Report error Found 191 Enz. Inhib. hit(s) with Target = 'Gamma-aminobutyric acid type B receptor subunit 1/2'
TargetGamma-aminobutyric acid type B receptor subunit 1/2(Human)
Beijing Institute of Biotechnology
Curated by ChEMBL
Beijing Institute of Biotechnology
Curated by ChEMBL
Affinity DataIC50: 0.200nMAssay Description:Activation of human GABAB1/GABAB2 expressed in HEK293 cells co-transfected with rat CaV2.2 channel assessed as reduction in CaV2.2-mediated peak-curr...More data for this Ligand-Target Pair
TargetGamma-aminobutyric acid type B receptor subunit 1/2(Human)
Beijing Institute of Biotechnology
Curated by ChEMBL
Beijing Institute of Biotechnology
Curated by ChEMBL
Affinity DataKd: 1nMAssay Description:Binding affinity to GABA-B receptor (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 1nMAssay Description:In vitro displacement of [3H]GABA from Gamma-aminobutyric acid type B receptor sites in rat brain membranesMore data for this Ligand-Target Pair
TargetGamma-aminobutyric acid type B receptor subunit 1/2(Human)
Beijing Institute of Biotechnology
Curated by ChEMBL
Beijing Institute of Biotechnology
Curated by ChEMBL
Affinity DataIC50: 1.20nMAssay Description:Activation of human GABAB1/GABAB2 expressed in HEK293 cells co-transfected with rat CaV2.2 channel assessed as reduction in CaV2.2-mediated peak-curr...More data for this Ligand-Target Pair
TargetGamma-aminobutyric acid type B receptor subunit 1/2(Human)
Beijing Institute of Biotechnology
Curated by ChEMBL
Beijing Institute of Biotechnology
Curated by ChEMBL
Affinity DataIC50: 2.40nMAssay Description:Inhibition of [3H]-baclofen binding to Gamma-aminobutyric acid type B receptor of cat cerebellumMore data for this Ligand-Target Pair
TargetGamma-aminobutyric acid type B receptor subunit 1/2(Human)
Beijing Institute of Biotechnology
Curated by ChEMBL
Beijing Institute of Biotechnology
Curated by ChEMBL
Affinity DataIC50: 2.40nMAssay Description:Activation of human GABAB1/GABAB2 expressed in HEK293 cells co-transfected with rat CaV2.2 channel assessed as reduction in CaV2.2-mediated peak-curr...More data for this Ligand-Target Pair
Affinity DataIC50: 3nMAssay Description:In vitro displacement of [3H]GABA from Gamma-aminobutyric acid type B receptor sites in rat brain membranesMore data for this Ligand-Target Pair
TargetGamma-aminobutyric acid type B receptor subunit 1/2(Human)
Beijing Institute of Biotechnology
Curated by ChEMBL
Beijing Institute of Biotechnology
Curated by ChEMBL
Affinity DataIC50: 4.90nMAssay Description:Activation of human GABAB1/GABAB2 expressed in HEK293 cells co-transfected with rat CaV2.2 channel assessed as reduction in CaV2.2-mediated peak-curr...More data for this Ligand-Target Pair
Affinity DataIC50: 5.40nMAssay Description:Inhibition of [3H]CGP-27492 binding to Gamma-aminobutyric acid type B receptor of rat cortexMore data for this Ligand-Target Pair
TargetGamma-aminobutyric acid type B receptor subunit 1/2(Human)
Beijing Institute of Biotechnology
Curated by ChEMBL
Beijing Institute of Biotechnology
Curated by ChEMBL
Affinity DataIC50: 6.60nMAssay Description:Inhibition of [3H]-baclofen binding to Gamma-aminobutyric acid type B receptor of cat cerebellumMore data for this Ligand-Target Pair
TargetGamma-aminobutyric acid type B receptor subunit 1/2(Human)
Beijing Institute of Biotechnology
Curated by ChEMBL
Beijing Institute of Biotechnology
Curated by ChEMBL
Affinity DataEC50: 8.60nMAssay Description:Agonist activity at human recombinant GABA-B receptorMore data for this Ligand-Target Pair
TargetGamma-aminobutyric acid type B receptor subunit 1/2(Human)
Beijing Institute of Biotechnology
Curated by ChEMBL
Beijing Institute of Biotechnology
Curated by ChEMBL
Affinity DataIC50: 13nMAssay Description:Agonist activity at human GABAB expressed in HEK293T cells co-transfected with human CaV2.2 channel assessed as inhibition of CaV2.2-mediated Ba2+ pe...More data for this Ligand-Target Pair
TargetGamma-aminobutyric acid type B receptor subunit 1/2(Human)
Beijing Institute of Biotechnology
Curated by ChEMBL
Beijing Institute of Biotechnology
Curated by ChEMBL
Affinity DataIC50: 15nMAssay Description:Inhibition of [3H]-baclofen binding to Gamma-aminobutyric acid type B receptor of cat cerebellumMore data for this Ligand-Target Pair
Affinity DataIC50: 16nMAssay Description:Inhibition of [3H]CGP-27492 binding to Gamma-aminobutyric acid type B receptor of rat cortexMore data for this Ligand-Target Pair
Affinity DataIC50: 17nMAssay Description:Inhibition of [3H]CGP-27492 binding to Gamma-aminobutyric acid type B receptor of rat cortexMore data for this Ligand-Target Pair
TargetGamma-aminobutyric acid type B receptor subunit 1/2(Human)
Beijing Institute of Biotechnology
Curated by ChEMBL
Beijing Institute of Biotechnology
Curated by ChEMBL
Affinity DataIC50: 18nMAssay Description:Inhibition of [3H]-baclofen binding to Gamma-aminobutyric acid type B receptor of cat cerebellumMore data for this Ligand-Target Pair
TargetGamma-aminobutyric acid type B receptor subunit 1/2(Human)
Beijing Institute of Biotechnology
Curated by ChEMBL
Beijing Institute of Biotechnology
Curated by ChEMBL
Affinity DataIC50: 19nMAssay Description:Activation of human GABAB1/GABAB2 expressed in HEK293 cells co-transfected with rat CaV2.2 channel assessed as reduction in CaV2.2-mediated peak-curr...More data for this Ligand-Target Pair
TargetGamma-aminobutyric acid type B receptor subunit 1/2(Human)
Beijing Institute of Biotechnology
Curated by ChEMBL
Beijing Institute of Biotechnology
Curated by ChEMBL
Affinity DataIC50: 19nMAssay Description:Activation of human GABAB1/GABAB2 expressed in HEK293 cells co-transfected with rat CaV2.2 channel assessed as reduction in CaV2.2-mediated peak-curr...More data for this Ligand-Target Pair
TargetGamma-aminobutyric acid type B receptor subunit 1/2(Human)
Beijing Institute of Biotechnology
Curated by ChEMBL
Beijing Institute of Biotechnology
Curated by ChEMBL
Affinity DataIC50: 21nMAssay Description:Agonist activity at human GABAB expressed in HEK293T cells co-transfected with human CaV2.2 channel assessed as inhibition of CaV2.2-mediated Ba2+ pe...More data for this Ligand-Target Pair
TargetGamma-aminobutyric acid type B receptor subunit 1/2(Human)
Beijing Institute of Biotechnology
Curated by ChEMBL
Beijing Institute of Biotechnology
Curated by ChEMBL
Affinity DataIC50: 23nMAssay Description:Activation of human GABAB1/GABAB2 expressed in HEK293 cells co-transfected with rat CaV2.2 channel assessed as reduction in CaV2.2-mediated peak-curr...More data for this Ligand-Target Pair
TargetGamma-aminobutyric acid type B receptor subunit 1/2(Human)
Beijing Institute of Biotechnology
Curated by ChEMBL
Beijing Institute of Biotechnology
Curated by ChEMBL
Affinity DataIC50: 25nMAssay Description:Inhibition of [3H]-baclofen binding to Gamma-aminobutyric acid type B receptor of cat cerebellumMore data for this Ligand-Target Pair
TargetGamma-aminobutyric acid type B receptor subunit 1/2(Human)
Beijing Institute of Biotechnology
Curated by ChEMBL
Beijing Institute of Biotechnology
Curated by ChEMBL
Affinity DataIC50: 29nMAssay Description:Inhibition of [3H]CGP-27492 binding to cat Gamma-aminobutyric acid type B receptorMore data for this Ligand-Target Pair
Affinity DataIC50: 30nMAssay Description:Displacement of [3H]baclofen from Gamma-aminobutyric acid type B receptor of rat brain membranesMore data for this Ligand-Target Pair
Affinity DataIC50: 30nMpH: 7.4Assay Description:In vitro binding affinity against Gamma-aminobutyric acid type B receptor in rat brain synaptic membranes at pH 7.4More data for this Ligand-Target Pair
Affinity DataIC50: 30nMAssay Description:In vitro displacement of [3H]GABA from Gamma-aminobutyric acid type B receptor sites in rat brain membranesMore data for this Ligand-Target Pair
Affinity DataIC50: 30nMAssay Description:Inhibition of Gamma-aminobutyric acid type B receptor of rat cortexMore data for this Ligand-Target Pair
Affinity DataIC50: 32nMAssay Description:Inhibition of [3H]CGP-27492 binding to Gamma-aminobutyric acid type B receptor of rat cortexMore data for this Ligand-Target Pair
TargetGamma-aminobutyric acid type B receptor subunit 1/2(Human)
Beijing Institute of Biotechnology
Curated by ChEMBL
Beijing Institute of Biotechnology
Curated by ChEMBL
Affinity DataIC50: 35nMAssay Description:Inhibition of [3H]-baclofen binding to Gamma-aminobutyric acid type B receptor of cat cerebellumMore data for this Ligand-Target Pair
TargetGamma-aminobutyric acid type B receptor subunit 1/2(Human)
Beijing Institute of Biotechnology
Curated by ChEMBL
Beijing Institute of Biotechnology
Curated by ChEMBL
Affinity DataIC50: 39nMAssay Description:Inhibition of [3H]baclofen binding to Gamma-aminobutyric acid type B receptor of cat cerebellumMore data for this Ligand-Target Pair
Affinity DataIC50: 40nMAssay Description:Binding affinity against Gamma-aminobutyric acid type B receptor in rat brain synaptosomes after 30 minutesMore data for this Ligand-Target Pair
Affinity DataIC50: 40nMAssay Description:Inhibition of [3H]baclofen binding to rat gamma-aminobutyric acid type B receptor.More data for this Ligand-Target Pair
Affinity DataIC50: 40nMAssay Description:Binding affinity against Gamma-aminobutyric acid type B receptor in rat brain synaptosomes after 30 minutesMore data for this Ligand-Target Pair
Affinity DataIC50: 45nMAssay Description:Inhibition of [3H]CGP-27492 binding to Gamma-aminobutyric acid type B receptor of rat cortexMore data for this Ligand-Target Pair
Affinity DataIC50: 45nMAssay Description:Inhibition of [3H]CGP-27492 binding to Gamma-aminobutyric acid type B receptor of rat cortexMore data for this Ligand-Target Pair
Affinity DataIC50: 60nMAssay Description:Displacement of [3H]baclofen from Gamma-aminobutyric acid type B receptor in rat brain membranesMore data for this Ligand-Target Pair
Affinity DataIC50: 60nMAssay Description:Binding affinity against Gamma-aminobutyric acid type B receptor in rat brain synaptosomes after 30 minutesMore data for this Ligand-Target Pair
Affinity DataIC50: 60nMAssay Description:In vitro displacement of [3H]GABA from Gamma-aminobutyric acid type B receptor sites in rat brain membranesMore data for this Ligand-Target Pair
TargetGamma-aminobutyric acid type B receptor subunit 1/2(Human)
Beijing Institute of Biotechnology
Curated by ChEMBL
Beijing Institute of Biotechnology
Curated by ChEMBL
Affinity DataEC50: 64nMAssay Description:Positive allosteric modulation of GABA-B receptor (unknown origin) assessed as stimulation of [35S]GTPgammaS binding by [35S]GTPgammaS binding assayMore data for this Ligand-Target Pair
Affinity DataIC50: 65nMAssay Description:Inhibition of [3H]CGP-27492 binding to Gamma-aminobutyric acid type B receptor of rat cortexMore data for this Ligand-Target Pair
Affinity DataIC50: 80nMAssay Description:Binding affinity against Gamma-aminobutyric acid type B receptor in rat brain synaptosomes after 30 minutesMore data for this Ligand-Target Pair
Affinity DataIC50: 89nMAssay Description:Inhibition of [3H]CGP-27492 binding to Gamma-aminobutyric acid type B receptor of rat cortexMore data for this Ligand-Target Pair
TargetGamma-aminobutyric acid type B receptor subunit 1/2(Human)
Beijing Institute of Biotechnology
Curated by ChEMBL
Beijing Institute of Biotechnology
Curated by ChEMBL
Affinity DataEC50: 90nMAssay Description:Positive allosteric modulation of GABA-B receptor (unknown origin) assessed as stimulation of [35S]GTPgammaS binding by [35S]GTPgammaS binding assayMore data for this Ligand-Target Pair
TargetGamma-aminobutyric acid type B receptor subunit 1/2(Human)
Beijing Institute of Biotechnology
Curated by ChEMBL
Beijing Institute of Biotechnology
Curated by ChEMBL
Affinity DataEC50: 97nMAssay Description:Positive allosteric modulation of GABA-B receptor (unknown origin) assessed as stimulation of [35S]GTPgammaS binding by [35S]GTPgammaS binding assayMore data for this Ligand-Target Pair
Affinity DataIC50: 107nMAssay Description:Inhibition of [3H]CGP-27492 binding to Gamma-aminobutyric acid type B receptor of rat cortexMore data for this Ligand-Target Pair
Affinity DataIC50: 140nMAssay Description:Displacement of [3H]GABA from Gamma-aminobutyric acid type B receptorMore data for this Ligand-Target Pair
Affinity DataIC50: 140nMAssay Description:Displacement of [3H]GABA from Gamma-aminobutyric acid type B receptorMore data for this Ligand-Target Pair
Affinity DataIC50: 140nMAssay Description:Inhibition of [3H]CGP-27492 binding to Gamma-aminobutyric acid type B receptor of rat cortexMore data for this Ligand-Target Pair
Affinity DataIC50: 140nMAssay Description:Displacement of [3H]GABA from Gamma-aminobutyric acid type B receptorMore data for this Ligand-Target Pair
Affinity DataIC50: 140nMAssay Description:Displacement of [3H]GABA from Gamma-aminobutyric acid type B receptorMore data for this Ligand-Target Pair
TargetGamma-aminobutyric acid type B receptor subunit 1/2(Human)
Beijing Institute of Biotechnology
Curated by ChEMBL
Beijing Institute of Biotechnology
Curated by ChEMBL
Affinity DataEC50: 142nMAssay Description:Positive allosteric modulation of GABA-B receptor (unknown origin) assessed as stimulation of [35S]GTPgammaS binding by [35S]GTPgammaS binding assayMore data for this Ligand-Target Pair



3D Structure (crystal)




























