Found 57 Enz. Inhib. hit(s) with all data for entry = 50002545 
Affinity DataKi: 0.0400nMAssay Description:Displacement of [3H]granisetron from human 5-HT3A receptor expressed in HEK293 cells by scintillation counting methodMore data for this Ligand-Target Pair
TargetGamma-aminobutyric acid receptor subunit alpha-3/beta-3/gamma-2(Homo sapiens (Human))
Amgen
Curated by ChEMBL
Amgen
Curated by ChEMBL
Affinity DataKi: 0.200nMAssay Description:Displacement of [3H]Ro15-1788 from human GABAA receptor alpha3beta3gamma2 expressed in LTK cells preincubated for 30 secs measured every 15 mins at -...More data for this Ligand-Target Pair
TargetGamma-aminobutyric acid receptor subunit alpha-1/beta-3/gamma-2(Homo sapiens (Human))
Amgen
Curated by ChEMBL
Amgen
Curated by ChEMBL
Affinity DataKi: 0.200nMAssay Description:Displacement of [3H]Ro15-1788 from human GABAA receptor alpha1beta3gamma2 expressed in LTK cells preincubated for 30 secs measured every 15 mins at -...More data for this Ligand-Target Pair
Affinity DataKi: 0.300nMAssay Description:Displacement of [3H]Ro15-1788 from human GABAA receptor alpha5beta3gamma2 expressed in LTK cells preincubated for 30 secs measured every 15 mins at -...More data for this Ligand-Target Pair
TargetGamma-aminobutyric acid receptor subunit alpha-6/beta-3/gamma-2(Homo sapiens (Human))
Amgen
Curated by ChEMBL
Amgen
Curated by ChEMBL
Affinity DataKi: 1.90nMAssay Description:Displacement of [3H]Ro15-1788 from human GABAA receptor alpha6beta3gamma2 expressed in LTK cells preincubated for 30 secs measured every 15 mins at -...More data for this Ligand-Target Pair
Affinity DataKi: 22nMAssay Description:Displacement of [3H]granisetron from human 5-HT3AB receptor expressed in HEK293 cells by scintillation counting methodMore data for this Ligand-Target Pair
TargetGamma-aminobutyric acid receptor subunit alpha-5/beta-3/gamma-2(Rattus norvegicus (Rat))
Amgen
Curated by ChEMBL
Amgen
Curated by ChEMBL
Affinity DataKi: 55nMAssay Description:Displacement of [3H]-flunitrazepam from recombinant rat GABAA receptor alpha5beta3gamma2S expressed in HEK293 cell membranes after 90 mins by liquid ...More data for this Ligand-Target Pair
TargetGamma-aminobutyric acid receptor subunit alpha-2/beta-3/gamma-2(Rattus norvegicus (Rat))
Amgen
Curated by ChEMBL
Amgen
Curated by ChEMBL
Affinity DataKi: 360nMAssay Description:Displacement of [3H]-flunitrazepam from recombinant rat GABAA receptor alpha2beta3gamma2S expressed in HEK293 cell membranes after 90 mins by liquid ...More data for this Ligand-Target Pair
TargetGamma-aminobutyric acid receptor subunit alpha-3/beta-3/gamma-2(Rattus norvegicus (Rat))
Amgen
Curated by ChEMBL
Amgen
Curated by ChEMBL
Affinity DataKi: 660nMAssay Description:Displacement of [3H]-flunitrazepam from recombinant rat GABAA receptor alpha3beta3gamma2S expressed in HEK293 cell membranes after 90 mins by liquid ...More data for this Ligand-Target Pair
TargetGamma-aminobutyric acid receptor subunit alpha-1/beta-3/gamma-2(Rattus norvegicus (Rat))
Amgen
Curated by ChEMBL
Amgen
Curated by ChEMBL
Affinity DataKi: 850nMAssay Description:Displacement of [3H]-flunitrazepam from recombinant rat GABAA receptor alpha1beta3gamma2S expressed in HEK293 cell membranes after 90 mins by liquid ...More data for this Ligand-Target Pair
Affinity DataKi: >1.00E+4nMAssay Description:Displacement of [3H]Ro15-4313 from human GABAA receptor alpha4beta3gamma2 expressed in LTK cells preincubated for 30 secs measured every 15 mins at -...More data for this Ligand-Target Pair
Affinity DataKi: >1.00E+4nMAssay Description:Displacement of [3H]Ro15-1788 from human GABAA receptor alpha2beta3gamma2 expressed in LTK cells preincubated for 30 secs measured every 15 mins at -...More data for this Ligand-Target Pair
Affinity DataIC50: 150nMAssay Description:Inhibition of recombinant human 5-HT3A receptor expressed in HEK293 cell membranes using 5-HT as substrate in presence of [3H]GR65630More data for this Ligand-Target Pair
Affinity DataIC50: 320nMAssay Description:Inhibition of human alpha7 nAChR expressed in Xenopus oocytes at -80 mV holding potential by electro-physiological analysisMore data for this Ligand-Target Pair
Affinity DataIC50: 430nMAssay Description:Inhibition of human 5-HT3AB receptor expressed in transient A201 cells after 30 mins by Fluo-4-AM dye based FLIPR assayMore data for this Ligand-Target Pair
Affinity DataIC50: 620nMAssay Description:Inhibition of human 5-HT3A receptor expressed in transient A201 cells after 30 mins by Fluo-4-AM dye based FLIPR assayMore data for this Ligand-Target Pair
Affinity DataIC50: 710nMAssay Description:Inhibition of human 5-HT3AE receptor expressed in transient A201 cells after 30 mins by Fluo-4-AM dye based FLIPR assayMore data for this Ligand-Target Pair
Affinity DataIC50: 840nMAssay Description:Inhibition of human 5-HT3AC receptor expressed in transient A201 cells after 30 mins by Fluo-4-AM dye based FLIPR assayMore data for this Ligand-Target Pair
Affinity DataIC50: 1.40E+3nMAssay Description:Antagonist activity at 5-HT3A receptor (unknown origin) assessed as inhibition of serotonin-induced peak currentsMore data for this Ligand-Target Pair
TargetNeuronal acetylcholine receptor subunit alpha-7(Rattus norvegicus (Rat))
Amgen
Curated by ChEMBL
Amgen
Curated by ChEMBL
Affinity DataIC50: 1.00E+4nMAssay Description:Agonist activity at rat brain membrane alpha7 nAChRMore data for this Ligand-Target Pair
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Homo sapiens (Human))
Amgen
Curated by ChEMBL
Amgen
Curated by ChEMBL
Affinity DataIC50: >2.50E+4nMAssay Description:Inhibition of alpha4beta2 nAChR (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 3.00E+4nMAssay Description:Inhibition of recombinant human glycine receptor alpha3beta expressed in HEK293 cellsMore data for this Ligand-Target Pair
TargetGamma-aminobutyric acid receptor subunit alpha-1/beta-3/gamma-2(Mus musculus)
Amgen
Curated by ChEMBL
Amgen
Curated by ChEMBL
Affinity DataIC50: >3.00E+4nMAssay Description:Inhibition of C57BL/6 mouse GABAA receptor alpha1beta3gamma2More data for this Ligand-Target Pair
Affinity DataIC50: >3.00E+4nMAssay Description:Inhibition of 5-HT3 receptor (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 3.00E+4nMAssay Description:Inhibition of recombinant human glycine receptor alpha2beta expressed in HEK293 cellsMore data for this Ligand-Target Pair
Affinity DataIC50: 3.00E+4nMAssay Description:Inhibition of recombinant human glycine receptor alpha1beta expressed in HEK293 cellsMore data for this Ligand-Target Pair
Affinity DataIC50: 1.41E+5nMAssay Description:Inhibition of human 5-HT3A receptor expressed in Xenopus laevis oocytes assessed as HT-induced current by electrophysiological methodMore data for this Ligand-Target Pair
Affinity DataIC50: 2.57E+5nMAssay Description:Inhibition of human 5-HT3A receptor expressed in Xenopus laevis oocytes assessed as HT-induced current by electrophysiological methodMore data for this Ligand-Target Pair
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Homo sapiens (Human))
Amgen
Curated by ChEMBL
Amgen
Curated by ChEMBL
Affinity DataEC50: >2.50E+4nMAssay Description:Agonist activity at alpha4beta2 nAChR (unknown origin)More data for this Ligand-Target Pair
Affinity DataEC50: 454nMAssay Description:Positive allosteric modulation of human glycine alpha3 receptor expressed in HEK293T cells assessed as glycine-induced increase in current response a...More data for this Ligand-Target Pair
Affinity DataEC50: 16nMAssay Description:Positive allosteric modulation of human glycine alpha1beta receptor expressed in HEK293T cells assessed as glycine-induced increase in current respon...More data for this Ligand-Target Pair
3D Structure (crystal)Affinity DataEC50: 171nMAssay Description:Positive allosteric modulation of human glycine alpha1beta receptor expressed in HEK293T cells assessed as glycine-induced increase in current respon...More data for this Ligand-Target Pair
TargetGamma-aminobutyric acid receptor subunit alpha-2/beta-2/gamma-2(Homo sapiens (Human))
Amgen
Curated by ChEMBL
Amgen
Curated by ChEMBL
Affinity DataEC50: 1.08E+3nMAssay Description:Agonist activity at recombinant human GABAA receptor alpha2beta2gamma2L expressed in Xenopus laevis oocytes incubated for 30 secs by electrophysiolog...More data for this Ligand-Target Pair
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-4(Homo sapiens (Human))
Amgen
Curated by ChEMBL
Amgen
Curated by ChEMBL
Affinity DataEC50: 237nMAssay Description:Positive allosteric modulation of human alpha4beta4 nAChR expressed in HEK cells preincubated for 15 mins followed by dihydro-beta-erythroidine hydro...More data for this Ligand-Target Pair
Affinity DataEC50: >5.00E+4nMAssay Description:Positive allosteric modulation of C57BL/6 mouse GABAA receptor alpha1beta2gamma2 assessed as increase in GABA-induced current response at -60 mV hold...More data for this Ligand-Target Pair
Affinity DataEC50: 50nMAssay Description:Positive allosteric modulation of human glycine alpha3 receptor expressed in HEK293T cells assessed as glycine-induced increase in current response a...More data for this Ligand-Target Pair
Affinity DataEC50: 3.90E+3nMAssay Description:Positive allosteric modulation of recombinant human glycine receptor alpha3 expressed in CHOK1 cells at -60 mV holding potential by whole cell patch-...More data for this Ligand-Target Pair
Affinity DataEC50: 590nMAssay Description:Positive allosteric modulation of recombinant human glycine receptor alpha1 expressed in HEK293 cells assessed as increase in glycine-induced current...More data for this Ligand-Target Pair
TargetGamma-aminobutyric acid receptor subunit alpha-1/beta-3/gamma-2(Mus musculus)
Amgen
Curated by ChEMBL
Amgen
Curated by ChEMBL
Affinity DataEC50: >3.00E+4nMAssay Description:Positive allosteric modulation of C57BL/6 mouse GABAA receptor alpha1beta3gamma2 assessed as increase in GABA-induced current response at -60 mV hold...More data for this Ligand-Target Pair
TargetGamma-aminobutyric acid receptor subunit alpha-1(Rattus norvegicus (Rat))
Amgen
Curated by ChEMBL
Amgen
Curated by ChEMBL
Affinity DataEC50: 1.50E+4nMAssay Description:Agonist activity at GABAA receptor in Sprague-Dawley rat forebrain membranes assessed as enhancement of [3H]muscimol binding after 2 hrs by radiometr...More data for this Ligand-Target Pair
TargetGamma-aminobutyric acid receptor subunit alpha-1/beta-2/gamma-2(Homo sapiens (Human))
Amgen
Curated by ChEMBL
Amgen
Curated by ChEMBL
Affinity DataEC50: 720nMAssay Description:Agonist activity at recombinant human GABAA receptor alpha1beta2gamma2L expressed in Xenopus laevis oocytes incubated for 30 secs by electrophysiolog...More data for this Ligand-Target Pair
TargetGamma-aminobutyric acid receptor subunit alpha-2/beta-2/gamma-2(Homo sapiens (Human))
Amgen
Curated by ChEMBL
Amgen
Curated by ChEMBL
Affinity DataEC50: 7.60E+3nMAssay Description:Positive allosteric modulation of recombinant wild type GABAA receptor alpha2beta2gamma2S (unknown origin) expressed in HEK293 cells assessed as pote...More data for this Ligand-Target Pair
TargetGamma-aminobutyric acid receptor subunit alpha-1/beta-2/gamma-2(Homo sapiens (Human))
Amgen
Curated by ChEMBL
Amgen
Curated by ChEMBL
Affinity DataEC50: 374nMAssay Description:Positive allosteric modulation of GABAA receptor alpha1beta2gamma2 (unknown origin)More data for this Ligand-Target Pair
TargetAcetylcholine receptor subunit alpha/Neuronal acetylcholine receptor subunit beta-4(Homo sapiens (Human))
Amgen
Curated by ChEMBL
Amgen
Curated by ChEMBL
Affinity DataEC50: 286nMAssay Description:Positive allosteric modulation of human alpha2beta4 nAChR expressed in HEK cells preincubated for 15 mins followed by dihydro-beta-erythroidine hydro...More data for this Ligand-Target Pair
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Homo sapiens (Human))
Amgen
Curated by ChEMBL
Amgen
Curated by ChEMBL
Affinity DataEC50: 446nMAssay Description:Positive allosteric modulation of human alpha4beta2 nAChR expressed in HEK cells preincubated for 15 mins followed by dihydro-beta-erythroidine hydro...More data for this Ligand-Target Pair
Affinity DataEC50: 3.80E+3nMAssay Description:Agonist activity at human 5-HT43A receptor expressed in Xenopus laevis oocytesMore data for this Ligand-Target Pair
Affinity DataEC50: 2.80E+3nMAssay Description:Agonist activity at human 5-HT43AB receptor expressed in Xenopus laevis oocytesMore data for this Ligand-Target Pair
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Homo sapiens (Human))
Amgen
Curated by ChEMBL
Amgen
Curated by ChEMBL
Affinity DataEC50: 275nMAssay Description:Positive allosteric modulation of human (alpha4beta2)2beta2 nAChR expressed in HEK cells preincubated for 15 mins followed by dihydro-beta-erythroidi...More data for this Ligand-Target Pair
Affinity DataEC50: 330nMAssay Description:Positive allosteric modulation of human glycine alpha3beta receptor expressed in HEK293T cells assessed as glycine-induced increase in current respon...More data for this Ligand-Target Pair
TargetAcetylcholine receptor subunit alpha/Neuronal acetylcholine receptor subunit beta-2(Homo sapiens (Human))
Amgen
Curated by ChEMBL
Amgen
Curated by ChEMBL
Affinity DataEC50: 660nMAssay Description:Positive allosteric modulation of human alpha2beta2 nAChR expressed in HEK cells preincubated for 15 mins followed by dihydro-beta-erythroidine hydro...More data for this Ligand-Target Pair
