Compile Data Set for Download or QSAR
Report error Found 137 Enz. Inhib. hit(s) with Target = 'Gamma-aminobutyric acid receptor subunit alpha-4'
LigandPNGBDBM50244261(5-Methyl-6-oxo-8-trimethylsilanylethynyl-3a,4,5,6-...)
Affinity DataKi:  2.61nMAssay Description:Binding affinity to GABAA alpha-4-beta-3-gamma-2 receptorMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/17/2012
Entry Details Article
PubMed
LigandPNGBDBM26267(RO-154513 | Ro15-4513 | ethyl 12-azido-8-methyl-9-...)
Affinity DataKi:  2.62nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/21/2012
Entry Details Article
PubMed
LigandPNGBDBM26267(RO-154513 | Ro15-4513 | ethyl 12-azido-8-methyl-9-...)
Affinity DataKi:  3.10nM ΔG°:  -48.1kJ/molepH: 7.4 T: 2°CAssay Description:Membrane homogenates were incubated at room temperature with a sub-Kd concentration of radioligand in the absence or presence of seven different conc...More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/4/2009
Entry Details Article
PubMed
TargetGamma-aminobutyric acid receptor subunit alpha-4(Rat)
National Institute of Diabetes, Digestive and Kidney Diseases

Curated by PDSP Ki Database
LigandPNGBDBM26267(RO-154513 | Ro15-4513 | ethyl 12-azido-8-methyl-9-...)
Affinity DataKi:  3.40nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/24/2012
Entry Details Article
PubMed
LigandPNGBDBM84956(2-(4-Methoxy-phenyl)-2,5-dihydro-pyrazolo[4,3-c]qu...)
In Depth
Date in BDB:
2/23/2012
Entry Details Article
PubMed
TargetGamma-aminobutyric acid receptor subunit alpha-4(Rat)
National Institute of Diabetes, Digestive and Kidney Diseases

Curated by PDSP Ki Database
LigandPNGBDBM50044941(CHEMBL6421 | ZG 234 | 8-Azido-5-methyl-6-oxo-5,6-d...)
Affinity DataKi:  5.20nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/24/2012
Entry Details Article
PubMed
LigandPNGBDBM25877(CHEMBL286594 | ethyl 12-ethynyl-8-methyl-9-oxo-2,4...)
Affinity DataKi:  5.30nMAssay Description:The affinity of compounds for human recombinant GABA (A) receptors was measured by competition binding using [3H]flunitrazepam. Assays were carried o...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/5/2008
Entry Details Article
PubMed
LigandPNGBDBM26267(RO-154513 | Ro15-4513 | ethyl 12-azido-8-methyl-9-...)
Affinity DataKi:  5.5nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/23/2012
Entry Details Article
PubMed
TargetGamma-aminobutyric acid receptor subunit alpha-4(Rat)
National Institute of Diabetes, Digestive and Kidney Diseases

Curated by PDSP Ki Database
LigandPNGBDBM50034835(Ro-19-4603 | CHEMBL269366 | Ro 19-4603 | 5-Methyl-...)
In Depth
Date in BDB:
2/24/2012
Entry Details Article
PubMed
LigandPNGBDBM84956(2-(4-Methoxy-phenyl)-2,5-dihydro-pyrazolo[4,3-c]qu...)
Affinity DataKi:  6.80nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/21/2012
Entry Details Article
PubMed
TargetGamma-aminobutyric acid receptor subunit alpha-4(Rat)
National Institute of Diabetes, Digestive and Kidney Diseases

Curated by PDSP Ki Database
LigandPNGBDBM84956(2-(4-Methoxy-phenyl)-2,5-dihydro-pyrazolo[4,3-c]qu...)
Affinity DataKi:  6.80nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/24/2012
Entry Details Article
PubMed
TargetGamma-aminobutyric acid receptor subunit alpha-4(Rat)
National Institute of Diabetes, Digestive and Kidney Diseases

Curated by PDSP Ki Database
LigandPNGBDBM50017009(CHEMBL19732 | 2-Phenyl-2,5-dihydro-pyrazolo[4,3-c]...)
In Depth
Date in BDB:
2/24/2012
Entry Details Article
PubMed
TargetGamma-aminobutyric acid receptor subunit alpha-4(Rat)
National Institute of Diabetes, Digestive and Kidney Diseases

Curated by PDSP Ki Database
LigandPNGBDBM50034816(CHEMBL415293 | ZG 63 | 8-Chloro-5-methyl-6-oxo-5,6...)
Affinity DataKi:  9.5nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/24/2012
Entry Details Article
PubMed
TargetGamma-aminobutyric acid receptor subunit alpha-4(Rat)
National Institute of Diabetes, Digestive and Kidney Diseases

Curated by PDSP Ki Database
LigandPNGBDBM50049739(DM 286 | CHEMBL58570 | 8-Ethyl-5-methyl-6-oxo-5,6-...)
Affinity DataKi:  10nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/24/2012
Entry Details Article
PubMed
LigandPNGBDBM26267(RO-154513 | Ro15-4513 | ethyl 12-azido-8-methyl-9-...)
Affinity DataKi:  10.5nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/23/2012
Entry Details Article
PubMed
LigandPNGBDBM81951(NSC_104999 | CAS_104999 | DMCM)
Affinity DataKi:  11.3nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/23/2012
Entry Details Article
PubMed
TargetGamma-aminobutyric acid receptor subunit alpha-4(Rat)
National Institute of Diabetes, Digestive and Kidney Diseases

Curated by PDSP Ki Database
LigandPNGBDBM85038(CHEMBL43948 | PZII-029)
Affinity DataKi:  11.6nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/24/2012
Entry Details Article
PubMed
LigandPNGBDBM50017009(CHEMBL19732 | 2-Phenyl-2,5-dihydro-pyrazolo[4,3-c]...)
Affinity DataKi:  11.9nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/23/2012
Entry Details Article
PubMed
TargetGamma-aminobutyric acid receptor subunit alpha-4(Rat)
National Institute of Diabetes, Digestive and Kidney Diseases

Curated by PDSP Ki Database
LigandPNGBDBM235902(US9365502, MQ-87)
Affinity DataIC50: 14nMAssay Description:The IC50 values for non-competitive displacers of [35S]-TBPS from the picrotoxin binding site on GABAA receptors.More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/3/2017
Entry Details
US Patent

LigandPNGBDBM81951(NSC_104999 | CAS_104999 | DMCM)
Affinity DataKi:  14.1nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/21/2012
Entry Details Article
PubMed
LigandPNGBDBM81951(NSC_104999 | CAS_104999 | DMCM)
Affinity DataKi:  20nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/23/2012
Entry Details Article
PubMed
LigandPNGBDBM84993(CGS-20625 | 5,6,7,8,9,10-Hexahydro-2-(4-methoxyphe...)
Affinity DataKi:  22.4nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/23/2012
Entry Details Article
PubMed
LigandPNGBDBM50017320(8-Bromo-7-oxo-3b,4,5,6-tetrahydro-7H-2,6a,11b-tria...)
Affinity DataKi:  22.5nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/23/2012
Entry Details Article
PubMed
TargetGamma-aminobutyric acid receptor subunit alpha-4(Rat)
National Institute of Diabetes, Digestive and Kidney Diseases

Curated by PDSP Ki Database
LigandPNGBDBM85042(CHEMBL44613 | PW-007A)
Affinity DataKi:  22.5nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/24/2012
Entry Details Article
PubMed
LigandPNGBDBM50142570(9-(4-Methyl-thiazol-2-yl)-11-pyridin-4-yl-6,7-dihy...)
Affinity DataKi:  28nMAssay Description:Displacement of [3H]Ro-151788 from human GABA-A receptor alpha4 subunit expressed in L(tk) cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetGamma-aminobutyric acid receptor subunit alpha-4(Rat)
National Institute of Diabetes, Digestive and Kidney Diseases

Curated by PDSP Ki Database
LigandPNGBDBM235905(US9365502, MQ-85)
Affinity DataIC50: 29nMAssay Description:The IC50 values for non-competitive displacers of [35S]-TBPS from the picrotoxin binding site on GABAA receptors.More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/3/2017
Entry Details
US Patent

LigandPNGBDBM84957(CHEMBL20042 | CGS 9896)
Affinity DataKi:  35.6nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/21/2012
Entry Details Article
PubMed
LigandPNGBDBM50017320(8-Bromo-7-oxo-3b,4,5,6-tetrahydro-7H-2,6a,11b-tria...)
Affinity DataKi:  36nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/23/2012
Entry Details Article
PubMed
TargetGamma-aminobutyric acid receptor subunit alpha-4(Rat)
National Institute of Diabetes, Digestive and Kidney Diseases

Curated by PDSP Ki Database
LigandPNGBDBM81951(NSC_104999 | CAS_104999 | DMCM)
Affinity DataKi:  38.5nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/24/2012
Entry Details Article
PubMed
TargetGamma-aminobutyric acid receptor subunit alpha-4(Rat)
National Institute of Diabetes, Digestive and Kidney Diseases

Curated by PDSP Ki Database
LigandPNGBDBM235901(US9365502, MQ-86)
Affinity DataIC50: 43nMAssay Description:The IC50 values for non-competitive displacers of [35S]-TBPS from the picrotoxin binding site on GABAA receptors.More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/3/2017
Entry Details
US Patent

TargetGamma-aminobutyric acid receptor subunit alpha-4(Rat)
National Institute of Diabetes, Digestive and Kidney Diseases

Curated by PDSP Ki Database
LigandPNGBDBM235900(US9365502, MQ-37)
Affinity DataIC50: 46nMAssay Description:The IC50 values for non-competitive displacers of [35S]-TBPS from the picrotoxin binding site on GABAA receptors.More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/3/2017
Entry Details
US Patent

TargetGamma-aminobutyric acid receptor subunit alpha-4(Rat)
National Institute of Diabetes, Digestive and Kidney Diseases

Curated by PDSP Ki Database
LigandPNGBDBM235898(US9365502, MQ-38)
Affinity DataIC50: 52nMAssay Description:The IC50 values for non-competitive displacers of [35S]-TBPS from the picrotoxin binding site on GABAA receptors.More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/3/2017
Entry Details
US Patent

LigandPNGBDBM50017320(8-Bromo-7-oxo-3b,4,5,6-tetrahydro-7H-2,6a,11b-tria...)
Affinity DataKi:  53.5nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/21/2012
Entry Details Article
PubMed
LigandPNGBDBM84957(CHEMBL20042 | CGS 9896)
Affinity DataKi:  59nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/23/2012
Entry Details Article
PubMed
TargetGamma-aminobutyric acid receptor subunit alpha-4/beta-1/delta(Human)
University of Copenhagen

Curated by ChEMBL
LigandPNGBDBM50587079(CHEMBL5072077)
Affinity DataEC50:  60nMAssay Description:Positive allosteric modulation of human recombinant alpha4beta1delta GABAA receptor expressed in delta-HEK cells assessed as potentiation of GABA-ind...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/7/2023
Entry Details Article
PubMed
TargetGamma-aminobutyric acid receptor subunit alpha-4/beta-3(Rat)
Johannes Gutenberg University Mainz

Curated by ChEMBL
LigandPNGBDBM50457439(CHEMBL4213357)
Affinity DataEC50:  60nMAssay Description:Modulation of rat eGFP-fused GABA-A receptor alpha4beta3 expressed in HEK293 cells in presence of GABA by patch-clamp assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/16/2020
Entry Details Article
PubMed
TargetGamma-aminobutyric acid receptor subunit alpha-4(Rat)
National Institute of Diabetes, Digestive and Kidney Diseases

Curated by PDSP Ki Database
LigandPNGBDBM235894(US9365502, MQ-31)
Affinity DataIC50: 61nMAssay Description:The IC50 values for non-competitive displacers of [35S]-TBPS from the picrotoxin binding site on GABAA receptors.More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/3/2017
Entry Details
US Patent

TargetGamma-aminobutyric acid receptor subunit alpha-4(Rat)
National Institute of Diabetes, Digestive and Kidney Diseases

Curated by PDSP Ki Database
LigandPNGBDBM235897(US9365502, MQ-33)
Affinity DataIC50: 62nMAssay Description:The IC50 values for non-competitive displacers of [35S]-TBPS from the picrotoxin binding site on GABAA receptors.More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/3/2017
Entry Details
US Patent

TargetGamma-aminobutyric acid receptor subunit alpha-4(Rat)
National Institute of Diabetes, Digestive and Kidney Diseases

Curated by PDSP Ki Database
LigandPNGBDBM235907(US9365502, MQ-39)
Affinity DataIC50: 65nMAssay Description:The IC50 values for non-competitive displacers of [35S]-TBPS from the picrotoxin binding site on GABAA receptors.More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/3/2017
Entry Details
US Patent

LigandPNGBDBM50191342(3alpha-hydroxy-5alpha-pregnan-20-one | CHEMBL20753...)
Affinity DataEC50:  76nMAssay Description:Positive allosteric modulation of GABAA receptor alpha4beta3delta (unknown origin) expressed in CHO cells assessed as potentiation of GABA-mediated i...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/25/2019
Entry Details Article
PubMedPDB3D3D Structure (crystal)
LigandPNGBDBM84993(CGS-20625 | 5,6,7,8,9,10-Hexahydro-2-(4-methoxyphe...)
Affinity DataKi:  77nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/23/2012
Entry Details Article
PubMed
TargetGamma-aminobutyric acid receptor subunit alpha-4/beta-1/delta(Human)
University of Copenhagen

Curated by ChEMBL
LigandPNGBDBM50588336(CHEMBL5186739)
Affinity DataKi:  88nMAssay Description:Antagonist activity at recombinant human alpha4beta1delta GABAA receptor expressed in HEK293 Flp-In cells by FMP assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/18/2023
Entry Details
PubMed
LigandPNGBDBM50258254(CHEMBL4073780)
Affinity DataEC50:  110nMAssay Description:Positive allosteric modulation of GABAA receptor alpha4beta3delta (unknown origin) expressed in CHO cells assessed as potentiation of GABA-mediated i...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/25/2019
Entry Details Article
PubMed
LigandPNGBDBM26263(ethyl 12-fluoro-8-methyl-9-oxo-2,4,8-triazatricycl...)
Affinity DataKi:  114nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/23/2012
Entry Details Article
PubMed
TargetGamma-aminobutyric acid receptor subunit alpha-4(Rat)
National Institute of Diabetes, Digestive and Kidney Diseases

Curated by PDSP Ki Database
LigandPNGBDBM26263(ethyl 12-fluoro-8-methyl-9-oxo-2,4,8-triazatricycl...)
Affinity DataKi:  118nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/24/2012
Entry Details Article
PubMed
TargetGamma-aminobutyric acid receptor subunit alpha-4/beta-1/delta(Human)
University of Copenhagen

Curated by ChEMBL
LigandPNGBDBM50587078(CHEMBL5088746)
Affinity DataEC50:  140nMAssay Description:Positive allosteric modulation of human recombinant alpha4beta1delta GABAA receptor expressed in delta-HEK cells assessed as potentiation of GABA-ind...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/7/2023
Entry Details Article
PubMed
TargetGamma-aminobutyric acid receptor subunit alpha-4(Rat)
National Institute of Diabetes, Digestive and Kidney Diseases

Curated by PDSP Ki Database
LigandPNGBDBM235896(US9365502, MQ-32)
Affinity DataIC50: 147nMAssay Description:The IC50 values for non-competitive displacers of [35S]-TBPS from the picrotoxin binding site on GABAA receptors.More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/3/2017
Entry Details
US Patent

TargetGamma-aminobutyric acid receptor subunit alpha-4/beta-3/delta(Rat)
Johannes Gutenberg University Mainz

Curated by ChEMBL
LigandPNGBDBM50457439(CHEMBL4213357)
Affinity DataEC50:  150nMAssay Description:Modulation of rat eGFP-fused GABA-A receptor alpha4beta3delta expressed in HEK293 cells in presence of GABA by patch-clamp assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/16/2020
Entry Details Article
PubMed
TargetGamma-aminobutyric acid receptor subunit alpha-4/beta-1/delta(Human)
University of Copenhagen

Curated by ChEMBL
LigandPNGBDBM50587075(CHEMBL5081682)
Affinity DataEC50:  160nMAssay Description:Positive allosteric modulation of human recombinant alpha4beta1delta GABAA receptor expressed in delta-HEK cells assessed as potentiation of GABA-ind...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/7/2023
Entry Details Article
PubMed
LigandPNGBDBM50258216(CHEMBL4105630)
Affinity DataEC50:  163nMAssay Description:Positive allosteric modulation of GABAA receptor alpha4beta2delta (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/16/2020
Entry Details Article
PubMed
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