also
                                                                                       translocation
                                                                                                          be given
                                                                                            of the
                                                                                                       systemically
                                                                                         elongation
                                                                                                       as tablets or
                                                                                       factor G (EF-
                                                                                                         injections.
                                                                                        G) from the
                                                                                         ribosome.

                                            acts as an
                                           inhibitor of
HC_toxin                                  proteins with
                                          deacetylase
                                             activity
                                                                                                        In chemical
                                                                                                          structure
                                                                                                        idoxuridine
                                                                                                            closely
                                                                                                       approximate
                                                                                       Idoxuridine           s the
                                                                                        acts as an     configuration
                                                                                          antiviral            of
                                                                                           agent         thymidine,
                                                                                      against DNA        one of the
                                                                                        viruses by     four building
                                                                                         inhibiting       blocks of
                                                                                       thymidilate        DNA (the
               D   J   S                                                               phosphoryla         genetic
               0   0   0                                                                                material of
                                                                                       se and viral
               6   5   1
                                                                                            DNA         the Herpes
idoxuridine    B   A   A       UL30
                                                                                      polymerases       virus). As a
               B   B   D
                                                                                       . The effect         result,
               0   0   0
               1   2   1                                                                      of        idoxuridine
                                                                                       Idoxuridine        is able to
                                                                                      results in the       replace
                                                                                        inability of   thymidine in
                                                                                       the virus to           the
                                                                                      reproduce or       enzymatic
                                                                                              to        step of viral
                                                                                      infect/destro      replication
                                                                                          y tissue.    or "growth".
                                                                                                              The
                                                                                                        consequent
                                                                                                         production
                                                                                                           of faulty
                                                                                                        DNA results
LY-294002                                                                                                     in a

                                             acts as an
                                            inhibitor of
                                              protein
                                          arachidonate
                                                 5-
                                          lipoxygenase
               P                             acts as an
               0                           intercalator
               1                            of proteins                   anti-
                                                         Helminthiasi
mepacrine      A                                with                   helminthic
                                                              s
               X                          oxidoreducta                anti-malarial
               0                                 se
               5                            activityacts
                                           as a blocker
                                            of proteins
                                                with
                                             potassium
                                              channel
                                              activity
                                                                                         Pergolide is
                                                                                           an ergot
                                                                                          derivative
                                                                                          dopamine
                                                                                           receptor
                                                                                          agonist at
                                                                                        both D1 and
                                                                                         D2 receptor
                                                                        Pergolide is         sites.
                                                                           a potent      Pergolide is
                                                                          dopamine       10 to 1,000
                                                                           receptor      times more
                                                                         agonist. It     potent than
                 N                                                          directly    bromocriptin
                 0                acts as an
                                                                         stimulates          e on a
                 4                agonist of
                                               Parkinson   neuroprotect      post-         milligram
     pergolide   B   DRD2 DRD1     protein
                                                Disease     ive agent      synaptic           per
                 C                dopamine
                                                                          dopamine         milligram
                 0               receptor D2
                 2                                                      receptors at        basis in
                                                                        both D1 and       various in
                                                                        D2 receptor      vitro and in
                                                                         sites in the      vivo test
                                                                        nigrostriatal      systems.
                                                                           system.         Pergolide
                                                                                           mesylate
                                                                                         inhibits the
                                                                                         secretion of
                                                                                         prolactin in
                                                                                          humans; it
                                                                                           causes a
                                                                                           transient
                                                                                        rise in serum
                                                                                        concentratio
                                                                                         Rifabutin is
                                                                                        an antibiotic
                                                                                        that inhibits
                                                                                             DNA-
                                                                                         dependent
                                                                                              RNA
                                                                                         polymerase
                                                                                          activity in
                                                                                         susceptible
                                                                                             cells.
                                                                          Rifabutin
                                                                                        Specifically,
                                                                        acts via the
                                                                                         it interacts
                                                                        inhibition of
                                                                                              with
                 J                                                          DNA-
                                                                                           bacterial
                 0                                                       dependent
                                                                                              RNA
                 4   rpoA                                                    RNA
                                                                                         polymerase
     rifabutin   A   HSP90AA1                                           polymerase,
                                                                                        but does not
                 B   HSP90B1                                            leading to a
                                                                                          inhibit the
                 0                                                      suppression
                 4
                                                                                        mammalian
                                                                           of RNA
                                                                                         enzyme. It
                                                                          synthesis
                                                                                               is
                                                                           and cell
                                                                                         bactericidal
                                                                            death.
                                                                                          and has a
                                                                                         very broad
                                                                                        spectrum of
                                                                                            activity
                                                                                        against most
                                                                                            gram-
                                                                                        positive and
                                                                                            gram-
                                                                                           negative
                                                                                          organisms
                                                                                          (including




16
                                                                            Rosiglitazon     Rosiglitazon
                                                                            e acts as an    e, a member
                                                                              agonist at      of the drug
                                                                             peroxisome     group known
                                                                             proliferator         as the
                                                                               activated    thiazolidined
                                                                               receptors        iones or
                                                                              (PPAR) in          "insulin
                                                                                 target      sensitizers",
                                                                              tissues for          is not
                                                                                 insulin      chemically
16                                 acts as an
                                                                             action such
                                                                             as adipose
                                                                                                      or
                                                                                             functionally
                      A                          Diabetes
                                  activator of                                   tissue,       related to
                      1                          Mellitus,
                                     protein                                    skeletal      the alpha-
                      0                        Type 2 Fatty
                                  peroxisome                                muscle, and      glucosidase
     rosiglitazone    B   PPARG                    Liver
                                  proliferator                                    liver.       inhibitors,
                      G                         Polycystic
                                   activated                                Activation of            the
                      0                           Ovary
                      2             receptor                                     PPAR-       biguanides,
                                                Syndrome
                                    gamma                                       gamma             or the
                                                                               receptors     sulfonylurea
                                                                               regulates              s.
                                                                                    the      Rosiglitazon
                                                                            transcription       e targets
                                                                              of insulin-         insulin
                                                                             responsive       resistance
                                                                                  genes      and, hence,
                                                                             involved in    is used alone
                                                                             the control         or with
                                                                              of glucose     metformine
                                                                             production,              or
                                                                              transport,     sulfonylurea
                                                                                   and        to improve
                                    acts as an
                                   inhibitor of
                                  proteins with
                                  deacetylase
                                   activityacts
     scriptaid
                                      as an
                                   inhibitor of
                                     protein
                                     Histone
                                  deacetylase
                                                                            Spironolacto    Spironolacto
                                                                                 ne is a          ne is a
                                                                                 specific   synthetic 17-
                                                                            pharmacolog          lactone
                                                                            ic antagonist        steroid
                                                                                    of        which is a
                                                                            aldosterone,           renal
                                                                                  acting     competitive
                                    acts as an                                  primarily    aldosterone
                                  antagonist of                                 through     antagonist in
                                      protein                                competitive      a class of
                                      nuclear                                 binding of    pharmaceuti
                                     receptor                                receptors at     cals called
                      C                         Hypokalemia
                                  subfamily 3,                                     the       potassium-
                      0                         Hyperaldost
                                     group C,                               aldosterone-        sparing
                      3                            eronism
                          AGTR1      member                   cardiovascul dependent        diuretics. On
     spironolactone   D                         Hypertensio
                          NR3C2    2acts as an                  ar agent        sodium-         its own,
                      A                               n
                                  antagonist of                               potassium     spironolacto
                      0                         Cardiovascul
                      1               protein                                  exchange      ne is only a
                                                 ar Diseases
                                      nuclear                                 site in the          weak
                                     receptor                                     distal    diuretic, but
                                  subfamily 3,                                convoluted       it can be
                                     group C,                               renal tubule.     combined
                                    member 2                                Spironolacto      with other
                                                                              ne causes       diuretics.
                                                                               increased      Due to its
                                                                             amounts of            anti-
                                                                             sodium and       androgen
                                                                             water to be    effect, it can
                                                                               excreted,    also be used
                                                                                  while         to treat
                                                                            potassium is      hirsutism,
                                    acts as an                    anti-        retained.        and is a
                                   inhibitor of               proliferative
     trichostatin_A                   protein                immunosupp
                                     Histone                     ressive
                                   deacetylase                    agent
                                                                                           Trimethoben
                                                                                   The      zamide is a
                                                                             mechanism           novel
                                                                             of action of    antiemetic
                                                                            trimethoben          which
                                                                              zamide as        prevents
                                                                             determined     nausea and
                                                                            in animals is   vomiting in
                                                                            obscure, but   humans. Its
                                                                             may involve     actions are
                                                                                   the      unclear but
                                                                            chemorecept      most likely
                                                                               or trigger  involves the
                                                                             zone (CTZ),   chemorecept
                                                                              an area in      or trigger
                                                                             the medulla   zone (CTZ).
trimethobenzamide                                  Vomiting     anti-emetic
                                                                              oblongata         In dogs
                                                                                through      pretreated
                                                                            which emetic          with
                                                                            impulses are   trimethoben
                                                                             conveyed to   zamide HCl,
                                                                            the vomiting     the emetic
                                                                                 center;    response to
                                                                                  direct   apomorphin
                                                                             impulses to           e is
                                                                            the vomiting      inhibited,
                                                                                 center    while little or
                                                                              apparently            no
                                                                                 are not   protection is
                                                                                similarly      afforded
                                                                               inhibited.       against
                                                                                                emesis
                                                                                             induced by
                                                                             Valproic Acid Valproic Acid
                                                                             binds to and         is an
                                                                                 inhibits  anticonvulsa
                                                                                  GABA     nt and mood-
                                                                             transaminas stabilizing
                                                                                  e. The      drug used
                                                                                  drug's    primarily in
                                                                             anticonvulsa          the
                                                                               nt activity treatment of
                                                                                 may be    epilepsy and
                                                                               related to       bipolar
                                     acts as an
                                                                               increased    disorder. It
                                    inhibitor of
                                                                                   brain    is also used
                    N                  protein
                                                                             concentratio       to treat
                    0                Glycogen       Bipolar
                                                                             ns of gamma- migraine
                    3                 synthase   DisorderSeiz
                                                                   anti-     aminobutyric headaches
valproic_acid       A   ABAT HDAC9 kinase-3acts      ures
                                                                convulsant   acid (GABA),          and
                    G                   as an      Migraine
                                                                             an inhibitory schizophreni
                    0               inhibitor of   Epilepsy
                    1
                                                                             neurotransm          a. In
                                   proteins with
                                                                              itter in the    epileptics,
                                   deacetylase
                                                                                CNS, by    valproic acid
                                       activity
                                                                               inhibiting     is used to
                                                                                enzymes         control
                                                                                   that        absence
                                                                               catabolize      seizures,
                                                                                GABA or     tonic-clonic
                                                                               block the       seizures
                                                                              reuptake of (grand mal),
                                                                               GABA into       complex
                                                                                glia and         partial
                                                                                  nerve        seizures,
                                                                                endings.        and the
                                                                             Valproic Acid     seizures
                                                                                          Vorinostat
                                                                                         inhibits the
                                                                                          enzymatic
                                                                                          activity of
                                                                                            histone
                                                                                       deacetylases
                                                                                            HDAC1,
                                                                                        HDAC2 and
                                                                                            HDAC3
                                                                                       (Class I) and
                                                                                            HDAC6
                                               acts as an                               (Class II) at
                                              inhibitor of                               nanomolar
                                 HDAC1          protein                                concentratio
                                 HDAC2          Histone                                        ns
                                 HDAC3       deacetylase                               (IC<sub>50           Not
     vorinostat
                                 HDAC6         acts as an                               </sub>&lt;        Available
                                 HDAC8        inhibitor of                                  86 nM).
                                 acuC1       proteins with                                   These
                                             deacetylase                                   enzymes
                                                activity                               catalyze the
                                                                                         removal of
                                                                                             acetyl
                                                                                       groups from
                                                                                          the lysine
                                                                                         residues of
                                                                                           proteins,
                                                                                           including
                                                                                       histones and
                                                                                       transcription
                                                                                          factors. In
                                                                                       some cancer
                                                                                         cells, there
                                                                                              Not           Not
     monastrol                   KIF11
                                                                                         Available        Available
     NU-1025
                                                                                        In patients     Thalidomide
                                                                                            with               is an
                                                                                         erythema       immunomod
                                                                                         nodosum              ulatory
                                                                                         leprosum       agent with a
                                               acts as an                                (ENL) the       spectrum of
                                              inhibitor of                             mechanism         activity that
                                                 protein                               of action is       is not fully
                                                 tumor                                    not fully     characterize
                                                necrosis                               understood.               d.
                                              factor (TNF                                Available      Thalidomide
                                             superfamily,                             data from in         is racemic
                                                member                                vitro studies       &mdash; it
                             L                2)acts as a                                    and             contains
17                           0
                             4
                                 TNF NFKB1
                                               binder of
                                             proteins with Inflammatio
                                                                         antiseptic
                                                                          hypnotic
                                                                                       preliminary
                                                                                      clinical trials
                                                                                                        both left and
                                                                                                        right handed
     thalidomide             A                                         sedative anti- suggest that
                                 PTGS2           tumor          n                                          isomers in
                             X                                         inflammator
                                                necrosis                                     the               equal
                             0                                               y
                                                  factor                              immunologic           amounts:
                             2
                                                receptor                                 effects of             one
                                              activity acts                                  this        enantiomer
                                                  as an                                 compound          is effective
                                             antagonist of                                can vary           against
                                                 protein                              substantially          morning
                                             interleukin 1                                 under            sickness,
                                               receptor,                                  different          and the
                                                 type I                                 conditions,          other is
                                                                                       but may be        teratogenic.
                                                                                         related to             The
                                                                                       suppression      enantiomers
                                                                                       of excessive             are
                                                                                           tumor        converted to
     3-nitropropionic_acid                                                                necrosis        each other
     PF-01378883-00




18
                                                    acts as an                               Both COX-1       Valdecoxib,
                                                   inhibitor of                               and COX-2        a selective
                                                      protein                                catalyze the    cyclooxygen
                                                  prostaglandi                                conversion     ase-2 (COX-
                                                         n-                                          of      2) inhibitor,
                                                  endoperoxid                                 arachidonic     is classified
                                                  e synthase 2                                   acid to           as a
                                                  (prostagland                               prostaglandi    nonsteroidal
                                                      in G/H                                  n (PG) H2,          anti-
                                                     synthase                                       the      inflammator
                                                        and                                  precursor of        y drug
                                                  cyclooxygen                                   PGs and         (NSAID).
                                                   ase)acts as                               thromboxan      Valdecoxib is
                                      M            an inhibitor    Osteoarthriti                     e.       used for its
                                      0                             s Arthritis,
18
                                                    of protein                     analgesic  Valdecoxib          anti-
                                      1              carbonic      Rheumatoid                 selectively    inflammator
                                                                                      anti-
     valdecoxib                       A   PTGS2                    Dysmenorrh
                                                   anhydrase                     inflammator inhibits the    y, analgesic,
                                      H                              ea Pain,
                                                  IX acts as an                        y     cyclooxygen           and
                                      0                            Postoperativ
                                                   inhibitor of                              ase-2 (COX-       antipyretic
                                      3                                  e
                                                      protein                                 2) enzyme,      activities in
                                                  prostaglandi                                 important           the
                                                         n-                                      for the     managemen
                                                  endoperoxid                                mediation of          t of
                                                  e synthase 2                               inflammatio     osteoarthriti
                                                  (prostagland                                n and pain.     s (OA) and
                                                      in G/H                                  Unlike non-        for the
                                                     synthase                                   selective    treatment of
                                                        and                                     NSAIDs,      dysmenorrh
                                                  cyclooxygen                                 valdecoxib      ea or acute
                                                   ase)acts as                                  does not     pain. Unlike
                                                   an inhibitor                                   inhibit      celecoxib,
                                                    of protein                                   platelet      valdecoxib
     0198306-0000                                 prostaglandi                               aggregation.        lacks a
     0316684-0000

                                                   acts as an
                                                   agonist of
                                                  proteins with              gastrointesti
     16,16-dimethylprostaglandin_E2                             Peptic Ulcer
                                                  prostaglandi                nal agent
                                                  n E receptor
                                                     activity

     6-bromoindirubin-3-oxime
                                                                                   anti-
     adenosine_phosphate                                           Arrhythmia
                                                                                arrhythmic
     AG-012559
     AG-013608
     AH-23848
     AH-6809
                                                                                                 Alprenolol Alprenolol is
                                                                                                     non-        a non-
                                                                                                 selectively    selective
                                                                                               blocks beta- beta-blocker
                                                                                               1 adrenergic used in the
                                                                                                  receptors  treatment of
                                                                                               mainly in the hypertension
                                                                                                    heart,     , edema,
                                                                                                  inhibiting  ventricular
                                                                                                 the effects tachycardias
                                                                                                       of     , and atrial
                                                                                               epinephrine fibrillation.
                                                                                                      and      Alprenolol
                                      C             acts as a
                                                                                               norepinephri impairs AV
                                      0            blocker of
                                                                                               ne resulting       node
                                      7   ADRB1   proteins with
                                                                                                      in a    conduction
     alprenolol                       A   ADRB2       beta-
                                                                                               decrease in         and
                                      A   HTR1A    adrenergic
                                                                                                 heart rate    decreases
                                      0             receptor
                                      1
                                                                                                 and blood     sinus rate
                                                     activity
                                                                                               pressure. By     and may
                                                                                               binding beta- also increase
                                                                                                2 receptors      plasma
                                                                                                    in the   triglycerides
                                                                                               juxtaglomer         and
                                                                                                      ular     decrease
                                                                                                apparatus,        HDL-
                                                                                                 alprenolol   cholesterol
                                                                                                inhibits the     levels.
                                                                                                 production Alprenolol is
                                                                                                   of renin,    nonpolar
                                                                                                   thereby         and
                                                                                                  inhibiting hydrophobic,
                                      C                                                        angiotensin with low to
                                      1             acts as an
                                      0            inhibitor of                    anti-
     benfluorex                       A               protein                   hyperlipidpr
                                      X               insulin                    oteinemic
                                      0              receptor
                                      4
                                                     acts as an
                                                    inhibitor of
                                                      protein
     caffeic_acid
                                                  arachidonate
                                                         5-
                                                  lipoxygenase
     CAY-10397
                                                  anti-
cotinine                          Depression
                                               depressant
dehydrocholic_acid
                     R
                     0
                     6
deptropine           A
                     X
                     1
                     6
                                                                             Dinoproston
                                                                                    e is
                                                                             equivalent to
                                                                             prostaglandi
                                                            Dinoproston
                                                                             n E2 (PGE2).
                                                                    e
                                                                             It stimulates
                                                            administered
                                                                               labor and
                                                            intravaginall
                                                                             delivery and
                                                            y stimulates
                                                                                   thus
                                                                  the
                                                                              terminates
                                                            myometrium
                                                                              pregnancy.
                                                            of the gravid
                                                                             Dinoproston
                                                               uterus to
                                                                                e is also
                     G                                      contract in a
                                                                               capable of
                     0                                      manner that
                         PTGER2                                               stimulating
                     2                                       is similar to
                         PTGER1                                               the smooth
dinoprostone         A                                            the
                         PTGER4                                                muscle of
                     D                                      contractions
                         PTGER3                                                     the
                     0                                       seen in the
                     2
                                                                             gastrointesti
                                                             term uterus
                                                                              nal tract of
                                                            during labor,
                                                                               man. This
                                                             resulting in
                                                                             activity may
                                                                  the
                                                                                    be
                                                              evacuation
                                                                              responsible
                                                                 of the
                                                                                 for the
                                                             products of
                                                                                vomiting
                                                              conception
                                                                                 and/or
                                                               from the
                                                                             diarrhea that
                                                                uterus.
                                                                                  is not
                                                                              uncommon
                                                                                  when
                                                                             dinoprostone
                     S                                                         is used to
                     0
                     1
dipivefrine          E
                     A
                     0
                     2
                                                            Disopyramid      Disopyramid
                                                            e is a Type 1         e is an
                                                            antiarrhythm     antiarrhythm
                                                              ic drug (ie,        ic drug
                                                                similar to   indicated for
                                                            procainamid              the
                                                                   e and     treatment of
                                                            quinidine). It   documented
                                                              inhibits the     ventricular
                                                             fast sodium     arrhythmias,
                                                            channels. In         such as
                                                                  animal        sustained
                                                                  studies      ventricular
                     C                                      Disopyramid       tachycardia
                     0                                       e decreases     that are life-
                     1
                         SCN5A                    anti-        the rate of   threatening.
disopyramide         B            Arrhythmia
                         ORM1                  arrhythmic        diastolic       In man,
                     A
                                                            depolarizatio    Disopyramid
                     0
                     3
                                                             n (phase 4)            e at
                                                             in cells with    therapeutic
                                                             augmented           plasma
                                                            automaticity           levels
                                                             , decreases     shortens the
                                                            the upstroke       sinus node
                                                                 velocity       recovery
                                                                (phase 0)          time,
                                                                    and        lengthens
                                                                increases    the effective
                                                               the action      refractory
                                                                 potential   period of the
                                                              duration of     atrium, and
                                                                  normal           has a
                                                            cardiac cells,       minimal
                                                                                       Erythromyci      Erythromyci
                                                                                         n acts by            n is
                                                                                       penetrating     produced by
                                                                                      the bacterial       a strain of
                                                                                            cell         <i>Strepto
                                                                                        membrane             myces
                                                                                            and        erythraeus<
                                                                                        reversibly          /i> and
                                                                                        binding to       belongs to
                                                                                         the 50 S              the
                                                                                        subunit of        macrolide
                                                                                         bacterial         group of
                                                                                      ribosomes or       antibiotics.
                   D   J   S                                                             near the             After
                   1   0   0                                                          &ldquo;P&rd        absorption,
                   0   1   1
                                                             Bacterial     anti-          quo; or       erythromyci
erythromycin       A   F   A   rplV rplD
                                                            Infections   bacterial    donor site so       n diffuses
                   F   A   A
                                                                                       that binding      readily into
                   0   0   1
                   2   1   7
                                                                                          of tRNA        most body
                                                                                         (transfer     fluids. In the
                                                                                       RNA) to the       absence of
                                                                                      donor site is      meningeal
                                                                                         blocked.       inflammatio
                                                                                       Translocatio          n, low
                                                                                      n of peptides    concentratio
                                                                                         from the            ns are
                                                                                      &ldquo;A&rd          normally
                                                                                          quo; or        achieved in
                                                                                      acceptor site       the spinal
                                                                                           to the      fluid, but the
                                                                                      &ldquo;P&rd        passage of
                                                                                          quo; or          the drug
                                                                                      donor site is       across the
                                            acts as an
                                           inhibitor of
                                          protein DNA
                                          topoisomera
                                          se II acts as
                                           an inhibitor
                                            of protein
                                               solute
                                              carrier
                                            family 12,
                               ESR2 TOP2A                                  anti-          Not              Not
genistein                                 (potassium-
                               PTK2B                                     neoplastic     Available        Available
                                             chloride
                                          transporter)
                                             member
                                           5acts as an
                                           inhibitor of
                                          proteins with
                                             protein-
                                             tyrosine
                                              kinase
                                              activity
                   N
                   0                                                     analgesic
                   2                                       Inflammatio      anti-
glafenine          B
                                                               nPain   inflammator
                   G
                                                                             y
                   0
                   3
                                                                                      Sulfonylurea      Glipizide, a
                                                                                      s likely bind        second-
                                                                                           to ATP-      generation
                                                                                          sensitive    sulfonylurea,
                                                                                        potassium-     is used with
                                                                                          channel      diet to lower
                                                                                      receptors on           blood
                                                                                             the         glucose in
                                                                                         pancreatic    patients with
                                                                                      cell surface,        diabetes
                                                                                          reducing     mellitus type
                                                                                         potassium          II. The
                                                                                      conductance          primary
                   A                         acts as a                                and causing          mode of
                   1                                        Diabetes
                                            blocker of                                depolarizatio       action of
                   0                                        Mellitus,
                                           proteins with                                  n of the      glipizide in
glipizide          B           KCNJ1                         Type 2
                                            potassium                                  membrane.       experimenta
                   B                                        Metabolic
                                             channel                                  Depolarizati        l animals
                   0                                        Diseases
                   7                          activity                                        on        appears to
                                                                                         stimulates         be the
                                                                                        calcium ion     stimulation
                                                                                            influx        of insulin
                                                                                          through        secretion
                                                                                          voltage-        from the
                                                                                          sensitive    beta cells of
                                                                                           calcium       pancreatic
                                                                                         channels,      islet tissue
                                                                                           raising      and is thus
                                                                                       intracellular    dependent
                                                                                      concentratio             on
                                                                                      ns of calcium     functioning
                                                                                        ions, which    beta cells in
glycocholic_acid                                                                       induces the            the
                                       acts as an
                                      inhibitor of
                                     proteins with
                                         cAMP-
     H-89
                                      dependent
                                        protein
                                         kinase
                                        activity
                                                     Parkinson
     harmaline                                                    cns agent
                                                      Disease
                                                                                Hesperetin
                                                                                reduces or
                                                                               inhibits the     Hesperetin is
                                                                                 activity of    a cholesterol
                                                                                    acyl-          lowering
                                                                                coenzyme           flavanoid
                                                                              A:cholesterol       found in a
                                                                              acyltransfera       number of
                                                                                 se genes       citrus juices.
                                                                              (ACAT<sub>        It appears to
                                                                                 1</sub>             reduce
                                                                                     and          cholesteryl
                                                                               ACAT<sub>         ester mass
                                                                                 2</sub>)         and inhibit
                                                                    muscle
                                                                                   and it             apoB
                                                                   relaxant
                        MTTP SOAT1                   Neoplasms                    reduces       secretion by
     hesperetin                                                  (spasmolytic
                        Soat2                          Spasm                   microsomal        up to 80%.
                                                                    )anti-
                                                                               triglyceride       Hesperetin
                                                                  neoplastic
                                                                                  transfer        may have
                                                                                  protein        antioxidant,
                                                                                   (MTP)              anti-
                                                                                  activity.     inflammator
                                                                                Hesperetin          y, anti-
                                                                                also seems          allergic,
                                                                                      to        hypolipidemi
                                                                                upregulate              c,
                                                                                  the LDL       vasoprotecti
                                                                                 receptor.           ve and
                                                                              This leads to     anticarcinog
                                                                               the reduced      enic actions.
                                                                                 assembly
                                                                                     and
                                                                               secretion of
                                                                                  Striatal      Levodopa (L-
                                                                                   dopamine         dopa) is
                                                                                    levels in       used to
                                                                                symptomatic         replace
                                                                                  Parkinson's      dopamine
                                                                                 disease are         lost in
                                                                                  decreased      Parkinson's
                                                                                    by 60 to        disease
                                                                                80%, striatal       because
                                                                                dopaminergi        dopamine
                                                                                         c      itself cannot
                                                                                neurotransm        cross the
                                                                                  ission may     blood-brain
                    N                                                           be enhanced          barrier
                    0                                                                   by         where its
                    4
                        DRD1 DRD2                    Parkinson                    exogenous        precursor
     levodopa       B                                             cns agent
                        COMT PAH                      Disease                   supplementa           can.
                    A
                                                                                     tion of    However, L-
                    0
                    1
                                                                                   dopamine         DOPA is
                                                                                    through     converted to
                                                                                administrati    dopamine in
                                                                                      on of            the
                                                                                 dopamine's     periphery as
19                                                                                precursor,
                                                                                 levodopa. A
                                                                                                   well as in
                                                                                                 the CNS, so
                                                                                      small            it is
                                                                                  percentage    administered
                                                                                     of each         with a
                                                                                   levodopa       peripheral
                                                                                dose crosses          DDC
                                                                                  the blood-      (dopamine
                                                                                brain barrier   decarboxylas
     lobelanidine                                                                     and is     e) inhibitor
                    A                                               muscle
                    0                                              relaxant
                    3                                            (spasmolytic
     mebeverine     A                                 Spasm
                                                                   ) smooth
                    A
                                                                    muscle
                    0
                                                                   relaxant
                    4
                                                                          The actions     Metolazone
                                                                                of              is a
                                                                         metolazone       quinazoline
                                                                          result from    diuretic, with
                                                                         interference      properties
                                                                            with the        generally
                                                                        renal tubular       similar to
                                                                          mechanism       the thiazide
                                                                        of electrolyte    diuretics. A
                                                                        reabsorption         proximal
                                                                        . Metolazone         action of
                                acts as an                                    acts        metolazone
                               inhibitor of                              primarily to       has been
             C                   protein                                     inhibit         shown in
             0                                                              sodium         humans by
                                  solute
             3
                 SLC12A1          carrier                               reabsorption        increased
metolazone   B                                              diuretic
                 SLC12A3        family 12                                    at the       excretion of
             A
                             (sodium/chlo                                   cortical       phosphate
             0
             8                     ride                                  diluting site          and
                              transporters                                 and to a       magnesium
                             ), member 3                                lesser extent     ions and by
                                                                             in the       a markedly
                                                                           proximal         increased
                                                                          convoluted        fractional
                                                                            tubule.       excretion of
                                                                         Sodium and         sodium in
                                                                        chloride ions    patients with
                                                                        are excreted         severely
                                                                                in       compromise
                                                                        approximate      d glomerular
                                                                        ly equivalent       filtration.
                                                                           amounts.        This action
                                                                               The          has been
                                                                                         Nilutamide is
                                                                                                an
                                                                                         antineoplasti
                                                                                          c hormonal
                                                                                              agent
                                                                                            primarily
                                                                         Nilutamide
                                                                                          used in the
                                                                          competes
                                                                                         treatment of
                                                                              with
                                                                                             prostate
                                                                        androgen for
                                                                                             cancer.
                                                                         the binding
                                                                                         Nilutamide is
                                                                        of androgen
                                                                                             a pure,
                                                                          receptors,
                                                                                         nonsteroidal
             L                                                          consequentl
                                                                                               anti-
             0                                                            y blocking
                                                              anti-                        androgen
             2                                                          the action of
                                               Prostatic   neoplastic                     with affinity
nilutamide   B   ADRA1A AR                                              androgens of
                                              Neoplasms     hormone                      for androgen
             B                                                           adrenal and
                                                           antagonist                      receptors
             0                                                             testicular
             2
                                                                                          (but not for
                                                                        origin which
                                                                                         progestogen
                                                                          stimulate
                                                                                          , estrogen,
                                                                         the growth
                                                                                                or
                                                                          of normal
                                                                                         glucocorticoi
                                                                              and
                                                                                         d receptors).
                                                                          malignant
                                                                                         Consequentl
                                                                           prostatic
                                                                                                y,
                                                                            tissue.
                                                                                           Nilutamide
                                                                                           blocks the
                                                                                            action of
                                                                                         androgens of
                                                                                          adrenal and
                                                                                            testicular
                                                                                          origin which
                                                                                    Orlistat is a    Orlistat is a
                                                                                      reversible         lipase
                                                                                     inhibitor of    inhibitor for
                                                                                      lipases. It       obesity
                                                                                       exerts its   managemen
                                                                                    therapeutic       t that acts
                                                                                      activity in   by inhibiting
                                                                                   the lumen of            the
                                                                                   the stomach        absorption
                                                                                      and small        of dietary
                                                                                    intestine by     fats. At the
                                           acts as an                                 forming a     recommende
                                          inhibitor of                                  covalent             d
                 A                       proteins with                                bond with      therapeutic
                 0                                                                    the active     dose of 120
                                             lipase
                 8
                             PNLIP LPL    activityacts                                   serine        mg three
orlistat         A                                       Obesity
                             FASN            as an                                  residue site    times a day,
                 B
                                          inhibitor of                                 of gastric        orlistat
                 0
                 1                          protein                                       and           inhibits
                                          pancreatic                                  pancreatic      dietary fat
                                             lipase                                lipases. The       absorption
                                                                                     inactivated            by
                                                                                   enzymes are      approximate
                                                                                          thus        ly 30%. It
                                                                                    unavailable        works by
                                                                                   to hydrolyze        inhibiting
                                                                                   dietary fat in     pancreatic
                                                                                    the form of       lipase, an
                                                                                   triglycerides    enzyme that
                                                                                          into      breaks down
                                                                                     absorbable        fat in the
                                                                                       free fatty      intestine.
                 G   J   P                                                            acids and      Without this
                 0   0   0
                 1   1   1
ornidazole       A   X   A
                 F   D   B
                 0   0   0
                 6   3   3
                                                                                                     Oxybutynin
                                                                                                          is an
                                                                                                    antispasmod
                                                                                                            ic,
                                                                                                    anticholinerg
                                                                                   Oxybutynin
                                                                                                        ic agent
                                                                                     exerts a
                                                                                                    indicated for
                                                                                       direct
                                                                                                           the
                                                                                  antispasmod
                                                                                                    treatment of
                                                                                   ic effect on
                                                                                                     overactive
                                                                                      smooth
                                                                                                    bladder with
                                                                                   muscle and
                                                                                                    symptoms of
                                                                                   inhibits the
                                                                                                    urge urinary
                 G                                                                 muscarinic
                                           acts as an                                               incontinence
                 0                                                                   action of
                                          inhibitor of    Urinary                                     , urgency,
                 4           CHRM1                                                acetylcholine
                                            protein    Incontinence gastrointesti                          and
oxybutynin       B           CHRM2                                                  on smooth
                                         acetylcholine   Bladder,    nal agent                       frequency.
                 D           CHRM3                                                 muscle. No
                                          sterase (Yt Neurogenic                                     Oxybutynin
                 0                                                                   blocking
                 4                       blood group)                                                    relaxes
                                                                                  effects occur
                                                                                                        bladder
                                                                                    at skeletal
                                                                                                         smooth
                                                                                  neuromuscul
                                                                                                        muscle.
                                                                                   ar junctions
                                                                                                     Oxybutynin
                                                                                         or
                                                                                                    exhibits only
                                                                                    autonomic
                                                                                                     one-fifth of
                                                                                      ganglia
                                                                                                           the
                                                                                  (antinicotinic
                                                                                                    anticholinerg
                                                                                     effects).
                                                                                                    ic activity of
                                                                                                     atropine on
                                                                                                      the rabbit
                                                                                                       detrusor
                                                                                                     muscle, but
PF-00562151-00                                                                                       four to ten
PHA-00665752
PHA-00767505E
PHA-00816795
                 J
                 0
                 1                                                       anti-
pipemidic_acid   M                                       Infection     infective
                 B                                                       agent
                 0
                 4
                                                                           Like other
                                                                              beta-
                                                                          adrenergic
                                                                         antagonists,
                                                                            practolol
                                                                           competes
                                                                               with
                                                                          adrenergic
                                                                         neurotransm
                                                                          itters such
                                                                                as       Practolol is a
                                                                         catecholami         beta-
                                                                             nes for      adrenergic
                        C             acts as an                           binding at      receptor
                        0                                                sympathetic
                                    antagonist of                                         antagonist
                        7
                                        protein             cardiovascul    receptor       that has
practolol               A   ADRB1
                                     adrenergic,              ar agent     sites. Like   been used in
                        B
                                       beta-1-,                           propranolol         the
                        0
                        1              receptor                          and timolol,     emergency
                                                                            practolol    treatment of
                                                                            binds at        cardiac
                                                                            beta(1)-     arrhythmias.
                                                                          adrenergic
                                                                         receptors in
                                                                           the heart
                                                                         and vascular
                                                                             smooth
                                                                            muscle,
                                                                           inhibiting
                                                                          the effects
                                                                              of the
                                                                         catecholami
                                                               muscle          nes
                                                              relaxant
propantheline_bromide                               Spasm
                                                            (spasmolytic
                                                                  )
pseudopelletierine
salsolinol
                                      acts as an
                                     inhibitor of
                                        protein
                                      mitogen-
                                      activated
                                        protein
                                      kinase 11
                                      acts as an
                                     inhibitor of
                                        protein
                                    prostaglandi
                                           n-
                                    endoperoxid
                                    e synthase 2
                                    (prostagland
                                        in G/H
SB-202190
                                       synthase
                                          and
                                    cyclooxygen
                                     ase)acts as
                                     an inhibitor
                                     of proteins
                                        with MP
                                        kinase
                                    activity acts
                                         as an
                                     inhibitor of
                                        protein
                                      mitogen-
                                      activated
                                        protein
                                      kinase 14
STOCK1N-28457
STOCK1N-35696
                                                                                        Sulfapyridine
                                                                                               is a
                                                                                        sulfonamide
                                                                                          antibiotic.
                                                                                               The
                                                                       Sulfapyridine    sulfonamide
                                                                              is a            s are
                                                                        competitive        synthetic
                                                                         inhibitor of   bacteriostati
                                                                           bacterial    c antibiotics
                                                                             para-       with a wide
                                                                       aminobenzoi        spectrum
                                                                             c acid     against most
                J                                                         (PABA), a          gram-
                0                                                                       positive and
                                                                       substrate of
                1
                                           Bacterial       anti-        the enzyme      many gram-
sulfapyridine   E   suf3
                                          Infections     bacterial     dihydroptero        negative
                B
                                                                              ate        organisms.
                0
                4                                                       synthetase.       However,
                                                                       The inhibited    many strains
                                                                         reaction is          of an
                                                                       necessary in       individual
                                                                             these      species may
                                                                          organisms     be resistant.
                                                                            for the     Sulfonamide
                                                                       synthesis of         s inhibit
                                                                          folic acid.   multiplicatio
                                                                                        n of bacteria
                                                                                        by acting as
                                                                                         competitive
                                                                                        inhibitors of
                                                                                         <i>p</i>-
                                                                                        aminobenzoi
                                                                     In contrast
                                                                       to most
                                                                         other
                                                                    neuroleptics
                                                                     which block        Sulpiride is a
                                                                         both            substituted
                                                                      dopamine           benzamide
                                                                      D1 and D2           derivative
                                                                      receptors,             and a
                                                                     Sulpiride is          selective
                                                                         more             dopamine
                                                                    selective and             D2
                N                                                         acts            antagonist
                0            acts as an
                                                                     primarily as             with
                5          antagonist of                anti-emetic
                                         Depression                  a dopamine         antipsychotic
sulpiride       A   DRD2      protein                      anti-
                                          Vomiting                         D2                 and
                L            dopamine                   depressant
                0                                                    antagonist.        antidepressa
                            receptor D2
                1                                                      Sulpiride          nt activity.
                                                                      appears to             Other
                                                                     lack effects        benzamide
                                                                           on            derivatives
                                                                    norepinephri            include
                                                                          ne,            metoclopra
                                                                    acetylcholine            mide,
                                                                     , serotonin,       tiapride, and
                                                                      histamine,          sultopride.
                                                                     or gamma-
                                                                    aminobutyric
                                                                    acid (GABA)
                                                                      receptors.

                             acts as an
                            inhibitor of                   anti-
                                         Hypersensiti
zaprinast                     protein                    asthmatic
                                         vityAsthma
                           Phosphodies                  anti-allergy
                               terase
0317956-0000
                                                                                 Indapamide           Indapamide
                                                                                   blocks the               is an
                                                                                       slow           antihyperten
                                                                                  component             sive and a
                                                                                   of delayed           diuretic. It
                                                                                     rectifier           contains
                                                                                   potassium          both a polar
                                                                                 current (IKs)          sulfamoyl
                                                                                     without          chlorobenza
                                                                                  altering the        mide moiety
                                                                                       rapid           and a lipid-
                                                                                  component               soluble
                                                                                  (IKr) or the        methylindoli
                            C                                                         inward           ne moiety.
                            0                                                        rectifier        Indapamide
                            3                                          anti-
                                KCNQ1                   Hypertensio                  current.             bears a
     indapamide             B                                       hypertensive
                                KCNE1                       n                     Specifically          structural
                            A                                         diuretic
                                                                                  it blocks or        similarity to
                            1
                            1
                                                                                 antagonizes           the triazide
                                                                                   the action            diuretics
                                                                                 the proteins           which are
                                                                                  KCNQ1 and              known to
                                                                                     KCNE1.              decrease
                                                                                 Indapamide              vascular
                                                                                      is also             smooth
                                                                                   thought to             muscle
                                                                                    stimulate           reactivity.
                                                                                        the            However, it
                                                                                  synthesis of             differs
                                                                                        the             chemically
                                                                                 vasodilatory            from the
                                                                                 hypotensive           thiazides in
                                                                                 prostaglandi
                                                                                  Mexiletine,          that it does
                                                                                                      Mexiletine is
                                                                                             like          a local
                                                                                        lidocaine,     anesthetic,
                                                                                      inhibits the    antiarrhythm

20                                                                                        inward
                                                                                          sodium
                                                                                                          ic agent
                                                                                                       (Class Ib),
                                                                                          current      structurally
                                                                                      required for      similar to
                                                                                     the initiation     lidocaine,
                                                                                            and         but orally
                                                                                       conduction          active.
                                                                                     of impulses,       Mexiletine
                                                                                            thus          has fast
                            C                                                        reducing the       onset and
                            0                                                         rate of rise          offset
                            1
                                                                        anti-        of the action        kinetics,
     mexiletine             B   SCN5A                   Arrhythmia
                                                                     arrhythmic         potential,       meaning
                            B
                                                                                         Phase 0.        that they
                            0
                            2
                                                                                        Mexiletine    have little or
                                                                                        decreases      no effect at
                                                                                     the effective    slower heart
                                                                                        refractory      rates, and
                                                                                     period (ERP)     more effects
                                                                                       in Purkinje       at faster
                                                                                     fibers in the     heart rates.
                                                                                       heart. The      It shortens
                                                                                      decrease in       the action
                                                                                         ERP is of       potential
                                                                                           lesser        duration,
                                                                                       magnitude          reduces
                                                                                         than the     refractorines
                                                                                      decrease in          s, and
     PHA-00851261E                                                                         action       decreases

                            A            acts as an
                            0
                                        antagonist of
                            2
                                        proteins with                gastrointesti
     proglumide             B
                                        cholecystoki                  nal agent
                            X
                            0           nin receptor
                            6              activity

                                                         Bacterial      anti-
     sulfachlorpyridazine
                                                        Infections    bacterial
     0173570-0000




21
                                                                 Like all beta-    Cefamandole
                                                                      lactam         is a broad-
                                                                   antibiotics,       spectrum
                                                                 cefamandole       cephalospori
                                                                     binds to       n antibiotic.
                                                                      specific     The clinically
                                                                    penicillin-    used form of
                                                                      binding      cefamandole
                                                                     proteins            is the
                                                                       (PBPs)          formate
                                                                      located            ester
                                                                    inside the     cefamandole
                                                                 bacterial cell        nafate, a
                        J                                        wall, causing         prodrug
                        0                                                the           which is
                        1                            anti-
                                                                  inhibition of    administered
     cefamandole        D   pbpA    Infection      infective
                                                                 the third and     parenterally.
                        C                            agent
                                                                 last stage of            The
                        0
                        3
                                                                 bacterial cell     bactericidal
                                                                        wall           action of
21                                                                 synthesis.      cefamandole
                                                                   Cell lysis is   results from
                                                                        then        inhibition of
                                                                 mediated by           cell-wall
                                                                 bacterial cell       synthesis.
                                                                        wall       Cephalospori
                                                                     autolytic        ns have in
                                                                     enzymes       vitro activity
                                                                      such as         against a
                                                                 autolysins; it      wide range
                                                                   is possible         of gram-
                                                                        that       positive and
                        M                                        cefamandole            gram-
                        0                            muscle
                        3                           relaxant
     mephenesin         B
                                                  (spasmolytic
                        X
                                                        )
                        0
                        6
     PNU-0230031
     PNU-0251126
     PNU-0293363
                                                                   Alkylating      Chlorambucil
                                                                 agents work            is an
                                                                    by three       antineoplasti
                                                                    different      c in the class
                                                                 mechanisms        of alkylating
                                                                        : 1)        agents and
                                                                  attachment         is used to
                                                                     of alkyl      treat various
                                                                   groups to          forms of
                                                                  DNA bases,           cancer.
                                                                  resulting in       Alkylating
                                                                    the DNA          agents are
                                                                      being          so named
                        L           Neoplasms                     fragmented         because of
                        0                                           by repair       their ability
                                    Leukemia,
                        1
                                   Lymphocytic       anti-        enzymes in        to add alkyl
     chlorambucil       A
                                        ,          neoplastic          their          groups to
                        A
                                   ChronicBreas                   attempts to           many
                        0
                        2          t Neoplasms                    replace the      electronegati
                                                                    alkylated        ve groups
                                                                      bases,            under
                                                                   preventing        conditions
                                                                       DNA           present in
                                                                    synthesis        cells. They
                                                                    and RNA         stop tumor
                                                                 transcription       growth by
                                                                    from the       cross-linking
                                                                     affected          guanine
                                                                 DNA, 2) DNA           bases in
                                                                  damage via       DNA double-
                                                                        the        helix strands
                                                                 formation of         - directly
     ciclacillin                                                   cross-links        attacking
     homosalate
                                     Bacterial       anti-
     levcycloserine
                                    Infections     bacterial
     lithocholic_acid




22
                                                                                 Nialamide
                                                                                was one of
                                                                                   the first
                                                                                    MAOI
                                                                              (monoamine
                      N                                                            oxidase
                      0                                                           inhibitor)
                      6                                                       antidepressa
                                                                                                    Not
     nialamide        A                                                            nts. It is
                                                                                                  Available
                      F                                                          chemically
                      0                                                          related to
                      2                                                        iproniazide,
                                                                                   another
                                                                                    MAOI
                                                                              derived from
                                                                                isonicotinic
                                                                                   acid. //
                                                                                                  Phenelzine
                                                                                                belongs to a
                                                                                                      class of
                                                                                                antidepressa
                                                                                                   nts called
                                                                                                 monoamine
22                                                                                                    oxidase
                                                                                                    inhibitors
                                                                                    The             (MAOIs).
                                                                               irreversible       Phenelzine
                                                                              inhibition of         works by
                                      acts as an
                                                                                  MAO by          irreversibly
                                     inhibitor of
                                                                               phenelzine       blocking the
                      N             proteins with
                                                                                causes an          action of a
                      0                 amine
                                                                               increase in           chemical
                      6                oxidase                    cns agent
                          AOC3 MAOB                                           the levels of        substance
     phenelzine       A              activityacts   Depression      anti-
                          MAOA                                                  serotonin,         known as
                      F                 as an                    depressant
                                                                              norepinephri       monoamine
                      0              inhibitor of
                      3                                                           ne, and             oxidase
                                       protein
                                                                              dopamine in       (MAO) in the
                                     monoamine
                                                                              the neuron,            nervous
                                      oxidase A
                                                                                 relieving           system.
                                                                               depressive             Within
                                                                               symptoms.             neurons,
                                                                                                        MAO
                                                                                                  appears to
                                                                                                regulate the
                                                                                                     levels of
                                                                                                monoamines
                                                                                                     released
                                                                                                       upon
                                                                                                     synaptic
     Prestwick-1080                                                                              firing. Since
     Prestwick-1100
     Prestwick-984
                                                                                     As a       Quinethazon
                                                                                  diuretic,           e is a
                                                                              quinethazon           thiazide
                                                                                 e inhibits     diuretic used
                                                                                   active           to treat
                                                                                  chloride      hypertension
                                                                              reabsorption       . It inhibits
                                                                               at the early     Na<sup>+<
                                                                              distal tubule     /sup>/Cl<su
                                                                              via the Na-Cl      p>-</sup>
                                                                              cotransporte      reabsorption
                                                                                r, resulting       from the
                                                                                    in an             distal
                      C                                                         increase in      convoluted
                      0                                                              the          tubules in
                          SLC12A3
                      3
                          CA1 CA2                                              excretion of     the kidneys.
     quinethazone     B
                          CA4                                                     sodium,         Thiazides
                      A
                          KCNMA1                                              chloride, and      also cause
                      0
                      2
                                                                                   water.            loss of
                                                                                 Thiazides        potassium
                                                                                     like            and an
                                                                              quinethazon        increase in
                                                                              e also inhibit     serum uric
                                                                                sodium ion            acid.
                                                                                 transport        Thiazides
                                                                                 across the        are often
                                                                              renal tubular     used to treat
                                                                                epithelium      hypertension
                                                                                  through         , but their
                                                                                 binding to     hypotensive
                                                                               the thiazide      effects are
                                                                                  sensitive            not
     santonin                                                                     sodium-        necessarily
                                                      acts as an
                                                     inhibitor of
                                                        protein
                                                    prostaglandi
                                                           n-
                                                    endoperoxid
                                                    e synthase 2
                                                    (prostagland
                                                        in G/H
                                                       synthase
     NS-398                                               and
                                                    cyclooxygen
                                                     ase)acts as
                                                     an inhibitor
                                                     of proteins
                                                         with
                                                    prostaglandi
                                                           n-
                                                    endoperoxid
                                                     e synthase
                                                        activity

                                                                                           Pioglitazone    Pioglitazone,
                                                                                             acts as an    a member of
                                                                                             agonist at       the drug
                                                                                            peroxisome     group known
                                                                                            proliferator        as the
                                                                                              activated    thiazolidined
                                                                                              receptors       iones or
                                                                                             (PPAR) in         "insulin
                                                                                                target      sensitizers",
                                                                                             tissues for         is not
                                                                                                insulin      chemically
                                                                                            action such             or
                                                                                            as adipose      functionally
                                        A                                                       tissue,      related to
                                        1                                                      skeletal      the alpha-
                                        0
                                                                                           muscle, and      glucosidase
     pioglitazone                       B   PPARG
                                                                                                 liver.      inhibitors,
                                        G
                                                                                           Activation of           the
                                        0
                                        3
                                                                                                PPAR-       biguanides,
                                                                                               gamma            or the
                                                                                              receptors     sulfonylurea
23                                                                                            regulates             s.
                                                                                                   the      Pioglitazone
                                                                                           transcription       targets
                                                                                             of insulin-        insulin
                                                                                            responsive       resistance
                                                                                                 genes      and, hence,
                                                                                            involved in    is used alone
                                                                                            the control           or in
                                                                                             of glucose     combination
                                                                                            production,     with insulin,
                                                                                             transport,     metformin,
                                                      acts as an                                  and               or
                                                     inhibitor of
                                                    proteins with
                                                     MAP kinase
                                                     activity acts
                                                         as an
                                                     inhibitor of
                                                        protein
                                                    interleukin 1
                                                       receptor,
                                                      type I acts
                                                         as an
                                                    antagonist of
                                                    proteins with
                                                    prostaglandi
                                                                                  anti-
                                                      n receptor Inflammatio
     SB-203580                                                               inflammator
                                                     activity acts    n
                                                                                   y
                                                         as an
                                                     inhibitor of
                                                        protein
                                                    prostaglandi
                                                           n-
                                                    endoperoxid
                                                    e synthase 2
                                                    (prostagland
                                                        in G/H
                                                       synthase
                                                          and
                                                    cyclooxygen
                                                     ase)acts as
                                                     an inhibitor
                                                      of proteins
     SC-19220                                        with protein
     docosahexaenoic_acid_ethyl_ester
     splitomicin



24
                                                    acts as an
                                                   inhibitor of
24   U0125
                                                  proteins with
                                                   MAP kinase
                                                      kinase
                                                      kinase
                                                     activity
                                                                                                 The       Acetazolami
                                                                                          anticonvulsa          de is a
                                                                                          nt activity of        potent
                                                                                          Acetazolami          carbonic
                                                                                              de may         anhydrase
                                                                                          depend on a         inhibitor,
                                                                                                direct      effective in
                                                                                          inhibition of     the control
                                                                                              carbonic          of fluid
                                                                                          anhydrase in     secretion, in
                                                                                             the CNS,             the
                                                                                                which      treatment of
                                                                                            decreases           certain
                           S                        acts as an                                 carbon        convulsive
                           0                                                                   dioxide        disorders
                                                   inhibitor of
                           1           CA1 AQP1                                 anti-
                                                  proteins with                             tension in       and in the
     acetazolamide         E           CA12 CA2                   Seizures   convulsant
                                                    carbonate                                    the       promotion of
                           C           Ca14                                   diuretic
                                                  dehydratase                              pulmonary         diuresis in
                           0
                           1                         activity                             alveoli, thus    instances of
                                                                                            increasing       abnormal
                                                                                               arterial          fluid
                                                                                               oxygen        retention.
                                                                                          tension. The     Acetazolami
                                                                                              diuretic      de is not a
                                                                                                effect       mercurial
                                                                                           depends on          diuretic.
                                                                                                 the        Rather, it is
                                                                                          inhibition of            a
                                                                                              carbonic     nonbacterios
                                                                                           anhydrase,            tatic
                                                                                             causing a     sulfonamide
                                                                                          reduction in     possessing a
     atracurium_besilate                                                                         the          chemical
                                                                                          Benzonatate
                                                                                                  acts
                                                                                          peripherally,
                                                                                          anesthetizin
                                                                                          g the stretch
                                                                                           receptors of
                                                                                                         Benzonatate
                                                                                                 vagal
                                                                                                            , a non-
                                                                                              afferent
                                                                                                            narcotic
                                                                                           fibers in the
                                                                                                          antitussive
                                                                                          alveoli of the
                                                                                                              agent
                                                                                                lungs,
                                                                                                          chemically
                                                                                          bronchi, and
                                                                                                           related to
                                                                                               pleura.
                           R                                                                              tetracaine
                                                                                                When
                           0                                                                               and other
                                                                                              applied
                           5                                                                              ester-type
                                                                                               locally,
     benzonatate           D           SCN5A                                                                   local
                                                                                          Benzonatate
                           B                                                                             anesthetics,
                                                                                          binds within
                           0                                                                               is used to
                           1
                                                                                                  the
                                                                                                            suppress
                                                                                           intracellular
                                                                                                              cough
                                                                                             portion of
                                                                                                          associated
                                                                                              voltage-
                                                                                                           with both
                                                                                                gated
                                                                                                           acute and
                                                                                              sodium
                                                                                                             chronic
                                                                                             channels,
                                                                                                          respiratory
                                                                                            decreasing
                                                                                                          conditions.
                                                                                            the rate of
                                                                                            membrane
                                                                                          depolarizatio
                                                                                                n and
                                                                                            increasing
                                                                                                  the
                           A   D   S                                                      threshold for
                           1   0   0
                           1   3   1
     dexpanthenol          H   A   X
                           A   X   A
                           3   0   1
                           0   3   2
     epirizole




25
                                                                              Mefenamic
                                                                              acid binds
                                                                                                Mefenamic
                                                                                  the
                                                                                                  acid, an
                                                                            prostaglandi
                                                                                                 anthranilic
                                                                            n synthetase
                                                                                                    acid
                                                                               receptors
                                                                                               derivative, is
                                                                             COX-1 and
                                                                                               a member of
                                                                                COX-2,
                                                                                                     the
                                                                               inhibiting
                                                                                                 fenamate
                                                                            the action of
                                                                                                  group of
                                                                            prostaglandi
                                                                                               nonsteroidal
                                                                                    n
                                                                                                    anti-
                      M                                                      synthetase.
                                       acts as an                                              inflammator
                      0                                  Pain                   As these
                                      antagonist of                                               y drugs
                      1                              Rheumatic       anti-     receptors
                              PTGS2   proteins with                                            (NSAIDs). It
     mefenamic_acid   A                               Diseases  inflammator have a role
                              PTGS1   prostaglandi                                             exhibits anti-
                      G                             Inflammatio       y       as a major
25                    0                n receptor                                              inflammator
                                                          n                  mediator of
                      1                  activity                                              y, analgesic,
                                                                            inflammatio
                                                                                                    and
                                                                              n and/or a
                                                                                                antipyretic
                                                                                role for
                                                                                                 activities.
                                                                              prostanoid
                                                                                                 Similar to
                                                                             signaling in
                                                                                                   other
                                                                                activity-
                                                                                                  NSAIDs,
                                                                              dependent
                                                                                                mefenamic
                                                                              plasticity,
                                                                                               acid inhibits
                                                                                  the
                                                                                               prostaglandi
                                                                            symptoms of
                                                                                                      n
                                                                                pain are
                                                                                                synthetase.
                                                                             temporarily
                                                                               reduced.

                      P
                      0
                      2
     metrifonate      B
                      B
                      0
                      1
                      C   G
                      0   0
                      4   4
     moxisylyte       A   B
                      X   E
                      1   0
                      0   6
                                                                                               Sulfacetamid
                                                                                                    e is a
                                                                                               sulfonamide
                                                                              Sulfacetamid       antibiotic.
                                                                                    e is a            The
                                                                               competitive     sulfonamide
                                                                               inhibitor of          s are
                                                                                  bacterial       synthetic
                                                                                    para-      bacteriostati
                                                                              aminobenzoi      c antibiotics
                                                                                    c acid      with a wide
                                                                               (PABA), an        spectrum
                                                                                  essential    against most
                      S                                                        component            gram-
                      0                                                                        positive and
                                                                              for bacterial
                      1                                            anti-
                                                     Bacterial                     growth      many gram-
     sulfacetamide    A       pabB                               bacterial
                                                    Infections                  (according        negative
                      B                                          antiseptic
                                                                                    to the      organisms.
                      0
                      4                                                            Woods-        However,
                                                                                    Fildes     many strains
                                                                              theory). The           of an
                                                                                  inhibited      individual
                                                                                reaction is    species may
                                                                              necessary in     be resistant.
                                                                                    these      Sulfonamide
                                                                                organisms          s inhibit
                                                                                   for the     multiplicatio
                                                                              synthesis of     n of bacteria
                                                                                 folic acid.   by acting as
                                                                                                competitive
                                                                                               inhibitors of
                                                                                                <i>p</i>-
                                                                                               aminobenzoi
                                                                    Triflupromaz     Triflupromaz
                                                                     ine binds to        ine is a
                                                                          the        member of a
                                                                      dopamine           class of
                                                                        D1 and       drugs called
                                                                      dopamine       phenthiazine
                                                                    D2 receptors     s, which are
                                                                     and inhibits      dopamine
                                                                         their            D1/D2
                                                                    activity. The       receptor
                                                                     mechanism       antagonists.
                                                                     of the anti-    Phenothiazin
                                                                    emetic effect     es are used
                  N                                                     is due          to treat
                  0                                    anti-emetic predominant           serious
                              DRD1 DRD2
                  5                                    tranquilizer      ly to        mental and
                              CHRM1
triflupromazine   A                                       anti-
                              CHRM2                                  blockage of       emotional
                  A                                     psychotic
                              HTR2B                                       the          disorders,
                  0                                   (neuroleptic) dopamine           including
                  5
                                                                          D2         schizophreni
                                                                    neurotransm       a and other
                                                                         itter         psychotic
                                                                     receptors in    disorders. It
                                                                          the           reduces
                                                                    chemorecept         anxiety,
                                                                      or trigger       emotional
                                                                     zone (CTZ)       withdrawal,
                                                                    and vomiting     hallucination
                                                                        centre.             s,
                                                                    Triflupromaz     disorganized
                                                                      ine blocks       thoughts,
                                                                          the           blunted
                                                                    neurotransm
                                                                     Viral (HSV-      mood, and
                                                                       1, HSV-2
                                                                                        Aciclovir
                                                                      and VZV)
                                                                                        (INN) or
                                                                      thymidine
                                                                                        acyclovir
                                                                        kinase
                                                                                         (USAN,
                                                                       converts
                                                                                     former BAN)
                                                                     aciclovir to
                                                                                            is a
                                                                    the aciclovir
                                                                                        synthetic
                                                                    monophosph
                                                                                     deoxyguano
                                                                    ate, which is
                                                                                      sine analog
                                                                          then
                                                                                     and it is the
                                                                    converted to
                                                                                       prototype
                                                                           the
                  D   J   S                                                             antiviral
                                                                    diphosphate
                  0   0   0                                                          agent that is
                                                                      by cellular
                  6   5   1                                                          activated by
                              UL30 28 TK     Virus                    guanylate
aciclovir         B   A   A                            anti-viral                          viral
                              NP           Diseases                  kinase, and
                  B   B   D                                                            thymidine
                                                                    finally to the
                  0   0   0                                                           kinase. The
                  3   1   3
                                                                    triphosphate
                                                                                        selective
                                                                            by
                                                                                       activity of
                                                                    phosphoglyc
                                                                                      aciclovir is
                                                                    erate kinase,
                                                                                       due to its
                                                                    phosphoenol
                                                                                       affinity for
                                                                       pyruvate
                                                                                            the
                                                                    carboxykinas
                                                                                       thymidine
                                                                        e, and
                                                                                          kinase
                                                                       pyruvate
                                                                                         enzyme
                                                                        kinase.
                                                                                      encoded by
                                                                       Aciclovir
                                                                                        HSV and
                                                                    triphosphate
                                                                                           VZV.
                                                                    competitivel
                                                                       y inhibits
                                                                      viral DNA
                                                                                      The          Finasteride
                                                                                 mechanism        is indicated
                                                                                 of action of         for the
                                                                                 Finasteride     treatment of
                                                                                 is based on    male pattern
                                                                                       its           hair loss
                                                                                 preferential   (androgeneti
                                                                                inhibition of      c alopecia)
                                                                                 Type II 5a-     in men only.
                                         acts as an                               reductase,       Finasteride
                                        inhibitor of                                   an               is a
                                           protein                              intracellular     competitive
                                         steroid-5-                             enzyme that       and specific
                   D   G                   alpha-                               converts the       inhibitor of
                   1   0                                                           androgen        Type II 5a-
                                        reductase,
                   1   4                             Neoplasms
                                            alpha                    anti-      testosterone       reductase,
     finasteride   A   C   SRD5A1 AR                  Prostatic
                                        polypeptide                neoplastic      into DHT.             an
                   X   B                             Hyperplasia
                                        2 (3-oxo-5                              Inhibition of     intracellular
                   1   0
                   0   1                   alpha-                                Type II 5a-     enzyme that
                                       steroid delta                               reductase     converts the
                                              4-                                  blocks the        androgen
                                       dehydrogena                                peripheral     testosterone
                                        se alpha 2)                               conversion        into DHT.
                                                                                       of        Two distinct
                                                                                testosterone    isozymes are
                                                                                    to DHT,          found in
                                                                                 resulting in      mice, rats,
                                                                                  significant       monkeys,
                                                                                decreases in            and
                                                                                  serum and          humans:
                                                                                  tissue DHT       Type I and
                                                                                concentratio       II. Each of
                                                                                       ns.
                                                                                Guanabenz's            these
                                                                              antihyperten
                                                                              sive effect is
                                                                                thought to
                                                                                 be due to
                                                                              central alpha-
                                                                                adrenergic
                                                                               stimulation,
                                                                              which results
                                                                                     in a
                                                                                decreased
                                                                              sympathetic Guanabenz,
                                                                                 outflow to   a centrally
                                        acts as an
                                                                                 the heart,     acting
                                        agonist of
                                                                              kidneys, and &alpha;-2
                                       proteins with
                                                     Hypertensio    anti-       peripheral    adrenergic
     guanabenz             ADRA2A        alpha2-
                                                         n       hypertensive vasculature     agonist, is
                                        adrenergic
                                                                                in addition indicated for
26                                       receptor
                                          activity
                                                                                     to a    treatment of
                                                                                decreased hypertension
                                                                               systolic and        .
                                                                                  diastolic
                                                                                    blood
                                                                              pressure and
                                                                                   a slight
                                                                                 slowing of
                                                                                pulse rate.
                                                                                  Chronic
                                                                              administrati
                                                                                    on of
                                                                               guanabenz
                                                                               also causes
                                                                               a decrease
                                                                             Lisuride is
                                                                              an anti-
                                                                             Parkinson
                                                                                drug
                                                                            chemically
                                                                             related to
                                                                                 the
                                                                           dopaminergi
                                                                             c ergoline
                                                                            Parkinson's
                                                                               drugs.
                                                                              Lisuride
                                                                           binds to the
               G   N                                                         5-HT(1A)
               0   0                                                           and 5-
               2   2
                       DRD1 HTR1A                                           HT(2A/2C)          Not
lisuride       C   C
                       DRD2                                                receptors. It     Available
               B   A
                                                                               is also
               0   0
               2   7
                                                                            thought to
                                                                            bind to the
                                                                             dopamine
                                                                           receptor and
                                                                            to act as a
                                                                             dopamine
                                                                              agonist.
                                                                           Evidence has
                                                                                 also
                                                                              emerged
                                                                           that Lisuride
                                                                           also binds to
                                                                                 the
                                                                             Histamine
                                      acts as an                           H1 receptor.
                                    antagonist of
thioperamide                           protein
                                      histamine
                                     receptor H3
                                                                                  Like       Similar to
                                                                            propranolol     propranolol
                                                                           and nadolol,    and nadolol,
                                                                                timolol     timolol is a
                                                                              competes          non-
                                                                                  with       selective,
                                                                             adrenergic         beta-
                                                                           neurotransm      adrenergic
                                                                             itters such      receptor
                                                                                   as       antagonist.
                                      acts as an                            catecholami    Timolol does
                                    antagonist of                               nes for       not have
                                    protein Beta                             binding at      significant
               C   S                 adrenergic                                beta(1)-       intrinsic
               0   0                                                         adrenergic    sympathomi
                                    receptor acts
               7   1                                                        receptors in   metic, direct
                       ADRB1            as an
timolol        A   E
                       ADRB2        antagonist of                             the heart     myocardial
               A   D
                                       protein                             and vascular     depressant,
               0   0
                                     adrenergic,                                smooth         or local
               6   1
                                       beta-2-,                             muscle and       anesthetic
                                      receptor,                                beta(2)-    (membrane-
                                       surface                              receptors in    stabilizing)
                                                                           the bronchial   activity, but
                                                                           and vascular    does possess
                                                                                smooth      a relatively
                                                                               muscle.     high degree
                                                                               Beta(1)-        of lipid
                                                                               receptor      solubility.
                                                                              blockade        Timolol,
                                                                            results in a        when
                                                                            decrease in        applied
                                                                            resting and     topically to
                                                               smooth          exercise    the eye, has
                                                               muscle
                                                              relaxant
adiphenine                                          Spasm      muscle
                                                              relaxant
                                                            (spasmolytic
                                                                  )
                                                                                        Carbimazole
                                                                      Carbimazole
                                                                                              is a
                                                                          is an
                                                                                         carbethoxy
                                                                       aitithyroid
                                                                                        derivative of
                                                                       agent that
                                                                                        methimazole
                                                                        decreases
                                                                                              . Its
                                                                       the uptake
                                                                                         antithyroid
                        H                                                  and
                                                                                        action is due
                        0                                             concentratio
                                                                                             to its
                        3                                                  n of
                                                                                         conversion
     carbimazole        B   TPO                                         inorganic
                                                                                               to
                        B                                               iodine by
                        0                                                               methimazole
                                                                        thyroid, it
                        1                                                                    after
                                                                      also reduces
                                                                                         absorption.
                                                                           the
                                                                                        It is used to
                                                                      formation of
                                                                                             treat
                                                                            di-
                                                                                        hyperthyroid
                                                                      iodotyrosine
                                                                                           ism and
                                                                           and
                                                                                        thyrotoxicosi
                                                                       thyroxine.
                                                                                                s.
     chlorogenic_acid
     clorsulon
                                                                          Dapsone       Dapsone is a
                                                                      acts against       sulfone with
                                                                      bacteria and             anti-
                                                                       protozoa in       inflammator
                                                                         the same                y
                                                                           way as       immunosupp
                                                                      sulphonamid             ressive
                                                                      es, that is by    properties as
                                                                         inhibiting           well as
                                                                             the        antibacterial
                                                                       synthesis of             and
                                                                       dihydrofolic        antibiotic
                                                                      acid through        properties.
                        J                                              competition        Dapsone is
                        0                                                               the principal
                                            Leprosy                     with para-
                        4                                  anti-
                            folP2 folP1   Pneumonia,                       amino-          drug in a
     dapsone            B                                infective
                            DHFR          Pneumocysti                 benzoate for         multidrug
                        A                                  agent
                                               s                         the active         regimen
                        0
                        2                                                  site of      recommende
                                                                      dihydroptero          d by the
                                                                             ate        World Health
                                                                       synthetase.      Organization
                                                                         The anti-            for the
                                                                      inflammator       treatment of
                                                                        y action of       leprosy. As
                                                                        the drug is          an anti-
                                                                      unrelated to          infective
                                                                              its         agent, it is
                                                                      antibacterial     also used for
                                                                      action and is          treating
                                                                      still not fully   malaria and,
                                                                      understood.        recently, for
     etiocholanolone                                                                    Pneumocysti
                        S
                        0
                        1
     homatropine        F
                        A
                        0
                        5
     isoflupredone
                        A
                        0
                        3
     isometheptene      A
                        X
                        1
                        0
                                                           anti-
                                          Inflammatio inflammator
     isoxicam
                                          nFever Pain yanti-pyretic
                                                        analgesic




27
                                                                                      Ketotifen is
                                                                                      a relatively
                                                                                        selective,
                                                                                           non-
                                                                                     competitive
                                                                                        histamine
                                                                                       antagonist
27                                                                                          (H1-
                                                                                        receptor)
                                                                                                       Ketotifen is
                                                                                                      a fast acting
                                                                                        and mast            non-
                                                                                             cell     competitive
                                                                                        stabilizer.     histamine
                                                                                        Ketotifen      antagonist.
                     R   S                                                            inhibits the       It inhibits
                     0   0                  acts as an                     anti-
                                                                                        release of     the release
                     6   1                antagonist of                 asthmatic
                             PDE7A HRH1                    Pruritus                    mediators      of mediators
     ketotifen       A   G                   protein                       anti-
                             PDE7B                         Asthma                      from mast        from mast
                     X   X                  histamine                   histamine
                                                                                            cells      cells. It is a
                     1   0                 receptor H1                 anti-pruritic
                     7   8
                                                                                      involved in           non-
                                                                                     hypersensiti     bronchodilat
                                                                                             vity             or
                                                                                        reactions.    antiasthmati
                                                                                       Decreased           c drug
                                                                                      chemotaxis      (when taken
                                                                                            and           orally).
                                                                                     activation of
                                                                                      eosinophils
                                                                                         has also
                                                                                           been
                                                                                     demonstrate
                                                                                     d. Ketotifen
                                                                                     also inhibits
                                                                        antiseptic         cAMP
                                                           Bacterial
     merbromin                                                             anti-
                                                          Infections
                                                                        bacterial
                                                                                       Like other      Nadolol is a
                                                                                           beta-      nonselective
                                                                                       adrenergic          beta-
                                                                                     antagonists,      adrenergic
                                                                                          nadolol        receptor
                                                                                        competes       antagonist
                                            acts as an                                      with       with a long
                                          antagonist of                                adrenergic     half-life, and
                                              protein                                neurotransm             is
                                           adrenergic,                                 itters such     structurally
                                             beta-2-,                                         as        similar to
                                             receptor,                               catecholami      propranolol.
                                           surface acts                                   nes for         Clinical
                     C                         as an                                   binding at     pharmacolog
                     0                                                               sympathetic         y studies
                                          antagonist of
                     7
                             ADRB1        proteins with                                  receptor          have
     nadolol         A
                             ADRB2             beta-                                   sites. Like    demonstrate
                     A
                                            adrenergic                                propranolol         d beta-
                     1
                     2                       receptor                                and timolol,        blocking
                                           activityacts                                   nadolol       activity by
                                               as an                                     binds at     showing (1)
                                          antagonist of                                  beta(1)-     reduction in
                                              protein                                  adrenergic       heart rate
                                           adrenergic,                               receptors in      and cardiac
                                             beta-1-,                                   the heart       output at
                                             receptor                                and vascular      rest and on
                                                                                          smooth      exercise, (2)
                                                                                         muscle,      reduction of
                                                                                        inhibiting    systolic and
                                                                                       the effects       diastolic
                                                                                           of the          blood
                                                                                     catecholami       pressure at
                     J                                                                       nes       rest and on
                     0
                     1                                     Bacterial
     pheneticillin   C
                                                          Infections
                     E
                     0
                     5
     Prestwick-692
                     J
                     0
                     1                                     Bacterial      anti-
     thiamphenicol   B
                                                          Infections    bacterial
                     A
                     0
                     2
                                                                                       Topical -
                                                                                     Fungicidal;
                                                                                         exact
                                                                                     mechanism
                     D                                                                unknown;
                                                                                                  Tolnaftate is
                     0                                                               however, it
                                                                                                   a synthetic
                     1                                                                 has been
                                                                                                    over-the-
     tolnaftate      A                                    Mycoses      anti-fungal   reported to
                                                                                                  counter anti-
                     E                                                                distort the
                     1                                                                               fungal
                                                                                     hyphae and
                     8                                                                               agent.
                                                                                        to stunt
                                                                                       mycelial
                                                                                      growth in
                                                                                     susceptible
                                                                                     organisms.
     viomycin
     alvespimycin
                                                                                  Fulvestrant
                                                                                    binds to
                                                                                    estrogen
                                                                                   receptors
                                                                                   present in
                                                                                  cancer cells
                                                                                 and achieves
                                                                                     its anti-
                                                                                    estrogen
                                                                                      effects
                                                                                                Fulvestrant
                                                                                 through two
                                                                                                      for
                                                                                    separate
                                                                                               intramuscula
                                                                                 mechanisms
                    L                                                                                  r
                                                                                 . First, when
                    0                                                                           administrati
                                                                                  fulvestrant
                    2                                                                             on is an
                                                                                 binds to the
     fulvestrant    B   ESR1                                                                      estrogen
                                                                                   receptors,
                    A                                                                             receptor
                                                                                  estrogen is
                    0                                                                            antagonist
                    3
                                                                                 crowded out
                                                                                                   without
                                                                                    and is no
                                                                                                   known
                                                                                  longer able
                                                                                                   agonist
                                                                                   to bind to
                                                                                                   effects.
                                                                                       these
                                                                                   receptors.
                                                                                    Second,
                                                                                  fulvestrant
                                                                                   degrades
                                                                                 the estrogen
                                                                                 receptors to
                                                                                   which it is
                                                                                 bound. Both
                                                                                    of these
                                     acts as an                                  mechanisms
                                    inhibitor of
28                                 protein heat
                                        shock        Gram-
                                   protein 9kDa     Negative
                                        alpha       Bacterial
                                    (cytosolic), InfectionsPro     anti-
                                       class A       tozoan      protozoal
                        HSP90AA1      member       Infections   anti-fungal
     geldanamycin
                        HSP82       1acts as an      Gram-         anti-
                                    inhibitor of    Positive   bacterial anti-
                                   protein heat     Bacterial   neoplastic
                                        shock    InfectionsMy
                                   protein 9kDa       coses
                                        alpha     Neoplasms
                                    (cytosolic),
                                       class A
                                     member 1
                                     acts as an
                                    inhibitor of
                                   protein v-src
                                      sarcoma
                                     (Schmidt-
                                   Ruppin A-2)
                                         viral
                                     oncogene
                                      homolog
     monorden                       (avian)acts
                                        as an
                                    inhibitor of
                                   protein heat
                                        shock
                                   protein 9kDa
                                        alpha
                                    (cytosolic),
                                       class A
                                     member 1
     tanespimycin
                    R
                    0                                        expectorant
                    5                            Inflammatio      anti-
     ambroxol       C
                                                      n      inflammator
                    B
                                                                   y
                    0
                    6
                                                              Aminoglycosi      Amikacin is
                                                                  des like            an
                                                                 Amikacin      aminoglycosi
                                                              "irreversibly"   de antibiotic.
                                                                  bind to      Aminoglycosi
                                                              specific 30S-    des work by
                                                                  subunit        binding to
                                                              proteins and     the bacterial
                                                                16S rRNA.            30S
                                                                 Amikacin        ribosomal
                                                                  inhibits         subunit,
                                                                  protein          causing
                                                              synthesis by      misreading
             D   J   S                                          binding to        of t-RNA,
             0   0   0                                           the 30S        leaving the
             6   1   1
                                 Bacterial        anti-         ribosomal        bacterium
amikacin     A   G   A   rpsL
                                Infections      bacterial       subunit to        unable to
             X   B   A
                                                               prevent the       synthesize
             1   0   2
             2   6   1
                                                              formation of     proteins vital
                                                               an initiation        to its
                                                                 complex           growth.
                                                                    with       Aminoglycosi
                                                               messenger           des are
                                                                   RNA.             useful
                                                               Specifically     primarily in
                                                                 Amikacin        infections
                                                              binds to four       involving
                                                               nucleotides         aerobic,
                                                              of 16S rRNA           Gram-
                                                              and a single        negative
                                                               amino acid         bacteria,
                                                                of protein         such as
boldine                                                         S12. This      Pseudomona
canadine
                                                                               Ceforanide is
                                                                                      a
                                                                               semisyntheti
                                                                                 c second-
                                                                                generation
                                                                    The        cephalospori
                                                               bactericidal        n. The
                                                                activity of    cephalospori
                                                                ceforanide         ns are
             J                                                results from      bactericidal
             0
                                                                    the         drugs with
             1
                                                               inhibition of    both gram-
ceforanide   D           pbpA
                                                                 cell wall     positive and
             C
             1                                                synthesis via        gram-
             1                                                  affinity for     negative
                                                                penicillin-       activity.
                                                                 binding       They inhibit
                                                                 proteins      bacterial cell
                                                                 (PBPs).            wall
                                                                               synthesis in
                                                                                   a way
                                                                                 similar to
                                                                                    the
                                                                                penicillins.


                                                                                Cefotiam is
                                                                                   a third
                                                                                generation
                                                                               beta-lactam
                                                                               cephalospori
                                                                               n antibiotic.
                                                                               It has broad
                                                                    The          spectrum
                                                               bactericidal        activity
                                                                activity of        against
                                                                 cefotiam           Gram
             J                                                results from     positive and
             0
                                                                    the             Gram
             1                  Respiratory       anti-
                                                               inhibition of      negative
cefotiam     D           pbpA      Tract        infective
                                                                 cell wall      bacteria. It
             C                   Infections       agent
             0                                                synthesis via       does not
             7                                                  affinity for   have activity
                                                                penicillin-        against
                                                                  binding      <i>Pseudom
                                                                 proteins           onas
                                                                  (PBPs).      aeruginosa<
                                                                                     /i>.
                                                                                 Cefotiam
                                                                                 works by
                                                                                 inhibiting
                                                                               bacterial cell
                                                                                     wall
                                                                               biosynthesis.


cinchonine                        Malaria     anti-malarial
                                                                                            Enoxacin is a
                                                                                             quinolone/fl
                                                                                            uoroquinolon
                                                                                             e antibiotic.
                                                                                             Enoxacin is
                                                                                             bactericidal
                                                                                            and its mode
                                                                                               of action
                                                                                             depends on
                                                                                             blocking of
                                                                              Enoxacin         bacterial
                                                                              exerts its          DNA
                                                                            bactericidal      replication
                  J                                                          action via       by binding
                  0                 acts as an
                                                                                 the         itself to an
                  1                inhibitor of
                      gyrA parC                    Bacterial     anti-      inhibition of       enzyme
enoxacin          M               protein DNA
                      TOP2A                       Infections   bacterial   the essential     called DNA
                  A               topoisomera
                                                                              bacterial         gyrase,
                  0                    se II
                  4                                                        enzyme DNA       which allows
                                                                           gyrase (DNA             the
                                                                           Topoisomera        untwisting
                                                                               se II).       required to
                                                                                            replicate one
                                                                                             DNA double
                                                                                               helix into
                                                                                                  two.
                                                                                            Enoxacin is a
                                                                                                broad-
                                                                                               spectrum
                                                                                               antibiotic
                                                                                            that is active
                                                                                            against both
                                                                                                 Gram-
                                                                                            Fludrocortiso
                                                                           Fludrocortiso        ne is a
                                                                           ne binds the        synthetic
                                                                           mineralocort     adrenocortic
                                                                                  icoid        al steroid
                                                                              receptor        possessing
                                                                           (aldosterone      very potent
                                                                             receptor).     mineralocort
                                                                           This binding           icoid
                                                                                   (or        properties
                                                                           activation of       and high
                                                                                   the      glucocorticoi
                                                                           mineralocort     d activity. It
                  H                                                               icoid      is indicated
                  0                                                                            as partial
                                                                            receptor by
                  2
                                                                           fludrocortiso    replacement
fludrocortisone   A   NR3C2
                                                                            ne) in turn      therapy for
                  A
                                                                             causes an      primary and
                  0
                  2                                                         increase in       secondary
                                                                               ion and      adrenocortic
                                                                                 water              al
                                                                             transport      insufficiency
                                                                              and thus              in
                                                                                 raises     Addison&rsq
                                                                           extracellular    uo;s disease
                                                                           fluid volume      and for the
                                                                             and blood      treatment of
                                                                           pressure and       salt-losing
                                                                                lowers      adrenogenit
                                                                             potassium      al syndrome.
                                                                                levels.            The
                                                                                             physiologic
                                                                                               action of
                                                                             Furosemide,
                                                                             by inhibiting
                                                                                    the
                                                                             reabsorption
                                                                               of sodium
                                                                             and chloride     Furosemide,
                                                                                  in the             a
                                                                               ascending     sulfonamide-
                                                                              limb of the       type loop
                                                                                 loop of         diuretic
                                                                                  Henle,      structurally
                                                                               increases       related to
                                                Hyperaldost                   the urinary    bumetanide,
                  C                               eronism                     excretion of     is used to
                  0                                                             sodium,
                                                  Fibrosis                                       manage
                  3
                      SLC12A1                   Hypokalemia   diuretic anti- chloride, and   hypertension
     furosemide   C
                      ATP1A1                    Hypertensio   hypertensive        water.      and edema
                  A
                                                 n Hepatic                    Furosemide       associated
                  0
                  1                             Encephalopa                        also            with
                                                 thyAscites                    increases       congestive
                                                                                    the      heart failure,
                                                                              excretion of      cirrhosis,
                                                                              potassium,        and renal
                                                                               hydrogen,         disease,
                                                                                calcium,     including the
                                                                             magnesium,         nephrotic
                                                                             ammonium,         syndrome.
                                                                                   and
                                                                               phosphate
                                                                               and, as it
                                                                                 inhibits
                                                                                carbonic
                  V                                                           anhydrase,
                  0
                  8                                            diagnostic
     iopamidol    A
                                                                 agent
                  B
                  0
                  4
                                                                           Isoniazid is a    Isoniazid is a
                                                                           prodrug and        bactericidal
                                                                               must be       agent active
                                                                           activated by          against
                                                                              bacterial      organisms of
                                                                              catalase.        the genus
                                                                            Specficially,     Mycobacteri
                                                                            activation is           um,
                                                                             associated        specifically
                                                                                 with             <i>M.
29                                  acts as an                              reduction of      tuberculosis
                                   inhibitor of                                   the        </i>, <i>M.
                                    protein 4-                              mycobacteri        bovis</i>
                  J                                              anti-
                                  aminobutyra                                  al ferric       and <i>M.
                  0                                            infective
                                        te                                      KatG         kansasii</i>
                  4                                          agent anti-
                      katG inhA    aminotransf                                catalase-          . It is a
     isoniazid    A                             Tuberculosis   bacterial
                      ABAT nat    eraseacts as                               peroxidase           highly
                  C                                           antiseptic
                                  an inducer of                            by hydrazine          specific
                  0                                              anti-
                  1               proteins with                            and reaction           agent,
                                                             proliferative
                                      protein                               with oxygen        ineffective
                                     kinase C                                to form an          against
                                      activity                               oxyferrous            other
                                                                               enzyme        microorganis
                                                                              complex.              ms.
                                                                                Once          Isoniazid is
                                                                             activated,       bactericidal
                                                                              isoniazid        to rapidly-
                                                                            inhibits the         dividing
                                                                            synthesis of      mycobacteri
                                                                              mycoloic          a, but is
                                                                              acids, an      bacteriostati
                                                                              essential          c if the
                  D                                                         component         mycobacteri
                  0
                  6                               Bacterial       anti-
     mafenide     B
                                                 Infections     bacterial
                  A
                  0
                  3
                                                                                                                  Metronidazol
                                                                                                                        e, a
                                                                                                                     synthetic
                                                                                                   Unionized      antibacterial
                                                                                                 metronidazol           and
                                                                                                 e is selective   antiprotozoal
                                                                                                         for      agent of the
                                                                                                   anaerobic      nitroimidazol
                                                                                                 bacteria due       e class, is
                                                                                                      to their    used against
                                                                                                    ability to       protozoa
                                                                                                 intracellularl       such as
                                                                                                     y reduce     <i>Trichomo
                A   D   G   J   P                                                                metronidazol           nas
                0   0   0   0   0                                                                                  vaginalis</i
                                                                                                      e to its
                1   6   1   1   1
                                                                  Protozoan        anti-         active form.            >,
metronidazole   A   B   A   X   A       rdxA
                                                                  Infections     protozoal       This reduced      amebiasis,
                B   X   F   D   B
                                                                                                 metronidazol           and
                1   0   0   0   0
                7   1   1   1   1                                                                      e then       giardiasis.
                                                                                                     disrupts     Metronidazol
                                                                                                 DNA's helical          e is
                                                                                                   structure,       extremely
                                                                                                    inhibiting       effective
                                                                                                     bacterial        against
                                                                                                  nucleic acid      anaerobic
                                                                                                    synthesis        bacterial
                                                                                                 and resulting      infections
                                                                                                  in bacterial      and is also
                                                                                                   cell death.    used to treat
                                                                                                                      Crohn's
                                                                                                                     disease,
                                                                                                                    antibiotic-
                J                                                                                                   associated
                0
                5
moroxydine      A
                X
                0
                1
                B   D   D   P   S   S
                0   0   0   0   0   0                                              anti-
                5   8   9   1   1   2                              Bacterial
                                                                               bacterial anti-
nitrofural      C   A   A   C   A   A                            InfectionsInf
                                                                                 infective
                A   F   A   C   X   A                               ection
                                                                                   agent
                0   0   0   0   0   0
                3   1   3   2   4   2
                                                                                                                  Primidone is
                                                                                                                  a barbiturate
                                                                                                                        with
                                                                                                                  anticonvulsa
                                                                                                                         nt
                                                                                                                    properties.
                                                                                                                    Primidone,
                                                                                                                  either alone
                                                                                                                      or used
                                                                                                                  concomitantl
                                                                                                                  y with other
                                                                                                 Primidone is     anticonvulsa
                                                                                                    a GABA             nts, is
                N                                                                                  receptor        indicated in
                0                                                                                                   the control
                                                                                                 agonist. The
                3
                                                                                   anti-         mechanism           of grand
primidone       A                       GABRA1                     Seizures
                                                                                convulsant             of               mal,
                A
                                                                                                 Primidone's      psychomotor
                0
                3                                                                                antiepileptic      , and focal
                                                                                                 action is not       epileptic
                                                                                                    known.         seizures. It
                                                                                                                   may control
                                                                                                                    grand mal
                                                                                                                      seizures
                                                                                                                  refractory to
                                                                                                                       other
                                                                                                                  anticonvulsa
                                                                                                                   nt therapy.
                                                                                                                    Primidone
                                                                                                                       raises
                                                                                                                    electro- or
                                                                                                                  chemoshock
                                                   acts as an                                                         seizure
                                                  inhibitor of
                                                 proteins with
                                                     cAMP-                        cardiac
sulmazole
                                                    specific                     stimulant
                                                 phosphodies
                                                     terase
                                                    activity
                                                           Tranexamic       Tranexamic
                                                                 acid         acid is an
                                                           competitivel    antifibrinolyt
                                                             y inhibits         ic that
                                                           activation of   competitivel
                                                          plasminogen      y inhibits the
                                                           (via binding    activation of
                                                                to the     plasminogen
                                                                kringle      to plasmin.
                                                             domain),       Tranexamic
                                                               thereby         acid is a
                                                              reducing      competitive
                                                            conversion       inhibitor of
                  B                                                of      plasminogen
                  0                                       plasminogen        activation,
                  2
                                             cardiovascul to plasmin       and at much
tranexamic_acid   A   PLG PLAT
                                               ar agent   (fibrinolysin)        higher
                  A
                                                          , an enzyme      concentratio
                  0
                  2
                                                                 that            ns, a
                                                             degrades      noncompetiti
                                                           fibrin clots,    ve inhibitor
                                                            fibrinogen,      of plasmin,
                                                             and other      i.e., actions
                                                               plasma         similar to
                                                              proteins,    aminocaproi
                                                          including the         c acid.
                                                          procoagulant      Tranexamic
                                                              factors V    acid is about
                                                             and VIII.        10 times
                                                           Tranexamic      more potent
                                                              acid also    in vitro than
                                                               directly    aminocaproi
                                                               inhibits
                                                          Trihexypheni          c acid.
                                                                           Trihexypheni
                                                              dyl is a         dyl is an
                                                          selective M1     anticholinerg
                                                           muscarinic         ic used in
                                                          acetylcholine            the
                                                             receptor      symptomatic
                                                           antagonist.     treatment of
                                                           It is able to    all etiologic
                                                          discriminate        groups of
                                                          between the       parkinsonis
                                                           M1 (cortical     m and drug
                                                          or neuronal)         induced
                                                              and the       extrapyrami
                  N                                         peripheral     dal reactions
                  0                                        muscarinic           (except
                  4
                                 Parkinson                   subtypes           tardive
trihexyphenidyl   A   CHRM1
                                  Disease                 (cardiac and      dyskinesia).
                  A
                                                           glandular).     Trihexypheni
                  0
                  1
                                                          Trihexypheni             dyl
                                                           dyl partially      possesses
                                                               blocks             both
                                                           cholinergic     anticholinerg
                                                            activity in          ic and
                                                             the CNS,      antihistamini
                                                              which is        c effects,
                                                           responsible         although
                                                              for the          only the
                                                          symptoms of        former has
                                                           Parkinson's            been
                                                          disease. It is    established
                                                          also thought              as
                                                           to increase     therapeutical
                                                                the        ly significant
                                                                            It is believed
                                                                                  that
                                                                               vigabatrin
                                                                               increases
                                                                                  brain
                                                                            concentratio
                                                                            ns of gamma-
                                                                            aminobutyric Vigabatrin,
                                                                            acid (GABA),         is an
                                                                            an inhibitory anticonvulsa
                                                                            neurotransm            nt
                                                                              itter in the   chemically
                                                                                CNS, by    unrelated to
                     N             acts as an                                irreversibly       other
                     0            inhibitor of                                 inhibiting  anticonvulsa
                     3             protein 4-                                   enzymes           nts.
     vigabatrin      A   ABAT    aminobutyra     Epilepsy    cns agent            that       Vigabatrin
                     G                 te                                      catabolize   inhibits the
                     0           aminotransf                                     GABA       catabolism
                     4               erase                                     (gamma-      of GABA. It
                                                                            aminobutyric is an analog
                                                                                  acid     of GABA, but
                                                                            transaminas      it is not a
                                                                              e GABA-T)       receptor
                                                                             or block the     agonist.
                                                                             reuptake of
                                                                               GABA into
                                                                                glia and
                                                                                 nerve
                                                                                endings.
                                                                              Vigabatrin
                                                                                may also
                                                              anti-viral        work by
                                                            immunomod
                                                   Virus
     amiprilose                                              ulator anti-
                                                 Diseases
                                                            inflammator
                                                                  y

                                                                                             Levobunolol
                                                                                                   is an
                                                                                              ophthalmic
                                                                                                   beta-
                                                                            Levobunolol'
                                                                                                 blocker,
                                                                            s mechanism
                                                                                                  equally
                                                                              of action in
                                                                                              effective at
                                                                            reducing IOP
                                                                                               &beta;(1)-
                                                                              is believed
                                                                                                    and
                                                                            to be due to
                     S                                                                         &beta;(2)-
                                                                              a reduction
                     0                                                                           receptor
                                                                                 of the
                     1                                                                          sites. The
                         ADRB1                                                production
     levobunolol     E                                                                       levorotatory
                         ADRB2                                                of aqueous
                     D                                                                          isomer of
                     0                                                         humor via
                                                                                                 bunolol,
                     3                                                       inhibition of
                                                                                              levobunolol
                                                                            adrenergicall
                                                                                               is used for
                                                                                y driven
                                                                                                    the
                                                                               processes
                                                                                             treatment of
                                                                               within the
                                                                                               IOP due to
                                                                                 ciliary
                                                                                              open-angle
                                                                              processes.
                                                                                             glaucoma or
                                                                                                  ocular
                                                                                             hypertension
                                                                                                      .


30
     Prestwick-864
30                                                            Suprofen         Suprofen is
                                                            binds to the           a non-
                                                           cyclooxygen        steroidal anti-
                                                           ase-1 (COX-        inflammator
                                                               1) and           y analgesic
                                                           cyclooxygen               and
                                                           ase-2 (COX-         antipyretic.
                                                                  2)           Ophthalmic
                                                           isoenzymes,               anti-
                                                             preventing       inflammator
                                                                 the           y medicines
                                                            synthesis of       are used in
                                                           prostaglandi         the eye to
                  M                                            ns and              lessen
                  0                                        reducing the          problems
                  1                                 anti-  inflammator            that can
                      PTGS1       Inflammatio
     suprofen     A                            inflammator y response.
                      PTGS2 ALB       nPain                                   occur during
                  E                             yanalgesic Cyclooxygen            or after
                  0
                                                                 ase           some kinds
                  7
                                                           catalyses the            of eye
                                                           formation of           surgery.
                                                           prostaglandi        Sometimes,
                                                               ns and          the pupil of
                                                           thromboxan         the eye gets
                                                               e from              smaller
                                                            arachidonic          during an
                                                             acid (itself        operation
                                                           derived from             (pupil
                                                            the cellular      constriction)
                                                           phospholipid         , making it
                                                             bilayer by             more
                                                           phospholipas         difficult for
                                   Protozoan                      e            the surgeon
                                                    anti-
     amprolium                    InfectionsCo
                                                 protozoal
                                    ccidiosis
                                                                               Cefotaxime
                                                                                  is a third
                                                                                generation
                                                                               intravenous
                                                                   The        cephalospori
                                                              bactericidal    n antibiotic.
                                                                activity of   It has broad
                                                               cefotaxime        spectrum
                                                             results from           activity
                                                                    the             against
                                                              inhibition of          Gram
                                                                 cell wall    positive and
                                                             synthesis via           Gram
                  J                                            affinity for       negative
                  0                                                             bacteria. It
                                                                penicillin-
                  1
                                    Bacterial      anti-         binding          does not
     cefotaxime   D   pbpA pbpC
                                   Infections    bacterial       proteins     have activity
                  D
                                                                 (PBPs).            against
                  0
                  1                                           Cefotaxime      <i>Pseudom
                                                               shows high            onas
                                                               affinity for   aeruginosa<
                                                                penicillin-           /i>.
                                                                 binding       Cefotaxime
                                                               proteins in        works by
                                                             the cell wall       inhibiting
                                                                including     bacterial cell
                                                               PBP Ib and             wall
                                                                 PBP III.     biosynthesis.
                                                                                 A positive
                                                                                 feature of
                                                                                cefotaxime
                                                                                   is that it
                                                                                  display a
                                                                                       Cimetidine is
                                                                                       a histamine
                                                                                       H<sub>2</s
                                                                       Cimetidine            ub>-
                                                                       binds to an         receptor
                                                                      H<sub>2</s        antagonist.
                                                                           ub>-          It reduces
                                                                         receptor        basal and
                                                                       located on        nocturnal
                                                                            the         gastric acid
                                                                       basolateral        secretion
                               acts as an                              membrane              and a
                            antagonist of                                  of the      reduction in
               A                protein                                   gastric           gastric
               0                                                                           volume,
                               histamine                              parietal cell,
               2
                   HRH2      receptor H2                gastrointesti    blocking      acidity, and
cimetidine     B                           Peptic Ulcer
                   hROAT1      acts as an                nal agent      histamine       amount of
               A
                              inhibitor of                            effects. This     gastric acid
               0
               1            proteins with                             competitive       released in
                            monooxygen                                  inhibition     response to
                             ase activity                               results in          stimuli
                                                                         reduced          including
                                                                       gastric acid          food,
                                                                        secretion         caffeine,
                                                                           and a            insulin,
                                                                      reduction in     betazole, or
                                                                          gastric      pentagastrin
                                                                      volume and        . It is used
                                                                          acidity.         to treat
                                                                                       gastrointesti
                                                                                       nal disorders
                                                                                            such as
                             acts as an                                                  gastric or
                            antagonist of
                            proteins with
corynanthine                  alpha1-
                             adrenergic
                              receptor
                               activity
                                                                                        Doxylamine
                                                                                            is an
                                                                                       antihistamin
                                                                                       e commonly
                                                                                         used as a
                                                                                         sleep aid.
                                                                                        This drug is
                                                                                       also used to
                                                                                           relieve
                                                                        Like other
                                                                                       symptoms of
                                                                      antihistamin
                                                                                         hay fever
                                                                            es,
                                                                                          (allergic
                                                                       doxylamine
                                                                                          rhinitis),
               R                                                          acts by
                                                                                        hives (rash
               0              acts as an                              competitivel
                                                                                        or itching),
               6            antagonist of                              y inhibiting
                   HRH1                                                                  and other
doxylamine     A               protein                    sedative    histamine at
                   CHRM1                                                                   allergic
               A              histamine                               H1&nbsp;rec
                                                                                         reactions.
               0             receptor H1                                eptors. It
               9
                                                                                        Doxylamine
                                                                         also has
                                                                                       is a member
                                                                       substantial
                                                                                            of the
                                                                      sedative and
                                                                                       ethanolamin
                                                                      anticholinerg
                                                                                         e class of
                                                                        ic effects.
                                                                                       antihistamin
                                                                                        es and has
                                                                                        anti-allergy
                                                                                         power far
                                                                                        superior to
                                                                                          virtually
                                                                                        every other
                                                                                       antihistamin
                                                                                          e on the
                                                                                       market, with
                                                                        Gemfibrozil
                                                                           increases
                                                                        the activity      Gemfibrozil,
                                                                                 of        a fibric acid
                                                                       extrahepatic        antilipemic
                                                                         lipoprotein     agent similar
                                                                        lipase (LL),     to clofibrate,
                                                                             thereby        is used to
                                                                          increasing            treat
                                                                         lipoprotein      hyperlipopro
                                                                        triglyceride     teinemia and
                                                                            lipolysis.   as a second-
                                                                       Chylomicron        line therapy
                     C                                                         s are       for type IIb
                     1                                                    degraded,      hypercholest
                     0                                    anti-lipemic
                             LPL PPARA                                    VLDLs are       erolemia. It
     gemfibrozil     A                                    cardiovascul
                             SLCO1B1                                   converted to           acts to
                     B                                      ar agent
                                                                          LDLs, and           reduce
                     0
                     4
                                                                            LDLs are       triglyceride
                                                                       converted to           levels,
                                                                        HDL. This is      reduce VLDL
                                                                       accompanied            levels,
                                                                         by a slight       reduce LDL
                                                                         increase in           levels
                                                                        secretion of      (moderately
                                                                          lipids into         ), and
                                                                        the bile and     increase HDL
                                                                          ultimately           levels
                                                                                the       (moderately
                                                                           intestine.             ).
                                                                        Gemfibrozil
                                                                        also inhibits
     idazoxan                                                                   the
                     C                     acts as an
                     0                    antagonist of
                     4                    proteins with
     isoxsuprine     A                        beta-       vasodilator
                     A                     adrenergic
                     0                      receptor
                     1                       activity
                                                                        Levocabastin     Levocabastin
31                                                                           e is a             e is a
                                                                            potent,           selective
                                                                           selective        histamine
                                                                          histamine       H1-receptor
                                                                        H1-receptor        antagonist
                                                                         antagonist.          exerting
                                                                         It works by         inhibitory
                                                                          competing         effects on
                                                                              with         the release
                                                                          histamine       of chemical
                                                                            for H1-         mediators
                                                                           receptor         from mast
                     R   S                                                 sites on       cells and on
                     0   0                                                  effector             the
                     1   1
                                                                            cells. It     chemotaxis
     levocabastine   A   G   NTSR2 HRH1
                                                                           thereby                of
                     C   X
                                                                          prevents,      polymorphon
                     0   0
                     2   2
                                                                        but does not           uclear
                                                                           reverse,        leukocytes
                                                                          responses              and
                                                                        mediated by       eosinophils.
                                                                          histamine             Both
                                                                             alone.         histamine
                                                                        Levocabastin     and antigens
                                                                          e does not          induced
                                                                             block       conjunctivitis
                                                                          histamine            can be
                                                                        release but,      inhibited by
                                                                            rather,      levocabastin
                                                                           prevents               e.
                                                                          histamine      Levocabastin
                                                                         binding and        e can also
                                                                           Minaprine       Minaprine is
                                                                            binds to         an amino-
                                                                           serotonin       phenylpyrida
                                                                             type 2               zine
                                                                           receptors       antidepressa
                                                                             and to         nt reported
                                                                          dopamine               to be
                                                                          D1 and D2           relatively
                                                                              type              free of
                                                                        receptors. It      cardiotoxicit
                                                                        also binds to              y,
                                                                               the          drowsiness,
                                                                           serotonin        and weight
              N                 acts as an                                 reuptake        gain. Similar
              0   DRD1 DRD2
                               inhibitor of                neuroprotect      pump.             to other
              6   HTR2A
                                protein 5-                  ive agent     Therefore,       antidepressa
minaprine     A   HTR2B
                              hydroxytrypt                 psychotropic minaprine                  nt
              X   HTR2C
                                 amine 2                      agent       blocks the        treatments,
              0   SLC6A4
              7                  receptor                                reuptake of         minaprine
                                                                              both           attenuates
                                                                          dopamine            the beta-
                                                                               and           adrenergic
                                                                        serotonin. It          receptor
                                                                         is also, to a        function.
                                                                              slight       Studies have
                                                                            degree,         also shown
                                                                        cholinomime               that
                                                                          tic. Thus it       minaprine
                                                                        may exhibit           improves
                                                                        both mood-             memory
                                                                         brightening       consolidation
                                                                               and             and that
              C                                                            nootropic          repeated
              0
              5
oxetacaine    A                                             anesthetic
              D
              0
              6
              N
              0                                            diagnostic
              2                                            agent anti-
phenazone     B                               Fever Pain
                                                             pyretic
              B
                                                            analgesic
              0
              1
                                                                          Pralidoxime       Pralidoxime
                                                                               is an             is to
                                                                           antidote to       reactivate
                                                                         organophosp       cholinesteras
                                                                               hate           e (mainly
                                                                            pesticides       outside of
                                                                                and         the central
                                                                           chemicals.          nervous
                                                                          Organophos           system)
                                                                          phates bind        which has
                                                                              to the             been
                                                                         esteratic site     inactivated
                                                                                 of                by
              V                                                          acetylcholine     phosphorylat
              0                 acts as an
                                                                             sterase,        ion due to
              3                activator of
                                                                         which results            an
pralidoxime   A               proteins with
                                                                            initially in   organophosp
              B               cholinesteras
                                                                            reversible           hate
              0                 e activity
              4
                                                                          inactivation      pesticide or
                                                                              of the            related
                                                                           enzyme. If       compound.
                                                                         given within             The
                                                                                 24         destruction
                                                                           hours,after             of
                                                                         organophosp       accumulated
                                                                               hate        acetylcholine
                                                                            exposure,         can then
                                                                          pralidoxime      proceed, and
                                                                           reactivates     neuromuscul
                                                                          the enzyme        ar junctions
                                                                         cholinesteras        will again
                                                                               e by            function
                                                                         cleaving the         normally.
                                                                                                   Pyrimethami
                                                                                                       ne is an
                                                                                                   antiparasitic
                                                                                   Pyrimethami
                                                                                                     compound
                                                                                    ne inhibits
                                                                                                     commonly
                                                                                         the
                                                                                                    used as an
                                                                                   dihydrofolat
                                                                                                     adjunct in
                                                                                   e reductase
                                                                                                         the
                                                                                   of plasmodia
                                                                                                   treatment of
                                                                                   and thereby
                                                                                                   uncomplicat
                                                                                     blocks the
                                                                                                         ed,
                                                                                   biosynthesis
                                                                                                    chloroquine
                                                                                     of purines
                                                                                                   resistant, P.
                         P                                                               and
                                                                                                     falciparum
                         0                   acts as an                            pyrimidines,
                                                                                                      malaria.
                         1                  inhibitor of   Malaria                   which are
                                                                                                   Pyrimethami
pyrimethamine            B           DHFR      protein   Toxoplasmos anti-malarial essential for
                                                                                                    ne is a folic
                         D                  dihydrofolat      is                        DNA
                                                                                                         acid
                         0                  e reductase                              synthesis
                         1
                                                                                                     antagonist
                                                                                      and cell
                                                                                                       and the
                                                                                   multiplicatio
                                                                                                   rationale for
                                                                                   n. This leads
                                                                                                          its
                                                                                   to failure of
                                                                                                    therapeutic
                                                                                      nuclear
                                                                                                      action is
                                                                                     division at
                                                                                                   based on the
                                                                                    the time of
                                                                                                    differential
                                                                                      schizont
                                                                                                   requirement
                                                                                   formation in
                                                                                                      between
                                                                                   erythrocytes
                                                                                                      host and
                                                                                     and liver.
                                                                                                    parasite for
                                                                                                    nucleic acid
                                                                                                     precursors
salsolidin                                                                                          involved in
SR-95531
                         D   J
                         0   0                           Staphylococc
                         6   1                           al Infections     anti-
sulfathiazole            B   E
                                                           Bacterial     bacterial
                         A   B
                                                          Infections
                         0   0
                         2   7
0175029-0000
2,6-dimethylpiperidine
                                                                     cardiovascul
                                                                       ar agent
                                                                        muscle
                                                         Inflammatio   relaxant
acacetin
                                                           n Spasm   (spasmolytic
                                                                         )anti-
                                                                     inflammator
                                                                           y

                                              acts as an
                                             inhibitor of
                                                protein
                         A   B   N          prostaglandi
                         0   0   0                 n-
                                                                       anti-pyretic
                         1   1   2          endoperoxid
                                                          Inflammatio      anti-
acetylsalicylic_acid     A   A   B          e synthase 2
                                                          nFever Pain inflammator
                         D   C   A          (prostagland
                         0   0   0                                     yanalgesic
                                                in G/H
                         5   6   1             synthase
                                                  and
                                            cyclooxygen
                                                 ase)
                                                                                         Amoxicillin    Amoxicillin is
                                                                                            binds to    a moderate-
                                                                                          penicillin-     spectrum
                                                                                             binding      antibiotic
                                                                                         protein 1A          active
                                                                                           (PBP-1A)       against a
                                                                                             located     wide range
                                                                                          inside the       of Gram-
                                                                                       bacterial cell   positive, and
                                                                                               well.       a limited
                                                                                          Penicillins      range of
                                                                                         acylate the         Gram-
                                                              Gram-                       penicillin-      negative
                       J                                     Positive                      sensitive     organisms.
                       0                                                               transpeptida      It is usually
                                                             Bacterial
                       1
                                                            Infections      anti-             se C-      the drug of
amoxicillin            C       pbpA
                                                              Gram-       bacterial         terminal    choice within
                       A
                                                             Negative                    domain by         the class
                       0
                       4                                     Bacterial                  opening the     because it is
                                                            Infections                  lactam ring.         better
                                                                                               This       absorbed,
                                                                                        inactivation       following
                                                                                              of the          oral
                                                                                            enzyme      administrati
                                                                                       prevents the        on, than
                                                                                       formation of      other beta-
                                                                                         a cross-link       lactam
                                                                                       of two linear     antibiotics.
                                                                                       peptidoglyca     Amoxicillin is
                                                                                          n strands,     susceptible
                                                                                           inhibiting          to
                                                                                       the third and    degradation
                                                                            anti-      last stage of     by &beta;-
                                                                       inflammator
                                                                         y muscle
                                                           Inflammatio
apigenin                                                                 relaxant
                                                           n Neoplasms
                                                                       (spasmolytic
                                                                           )anti-
                                                                        neoplastic
                       A   D
                       1   0
                       1   3
calcium_pantothenate   H   A
                       A   X
                       3   0
                       1   4

                                                                                                           Cefalotin
                                                                                             The           (INN) or
                                                                                        bactericidal     cephalothin
                                                                                         activity of     (USAN) is a
                                                                                          cefalotin     semisyntheti
                       J                                                               results from          c first
                       0
                                                                                             the          generation
                       1       pbpA ALB
                                                             Bacterial      anti-       inhibition of   cephalospori
cefalotin              D       CD248
                                                            Infections    bacterial       cell wall       n having a
                       B       ampC
                       0                                                               synthesis via        broad
                       3                                                                 affinity for    spectrum of
                                                                                         penicillin-       antibiotic
                                                                                           binding      activity that
                                                                                          proteins             is
                                                                                           (PBPs).      administered
                                                                                                        parenterally.


                                             acts as an
                                            inhibitor of
                                              protein
chrysin                                                      Mycoses     anti-fungal
                                          arachidonate
                                                 5-
                                          lipoxygenase
                                                        Dextrometho      Dextrometho
                                                          rphan is an         rphan
                                                          opioid-like     suppresses
                                                           drug that       the cough
                                                        binds to and       reflex by a
                                                             acts as     direct action
                                                          antagonist     on the cough
                                                        to the NMDA      center in the
                                                        glutamatergi       medulla of
                                                        c receptor, it     the brain.
                                                        is an agonist    Dextrometho
                                                        to the opioid    rphan shows
                                                        sigma 1 and       high affinity
                   R                                         sigma 2       binding to
                   0   OPRS1
                                                         receptors, it       several
                   5   OPRS1                   anti-
                                 Cough                     is also an      regions of
dextromethorphan   D   CHRNA2              convulsant
                                Seizures                 alpha3/beta       the brain,
                   A   SLC6A4              anti-tussive
                                                           4 nicotinic   including the
                   0   GRIN3A
                   9
                                                            receptor       medullary
                                                          antagonist          cough
                                                         and targets      center. This
                                                                the      compound is
                                                           serotonin        an NMDA
                                                            reuptake        receptor
                                                              pump.        antagonist
                                                        Dextrometho       and acts as
                                                            rphan is          a non-
                                                              rapidly     competitive
                                                           absorbed          channel
                                                            from the     blocker. It is
                                                        gastrointesti      one of the
                                                           nal tract,     widely used
                                                            where it
                                                                The      antitussives,
                                                                         Ethotoin is a
                                                         mechanism      hydantoin
                                                          of action is  derivative
                                                           probably          and
                                                         very similar anticonvulsa
                                                           to that of  nt. Ethotoin
                                                          phenytoin.     exerts an
                                                          The latter   antiepileptic
                                                              drug          effect
                                                          appears to      without
                                                            stabilize     causing
                                                         rather than      general
                                                         to raise the      central
                   N                                         normal       nervous
                   0                                         seizure       system
                   3
                                                          threshold,   depression.
ethotoin           A   SCN5A
                                                             and to          The
                   B
                                                         prevent the mechanism
                   0
                   1
                                                           spread of    of action is
                                                             seizure     probably
                                                            activity   very similar
                                                         rather than     to that of
                                                          to abolish    phenytoin.
                                                         the primary    The latter
                                                            focus of        drug
                                                             seizure    appears to
                                                         discharges.      stabilize
                                                            Ethotoin   rather than
                                                            inhibits   to raise the
                                                              nerve        normal
                                                         impulses in       seizure
                                                          the motor     threshold,
                                                           cortex by       and to
                                                                            Bisphosphon         Etidronic
                                                                             ates, when      acid is a first
                                                                             attached to       generation
                                                                            bone tissue,          (non-
                                                                                  are        nitrogenous)
                                                                            absorbed by      bisphosphon
                                                                             osteoclasts,      ate in the
                                                                              the bone       same family
                                                                              cells that             as
                                                                            breaks down        clodronate
                                                                            bone tissue.            and
                                                                            Although the      tiludronate.
                                                                             mechanism          Etidronic
                      M                                                      of action of     acid affects
                      0                                                          non-            calcium
                      5
                                                                             nitrogenous     metabolism
     etidronic_acid   B
                                                                            bisphosphon       and inhibits
                      A
                                                                            ates has not           bone
                      0
                      1
                                                                              been fully       resorption
                                                                             elucidated,         and soft
                                                                              available           tissue
                                                                            data suggest     calcification.
                                                                              that they           Of the
                                                                            bind strongly       etidronic
                                                                                   to         acid that is
                                                                            hydroxyapati        resorbed
                                                                            te crystals in     (from oral
                                                                              the bone       preparation)
                                                                                matrix,        or infused
                                                                            preferentiall           (for
                                                                            y at the sites   intravenous
                                                                            of increased         drugs),
     flunixin                                                                    bone         about 50%
     harman
     harmine
     harmol
     heliotrine
                                                                                             Irinotecan is
                                                                                                    an
                                                                                             antineoplasti
                                                                                               c enzyme
                                                                                                inhibitor
                                                                                                primarily
                                                                              Irinotecan      used in the
                                                                             inhibits the    treatment of
                                                                               action of       colorectal
                                                                            topoisomera          cancer.
                                                                                  se I.      Irinotecan is
                                     acts as an                               Irinotecan      a derivative
                                    inhibitor of                               prevents              of
                      L               protein                               religation of    camptotheci
                      0                                                                              n.
                                   topoisomera                                 the DNA
                      1                           Colorectal
                          TOP1MT     se (DNA)                    anti-        strand by      Camptotheci
     irinotecan       X                          NeoplasmsN
                          TOP1      Iacts as an                neoplastic     binding to       ns interact
                      X                           eoplasms
                                    inhibitor of                            topoisomera       specifically
                      1
                      9               protein                                  se I-DNA         with the
                                   topoisomera                                 complex,          enzyme
                                    se (DNA) I                               and causes      topoisomera
                                                                                double-        se I which
                                                                             strand DNA          relieves
                                                                              breakage          torsional
                                                                                and cell        strain in
                                                                                 death.          DNA by
                                                                                                inducing
                                                                                               reversible
                                                                                             single-strand
                                                                                                 breaks.
                                                                                               Irinotecan
                                                                                                  and its
                                     acts as an                                                   active
                                    inhibitor of
     luteolin                         protein
                                   topoisomera
                                    se (DNA) I




32
                                                            Lymecycline      Lymecycline
                                                             inhibits cell         is a
                                                              growth by       tetracycline
                                                               inhibiting         broad-
                                                             translation.      spectrum
                                                              It binds to    antibiotic. It
                                                                the 30S             is
                                                              ribosomal      approximate
                                                             subunit and         ly 5000
                                                            prevents the      times more
                                                             amino-acyl      soluble than
                                                              tRNA from       tetracycline
                                                              binding to      base and is
                   J                                        the A site of         unique
                   0                                               the          amongst
                   1
                       rpsD rpsI                              ribosome.      tetracyclines
     lymecycline   A
                       tetR                                  The binding      in that it is
                   A
                                                            is reversible    absorbed by
                   0
                                                              in nature.      the "active
32
                   4
                                                            Lymecycline        transport"
                                                             is lipophilic       process
                                                                and can        across the
                                                              easily pass       intestinal
                                                             through the     wall, making
                                                                   cell        use of the
                                                              membrane         same fast
                                                            or passively     and efficient
                                                                diffuses      mechanism
                                                                through         by which
                                                                 porin       carbohydrat
                                                             channels in          es are
                                                            the bacterial    absorbed. It
     lysergol                                                membrane.        inhibits cell
                   J
                   0
                   1                Bacterial     anti-
     metacycline   A
                                   Infections   bacterial
                   A
                   0
                   5
                                                                    The
                                                            pharmacolog
                                                            ical effect of
                                                              Metopirone
                                                             is to reduce
                                                             cortisol and
                                                            corticosteron
                                                            e production
                                                            by inhibiting
                                                                  the 11-
                                                                 &szlig;-
                                                            hydroxylatio
                                                            n reaction in
                   V                                                        Metopirone
                                                             the adrenal
                   0                                                           is an
                                                                  cortex.
                   4                                                        inhibitor of
                       camC                                  Removal of
     metyrapone    C                                                       endogenous
                       CYP3A4                                  the strong
                   D                                                          adrenal
                                                                inhibitory
                   0                                                       corticosteroi
                   1
                                                                feedback
                                                                           d synthesis.
                                                             mechanism
                                                              exerted by
                                                                  cortisol
                                                            results in an
                                                              increase in
                                                            adrenocortic
                                                                  otropic
                                                                 hormone
                                                                  (ACTH)
                                                              production
                                                                   by the
                                                                pituitary.
                                                                    With
                                                               continued
                                                    Nifedipine       Nifedipine,
                                                   inhibits the           the
                                                     influx of     prototype of
                                                 extracellular            the
                                                     calcium       dihydropyridi
                                                     through         ne class of
                                                   myocardial          calcium-
                                                 and vascular          channel
                                                   membrane        antagonists,
                                                     pores by       is similar to
                                                    physically          other
                                                 plugging the      dihydropyridi
                                                 channel. The      nes including
                      C                           decrease in       amlodipine,
                      0                           intracellular      felodipine,
                      8
                                      cardiac        calcium         isradipine,
nifedipine            C   CACNA2D1
                                     stimulant     inhibits the          and
                      A
                                                    contractile     nicardipine.
                      0
                      5
                                                 processes of      Nifedipine is
                                                      smooth       used to treat
                                                 muscle cells,     Prinzmetal's
                                                     causing           angina,
                                                    dilation of    hypertension
                                                 the coronary        , and other
                                                 and systemic          vascular
                                                     arteries,        disorders
                                                    increased          such as
                                                      oxygen          Raynaud's
                                                    delivery to    phenomenon
                                                        the        . By blocking
                                                   myocardial       the calcium
                                                      tissue,         channels,
pancuronium_bromide                                 decreased         Nifedipine
                                                 Paroxetine is      Paroxetine,
                                                 a potent and              an
                                                       highly      antidepressa
                                                     selective       nt drug of
                                                   inhibitor of    the selective
                                                    neuronal          serotonin
                                                    serotonin         reuptake
                                                    reuptake.          inhibitor
                                                   Paroxetine      (SSRI) type,
                                                 likely inhibits        has no
                                                 the reuptake            active
                                                  of serotonin      metabolites
                                                       at the       and has the
                      N                             neuronal            highest
                      0                           membrane,          specificity
                      6   SLC6A4
                                                    enhances       for serotonin
paroxetine            A   SLC6A2
                                                  serotonergic      receptors of
                      B   HTR2A
                                                 neurotransm            all the
                      0
                      5
                                                     ission by      SSRIs. It is
                                                     reducing      used to treat
                                                   turnover of       depression
                                                        the         resistant to
                                                 neurotransm             other
                                                       itter,      antidepressa
                                                   therefore it           nts,
                                                  prolongs its       depression
                                                    activity at     complicated
                                                     synaptic       by anxiety,
                                                     receptor            panic
                                                    sites and         disorder,
                                                   potentiates       social and
                                                   5-HT in the          general
Prestwick-664                                          CNS;             anxiety
Prestwick-665
                      S
                      0
                      1
proxymetacaine        H
                      A
                      0
                      4
                                                                                       Rimexolone
                                                                                             is a
                                                                      Betamethas      glucocorticoi
                                                                          one is a             d
                                                                     glucocorticoi    corticosteroi
                                                                        d receptor          d for
                                                                      agonist. The        systemic
                                                                      antiinflamm            use.
                                                                     atory actions    Corticosteroi
                                                                              of       ds suppress
                                                                      corticosteroi          the
                                                                           ds are      inflammator
                                                                        thought to      y response
                     H   S                                                involve       to a variety
                     0   0                                                               of inciting
                                                                       lipocortins,
                     2   1
                             SERPINA6                                phospholipas       agents of a
rimexolone           A   B
                             ANXA1                                          e A2       mechanical,
                     B   A
                                                                         inhibitory   chemical, or
                     1   1
                     2   3                                                proteins    immunologic
                                                                           which,        al nature.
                                                                          through      They inhibit
                                                                      inhibition of        edema,
                                                                      arachidonic          cellular
                                                                      acid, control     infiltration,
                                                                             the          capillary
                                                                      biosynthesis       dilatation,
                                                                              of        fibroblastic
                                                                      prostaglandi    proliferation,
                                                                           ns and     deposition of
                                                                     leukotrienes.    collagen and
                                                                                             scar
                                                                                         formation
skimmianine                                                                              associated
                     J
                     0
                     1                   Bacterial      anti-
sulfametoxydiazine   E
                                        Infections    bacterial
                     D
                     0
                     4
                     J
                     0
                     1                   Bacterial      anti-
sulfaphenazole       E
                                        Infections    bacterial
                     D
                     0
                     8
thioguanosine
                     D   P                               anti-
                     0   0                           proliferative
                     1   2                               anti-
tiabendazole         A   C                            helminthic
                     C   A                               anti-
                     0   0                            protozoal
                     6   2                           anti-fungal
                                                                     Tinidazole is    Tinidazole is
                                                                             an         a synthetic
                                                                     antiprotozoal    antiprotozoal
                                                                      agent. The           agent.
                                                                      nitro group       Tinidazole
                                                                     of tinidazole    demonstrate
                                                                       is reduced         s activity
                                                                           by cell     both in vitro
                                                                       extracts of          and in
                                                                     <i>Trichomo           clinical
                                                                        nas</i>.         infections
                                                                         The free      against the
                                                                      nitro radical       following
                     J   P                                           generated as        protozoa:
                     0   0                                             a result of    <i>Trichomo
                     1   1
                                        Protozoan       anti-               this             nas
tinidazole           X   A
                                        Infections    protozoal         reduction      vaginalis</i
                     D   B
                                                                          may be               >,
                     0   0
                     2   2
                                                                      responsible       <i>Giardia
                                                                          for the     duodenalis<
                                                                     antiprotozoal        /i> (also
                                                                     activity. The         termed
                                                                      mechanism             <i>G.
                                                                         by which     lamblia</i>)
                                                                        tinidazole          , and
                                                                         exhibits     <i>Entamoe
                                                                          activity            ba
                                                                          against     histolytica</
                                                                     <i>Giardia<              i>.
                                                                          /i> and       Tinidazole
                                                                     <i>Entamoe           does not
                                                                          ba</i>         appear to
                                                                        species is    have activity
                                        Hypertensio    anti-
todralazine
                                            n       hypertensive
                     D   D
                     0   0
                     5   5
trioxysalen          A   B
                     D   A
                     0   0
                     1   1
                                                                                                   Vidarabine is
                                                                                                    a synthetic
                                                                                                        purine
                                                                                                     nucleoside
                                                                                                      analogue
                                                                                    Vidarabine       with <i>in
                                                                                       stops          vitro</i>
                                                                                  replication of     and <i>in
                                                                                   herpes viral       vivo</i>
                                           acts as a                                                 inhibitory
                                                                                     DNA in 3
                                          substrate                                                    activity
                                                                                     ways: 1)
                                          analog of                                                    against
                                                                                   competitive
                                        proteins with                                                  herpes
                                                                                   inhibition of
                   J   S                nucleobase,                                                    simplex
                                                                                     viral DNA
                   0   0                 nucleoside,                                               virus types 1
                                                                                  polymerase,
                   5   1                  nucleotide                                                (HSV-1), 2
                                                          Virus                          2)
     vidarabine    A   A   36 TK deoD    and nucleic                anti-viral
                                                        Diseases                   incorporatio       (HSV-2),
                   B   D                     acid
                                                                                    n into and     and varicella-
                   0   0                 transporter
                                                                                   termination      zoster virus
                   3   6                 activityacts
                                                                                       of the       (VZV). The
                                         as a binder                                                 inhibitory
                                                                                  growing viral
                                          of protein                                                 activity of
                                                                                    DNA chain,
                                        topoisomera                                                Vidarabine is
                                                                                      and 3)
                                         se (DNA) I                                                     highly
                                                                                   inactivation
                                                                                    of the viral   selective due
                                                                                        DNA        to its affinity
                                                                                  polymerase.           for the
                                                                                                       enzyme
                                                                                                     thymidine
                                                                                                    kinase (TK)
                                                                                                    encoded by
                                                                                                      HSV and
                                                                   cardiovascul       Not            VZV. This
                                                                                                          Not
     arecoline             CHRM1
                                                                     ar agent       Available         Available
                                                                                                   Carteolol is a
                                                                                                     beta1 and
                                                                                                   beta2 (non-
                                                                                                     selective)
                                                                                                    adrenergic
                                                                                                      receptor-
                                                                                                       blocking
                                                                                                     agent that
                                                                                                      does not
                                                                                  The primary            have
                                                                                  mechanism          significant
                                                                                  of the ocular        intrinsic
                                                                                  hypotensive      sympathomi
                   C   S                                                            action of      metic, direct
                   0   0                                                                            myocardial
                                                                                   carteolol in
                   7   1
                           ADRB2                                                    reducing        depressant,
     carteolol     A   E
                           ADRB1                                                   intraocular          or local
                   A   D
                                                                                   pressure is       anesthetic
                   1   0
                   5   5                                                          most likely a    (membrane-
                                                                                  decrease in       stabilizing)
                                                                                    aqueous            activity.
                                                                                      humor          Carteolol,
                                                                                  production.            when
                                                                                                        applied
                                                                                                    topically to
                                                                                                   the eye, has
                                                                                                   the action of
                                                                                                      reducing
                                                                                                   elevated, as
                                                                                                        well as
                                                                                                       normal,
                                                                                                    intraocular
                   A                                                                                 pressure,
                   0
                   3
     clebopride    F
                   A

33
                   0
                   6
     coralyne
                   G
                   0
                   3
     nomegestrol   D
                   B
                   0
                   4
33



                                                                                            Prazosin is
                                                                                             an alpha-
                                                                                            adrenergic
                                                                                              blocking
                                                                          Prazosin acts     agent used
                                                                          by inhibiting        to treat
                                                                                the        hypertension
                                                                          postsynaptic      and benign
                                                                            alpha(1)-         prostatic
                                                                          adrenocepto      hyperplasia.
                                                                               rs on       Accordingly,
                                                                             vascular      Prazosin is a
                                                                              smooth          selective
                      C                                                   muscle. This      inhibitor of
                                     acts as an
                      0                                                    inhibits the     the alpha1
                                   antagonist of
                      2   ADRA1A                                          vasoconstrict     subtype of
                                       protein   Hypertensio    anti-
     prazosin         C   ADRA1B                                           or effect of
                                    adrenergic,      n       hypertensive                       alpha
                      A   ADRA1D                                            circulating
                                    alpha-2B-,                                              adrenergic
                      0                                                    and locally
                                      receptor                                             receptors. In
                      1                                                      released       the human
                                                                          catecholami        prostate,
                                                                                nes           Prazosin
                                                                          (epinephrine     antagonizes
                                                                                and        phenylephrin
                                                                          norepinephri       e (alpha1
                                                                                ne),         agonist)-
                                                                           resulting in       induced
                                                                            peripheral     contractions,
                                                                          vasodilation.         <i>in
                                                                                             vitro</i>,
                                                                                             and binds
                                                                                             with high
                                                                                             affinity to

                                                                                            Aminophena
                                                                                               zone is a
                                                                                             pyrazolone
                                                                                                  with
                                                                                              analgesic,
                                                                                                  anti-
                                                                                            inflammator
                                                                                                y, and
                                                                                             antipyretic
                                                                                              properties
                      N                                                                     but has risk
                      0                                                                            of
                      2                                                                    agranulocyto
                                                                               Not
     aminophenazone   B                                                                    sis. A breath
                                                                             Available
                      B                                                                        test with
                      0                                                                     13C-labeled
                      3                                                                     aminopyrine
                                                                                              has been
                                                                                              used as a
                                                                                           non-invasive
                                                                                             measure of
                                                                                             cytochrome
                                                                                                 P-450
                                                                                              metabolic
                                                                                              activity in
                                                                                           liver function
                                                                                                 tests.


                                                                            Astemizole
                                                                             competes
                                                                                 with
                                                                             histamine
                                                                            for binding
                                                                                  at
                                                                                            Astemizole,
                                                                           H<sub>1</s
                                                                                                   an
                                                                                ub>-
                                                                                           H<sub>1</s
                                                                              receptor
                                                                                                 ub>-
                                                                            sites in the
                                                                                              receptor
                                                                              GI tract,
                                                                                            antagonist,
                                     acts as an                            uterus, large
                                                                                            is similar in
                                   antagonist of                                blood
                      R                                                                     structure to
                                       protein                             vessels, and
                      0                                                                     terfenadine
                                     histamine                               bronchial
                      6   HRH1                                                                    and
                                      receptor                    anti-    muscle. This
     astemizole       A   CYP3A3                                                            haloperidol,
                                    H1acts as a                histamine     reversible
                      X   KCNH2                                                                     a
                                     binder of                               binding of
                      1                                                                    butyropheno
                      1                protein                              astemizole
                                                                                                   ne
                                     histamine                                    to
                                                                                           antipsychotic
                                    receptor H1                            H<sub>1</s
                                                                                               . It has
                                                                                ub>-
                                                                                           anticholinerg
                                                                             receptors
                                                                                           ic (atropine-
                                                                            suppresses
                                                                                              like) and
                                                                                 the
                                                                                             antipruritic
                                                                           formation of
                                                                                               effects.
                                                                               edema,
                                                                             flare, and
                                                                               pruritus
                                                                              resulting
                                                                                from
                                                                            histaminic
     atropine_oxide                                                         activity. As
                         R
                         0                 acts as an
                         6               antagonist of
                                                                        anti-
     chlorphenamine      A                  protein
                                                                     histamine
                         B                 histamine
                         0                receptor H1
                         4
                                                                                 Two theories     Dihydroergot
                                                                                   have been         amine is
                                                                                  proposed to     indicated for
                                                                                   explain the      the acute
                                                                                 efficacy of 5-   treatment of
                                                                                  HT<sub>1D          migraine
                                                                                      </sub>       headaches
                                                                                     receptor         with or
                                                                                   agonists in    without aura
                                           acts as an                             migraine: 1)       and the
                                         antagonist of                            activation of        acute
                                           protein 5-                                    5-       treatment of
                                         hydroxytrypt                             HT<sub>1D           cluster
                         N                   amine                                    </sub>        headache
                         0                                                          receptors       episodes.
                                          (serotonin)
                         2       HTR1D
                                            receptor                vasoconstrict located on      Dihydroergot
     dihydroergotamine   C       HTR1B                   Migraine
                                         2Aacts as an                    or       intracranial    amine binds
                         A       HTR2A
                                           agonist of                                  blood        with high
                         0
                         1                 protein 5-                                vessels,     affinity to 5-
                                         hydroxytrypt                               including     HT<sub>1D
                                             amine                                   those on       </sub>a
                                          (serotonin)                                 arterio-        and 5-
                                          receptor 1D                                 venous      HT<sub>1D
                                                                                 anastomoses        </sub>b
                                                                                    , leads to    receptors. It
                                                                                 vasoconstrict      also binds
                                                                                   ion, which       with high
                                                                                    correlates      affinity to
                                                                                     with the     serotonin 5-
                                                                                      relief of   HT<sub>1A
                                                                                    migraine       </sub>, 5-
                                                                                    headache      HT<sub>2A
                         N                                                             and 2)     </sub>, and
                         0
                         6
     dosulepin           A
                         A
                         1
                         6
                         D   G
                         0   0
                         1   1
     isoconazole         A   A
                         C   F
                         0   0
                         5   7
                                                                                                  Mefloquine is
                                                                                                         an
                                                                                                   antimalarial
                                                                                                  agent which
                                                                                                    acts as a
                                                                                    Mefloquine
                                                                                                       blood
                                                                                     has been
                                                                                                  schizonticide
                                                                                     found to
                                                                                                  . Mefloquine
                                                                                     produce
                                                                                                     is active
                                                                                    swelling of
                                                                                                   against the
                                                                                         the
                                                                                                   erythrocytic
                                                                                  <i>Plasmodi
                                                                                                    stages of
                                                                                         um
                                                                                                  Plasmodium
                         P                                                        falciparum</
                                                                                                     species.
                         0                                                            i> food
                                                                                                    However,
                         1                                                         vacuoles. It
                                                                                                  the drug has
     mefloquine          B       HBA1                    Malaria    anti-malarial may act by
                                                                                                    no effect
                         C                                                            forming
                                                                                                   against the
                         0                                                              toxic
                         2
                                                                                                  exoerythrocy
                                                                                    complexes
                                                                                                  tic (hepatic)
                                                                                     with free
                                                                                                  stages of the
                                                                                    heme that
                                                                                                    parasite.
                                                                                     damage
                                                                                                  Mefloquine is
                                                                                   membranes
                                                                                                     effective
                                                                                   and interact
                                                                                                      against
                                                                                    with other
                                                                                                      malaria
                                                                                    plasmodial
                                                                                                    parasites
                                                                                  components.
                                                                                                   resistant to
                                                                                                  chloroquine.
                                                                                                  Mefloquine is
                                                                                                      a chiral
                                                                                                    molecule.
                                                                                                  According to




34
                                                                            Nicergoline      Nicergoline
                                                                               acts by       is a potent
                                                                             inhibiting      vasodilator
                                                                                  the         (improves
                                                                           postsynaptic      brain blood
                                                                             alpha(1)-         flow). On
                                                                           adrenocepto      the cerebral
                                                                                rs on            level it
                                                                              vascular        prompts a
                                                                               smooth        lowering of
                                                                           muscle. This         vascular
                                                                            inhibits the     resistance,
                                                                           vasoconstrict     an increase
                                 C                                          or effect of      in arterial
                                 0                                           circulating        flow and
                                 4                                anti-
                                                                            and locally       stimulates
     nicergoline                 A   ADRA1A                     coagulant
                                                                              released        the use of
                                 E                             vasodilator
34
                                                                           catecholami       oxygen and
                                 0
                                 2
                                                                                  nes           glucose.
                                                                           (epinephrine      Nicergoline
                                                                                  and              also
                                                                           norepinephri        improves
                                                                                 ne),             blood
                                                                            resulting in    circulation in
                                                                             peripheral        the lungs
                                                                           vasodilation.      and limbs
                                                                             Therefore          and has
                                                                                  the       been shown
                                                                            mechanism          to inhibit
                                                                                   of             blood
                                                                            Nicergoline          platelet
                                                                                 is to      aggregation.
                                                                              increase
                                                 acts as an
                                                inhibitor of
     nordihydroguaiaretic_acid                proteins with
                                              lipoxygenase
                                                  activity
                                                                              Penbutolol
                                                                               competes
                                                                                  with
                                                                              adrenergic    Penbutolol is
                                                                            neurotransm         a non-
                                                                              itters such      selective
                                                                                   as       beta blocker.
                                                                             catecholami         Beta-
                                                                                 nes for       blockers
                                                                              binding at        work by
                                                                                beta(1)-    affecting the
                                                                              adrenergic     response to
                                                                             receptors in    some nerve
                                 C                                             the heart     impulses in
                                 0                                          and vascular    certain parts
                                 7   ORM1
                                                                                 smooth      of the body.
     penbutolol                  A   ADRB1
                                                                             muscle and      As a result,
                                 A   ADRB2
                                                                                beta(2)-         they
                                 2
                                 3
                                                                             receptors in   decrease the
                                                                            the bronchial   heart's need
                                                                            and vascular       for blood
                                                                                 smooth      and oxygen
                                                                                muscle.      by reducing
                                                                                Beta(1)-    its workload.
                                                                                receptor      They also
                                                                               blockade        help the
                                                                             results in a   heart to beat
                                                                             decrease in         more
                                                                             resting and      regularly.
                                                                                exercise
                                                                              heart rate
                                                                             and cardiac
                                 C                                             output, a
                                 0
                                 1                                              Not             Not
     prenylamine                 D
                                                                              Available       Available
                                 X
                                 0
                                 2
                                                               diagnostic
     proadifen
                                                                 agent
                                                                     Binds to and
                                                                      inhibits the    Used to treat
                                                                      angiotensin     hypertension
                                                                       converting              .
                                                                        enzyme.       Rescinnamin
                                                                     Rescinnamin         e inhibits
                                                                      e competes      angiotensin-
                                                                           with         converting
                                                                     angiotensin I       enzyme.
                                                                      for binding         ACE is a
                                                                          at the          peptidyl
                                                                     angiotensin-      dipeptidase
                                                                       converting           that
               C                                                        enzyme,          catalyzes
               0                                                     blocking the            the
               2
                                                                      conversion       conversion
rescinnamine   A   ACE
                                                                            of                of
               A
                                                                     angiotensin I    angiotensin I
               0
               1
                                                                            to             to the
                                                                      angiotensin     vasoconstrict
                                                                     II. Inhibition           or
                                                                         of ACE        substance,
                                                                        results in     angiotensin
                                                                       decreased              II.
                                                                         plasma        Angiotensin
                                                                      angiotensin          II also
                                                                          II. As        stimulates
                                                                      angiotensin      aldosterone
                                                                          II is a     secretion by
                                                                     vasoconstrict     the adrenal
                                                                        or and a          cortex.
                                                                       negative-
spiperone                                               tranquilizer    feedback
               C
               0
               4                                           anti-
suloctidil     A                           Thrombosis    coagulant
               X                                        vasodilator
               1
               9
                                                                     Terfenadine
                                                                       competes
                                                                           with
                                                                       histamine
                                                                      for binding
                                                                          at H1-      Terfenadine,
                                                                         receptor         an H1-
                                                                      sites in the       receptor
                                                                         GI tract,      antagonist
                                                                     uterus, large    antihistamin
                                                                           blood       e, is similar
                                                                     vessels, and      in structure
                                                                        bronchial            to
               R                                                     muscle. This       astemizole
               0             acts as an
                                                                       reversible           and
               6           antagonist of                bronchodilat
                   HRH1                                                binding of      haloperidol,
terfenadine    A              protein                     or anti-
                   KCNH2                                              terfenadine            a
               X             histamine                   histamine
                                                                          to H1-      butyropheno
               1            receptor H1
               2
                                                                        receptors            ne
                                                                      suppresses      antipsychotic
                                                                            the        . The active
                                                                     formation of       metabolite
                                                                         edema,              of
                                                                       flare, and      terfenadine
                                                                         pruritus            is
                                                                        resulting     fexofenadine
                                                                           from               .
                                                                       histaminic
                                                                      activity. As
                                                                        the drug
                                                                        does not
                                                                     readily cross
                                                                       the blood-
                                                                                        Trimipramin
                                                                                              e is a
                                                                                             tricyclic
                                                                                       antidepressa
                                                                                           nt. It was
                                                                                        thought that
                                                                                             tricyclic
                                                                      Trimipramin      antidepressa
                                                                            e's          nts work by
                                                                       mechanism           inhibiting
                                                                         of action           the re-
                                                                       differs from        uptake of
                                                                           other                the
                             N                                           tricyclic     neurotransm
                             0                                                                itters
                                                                      antidepressa
                             6                                                         norepinephri
                                 SLC6A4                     anti-           nts.
     trimipramine            A              Depression
                                 SLC6A2                  depressant   Trimipramin            ne and
                             A
                                                                        e acts by       serotonin by
                             0
                                                                       decreasing        nerve cells.
                             6
                                                                      the reuptake         However,
                                                                             of                 this
                                                                      norepinephri         response
                                                                          ne and              occurs
                                                                      serotonin (5-    immediately,
                                                                           HT).            yet mood
                                                                                        does not lift
                                                                                          for around
                                                                                         two weeks.
                                                                                            It is now
                                                                                        thought that
                                                                                            changes
                                                                                            occur in
     alfadolone                                                                             receptor
                                                                                       Aminocaproi
                                                                                       c acid works
                                                                                              as an
                                                                                       antifibrinolyt
                                                                                           ic. It is a
                                                                                       derivative of
                                                                                         the amino
                                                                      Aminocaproi       acid lysine.
                                                                       c acid binds            The
                                                                      reversibly to     fibrinolysis-
                             B                                          the kringle       inhibitory
                             0                                           domain of        effects of
                             2                                        plasminogen      aminocaproi
                                 PLG PLAT
     aminocaproic_acid       A                                          and blocks           c acid
                                 LPA
                             A                                          the binding    appear to be
                             0                                               of             exerted
                             1                                        plasminogen        principally
                                                                       to fibrin and   via inhibition
                                                                      its activation            of
                                                                        to plasmin.    plasminogen
                                                                                         activators
                                                                                           and to a
                                                                                             lesser
                                                                                             degree
                                                                                            through
                                                                                        antiplasmin
                                                                                            activity.
                             N
                             0
                             1
     articaine               B
                             B
                             0
                             8
     atropine_methonitrate
     enilconazole




35
                                                 The      Gliquidone is
                                          mechanism          an anti-
                                          of action of    diabetic drug
                                         gliquidone in          in the
                                             lowering     sulfonylurea
                                               blood         class. In
                                              glucose     patients with
                                           appears to        diabetes
                                                  be         mellitus,
                                           dependent        there is a
                                                  on      deficiency or
                                          stimulating     absence of a
                                          the release       hormone
                     A                      of insulin    manufacture
                     1                          from         d by the
                     0
                                          functioning       pancreas
     gliquidone      B
                                           pancreatic           called
35
                     B
                                           beta cells,        insulin.
                     0
                     8
                                                 and      Insulin is the
                                           increasing            main
                                         sensitivity of     hormone
                                           peripheral      responsible
                                            tissues to         for the
                                              insulin.      control of
                                           Gliquidone      sugar in the
                                          likely binds         blood.
                                              to ATP-     Gliquidone is
                                            sensitive             an
                                           potassium       antidiabetic
                                              channel      medication
                                         receptors on        which is
                                                 the          used in
                                           pancreatic
                                              Organic           those
                                              iodine
                                          compounds
                                             such as
                                         metrizamide
                                         block x-rays
                                         as they pass
                                         through the
                                              body,
                                            thereby
                                            allowing
                                               body
                                           structures
                     V                     containing
                     0                   iodine to be
                     8
                                         delineated in        Not
     metrizamide     A
                                          contrast to       Available
                     B
                                               those
                     0
                     1
                                           structures
                                          that do not
                                             contain
                                          iodine. The
                                           degree of
                                             opacity
                                         produced by
                                               these
                                          compounds
                                           is directly
                                         proportional
                                          to the total
                                            amount
                                         (concentrati
                          acts as an         on and
                          agonist of
                         proteins with
     Prestwick-972
                             GABA
                           receptor
                            activity
     tiletamine
                                                                                   The        Amantadine
                                                                              mechanism             is an
                                                                                  of its         antiviral
                                                                             antiparkinso      drug which
                                                                              nic effect is    also acts as
                                                                                 not fully            an
                                                                             understood,      antiparkinso
                                                                                  but it       n agent, for
                                                                              appears to        which it is
                                                                             be releasing         usually
                                                                               dopamine         combined
                                                                                from the      with L-DOPA
                                                                                  nerve          when L-
                        N                                                     endings of           DOPA
                        0                           Influenza
                                                                                the brain       responses
                        4                           Parkinson
                                        DRD2 DRD1                                 cells,          decline
     amantadine         B                            Disease    anti-viral
                                        M                                       together        (probably
                        B                             Virus
                                                                                   with           due to
                        0                           Diseases
                        1
                                                                              stimulation      tolerance).
                                                                                    of             It is a
                                                                             norepinephri      derivate of
                                                                             ne response.     adamantane
                                                                             The antiviral        , like a
                                                                              mechanism       similar drug
                                                                             seems to be      rimantadine.
                                                                              unrelated.             The
                                                                                The drug       mechanism
                                                                               interferes      of action of
                                                                              with a viral     amantadine
                                                                              protein, M2          in the
                                                                                 (an ion      treatment of
                                                                               channel),       Parkinson's
                                                                                 which is      disease and
                                                                                               Benzocaine
                                                                                                  is a local
                                                                                                 anesthetic
                                                                                                 commonly
                                                                              Benzocaine          used as a
                                                                                  binds to      topical pain
                                                                                  sodium      reliever. It is
                                                                              channel and        the active
                                                                               reversibly     ingredient in
                                                                                stabilizes      many over-
                                                                             the neuronal       the-counter
                                                                               membrane           analgesic
                                                                                   which      ointments. It
                        C   D   N   R                                        decreases its          is also
                        0   0   0   0                                                          indicated for
                                                                              permeability
                        5   4   1   2
                                                                               to sodium        general use
     benzocaine         A   A   B   A   SCN10A                  anesthetic
                                                                                    ions.            as a
36
                        D   B   A   D
                                                                              Depolarizati    lubricant and
                        0   0   0   0
                        3   4   5   1                                            on of the         topical
                                                                                 neuronal        anesthetic
                                                                             membrane is               on
                                                                                 inhibited    intratracheal
                                                                                  thereby         catheters
                                                                              blocking the            and
                                                                             initiation and     pharyngeal
                                                                               conduction         and nasal
                                                                                 of nerve        airways to
                                                                                impulses.        obtund the
                                                                                                pharyngeal
                                                                                               and tracheal
                                                                                                reflexes; on
                                                                                                nasogastric
     gabexate                                                                                         and
     levopropoxyphene
                                                                                                Nystatin is
                                                                                               an antibiotic
                                                                                                   which is
                                                                                                     both
                                                                                  Nystatin
                                                                                                 fungistatic
                                                                                  interacts
                                                                                                     and
                                                                                  with 14-
                                                                                               fungicidal in
                                                                                   &alpha;
                                                                                               vitro against
                                                                               demethylase
                                                                                                    a wide
                                                                                      ,a
                                                                                                  variety of
                                                                               cytochrome
                                                                                                yeasts and
                                                                                    P-450
                                                                                                 yeast-like
                                                                                   enzyme
                                                                                                    fungi,
                A   D   G                                                        necessary
                                                                                                  including
                0   0   0                                                          for the
                                                                                               <i>Candida
                7   1   1                                                       conversion
                                                                                               albicans</i>
nystatin        A   A   A   ERG11                     Mycoses    anti-fungal   of lanosterol
                                                                                                   , <i>C.
                A   A   A                                                             to
                                                                                                parapsilosis
                0   0   0                                                       ergosterol.
                2   1   1
                                                                                               </i>, <i>C.
                                                                                This results
                                                                                               tropicalis</i
                                                                               in inhibition
                                                                                                  >, <i>C.
                                                                               of ergosterol
                                                                                               guilliermondi
                                                                                 synthesis
                                                                                               </i>, <i>C.
                                                                                     and
                                                                                               pseudotropic
                                                                                 increased
                                                                                                  alis</i>,
                                                                                    fungal
                                                                                                    <i>C.
                                                                                   cellular
                                                                                                krusei</i>,
                                                                               permeability
                                                                                               <i>Torulopsi
                                                                                       .
                                                                                                       s
                                                                                               glabrata</i>
                                                                                                       ,
                                                                                               <i>Tricophyt
Prestwick-682                                                                                         on
                M
                0                                                  analgesic
                1                                    Inflammatio      anti-
acemetacin      A
                                                         nPain   inflammator
                B
                                                                       y
                1
                1
                                                                               Bumetanide       Bumetanide
                                                                                 interferes        is a loop
                                                                                 with renal      diuretic of
                                                                               cAMP and/or     the sulfamyl
                                                                                inhibits the    category to
                                                                                   sodium-       treat heart
                                                                                 potassium      failure. It is
                                                                                   ATPase      often used in
                                                                                    pump.        patients in
                                                                               Bumetanide       whom high
                                                                                 appears to        doses of
                                        acts as a
                                                                                  block the     furosemide
                                        binder of
                                                                                     active            are
                C                        protein
                                                                               reabsorption     ineffective.
                0           SLC12A1       solute
                                                                                 of chloride       There is
                3           CFTR          carrier
                                                                               and possibly     however no
bumetanide      C           SLC12A2     family 12                  diuretic
                                                                                 sodium in       reason not
                A           SLC12A4   (sodium/pot
                                                                                      the            to use
                0           SLC12A5   assium/chlor
                2
                                                                                 ascending      bumetanide
                                            ide
                                                                                    loop of       as a first
                                      transporters
                                                                                    Henle,     choice drug.
                                      ), member 1
                                                                                   altering       The main
                                                                                 electrolyte      difference
                                                                                 transfer in   between the
                                                                               the proximal           two
                                                                                tubule. This    substances
                                                                                  results in          is in
                                                                                excretion of   bioavailabilit
                                                                                   sodium,      y. It is said
                                                                               chloride, and   to be a more
                                                                                 water and,     predictable
                                                                                    hence,         diuretic,
                                                                                  diuresis.        meaning
                                                                                Local      Bupivacaine
                                                                           anesthetics       is a widely
                                                                               such as        used local
                                                                           bupivacaine       anesthetic
                                                                             block the           agent.
                                                                            generation     Bupivacaine
                                                                               and the          is often
                                                                            conduction     administered
                                                                              of nerve        by spinal
                                                                             impulses,         injection
                                                                           presumably      prior to total
                                                                                  by               hip
                                                                            increasing     arthroplasty.
                             N                                                   the           It is also
                             0                                            threshold for      commonly
                             1
                                 SCN10A                                       electrical   injected into
     bupivacaine             B                             anesthetic
                                 PTGER1                                    excitation in        surgical
                             B
                                                                            the nerve,      wound sites
                             0
                             1
                                                                            by slowing        to reduce
                                                                                 the        pain for up
                                                                           propagation      to 20 hours
                                                                           of the nerve           after
                                                                          impulse, and      surgery. In
                                                                           by reducing      comparison
                                                                            the rate of         to other
                                                                            rise of the           local
                                                                                action      anesthetics
                                                                           potential. In   it has a long
                                                                           general, the     duration of
                                                                           progression      action. It is
                                                                                  of            also the
                                                                          anesthesia is    most toxic to
                             A                                               related to       the heart
                             0
                             5                            gastrointesti
     chenodeoxycholic_acid   A               Gallstones
                                                           nal agent
                             A
                             0
                             1
                                                                                 The       Diethylcarba
                                                                           mechanism       mazine is an
                                                                            of action of   anthelmintic
                                                                           diethylcarba       drug that
                                                                             mazine is        does not
                                                                            thought to        resemble
                                                                               involve          other
                                                                            sensitizing    antiparasitic
                                                                                 the       compounds.
                                                                           microfilariae        It is a
                                                                                  to          synthetic
                                                                          phagocytosis         organic
                                                                           . One study       compound
                             P                                             showed that         which is
                             0                                             diethylcarba         highly
                             2
                                 ALOX5 MT-   Parasitic        anti-           mazine's      specific for
     diethylcarbamazine      C
                                 CO1         Diseases       parasitic          activity        several
                             B
                                                                               against        parasites
                             0
                             2
                                                                            <i>Brugia      and does not
                                                                           malayi</i>       contain any
                                                                           microfilariae         toxic
                                                                          is dependent         metallic
                                                                           on inducible      elements.
                                                                           nitric-oxide    Diethylcarba
                                                                              synthase         mazine
                                                                               and the     continues to
                                                                           cyclooxygen         be the
                                                                                 ase       mainstay for
                                                                           pathway. It     treatment of
                                                                            confirmed      patients with
                                                                                 the         lymphatic
                                                                             important     filariasis and
                                                                            role of the        loiasis.




37
                                                                                      The
                                                                                               Dimenhydrin
                                                                               mechanism
                                                                                                   ate is an
                                                                                  by which
                                                                                                antiemetics
                                                                                    some
                                                                                                     drug
                                                                              antihistamin
                                                                                                combination
                                                                                  es exert
                                                                                               that contains
                                                                                     their
                                                                                               diphenhydra
                                                                                antiemetic,
                                                                                                  mine and
                                                                              anti&ndash;
                                                                                               theophylline.
                                                                                   motion
                                                                                                   It is not
                                                                                  sickness,
                                                                                                 effective in
                                                                                      and
                                                                                                      the
                                                                                antivertigo
                                                                                               treatment of
                                                                              effects is not
                                                                                                    nausea
                                                                                  precisely
                                                                                                  associated
                                                                                known but
     dimenhydrinate       HRH1                                                                  with cancer
                                                                                   may be
                                                                                                chemothera
                                                                                 related to
                                                                                                      py.
                                                                              their central
                                                                                               Dimenhydrin
                                                                              anticholinerg
37                                                                               ic actions.
                                                                                    They
                                                                                                ate directly
                                                                                                 inhibits the
                                                                                                 stimulation
                                                                                  diminish
                                                                                                  of certain
                                                                                 vestibular
                                                                                               nerves in the
                                                                                stimulation
                                                                                                  brain and
                                                                              and depress
                                                                                                inner ear to
                                                                               labyrinthine
                                                                                                   suppress
                                                                              function. An
                                                                                                   nausea,
                                                                              action on the
                                                                                                  vomiting,
                                                                                 medullary
                                                                                                  dizziness,
                                                                              chemorecept
                                                                                                and vertigo.
                                                                                ive trigger
                      R                                                          zone may
                      0
                      5
     dropropizine     D                             Cough      anti-tussive
                      B
                      1
                      9
                                                                            Enalaprilat,       Enalapril, an
                                                                             the active        angiotensin-
                                                                            metabolite           converting
                                                                           of enalapril,           enzyme
                                                                             competes                (ACE)
                                                                                 with           inhibitor, is
                                                                           angiotensin I         a prodrug
                                                                            for binding        which, when
                                                                                at the          hydrolyzed
                                                                           angiotensin-        by estarases
                                                                            converting          to its active
                                                                              enzyme,           Enalaprilat,
                                      acts as an
                                                                           blocking the          is used to
                      C              inhibitor of
                                                                            conversion                treat
                      0                protein
                                                                                  of           hypertension
                      9             angiotensin I
                                                  Hypertensio    anti-     angiotensin I         and heart
     enalapril        A   ACE ACE    converting
                                                      n       hypertensive        to             failure, to
                      A                enzyme
                                                                            angiotensin             reduce
                      0               (peptidyl-
                      2
                                                                           II. Inhibition       proteinuria
                                     dipeptidase
                                                                               of ACE             and renal
                                         A) 1
                                                                             results in          disease in
                                                                             decreased         patients with
                                                                               plasma          nephropathi
                                                                            angiotensin          es, and to
                                                                                II. As             prevent
                                                                            angiotensin            stroke,
                                                                                II is a         myocardial
                                                                           vasoconstrict         infarction,
                                                                              or and a          and cardiac
                                                                             negative-             death in
                                                                              feedback            high-risk
                                                                           mediator for           patients.
                                                                                renin          Enalapril and
                                                                                                                           Fenofibrate Fenofibrate
                                                                                                                             exerts its    is a lipid
                                                                                                                           therapeutic    regulating
                                                                                                                                effects       agent
                                                                                                                              through    indicated as
                                                                                                                          activation of adjunctive
                                                                                                                           peroxisome     therapy to
                                                                                                                           proliferator      diet to
                                                                                                                             activated      reduce
                                                                                                                            receptor a elevated LDL-
                                                                                                                             (PPARa).      C, Total-
                                                                                                                                 This    C,Triglycerid
                                                                                  acts as an                                 increases    es and Apo
                              C                                                   agonist of                              lipolysis and    B, and to
                              1                                                                                            elimination increase HDL-
                                                                                    protein
                              0                                                                                 anti-
                                                                      PPARA      peroxisome      Hyperlipide                       of      C in adult
     fenofibrate              A                                                                              hyperlipidem
                                                                      mmp20      proliferator-      mia                   triglyceride- patients with
                              B                                                                                   ic
                                                                                  activated                               rich particles    primary
                              0
                              5                                                    receptor                               from plasma hypercholest
                                                                                     alpha                                by activating erolemia or
                                                                                                                           lipoprotein       mixed
                                                                                                                            lipase and dyslipidemia
                                                                                                                              reducing   (Fredrickson
                                                                                                                            production     Types IIa
                                                                                                                                   of      and IIb).
                                                                                                                          apoprotein C- Fenofibrate
                                                                                                                               III. The      is also
                                                                                                                          resulting fall indicated as
                                                                                                                                   in     adjunctive
                                                                                                                          triglycerides therapy to
                                                                                                                          produces an       diet for
                                                                                                                          alteration in treatment of
                                                                                                                          the size and        adult
                                                                                                                                            Niflumic
                                                                                                                                                  acid, a
                                                                                                                                             nonsteroidal
                                                                                                                                                    anti-
                              M   M                                                                                                          inflammator
                              0   0
                                                                                                                                             y fenamate,
                              1   2                                                                               anti-
                                                                                                 Inflammatio                    Not                  is a
     niflumic_acid            A   A                                   CLCNKA                                 inflammator
                                                                                                     nPain                    Available      Ca<sup>2+
                              X   A                                                                           yanalgesic
                              0   1                                                                                                             </sup>-
                              2   7                                                                                                             activated
                                                                                                                                                Cl<sup>-
                                                                                                                                                 </sup>
                                                                                                                                                 channel
                                                                                                                                                 blocker.
                                                                                                                          Glucocorticoi     Prednisolone
                                                                                                                             ds such as              is a
                                                                                                                          Prednisolone          synthetic
                                                                                                                             can inhibit    glucocorticoi
                                                                                                                              leukocyte         d used as
                                                                                                                          infiltration at    antiinflamm
                                                                                                                             the site of         atory or
                                                                                                                           inflammatio      immunosupp
                                                                                                                            n, interfere          ressive
                                                                                                                                  with            agent.
                                                                                                                          mediators of      Prednisolone
                                                                                                                           inflammator        is indicated
                                                                                                                            y response,            in the
                              A   C   D   D   H   R   S   S   S   S                                                               and       treatment of
                              0   0   0   0   0   0   0   0   0   0                                                            suppress          various
                                                                                                 Inflammatio       anti-
                              7   5   7   7   2   1   1   1   2   3
                                                                                                       n      inflammator      humoral         conditions,
     prednisolone             E   A   A   X   A   A   B   C   B   B   SERPINA6
                                                                                                 Hypersensiti     y anti-      immune           including
                              A   A   A   A   B   D   A   B   A   A
                                                                                                      vity       allergy    responses.         congenital
                              0   0   0   0   0   0   0   0   0   0
                              1   4   3   2   6   2   4   2   3   2
                                                                                                                                  The            adrenal
                                                                                                                           antiinflamm       hyperplasia,
                                                                                                                          atory actions          psoriatic
                                                                                                                                   of           arthritis,
                                                                                                                          glucocorticoi         systemic
                                                                                                                                 ds are            lupus
                                                                                                                             thought to     erythematos
                                                                                                                                involve        us, bullous
                                                                                                                          phospholipas         dermatitis
                                                                                                                                  e A2       herpetiformi
                                                                                                                              inhibitory      s, seasonal
                                                                                                                               proteins,     or perennial
                                                                                                                            lipocortins,         allergic
                                                                                                                                 which           rhinitis,
     telenzepine                                                                                                            control the          allergic
     atractyloside
                              V
                              0
                              3                                                                                 nutritive
     calcium_folinate         A
                                                                                                                 agent
                              F
                              0
                              3
     glycopyrronium_bromide
     guanadrel
                                                                                                                  cardiac
38                                                                                                              stimulant
                                                                                                                  muscle
     khellin                                                                                       Spasm
                                                                                                                 relaxant
                                                                                                              (spasmolytic
                                                                                                                     )
38

                           J
                           0
                           1                                   Bacterial
     sulfadimethoxine      E
                                                              Infections
                           D
                           0
                           1
     butirosin
                                                                                          Carbinoxami      Carbinoxami
                                                                                          ne competes          ne is an
                                                                                             with free     antihistamin
                                                                                            histamine          e of the
                                                                                           for binding     ethanolamin
                                                                                              at HA-           e class.
                                                                                             receptor      Ethanolamin
                                                                                            sites. This            e
                                                                                          antagonizes      antihistamin
                                                                                           the effects         es have
                                                                                          of histamine       significant
                                                                                              on HA-       antimuscarin
                                                                                            receptors,       ic activity
                           R                                                              leading to a     and produce
                           0                    acts as an
                                                                                          reduction of         marked
                           6                  antagonist of
                               HRH1                                                       the negative      sedation in
     carbinoxamine         A                     protein
                               CHRM1                                                        symptoms            most
                           A                    histamine
                                                                                           brought on       patients. In
                           0                   receptor H1
                           8
                                                                                          by histamine      addition to
                                                                                          HA-receptor         the usual
                                                                                             binding.          allergic
                                                                                          Carbinoxami       symptoms,
                                                                                                ne's          the drug
                                                                                          anticholinerg      also treats
                                                                                             ic action         irritant
                                                                                           appears to        cough and
                                                                                           be due to a         nausea,
                                                                                              central        vomiting,
                                                                                          antimuscarin      and vertigo
                                                                                             ic effect,      associated
                                                                                            which also     with motion
                                                                                              may be        sickness. It
                                                                              muscle       responsible      also is used
                                                                             relaxant
     drofenine
                                                                           (spasmolytic
                                                                                 )

39                                              acts as an
                                               inhibitor of
                                              proteins with
     isopropamide_iodide
                                              acetylcholine
                                                 receptor
                                                  activity
                                                                                          Aminoglycosi
                                                                                           des work by
                                                                                            binding to
                                                                                          the bacterial
                                                                                                 30S
                                                                                             ribosomal
                                                                                               subunit
                                                                                           (some work
                                                                                            by binding
                                                                                            to the 50S
                                                                                             subunit),
                                                                                             inhibiting
                                                                                                 the
                           J                                                              translocation
                           0                                                                    of the
                           1                                                                 peptidyl-
                               P4HB rpsL                       Bacterial      anti-                           Not
     ribostamycin          G
                               aac6)-Iy aac                   Infections    bacterial       tRNA from       Available
                           B
                                                                                          the A-site to
                           1
                                                                                             the P-site
                           0
                                                                                              and also
                                                                                               causing
                                                                                           misreading
                                                                                             of mRNA,
                                                                                           leaving the
                                                                                            bacterium
                                                                                             unable to
                                                                                            synthesize
                                                                                          proteins vital
                                                                                                to its
                                                                                              growth.
                                                                                             However,
                                                                                            their exact
     (+)-chelidonine                                                                       mechanism
     1,4-chrysenequinone
     5224221
     5230742
     5253409
                                                                                                 Betazole is a
                                                                                                   histamine
                                                                                                  H2 agonist
                                                                                                   used in a
                                                                                                     test for
                                                                                 Betazole is a    measuring
                                                                                   histamine        maximal
                                                                                 analogue. It     production
                                                                                 produces the      of gastric
                                                                                 same effects      acidity or
                                                                                       as          anacidity.
                                                                                  histamine,           This
                                                                                  binding the    measuremen
                 V                                                               H2 receptor        t can be
                 0                                                                                  used to
                                                                                   which is a
                 4
                                                                                  mediator of      diagnose
betazole         C   HRH2
                                                                                  gastric acid      diseases
                 G
                                                                                   secretion.       such as
                 0
                 2                                                               This agonist      Zollinger-
                                                                                     action           Ellison
                                                                                    thereby       syndrome,
                                                                                 results in an   whereby the
                                                                                  increase in      volume of
                                                                                  the volume      gastric and
                                                                                   of gastric         basal
                                                                                      acid       secretions is
                                                                                   produced.       measured
                                                                                                   following
                                                                                                    betazole
                                                                                                 administrati
                                                                                                  on (greater
                                                                                                 than 60% of
                                                                                                 the maximal
                                                                   anti-
                                                   Bacterial
celastrol                                                      bacterial anti-
                                                  Infections
                                                               proliferative
                                                                                                 Cyproheptad
                                                                                                     ine is a
                                                                                                   piperidine
                                                                                                 antihistamin
                                                                                                    e. Unlike
                                                                                 Cyproheptad          other
                                                                                       ine       antihistamin
                                                                                   competes      es, this drug
                                                                                   with free           also
                                                                                   histamine     antagonizes
                                                                                  for binding      serotonin
                                                                                     at HA-        receptors.
                                                                                    receptor      This action
                 R                                                                sites. This         makes
                 0                                                                               Cyproheptad
                                                                                 antagonizes
                 6
                                                                                  the effects    ine useful in
cyproheptadine   A   HTR2A HRH1
                                                                                 of histamine      conditions
                 X
                                                                                     on HA-          such as
                 0
                 2                                                                receptors,        vascular
                                                                                 leading to a      headache
                                                                                 reduction of          and
                                                                                 the negative      anorexia.
                                                                                  symptoms       Cyproheptad
                                                                                  brought on     ine does not
                                                                                 by histamine     prevent the
                                                                                 HA-receptor       release of
                                                                                    binding.       histamine
                                                                                                   but rather
                                                                                                   competes
                                                                                                    with free
                                                                                                   histamine
                                                                                                  for binding
                                                                                                      at HA-
                 A                  acts as an
                 0
                                   inhibitor of
                 3
                                  proteins with
dicycloverine    A                                              cns agent
                                  acetylcholine
                 A
                 0                   receptor
                 7                    activity
                                                             Estrogens
                                                            diffuse into
                                                            their target
                                                                           Dienestrol is
                                                              cells and
                                                                            a synthetic,
                                                           interact with
                                                                                 non-
                                                              a protein
                                                                              steroidal
                                                             receptor.
                                                                             estrogen.
                                                            Target cells
                                                                             Estrogens
                                                            include the
                                                                              passively
                                                               female
                                                                            diffuse into
                                                           reproductive
                                                                            target cells
                                                             tract, the
                                                                                   of
                                                             mammary
             G   G                                                          responsive
                                                             gland, the
             0   0                                                             tissues,
                                                           hypothalamu
             3   3                                                            complex
                                                hormonal     s, and the
dienestrol   C   C   ESR1                                                     with the
                                                  agent      pituitary.
             B   C                                                            estrogen
                                                             Estrogens
             0   0                                                           receptors,
             1   2
                                                           increase the
                                                                             and enter
                                                               hepatic
                                                                              the cell's
                                                            synthesis of
                                                                             nucleus to
                                                           sex hormone
                                                                             initiate or
                                                               binding
                                                                              enhance
                                                              globulin
                                                                                 gene
                                                              (SHBG),
                                                                           transcription
                                                              thyroid-
                                                                             of protein
                                                               binding
                                                                             synthesis
                                                              globulin
                                                                           after binding
                                                            (TBG), and
                                                                               to DNA.
                                                           other serum
                                                           proteins and
                                                              suppress
                                                               follicle-
                                                             Disulfiram       Disulfiram
                                                             blocks the     produces a
                                                            oxidation of   sensitivity to
                                                              alcohol at         alcohol
                                                                  the      which results
                                                           acetaldehyd       in a highly
                                                               e stage      unpleasant
                                                                during          reaction
                                                               alcohol        when the
                                                            metabolism           patient
                                                              following           under
                                                              disulfiram      treatment
                                                                intake     ingests even
             N   P                acts as an                 causing an           small
             0   0                                         accumulatio      amounts of
                                 inhibitor of
             7   3
                                proteins with                     n of          alcohol.
disulfiram   B   A   ALDH2 BZRP
                                   alcohol                 acetaldehyd        Disulfiram
             B   A
                                dehydrogena                    e in the       blocks the
             0   0
             1   4                se activity                    blood      oxidation of
                                                              producing       alcohol at
                                                                highly             the
                                                             unpleasant     acetaldehyd
                                                            symptoms.           e stage
                                                             Disulfiram          during
                                                             blocks the          alcohol
                                                            oxidation of    metabolism
                                                               alcohol         following
                                                             through its      disulfiram
                                                            irreversible     intake, the
                                                            inactivation   concentratio
                                                            of aldehyde            n of
                                                           dehydrogena      acetaldehyd
                                                              se, which     e occurring
                                                                                          Dyclonine is
                                                                              Local          an oral
                                                                          anesthetics     anasthetic.
                                                                          block both     If substantial
                                                                        the initiation   quantities of
                                                                               and             local
                                                                          conduction      anesthetics
                                                                            of nerve            are
                                                                         impulses by        absorbed
                                                                          decreasing      through the
                                                                        the neuronal         mucosa,
                                                                        membrane's         actions on
                                                                        permeability       the central
            N   R                                                          to sodium         nervous
            0   0                                                                            system
                                                                           ions. This
            1   2                                            anti-
                                                                           reversibly     (CNS) may
dyclonine   B   A   SCN10A                   Arrhythmia   arrhythmic
                                                                           stabilizes      cause CNS
            X   D                                         anesthetic
                                                                               the        stimulation
            0   0
            2   4                                                         membrane        and/or CNS
                                                                         and inhibits     depression.
                                                                        depolarizatio      Actions on
                                                                         n, resulting           the
                                                                        in the failure   cardiovascul
                                                                               of a         ar system
                                                                         propagated        may cause
                                                                             action        depression
                                                                            potential       of cardiac
                                                                               and         conduction
                                                                         subsequent             and
                                                                          conduction       excitability
                                                                           blockade.        and, with
                                                                                             some of
                                                                           Econazole          these
                                                                                         Econazole is
                                                                            interacts             an
                                                                            with 14-        antifungal
                                                                             &alpha;      medication
                                                                        demethylase         related to
                                                                                ,a        fluconazole
                                                                         cytochrome        (Diflucan),
                                                                              P-450      ketoconazole
                                                                             enzyme         (Nizoral),
                                                                        necessary to     itraconazole
                                                                             convert     (Sporanox),
                                                                        lanosterol to            and
                                                                          ergosterol.    clotrimazole
            D   G                                                               As          (Lotrimin,
            0   0                                                       ergosterol is       Mycelex).
            1   1
                                                                         an essential       Econazole
econazole   A   A   ERG11                     Mycoses     anti-fungal
                                                                          component          prevents
            C   F
                                                                        of the fungal          fungal
            0   0
            3   5
                                                                                cell       organisms
                                                                         membrane,              from
                                                                         inhibition of      producing
                                                                        its synthesis           vital
                                                                           results in     substances
                                                                           increased      required for
                                                                             cellular     growth and
                                                                        permeability         function.
                                                                             causing            This
                                                                          leakage of      medication
                                                                             cellular      is effective
                                                                           contents.          only for
                                                                           Econazole        infections
                                                                            may also        caused by
                                                                              inhibit          fungal
                              acts as an
            C                antagonist of
            0
                             proteins with
            8
                              calmodulin
fendiline   E                                             vasodilator
                               regulated
            A
            0                   protein
            1                    kinase
                                activity
ionomycin
                                                                                       Isotretinoin,
                                                                                       a retinoid, is
                                                                                        indicated in
                                                                                              the
                                                                       Isotretinoin
                                                                                       treatment of
                                                                        noticeably
                                                                                            severe
                                                                       reduces the
                                                                                        recalcitrant
                                                                        production
                                                                                           nodular
                                                                         of sebum
                                                                                             acne.
                                                                       and shrinks
                                                                                        Nodules are
                                                                             the
                                                                                       inflammator
                                                                        sebaceous
                                                                                           y lesions
                                                                        glands. It
                                                                                             with a
                    D   D                                                stabilises
                                         acts as an                                     diameter of
                    1   1                                             keratinizatio
                                         agonist of                                        5 mm or
                    0   0                                 Acne             n and
                                        proteins with                                  greater. The
     isotretinoin   A   B   RARA                      Vulgaris Skin      prevents
                                        retinoic acid                                  nodules may
                    D   A                               Diseases       comedones
                                          receptor                                         become
                    0   0                                                   from
                    4   1                  activity                                     suppurative
                                                                      forming. The
                                                                                               or
                                                                           exact
                                                                                       hemorrhagic
                                                                       mechanism
                                                                                         . "Severe,"
                                                                       of action is
                                                                                               by
                                                                        unknown,
                                                                                          definition,
                                                                      however it is
                                                                                            means
                                                                       known that
                                                                                         "many" as
                                                                      it alters DNA
                                                                                        opposed to
                                                                      transcription
                                                                                            "few or
                                                                              .
                                                                                           several"
                                                                                           nodules.
                                                                                            Clinical
                                                                                       improvemen
                                                                      Loxapine is a     t in nodular

40                                                                      dopamine
                                                                       antagonist,
                                                                                        Loxapine, a
                                                                        and also a
                                                                                       dibenzoxaze
                                                                       serotonin 5-
                                                                                             pine
                                                                      HT2 blocker.
                                                                                        compound,
                                                                         The exact
                                                                                       represents a
                                                                          mode of
                                                                                        subclass of
                                                                          action of
                                                                                           tricyclic
                                                                      Loxapine has
                                                                                       antipsychotic
                                                                          not been
                                                                                           agents,
                                                                       established,
                                                                                         chemically
                                                                          however
                    N                                                                  distinct from
                                                                        changes in
                    0                                                                         the
                                                                       the level of
                    5                                                                  thioxanthene
                                                                        excitability
     loxapine       A       DRD1 DRD2                                                          s,
                                                                              of
                    H                                                                  butyropheno
                                                                        subcortical
                    0                                                                     nes, and
                    1
                                                                         inhibitory
                                                                                       phenothiazin
                                                                        areas have
                                                                                              es.
                                                                            been
                                                                                       Pharmacolog
                                                                       observed in
                                                                                            ically,
                                                                           several
                                                                                       Loxapine is a
                                                                           animal
                                                                                        tranquilizer
                                                                         species in
                                                                                       for which the
                                                                        association
                                                                                        exact mode
                                                                         with such
                                                                                       of action has
                                                                      manifestatio
                                                                                          not been
                                                                            ns of
                                                                                        established.
                                                                      tranquilizatio
                                                                      n as calming
                                                                        effects and
                    G   G                                              suppression
                    0   0
                    3   3
     lynestrenol    A   D
                    C   C
                    0   0
                    2   3
                                          acts as an
                                         inhibitor of
                                        proteins with
     MG-132                               cysteine-
                                             type
                                        endopeptida
                                          se activity
     MG-262
                                                                                            Mianserin is
                                                                                            a tetracyclic
                                                                                            antidepressa
                                                                                              nt that has
                                                                                            antihistamini
                                                                                                  c and
                                                                                            hypnosedati
                                                                                                 ve, but
                                                                               Mianserin's     almost no
                                                                              mechanism anticholinerg
                                                                                    of       ic, effect. It
                                                                              therapeutic      is a weak
                                                                              action is not inhibitor of
             N                         acts as an                                  well     norepinephri
             0
                             HRH1     antagonist of                  anti-    understood, ne reuptake
             6
                             ADRA2A    protein 5-                 histamine    although it and strongly
mianserin    A                                      Depression
                             HTR2A    hydroxytrypt                   anti-     apparently     stimulates
             X
             0               HTR2C      amine 2                  depressant   blocks alpha- the release
             3                          receptor                              adrenergic,           of
                                                                               histamine norepinephri
                                                                                 H1, and           ne.
                                                                              some types Interactions
                                                                              of serotonin         with
                                                                               receptors.      serotonin
                                                                                            receptors in
                                                                                              the central
                                                                                                nervous
                                                                                            system have
                                                                                               also been
                                                                                               found. Its
                                                                                                effect is
                                                                                                 usually
                                                                                Unbound       noticeable
                                                                                            Mometasone
                                                                              corticosteroi   is a medium-
                                                                              ds cross cell       potency
                                                                              membranes          synthetic
                                                                                 and bind     corticosteroi
                                                                                 with high         d with
                                                                                affinity to   antiinflamm
                                                                                  specific         atory,
                                                                              cytoplasmic      antipruritic,
                                                                                receptors.          and
                                                                              Inflammatio     vasoconstrict
                                                                                    n is             ive
                                                                                decreased      properties.
             D   D   R   R                                                           by         Studies in
             0   0   0   0                                                     diminishing      asthmatic
             7   7   1   3
                             NR3C1                                             the release       patients
mometasone   A   X   A   B
                             ANXA1                                            of leukocytic         have
             C   C   D   A
                                                                                    acid      demonstrate
             1   0   0   0
             3   3   9   7
                                                                               hydrolases,         d that
                                                                               prevention     mometasone
                                                                                     of         provides a
                                                                              macrophage        favorable
                                                                              accumulatio         ratio of
                                                                                    n at        topical to
                                                                                 inflamed        systemic
                                                                                   sites,      activity due
                                                                              interference         to its
                                                                                    with      primary local
                                                                                leukocyte      effect along
                                                                              adhesion to        with the
                                                                              the capillary     extensive
                                                                                   wall,          hepatic
                                                                              reduction of     metabolism
                                                                                     Nalbuphine
                                                                                          is a
                                                                                       synthetic
                                                                                        opioid
                                                                                       agonist-
                                                                                      antagonist
                                                                      Receptor       analgesic of
                                                                   studies show           the
                                                                         that       phenanthren
                                                                    nalbuphine         e series.
                                                                      exerts its    Nalbuphine's
                                                                     action via        analgesic
                                                                     binding to       potency is
                 N                                                  mu, kappa,        essentially
                 0                                                                  equivalent to
                                                                     and delta
                 2   OPRK1
                                                                     receptors,         that of
nalbuphine       A   OPRM1                   Pain    analgesic
                                                                     but not to     morphine on
                 F   OPRD1
                                                                       sigma         a milligram
                 0
                 2                                                   receptors.       basis. The
                                                                    Nalbuphine          opioid
                                                                   is primarily a     antagonist
                                                                       kappa          activity of
                                                                   agonist/parti      nalbuphine
                                                                        al mu       is one-fourth
                                                                     antagonist      as potent as
                                                                     analgesic.       nalorphine
                                                                                    and 10 times
                                                                                        that of
                                                                                    pentazocine.
                                                                                     Nalbuphine
                                                                                     by itself has
                                                                                        potent
PF-00875133-00                                                                          opioid
PHA-00846566E
                 R
                 0             acts as an
                                                    bronchodilat
                 6           antagonist of
                                                     or sedative
pimethixene      A              protein
                                                         anti-
                 X             histamine
                                                      histamine
                 2            receptor H1
                 3
piperlongumine

                                                                                    Prilocaine, a
                                                                                      hydantoin
                                                                                    anticonvulsa
                                                                      Prilocaine      nt, is used
                                                                        acts on     alone or with
                                                                        sodium      phenobarbit
                                                                    channels on       al or other
                                                                   the neuronal     anticonvulsa
                                                                          cell            nts to
                                                                    membrane,           manage
                                                                    limiting the     tonic-clonic
                                                                      spread of        seizures,
                 N                                                      seizure     psychomotor
                 0                                                  activity and       seizures,
                 1                                                     reducing      neuropathic
prilocaine       B   SCN5A                          anesthetic          seizure            pain
                 B                                                 propagation.      syndromes
                 0                                                        The          including
                 4                                                 antiarrhythm         diabetic
                                                                      ic actions    neuropathy,
                                                                          are          digitalis-
                                                                      mediated          induced
                                                                       through           cardiac
                                                                      effects on    arrhythmias,
                                                                        sodium       and cardiac
                                                                    channels in     arrhythmias
                                                                       Purkinje       associated
                                                                        fibers.        with QT-
                                                                                        interval
                                                                                    prolongation
                                                                                            .
                                                                                            Primaquine
                                                                                                 is an
                                                                                            antimalarial
                                                                                           agent and is
                                                                                           the essential
                                                                                           co-drug with
                                                                                            chloroquine
                                                                                             in treating
                                                                           Primaquine's     all cases of
                                                                            mechanism       malaria. In
                                                                            of action is     the blood,
                                                                               not well         malaria
                                                                            understood.       parasites
                     P                                                        It may be     break down
                     0                                                                     a part of the
                                                                              acting by
                     1
                                                                             generating       red blood
primaquine           B   HBA1                      Malaria   anti-malarial
                                                                               reactive     cells known
                     A
                                                                                oxygen             as
                     0
                     3                                                     species or by   haemoglobin
                                                                             interfering    . When this
                                                                               with the        happens
                                                                               electron    haemoglobin
                                                                            transport in      is divided
                                                                           the parasite.       into two
                                                                                           parts; haem
                                                                                            and globin.
                                                                                               Haem is
                                                                                            toxic to the
                                                                                                malaria
                                                                                           parasite. To
                                                                                              prevent it
                                                                                            from being
propidium_iodide                                                                             damaged,
puromycin
thapsigargin

                                   acts as an
                                  inhibitor of
                                     protein
                                   epidermal
                                     growth
                                      factor
tyrphostin_AG-1478                  receptor
                                (erythroblast
                                 ic leukemia
                                viral (v-erb-
                                b) oncogene
                                   homolog,
                                     avian)
                     C
                     0
                     4
vinburnine           A                                       vasodilator
                     X
                     1
                     7
                                  acts as an
                                 inhibitor of
                                proteins with
                                    protein
                                    kinase
                                activity acts
                                     as an
Y-27632
                                 inhibitor of
                                protein Rho-
                                 associated,
                                  coiled-coil
                                 containing
                                    protein
                                   kinase 2
                                                                  anti-
                                                 Inflammatio
allantoin                                                    inflammator
                                                      n
                                                                   y
                                                                                                            Chloramphe        Chloramphe
                                                                                                            nicol is lipid-      nicol is a
                                                                                                                soluble,          broad-
                                                                                                            allowing it to      spectrum
                                                                                                                 diffuse        antibiotic
                                                                                                             through the         that was
                                                                                                            bacterial cell    derived from
                                                                                                             membrane.              the
                                                                                                                 It then        bacterium
                                                                                                               reversibly     Streptomyce
                                                                                                            binds to the      s venezuelae
                                                                                                            50S subunit        and is now
                                                                                                             of bacterial       produced
                       D   D   G   J   S   S   S                               Rickettsia                     ribosomes       synthetically
                       0   1   0   0   0   0   0                                                                  where               .
                                                                               Infections
                       6   0   1   1   1   2   3   rplJ CD55
                                                                               Meningitis,      anti-         transfer of     Chloramphe
     chloramphenicol   A   A   A   B   A   A   A   cat3 cat
                                                                                Bacterial     bacterial     amino acids           nicol is
                       X   F   A   A   A   A   A   draA
                                                                                Bacterial                     to growing         effective
                       0   0   0   0   0   0   0
                       2   3   5   1   1   1   8                               Infections                        peptide        against a
                                                                                                                chains is     wide variety
                                                                                                              prevented              of
                                                                                                            (perhaps by       microorganis
                                                                                                            suppression       ms, but due
                                                                                                              of peptidyl       to serious
                                                                                                             transferase       side-effects
                                                                                                                activity),         (e.g.,
                                                                                                                   thus        damage to
                                                                                                               inhibiting        the bone
                                                                                                                 peptide          marrow,
                                                                                                                  bond           including
                                                                                                               formation          aplastic
                                                                                                                   and         anemia) in
                                                                                                             subsequent       humans, it is
                                                                  acts as a
                                                                 blocker of
                                                               proteins with
                                                                 potassium
                                                                   channel
     etofylline                                                 activityacts                   antidote
                                                                as a blocker
                                                                 of proteins
                                                                     with
                                                               cholinesteras
                                                                  e activity
     imidurea
                       P
41                     0
                       2
     niridazole        B
                       X
                       0
                       2
                       C
                       0
                       1
     octopamine        C
                       A
                       1
                       8
                                                                                                muscle
                                                                                               relaxant
     Prestwick-920
                                                                                             (spasmolytic
                                                                                                   )
                                                                                Bacterial        anti-
     roxarsone
                                                                               Infections      bacterial
                                                                                                             Torasemide        Torasemide
                                                                                                              inhibits the       (INN) or
                                                                                                            Na<sup>+<           torsemide
                                                                                                            /sup>/K<su         (USAN) is a
                                                                                                            p>+</sup>/          novel loop
                                                                                                              2Cl<sup>-           diuretic
                                                                                                                </sup>-       belonging to
                                                                                                                  carrier         pridine
                                                                                                             system (via        sulphonyl
                                                                                                             interference        urea. It
                                                                                                                  of the       differs form
                                                                 acts as a                                       chloride           other
                                                                 binder of                                  binding site)        thiazide
                       C                                          protein                                   in the lumen       diuretics in
                       0                                           solute                                     of the thick         that a
                       3                                           carrier                                     ascending       double ring
     torasemide        C                           SLC12A1       family 12       Edema                          portion of      system is
                       A                                       (sodium/pot                                    the loop of     incorporated
                       0                                       assium/chlor                                       Henle,          into its
                       4                                             ide                                    resulting in a      structure.
                                                               transporters                                   decrease in           Like
                                                               ), member 1                                  reabsorption        thiazides,
                                                                                                               of sodium            loop
                                                                                                            and chloride.        diuretics
                                                                                                              This results       must be
                                                                                                                   in an      secreted into
                                                                                                              increase in      the tubular
                                                                                                               the rate of        fluid by
                                                                                                               delivery of       proximal
                                                                                                             tubular fluid    tubule cells.
                                                                                                                    and        In the thick
                                                                                                             electrolytes       ascending
                                                                                                             to the distal      loop Na+
                                                             acts as an
                                                            inhibitor of
                    C                                          protein
                    0
                                                              platelet-                   anti-
                    1
                                                              derived    Inflammatio inflammator         Not               Not
ajmaline            B
                                                               growth    n Arrhythmia    y anti-       Available         Available
                    A
                    0                                           factor                arrhythmic
                    5                                        receptor,
                                                                 beta
                                                            polypeptide
                                                                                      anti-pyretic
ampyrone                                                                  Fever Pain
                                                                                       analgesic
                                                                                                     Betaxolol          Betaxolol is
                                                                                                    selectively                 a
                                                                                                       blocks          competitive,
                                                                                                   catecholami             beta(1)-
                                                                                                          ne               selective
                                                                                                    stimulation        (cardioselect
                                                                                                    of beta(1)-               ive)
                                                                                                    adrenergic           adrenergic
                                                                                                   receptors in         antagonist.
                                                                                                     the heart          Betaxolol is
                                                                                                   and vascular        used to treat
                                                                                                      smooth           hypertension
                                                                                                   muscle. This                 ,
                    C   S                                     acts as an                            results in a       arrhythmias,
                    0   0                                                                          reduction of            coronary
                                                            antagonist of
                    7   1
                                                                protein   Hypertensio    anti-      heart rate,              heart
betaxolol           A   E                           ADRB1
                                                             adrenergic,      n       hypertensive     cardiac             disease,
                    B   D
                                                               beta-1-,                               output,            glaucoma,
                    0   0
                    5   2                                      receptor                            systolic and          and is also
                                                                                                      diastolic             used to
                                                                                                        blood          reduce non-
                                                                                                     pressure,         fatal cardiac
                                                                                                   and possibly           events in
                                                                                                        reflex         patients with
                                                                                                    orthostatic        heart failure.
                                                                                                   hypotension.        Activation of
                                                                                                     Betaxolol             beta(1)-
                                                                                                      can also            receptors
                                                                                                   competitivel            (located
                                                                                                       y block         mainly in the
                                                                                                     beta(2)-             heart) by
                                                                                                    adrenergic          epinephrine
                                                                                                   responses in
                                                                                                   Chlorhexidin           increases
                                                                                                            e's
                                                                                                     antimicrobial
                                                                                                                       Chlorhexidin
                                                                                                       effects are
                                                                                                                        e, a topical
                                                                                                       associated
                                                                                                                       antimicrobial
                                                                                                        with the
                                                                                                                           agent, is
                                                                                                       attractions
                                                                                                                        bactericidal.
                                                                                                        between
                                                                                                                         Because of
                                                                                                     chlorhexidin
                                                                                                                         its positive
                                                                                                       e (cation)
                                                                                                                        charge, the
                                                                                                           and
                                                                                                                        chlorhexidin
                                                                                                       negatively
                                                                                                                         e molecule
                                                                                                        charged
                    A   B   D   D   R   S   S   S                                                                        reacts with
                                                                                                        bacterial
                    0   0   0   0   0   0   0   0                                                                      the microbial
                                                                                        antiseptic     cells. After
                    1   5   8   9   2   1   2   3                                                                       cell surface
                                                                                           anti-     chlorhexidin
chlorhexidine       A   C   A   A   A   A   A   A                          Infection                                      to destroy
                                                                                         infective         e is
                    B   A   C   A   A   X   A   A                                                                      the integrity
                    0   0   0   1   0   0   0   0                                          agent       absorpted
                                                                                                                          of the cell
                    3   2   2   2   5   9   9   4                                                       onto the
                                                                                                                        membrane.
                                                                                                       organism's
                                                                                                                          This novel
                                                                                                       cell wall, it
                                                                                                                        mechanism
                                                                                                     disrupts the
                                                                                                                           of action
                                                                                                      integrity of
                                                                                                                           makes it
                                                                                                         the cell
                                                                                                                            highly
                                                                                                       membrane
                                                                                                                        unlikely for
                                                                                                      and causes
                                                                                                                              the
                                                                                                      the leakage
                                                                                                                       development
                                                                                                            of
                                                                                                                        of bacterial
                                                                                                     intracellular
                                                                                                                         resistance.
                                                                                                     components
                                                                                                          of the
                                                                                                      organisms.
                    A   D   J   S
                    0   0   0   0                                         Protozoan       anti-
                    1   6   1   1                                         Infections    protozoal
chlortetracycline   A   A   A   A
                                                                           Bacterial      anti-
                    B   A   A   A
                                                                          Infections    bacterial
                    2   0   0   0
                    1   2   3   2
                                                                                     Chlorzoxazo
                                                                     Chlorzoxazo            ne, a
                                                                      ne inhibits       synthetic
                                                                    degranulatio      compound,
                                                                       n of mast          inhibits
                                                                           cells,       antigen-
                                                                     subsequentl         induced
                                                                    y preventing     bronchospas
                                                                      the release       ms and,
                                                                     of histamine       hence, is
                                                                       and slow-     used to treat
                                                                        reacting      asthma and
                                                                    substance of          allergic
                     M                                               anaphylaxis         rhinitis.
                     0                                                               Chlorzoxazo
                                                          muscle        (SRS-A),
                     3
                                                         relaxant   mediators of     ne is used as
     chlorzoxazone   B           KCNMA1
                                                       (spasmolytic       type I              an
                     B
                                                             )           allergic     ophthalmic
                     0
                     3                                                 reactions.      solution to
                                                                     Chlorzoxazo            treat
                                                                     ne also may     conjunctivitis
                                                                      reduce the     and is taken
                                                                       release of       orally to
                                                                     inflammator            treat
                                                                             y          systemic
                                                                    leukotrienes.    mastocytosis
                                                                     Chlorzoxazo             and
                                                                      ne may act       ulcerative
                                                                     by inhibiting         colitis.
                                                                         calcium     Chlorzoxazo
                                                                          influx.     ne is also a
                                                                                       centrally-
                                                                                     acting agent
                                                                     Systemic/Va
                                                                          ginal-
                                                                     Clindamycin
                                                                         inhibits
                                                                         protein
                                                                      synthesis of
                                                                      bacteria by     Clindamycin
                                                                       binding to          is an
                                                                        the 50 S        antibiotic,
                                                                       ribosomal         similar to
                                                                      subunits of          and a
                                                                     the bacteria.   derivative of
                     D   G   J                                          Topical-       lincomycin.
                     1   0   0                                       Clindamycin      Clindamycin
                     0   1   1                                       reduces free     can be used
                                           Bacterial       anti-
     clindamycin     A   A   F   rplJ                                  fatty acid     in topical or
                                          Infections     bacterial
                     F   A   F                                       concentratio        systemic
                     0   1   0                                         ns on the     treatment. It
                     1   0   1                                        skin and to      is effective
                                                                     suppress the      as an anti-
                                                                       growth of        anaerobic
                                                                     Propionibact        antibiotic
                                                                     erium acnes            and
                                                                     (Corynebact     antiprotozoal
                                                                     erium acnes)             .
                                                                           , an

42
                                                                       anaerobe
                                                                        found in
                                                                       sebaceous
                                                                      glands and
                                                                        follicles.

                     C
                     0
                     3                                   anti-
                                          Hypertensio
     clopamide       B                                hypertensive
                                              n
                     A                                  diuretic
                     0
                     3
42




                                                           As a    Danazol is a
                                                     gonadotropi derivative of
                                                     n inhibitor, the synthetic
                                                        danazol         steroid
                                                     suppresses ethisterone,
                                                    the pituitary- a modified
                                                     ovarian axis testosterone
                                                     possibly by       . It was
                                                       inhibiting  approved by
                                                    the output of     the U.S.
                                                        pituitary    Food and
                                                     gonadotropi         Drug
                                                     ns. Danazol Administrati
                     G                                     also    on (FDA) as
                     0               Menorrhagia
                         ESR1                         depresses the first drug
                     3               Premenstrua
                         GNRHR                             the             to
     danazol         X                    l
                         GNRHR2                     preovulatory specifically
                     A               SyndromeEn
                         SHBG CCL2                      surge in         treat
                     0                dometriosis
                     1
                                                       output of endometriosi
                                                         follicle-    s, but its
                                                     stimulating      role as a
                                                       hormone       treatment
                                                      (FSH) and           for
                                                      luteinizing endometriosi
                                                       hormone      s has been
                                                       (LH) and         largely
                                                       therefore   replaced by
                                                        reduces           the
                                                         ovarian   gonadotropi
                                                        estrogen    n-releasing
                                                     production.      hormone
                                                    Danazol also       (GnRH)
                                                                      agonists.
                                                    may directly Dirithromyci
                                                     Dirithromyci
                                                      n prevents       n is a pro-
                                                        bacteria       drug which
                                                          from       is converted
                                                     growing, by           non-
                                                      interfering    enzymaticall
                                                       with their        y during
                                                        protein         intestinal
                                                      synthesis.       absorption
                                                    Dirithromyci         into the
                                                      n binds to     microbiologi
                                                        the 50S        cally active
                                                      subunit of          moiety
                     J                                  the 70S      erythromycyl
                     0                                 bacterial          amine.
                     1
                                                      ribosome,      Erythromycy
     dirithromycin   F
                                                       and thus           lamine
                     A
                                                     inhibits the       exerts its
                     1
                     3
                                                    translocation      activity by
                                                     of peptides.      binding to
                                                    Dirithromyci         the 50S
                                                      n has over        ribosomal
                                                       10 times        subunits of
                                                         higher        susceptible
                                                       affinity to   mircoorganis
                                                     the subunit     ms resulting
                                                       50S than       in inhibition
                                                     erythromyci        of protein
                                                          n. In         synthesis.
                                                       addition,     Dirithromyci
                                                     dirithromyci    n/erythromy
                                                        n binds      cylamine has
                                                    simultaneou       been shown
                                                                           Sulfonylurea     Glibenclamid
                                                                              s such as     e (INN), also
                                                                           glibenclamid       known as
                                                                           e likely bind      glyburide
                                                                               to ATP-        (USAN), a
                                                                              sensitive         second-
                                                                             potassium-      generation
                                                                               channel      sulfonylurea
                                                                           receptors on      antidiabetic
                                                                                  the            agent,
                                                                             pancreatic      appears to
                                  acts as a                                cell surface,      lower the
                     KCNJ1       blocker of                                   reducing           blood
                 A   ABCC3      proteins with                                potassium          glucose
                 1                                                         conductance        acutely by
                     ABCC9           ATP-
                 0                               Diabetes
                     ABCB11       activated                  vasoconstrict and causing       stimulating
glibenclamide    B                               Mellitus,
                     ABCA1 CFTR     inward                        or       depolarizatio     the release
                 B                                Type 2
                     ABCC1         rectifier                                   n of the        of insulin
                 0
                 1   ABCC8       potassium                                  membrane.          from the
                     KCNJ11        channel                                 Depolarizati     pancreas, an
                                   activity                                        on            effect
                                                                             stimulates      dependent
                                                                             calcium ion          upon
                                                                                 influx      functioning
                                                                               through      beta cells in
                                                                               voltage-            the
                                                                              sensitive       pancreatic
                                                                               calcium       islets. With
                                                                              channels,         chronic
                                                                                raising     administrati
                                                                            intracellular   on in Type II
                                                                           concentratio         diabetic
hydrastinine                                                               ns of calcium    patients, the
lobeline
                                                                                            Methazolami
                                                                                             de is topical
                                                                                                 carbonic
                                                                            Methazolami
                                                                                              anhydrase
                                                                                 de is a
                                                                                                inhibitor.
                                                                                 potent
                                                                                            Methazolami
                                                                             inhibitor of
                                                                                                    de is
                                                                                carbonic
                                                                                            indicated for
                                                                             anhydrase.
                                                                                                     the
                                                                            Inhibition of
                                                                                             reduction of
                                                                                carbonic
                                                                                                elevated
                                                                            anhydrase in
                                                                                              intraocular
                                                                              the ciliary
                                                                                             pressure in
                 S                                                          processes of
                                   acts as an                                               patients with
                 0                                                              the eye
                                  inhibitor of                                               open-angle
                 1                                                            decreases
                                 proteins with                                              glaucoma or
methazolamide    E   CA1                                       diuretic         aqueous
                                   carbonate                                                      ocular
                 C                                                               humor
                                 dehydratase                                                hypertension
                 0                                                            secretion,
                 5                  activity                                                     who are
                                                                             presumably
                                                                                            insufficiently
                                                                             by slowing
                                                                                              responsive
                                                                                   the
                                                                                                 to beta-
                                                                            formation of
                                                                                                blockers.
                                                                            bicarbonate
                                                                                            Methazolami
                                                                               ions with
                                                                                                  de is a
                                                                             subsequent
                                                                                            sulfonamide
                                                                            reduction in
                                                                                              derivative;
                                                                             sodium and
                                                                                             however, it
                                                                                  fluid
                                                                                                does not
                                                                              transport.
                                                                                               have any
                                                                                                 clinically
                                                                                               significant
Prestwick-689                                                                               antimicrobial
                                                   Virus
betulinic_acid                                                 anti-viral
                                                 Diseases
                 L
                 0                                            anti-fungal
                 4                                           immunosupp
ciclosporin      A
                                                                ressive
                 D
                                                                 agent
                 0
                 1
                                                                                                Estrogens          Diethylstilbe
                                                                                               diffuse into           strol is a
                                                                                               their target          synthetic
                                                                                                 cells and            estrogen
                                                                                              interact with           that was
                                                                                                 a protein         developed to
                                                                                                receptor.           supplement
                                                                                               Target cells         a woman's
                                                                                               include the             natural
                                                                                                  female              estrogen
                                                                                              reproductive          production.
                                                                                                tract, the         In 1971, the
                                                                                                mammary              Food and
                          G   G   L                                                             gland, the              Drug
                          0   0   0
                                                                                   hormonal hypothalamu            Administrati
                          3   3   2
                                      ESR1 ESRRG                                  agent anti-   s, and the           on (FDA)
     diethylstilbestrol   C   C   A                                Neoplasms
                                      TTR Esrrg                                   neoplastic    pituitary.            issued a
                          B   C   A
                                                                                  vasodilator   Estrogens          Drug Bulletin
                          0   0   0
                          2   5   1
                                                                                              increase the            advising
                                                                                                  hepatic          physicians to
                                                                                               synthesis of             stop
                                                                                              sex hormone           prescribing
                                                                                                  binding              DES to
                                                                                                 globulin            pregnant
                                                                                                 (SHBG),               women
                                                                                                 thyroid-            because it
                                                                                                  binding            was linked
                                                                                                 globulin             to a rare
                                                                                               (TBG), and              vaginal
                                                                                              other serum            cancer in
                                                                                              proteins and             female
                                                                                                 suppress            offspring.
                                                                                                  follicle-
                                                     acts as an
                                                    inhibitor of
                                                   proteins with
                                                                                   hormonal           Not              Not
     equilin                          HSD17B1      estradiol 17-
                                                                                     agent          Available        Available
                                                       beta-
                                                   dehydrogena
                                                     se activity
                                                                                                     Estrogens       Estrone, a
                                                                                                     enter the     synthetically
                                                                                                       cells of     prepared or
                                                                                                    responsive        naturally
                                                                                                       tissues       occurring
                                                                                                  (e.g., female       steroidal
                                                                                                      organs,         estrogen
                                                                                                      breasts,        obtained
                                                                                                  hypothalamu           from
                                                                                                   s, pituitary)      pregnant
                                                                                                    where they         equine
                                                                                                  interact with    urine, is the
43                        G   G
                                                                                                     a protein
                                                                                                     receptor,
                                                                                                                       primary
                                                                                                                     circulating
                          0   0                                                                      estrogen         estrogen
                          3   3       ESR1 ALB
                                                                                   hormonal         receptors,          after
     estrone              C   C       SHBG STS
                                                                                     agent         subsequentl     menopause.
                          A   C       CYP1B1
                                                                                                   y increasing      Estrone is
                          0   0
                          7   4
                                                                                                    the rate of       naturally
                                                                                                   synthesis of    derived from
                                                                                                    DNA, RNA,            the
                                                                                                     and some        peripheral
                                                                                                     proteins.      conversion
                                                                                                     Estrogens            of
                                                                                                   increase the    androstenedi
                                                                                                       hepatic       one by an
                                                                                                   synthesis of     aromatase
                                                                                                  sex hormone         enzyme
                                                                                                       binding        found in
                                                                                                      globulin         adipose
                                                                                                      (SHBG),       tissues and
                                                                                                      thyroid-     is converted
     MK-886                                                                                            binding      to estradiol
                                                                                  gastrointesti       Not              Not
     naringenin                       CHS2 CHI-1                   Peptic Ulcer
                                                                                   nal agent        Available        Available
                          N
                          0
                          2
     pizotifen            C
                          X
                          0
                          1
                                                                                                      Saquinavir is
                                                                                                       a protease
                                                                                                         inhibitor
                                                                                                      with activity
                                                                                                          against
                                                                                                          Human
                                                                                                      Immunodefi
                                                                                                      ciency Virus
                                                                                                      Type 1 (HIV-
                                                                                        Saquinavir    1). Protease
                                                                                       inhibits the     inhibitors
                                                                                         HIV viral      block the
                                                                                        proteinase     part of HIV
                              J               HIV-1                                       enzyme           called
                              0               protease                                     which        protease.
                              5               TNF ALB                                    prevents          HIV-1
     saquinavir               A               ABCB1                                    cleavage of     protease is
                              E               ABCC1                                    the gag-pol     an enzyme
                              0               ABCC2                                    polyprotein,   required for
                              1               ABCG2                                    resulting in         the
                                                                                       noninfectiou    proteolytic
                                                                                       s, immature     cleavage of
                                                                                           viral         the viral
                                                                                         particles.    polyprotein
                                                                                                       precursors
                                                                                                         into the
                                                                                                        individual
                                                                                                        functional
                                                                                                         proteins
                                                                                                         found in
                                                                                                        infectious
                                                                                                          HIV-1.
     cobalt_chloride                                                                                   Saquinavir
                                                                                   Dopamine is        Dopamine is
                                                                                    a precursor          a natural
                                                                                          to           catecholami
                                                                                   norepinephri         ne formed
                                                                                        ne in              by the
                                                                                   noradrenergi       decarboxylat
                                                                                   c nerves and         ion of 3,4-
                                                                                      is also a       dihydroxyph
                                                                                   neurotransm         enylalanine
                                                                                       itter in       (DOPA). It is
                                                                                   certain areas       a precursor
                                                                                        of the                to
                                                                                       central        norepinephri
                              C                                                       nervous               ne in
                              0                                                       system.         noradrenergi
                              1                            Parkinson   cns agent
                                              DRD1 DBH                               Dopamine         c nerves and
     dopamine                 C                             Disease   cardiovascul
                                              ADRB1                                  produces            is also a
                              A                           Hypotension   ar agent
                                                                                      positive        neurotransm
                              0
                                                                                   chronotropic            itter in
44                            4
                                                                                   and inotropic      certain areas
                                                                                     effects on             of the
                                                                                         the              central
                                                                                   myocardium,            nervous
                                                                                    resulting in          system,
                                                                                     increased        especially in
                                                                                     heart rate              the
                                                                                    and cardiac       nigrostriatal
                                                                                   contractility.     tract, and in
                                                                                       This is              a few
                                                                                   accomplishe          peripheral
                                                                                   d directly by      sympathetic
                                                                                    exerting an           nerves.
                              C   M   M   S                                            agonist          Dopamine
                              0   0   0   0
                              1   1   2   1
     indometacin              E   A   A   B
                              B   B   A   C
                              0   0   2   0
                              3   1   3   1
     quinpirole
                              V
                              0
                              3
     copper_sulfate           A
                              B
45                            2
                              0
                                              ldh LDHA
                                                                                          Not            Not
     oxamic_acid                              LDHB pflB
                                                                                        Available      Available
                                              LDHA
     tetraethylenepentamine
                                                                       vasoconstrict
     corbadrine
                                                                            or
                                                          Inflammatio
                                                                             anti-
                                                             n Liver
                                                                        inflammator
     ebselen                                                Diseases
                                                                            y anti-
                                                          Cerebrovasc
                                                                           oxidant
                                                          ular Accident
                                                                                    Gabapentin      Gabapentin,
                                                                                       interacts    an analog of
                                                                                    with cortical      GABA, is
                                                                                     neurons at      used as an
                                                                                       auxillary    anticonvulsa
                                                                                     subunits of      nt to treat
                                                                                       voltage-          partial
                                                                                       sensitive       seizures,
                                                                                        calcium     amyotrophic
                                                                                      channels.          lateral
                                                                                    Gabapentin         sclerosis
                                                                                      increases      (ALS), and
                                                                                    the synaptic         painful
                     N       ADORA1      acts as an                                concentratio     neuropathies
                     0                                                               n of GABA,       . Potential
                             CACNA1B     agonist of
                     3
                             CACNA1B       protein                                    enhances      uses include
     gabapentin      A                                   Epilepsy     cns agent
                             BCAT1        Gamma-                                         GABA       monotherap
                     X
                             CACNA2D1   aminobutyric                               responses at            y of
                     1
                     2       CACNA2D2   acid receptor                              non-synaptic       refractory
                                                                                        sites in         partial
                                                                                       neuronal         seizure

46                                                                                  tissues, and
                                                                                    reduces the
                                                                                                      disorders,
                                                                                                           and
                                                                                      release of    treatment of
                                                                                   mono-amine       spasticity in
                                                                                   neurotransm         multiple
                                                                                     itters. One       sclerosis,
                                                                                         of the         tremor.
                                                                                   mechanisms             mood
                                                                                   implicated in      disorders,
                                                                                   this effect of          and
                                                                                     gabapentin      attenuation
     hecogenin                                                                           is the     of disruptive
                     R   R
                     0   0
                     3   3
     isoetarine      A   C
                     C   C
                     0   0
                     7   6
                     M                                                 muscle
                     0                                     Spasm
                                                                      relaxant
                     3                                   Parkinson
                                                                    (spasmolytic
     pridinol        B                                    Disease
                                                                        )anti-
                     X                                  Inflammatio
                                                                    inflammator
                     0                                       n
                                                                          y
                     3
                     M
                     0
                     1                                                   anti-
                                                        Inflammatio                    Not             Not
     zomepirac       A                                              inflammator
                                                            nPain                    Available       Available
                     B                                               yanalgesic
                     0
                     4


                                                                                       During
                                                                                     absorption
                                                                                      from the
                                                                                   gastrointesti
                                                                                      nal tract,
                                                                                   bacampicillin
                                                                                           is
                                                                                     hydrolyzed
                                                                                   by esterases
                     J                                                               present in     Bacampicillin
                     0                                                             the intestinal   is a prodrug
                     1                                                                wall. It is   of ampicillin
                                                          Bacterial     anti-
     bacampicillin   C       pbpA                                                   microbiologi        and is
                                                         Infections   bacterial
                     A                                                               cally active   microbiologi
                     0                                                             as ampicillin,        cally
                     6                                                             and exerts a       inactive.
                                                                                    bactericidal
                                                                                        action
                                                                                    through the
                                                                                    inhibition of
                                                                                          the
                                                                                    biosynthesis
                                                                                     of cell wall
                                                                                   mucopeptide
                                                                                           s.




47
                                                                                              Like all beta-    Cefixime, an
                                                                                                   lactam       antibiotic, is
                                                                                                antibiotics,         a third-
                                                                                                  cefixime        generation
                                                                                                  binds to      cephalospori
                                                                                                   specific           n like
                                                                                                 penicillin-      ceftriaxone
                                                                                                   binding             and
                                                                                                  proteins       cefotaxime.
                                                                                                    (PBPs)        Cefixime is
                                                                                                   located      highly stable
                                                                                                 inside the           in the
                                                                                              bacterial cell     presence of
                               J                                                              wall, causing           beta-
                               0                                                                      the          lactamase
                               1
                                                                                               inhibition of    enzymes. As
     cefixime                  D       pbpA
                                                                                              the third and         a result,
                               D
                                                                                              last stage of           many
                               0
                               8
                                                                                              bacterial cell       organisms
                                                                                                     wall         resistant to
                                                                                                synthesis.         penicillins
                                                                                                Cell lysis is      and some
                                                                                                     then       cephalospori
                                                                                              mediated by           ns due to
47                                                                                            bacterial cell    the presence
                                                                                                     wall            of beta-
                                                                                                  autolytic      lactamases,
                                                                                                  enzymes            may be
                                                                                                   such as        susceptible
                                                                                              autolysins; it     to cefixime.
                                                                                                is possible            The
                                                                                              that cefixime     antibacterial
                                                                                                 interferes
                                                                                               Vitamin B12          effect of
                                                                                                 is used in
                                                                                                the body in
                                                                                                two forms:
                                                                                                                Cyanocobala
                                                                                              Methylcobala
                                                                                                                min (Vitamin
                                                                                                min and 5-
                                                                                                                  B12) is a
                                                                                              deoxyadenos
                                                                                                                    water-
                                                                                                      yl
                                                                                                                    soluble
                                                                                                cobalamin.
                                                                                                                organometal
                                                                                               The enzyme
                                                                                                                       lic
                                                                                                methionine
                                                                                                                 compound
                                                                                                  synthase
                                                                                                                     with a
                                                                                                    needs
                               B                                                                                   trivalent
                                                                                               methylcobal
                               0       AMN TCN1                                                                   cobalt ion
                                                                                                 amin as a
                               3       MTRR TCN2                                                                bound inside
                                                                                                  cofactor.
     cyanocobalamin            B       MMAA MMAB                                                                a corrin ring.
                                                                                               This enzyme
                               A       CUBN MUT                                                                 It is needed
                                                                                              is involved in
                               0       MMACHC                                                                     for nerve
                               1
                                                                                                     the
                                                                                                                cells and red
                                                                                                conversion
                                                                                                                 blood cells,
                                                                                              of the amino
                                                                                                                and to make
                                                                                                     acid
                                                                                                                     DNA.
                                                                                               homocystein
                                                                                                                Vitamin B12
                                                                                                    e into
                                                                                                                deficiency is
                                                                                               methionine.
                                                                                                                the cause of
                                                                                                Methionine
                                                                                                                    several
                                                                                                  in turn is
                                                                                                                   forms of
                                                                                               required for
                                                                                                                   anemia.
                                                                                                     DNA
                                                                                              methylation.
                                                                                                      5-
                                                                                               Deoxyadeno
     N-acetylmuramic_acid                                                                             syl
                               N   S
                               0   0                 acts as an
                               7   1                inhibitor of
                                                                 Myasthenia    muscular
     neostigmine_bromide       A   E               proteins with
                                                                   Gravis       agent
                               A   B               cholinesteras
                               0   0                 e activity
                               1   6
                               C                                                   anti-
                               0                                              inflammator
                               1                                  Infection
                                                                                y diuretic
     sparteine                 B                                Inflammatio
                                                                                   anti-
                               A                                      n
                                                                                infective
                               0
                                                                                  agent
                               4
     (-)-catechin
                                                                              vasoconstrict
                                                                                   or
     12,13-EODE
                                                                              cardiovascul
                                                                                ar agent
     3-hydroxy-DL-kynurenine
     5252917
                                                                                                              Chloroquine
                                                                                                                   is the
                                                                                                                prototype
                                                                                                             anti malarial
                                                                                                  The         drug, most
                                                                                             mechanism        widely used
                                                                                                    of         to treat all
                                                                                            plasmodicida         types of
                                                                                              l action of         malaria
                                                                                             chloroquine       except for
                                                 acts as an                                      is not           disease
                                                inhibitor of                                 completely        caused by
                                                   protein                                  certain. Like     chloroquine
                                P               Glutathione                                      other          resistant
                                0                                                                            <i>Plasmodi
                                                      S-                                       quinoline
                                1                                             anti-malarial
                                    HBA1 TNF   transferasea        Malaria                   derivatives,            um
     chloroquine                B                                                 anti-
                                    TLR9 GSTA2    cts as an       Amebiasis                 it is thought    falciparum</
                                A                                               parasitic
                                                inhibitor of                                   to inhibit         i>. It is
                                0
                                1                  protein                                       heme              highly
                                                Glutamate                                    polymerase         effective
                                               dehydrogena                                  activity. This        against
                                                      se                                       results in     erythrocytic
                                                                                            accumulatio          forms of
                                                                                               n of free     <i>Plasmodi
                                                                                            heme, which              um
                                                                                              is toxic to     vivax</i>,
                                                                                                   the       <i>Plasmodi
                                                                                              parasites.             um
                                                                                                               ovale</i>
                                                                                                                    and
                                                                                                             <i>Plasmodi
                                                                                                                     um
                                L                                                                             malariae</i

48                              0
                                1                                                 anti-
     demecolcine                C
                                                                              proliferative
                                C
                                0
                                1
     DL-PPMP
                                                                                            Paclitaxel        Paclitaxel is
                                                                                            interferes            a taxoid
                                                                                             with the        antineoplasti
                                                                                              normal              c agent
                                                                                           function of        indicated as
                                                                                          microtubule        first-line and
                                                                                             growth.          subsequent
                                                                                             Whereas           therapy for
                                                                                            drugs like               the
                                                                                            colchicine       treatment of
                                                                                            cause the           advanced
                                                                                          depolymeriz        carcinoma of
                                                                                             ation of           the ovary,
                                L                                                         microtubules          and other
                                0                                                             in vivo,            various
                                1
                                                                                 anti-      paclitaxel            cancers
     paclitaxel                 C   BCL2 TUBB1                    Neoplasms
                                                                               neoplastic arrests their          including
                                D
                                                                                           function by             breast
                                0
                                1
                                                                                           having the             cancer.
                                                                                             opposite         Paclitaxel is
                                                                                             effect; it           a novel
                                                                                               hyper-        antimicrotub
                                                                                            stabilizes           ule agent
                                                                                                their               that
                                                                                            structure.          promotes
                                                                                                This                 the
                                                                                          destroys the        assembly of
                                                                                          cell's ability     microtubules
                                                                                            to use its       from tubulin
                                                                                          cytoskeleton         dimers and
                                                                                          in a flexible          stabilizes
                                                                                             manner.         microtubules
                                                                              immunosupp Specifically,                by
     phenanthridinone                                                           ressive
                                                                                 agent

                                                    acts as an
                                                   inhibitor of
                                                      protein
                                                    epidermal
                                                      growth
                                                       factor
     4,5-dianilinophthalimide                        receptor
                                                 (erythroblast
                                                  ic leukemia
                                                 viral (v-erb-
                                                 b) oncogene
                                                    homolog,
                                                      avian)
     alpha-estradiol
                               acts as an
                              inhibitor of
                                 protein
                                Voltage-
                             dependent L-
                             type calcium
                             channel acts
                                  as an
                              inhibitor of
                                 protein
                                Voltage-
                             dependent L-
                             type calcium
                                           Tachycardia,     anti-
                             channel acts
                                           VentricularH arrhythmic
                                  as an
dexverapamil                               ypertension      anti-
                              inhibitor of
                                             Angina     hypertensive
                             proteins with
                                             Pectoris    vasodilator
                             low voltage-
                                  gated
                                calcium
                                channel
                             activity acts
                             as a blocker
                               of protein
                                calcium
                                channel,
                                voltage-
                              dependent,
                               alpha 1G
                                 subunit

                                                                            Breast      Aromatase is
                                                                         cancer cell     an enzyme
                                                                        growth may            that
                                                                       be estrogen-         converts
                                                                        dependent.      hormones to
                                                                         Aromatase       estrogen in
                                                                       (exemestane        the body's
                                                                           ) is the          adrenal
                                                                          principal      glands. The
                                                                       enzyme that        aromatase
                                                                          converts         inhibitors
                                                                         androgens         (AIs) are
                                                                       to estrogens       drugs that
               L                                                        both in pre-         reduce
               0                                                             and           estrogen
               2
                                                                       postmenopa          levels by
exemestane     B   CYP19A1
                                                                       usal women.      blocking the
               G
                                                                          While the         action of
               0
               6
                                                                        main source     aromatase in
                                                                        of estrogen      the adrenal
                                                                         (primarily      glands. The
                                                                        estradiol) is   selective AIs
                                                                        the ovary in         (SAIs)
                                                                       premenopau         selectively
                                                                        sal women,           reduce
                                                                       the principal        levels of
                                                                          source of        estrogen
                                                                         circulating         without
                                                                       estrogens in       interfering
                                                                       postmenopa         with levels
                                                                        usal women          of other
                                                                           is from           steroid
                                                                         conversion        hormones
                                                                                   Aminoglycosi      Kanamycin
                                                                                        des like          is an
                                                                                     kanamycin      aminoglycosi
                                                                                   "irreversibly"   de antibiotic.
                                                                                        bind to     Aminoglycosi
                                                                                   specific 30S-    des work by
                                                                                        subunit       binding to
                                                                                   proteins and     the bacterial
                                                                                     16S rRNA.             30S
                                                                                    Specifically      ribosomal
                                                                                    Kanamycin           subunit,
                                                                                   binds to four        causing
                                                                                    nucleotides      misreading
                    A   J   S                                                      of 16S rRNA         of t-RNA,
                    0   0   0                                                      and a single      leaving the
                    7   1   1                                            anti-
                                                                                    amino acid        bacterium
     kanamycin      A   G   A   rpsL                    Infection      infective
                                                                                     of protein        unable to
                    A   B   A                                            agent
                                                                                      S12. This       synthesize
                    0   0   2
                    8   4   4
                                                                                      interferes    proteins vital
                                                                                          with           to its
                                                                                       decoding         growth.
                                                                                     site in the    Aminoglycosi
                                                                                     vicinity of        des are
                                                                                     nucleotide          useful
                                                                                    1400 in 16S      primarily in
                                                                                   rRNA of 30S        infections
                                                                                   subunit. This       involving
                                                                                         region         aerobic,
                                                                                       interacts         Gram-
                                                                                       with the        negative
                                                                                   wobble base         bacteria,
                                                                                         in the         such as
                    D   R                                                          anticodon of     Pseudomona
                    0   0
                    4   6                                                anti-
     mepyramine     A   A
                                                                      histamine
                    A   C
                    0   0
                    2   1
                                                                                   Although the       Mesalazine
                                                                                     mechanism       (INN, BAN),
                                                                                     of action of     also known
                                                                                     mesalazine              as
                                                                                     is not fully    Mesalamine
                                                                                    understood,     (USAN) or 5-
                                                                                   it appears to    aminosalicyli
                                                                                      be topical       c acid (5-
                                                                                     rather than      ASA), is an
                                                                                      systemic.            anti-
                                                                                       Mucosal       inflammator
49                                        acts as an
                                                                                     production
                                                                                           of
                                                                                                     y drug used
                                                                                                         to treat
                    A                    inhibitor of                                arachidonic     inflammatio
                    0                                                                    acid           n of the
                                        proteins with
                    7
                                PTGS1   prostaglandi     Colitis,    gastrointesti metabolites,         digestive
     mesalazine     E
                                PTGS2         n-        Ulcerative    nal agent both through               tract
                    C
                                        endoperoxid                                       the           (Crohn's
                    0
                    2                    e synthase                                 cyclooxygen     disease) and
                                           activity                                       ase            mild to
                                                                                      pathways,        moderate
                                                                                         i.e.,         ulcerative
                                                                                    prostanoids,          colitis.
                                                                                    and through       Mesalazine
                                                                                          the         is a bowel-
                                                                                   lipoxygenase          specific
                                                                                      pathways,     aminosalicyl
                                                                                         i.e.,          ate drug
                                                                                    leukotrienes          that is
                                                                                         and        metabolized
                                                                                   hydroxyeicos        in the gut
                                                                                     atetraenoic      and has its
                    J                                                                  acids, is    predominant
                    0
                    1                                                    anti-
     midecamycin    F                                   Infection      infective
                    A                                                    agent
                    0
                    3
                    A
                    0
                    7
     racecadotril   X
                    A
                    0
                    4
                                                                         Both COX-1      Rofecoxib, a
                                                                          and COX-2         selective
                                                                         catalyze the    cyclooxygen
                                                                          conversion     ase-2 (COX-
                                                                                  of     2) inhibitor,
                                                                          arachidonic     is classified
                                                                              acid to          as a
                                                                        prostaglandi     nonsteroidal
                                                                          n (PG) H2,          anti-
                                                                                 the     inflammator
                                   acts as an
                                                                         precursor of        y drug
                                  inhibitor of
                                                                             PGs and        (NSAID).
                                     protein
                                                                         thromboxan      Rofecoxib is
                 M               prostaglandi
                                                                        e. Rofecoxib      used for its
                 0                      n-     Inflammatio
                                                                           selectively        anti-
                 1               endoperoxid        n            anti-
                     PTGS2 ELN                                            inhibits the   inflammator
rofecoxib        A               e synthase 2 Osteoarthriti inflammator
                     PTGS1                                              cyclooxygen      y, analgesic,
                 H               (prostagland sDysmenorr yanalgesic
                                                                        ase-2 (COX-            and
                 0                   in G/H      hea Pain
                 2                                                       2) enzyme,        antipyretic
                                    synthase
                                                                           important      activities in
                                       and
                                                                              for the          the
                                 cyclooxygen
                                                                        mediation of     managemen
                                      ase)
                                                                         inflammatio           t of
                                                                          n and pain.    osteoarthriti
                                                                         Unlike non-      s (OA) and
                                                                            selective        for the
                                                                            NSAIDs,      treatment of
                                                                            rofecoxib    dysmenorrh
                                                                            does not      ea or acute
                                                                              inhibit    pain. Unlike
                                                                             platelet      celecoxib,
                                                                        aggregation.        rofecoxib
                                                                        Troleandomy          lacks a
                                                                          cin acts by
                                                                         penetrating
                                                                        the bacterial
                                                                                cell
                                                                          membrane       Troleandomy
                                                                                and          cin is a
                                                                           reversibly      macrolide
                                                                           binding to      antibiotic
                                                                            the 50 S         that is
                                                                           subunit of      similar to
                                                                            bacterial     erythromyci
                                                                        ribosomes or         n. It is
                 J                                                      near the "P"        active in
                 0                                                      or donor site    vitro against
                 1
                                                                             so that     the following
troleandomycin   F   ermC
                                                                           binding of        gram-
                 A
                                                                               tRNA         positive
                 0
                 8
                                                                            (transfer     organisms:
                                                                         RNA) to the     <i>Streptoc
                                                                        donor site is         occus
                                                                            blocked.     pyogenes</i
                                                                         Translocatio        > and
                                                                        n of peptides    <i>Diplococ
                                                                        from the "A"           cus
                                                                          or acceptor    pneumoniae
                                                                           site to the        </i>.
                                                                        "P" or donor
                                                                               site is
                                                                          prevented,
                                                                                and
                                                                         subsequent
                                                                             protein
                                                                                  Possibly by
                                                                                   deforming
                                                                                 the channel,
                                                                                inhibiting ion-
                                                                                      control
                                                                                       gating
                                                                                 mechanisms
                                                                                     , and/or   Verapamil, a
                                                                                   interfering      class IV
                                                                                     with the   antiarrhythm
                                                                                    release of   ic agent, is
                                                                                calcium from used as a
                        SCN5A CA1                                                       the        calcium-
                    C   KCNJ11                                                  sarcoplasmic        channel
                    0                                                              reticulum,
                        CACNB4                                                                     blocking
                    8                                                             verapamil, (CCB) agent
                        CACNA1G
     verapamil      D
                        CACNA1F                                                         like        for the
                    A
                        CACNB3                                                      diltiazem, treatment of
                    0
                        CACNA1D                                                   inhibits the      angina,
                    1
                        CACNB1                                                       influx of  hypertension
                                                                                 extracellular     , and for
                                                                                      calcium   supraventric
                                                                                  across both         ular
                                                                                        the     tachyarrhyth
                                                                                  myocardial         mias.
                                                                                and vascular
                                                                                      smooth
                                                                                  muscle cell
                                                                                membranes.
                                                                                        The
                                                                                     resultant
                                                                                 inhibition of
                    A                                                                   the
                    1
                    1                                              vitamin
     benfotiamine   D                                 Pain
                                                                  analgesic
                    A
                    0
                    3
                    B
                    0                                                anti-
                    1                                Bacterial    coagulant
     dicoumarol     A
                                                    Infections       anti-
                    A
                                                                   bacterial
                    0
                    1
                                      acts as an
                                     inhibitor of
                                                                  pesticide
     ethoxyquin                     proteins with
                                                                 anti-oxidant
                                       ATPase
                                       activity

                                                                                  Flecainide
                                                                                     acts on
                                                                                     sodium
                                                                                                  Flecainide
                                                                                 channels on
                                                                                                   has local
                                                                                the neuronal
                                                                                                  anesthetic
                                                                                       cell
                                                                                                 activity and
                                                                                 membrane,
                                                                                                  belongs to
                                                                                 limiting the
                                                                                                      the
                                                                                   spread of
                                                                                                 membrane
                    C                                                                seizure
                                      acts as a                                                   stabilizing
                    0                                                            activity and
                                     blocker of                                                    (Class 1)
                    1                                                               reducing
                                    proteins with                   anti-                          group of
     flecainide     B   SCN5A                     Arrhythmia                         seizure
                                       sodium                    arrhythmic                     antiarrhythm
                    C                                                           propagation.
                    0                 channel                                                   ic agents; it
                                                                                       The
                    4                  activity                                                       has
                                                                                antiarrhythm
                                                                                                electrophysi
                                                                                   ic actions
                                                                                                ologic effects
                                                                                       are
                                                                                                characteristi
                                                                                   mediated
                                                                                                  c of the IC
                                                                                    through
                                                                                                    class of
                                                                                   effects on
                                                                                                antiarrhythm
                                                                                     sodium
                                                                                                      ics.
                                                                                 channels in
                                                                                    Purkinje
                                                                                     fibers.
50
50                                                                                   By binding     Piperacillin is
                                                                                     to specific      a penicillin
                                                                                      penicillin-   beta-lactam
                                                                                        binding        antibiotic
                                                                                        proteins     used in the
                                                                                         (PBPs)     treatment of
                                                                                        located         bacterial
                                                                                      inside the       infections
                                                                                   bacterial cell     caused by