Compile Data Set for Download or QSAR
Report error Found 2808 Enz. Inhib. hit(s) with Target = 'Gamma-aminobutyric acid receptor subunit alpha-1'
LigandPNGBDBM26263(ethyl 12-fluoro-8-methyl-9-oxo-2,4,8-triazatricycl...)
Affinity DatapH: 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
LigandPNGBDBM26263(ethyl 12-fluoro-8-methyl-9-oxo-2,4,8-triazatricycl...)
Affinity DataT: 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
LigandPNGBDBM26263(ethyl 12-fluoro-8-methyl-9-oxo-2,4,8-triazatricycl...)
Affinity DataT: 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-1/beta-3/gamma-2(Human)
The Royal Danish School of Pharmacy

Curated by ChEMBL
LigandPNGBDBM85712(1H-imidazol-4-ylacetic acid | NSC_96215 | CAS_645-...)
Affinity DataEC50:  3.10E+5nMAssay Description:Effective agonist dose for human Gamma-aminobutyric acid A receptor alpha-1-beta-3-gamma-2 expressed in Xenopus oocytesMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetGamma-aminobutyric acid receptor subunit alpha-1/beta-3/gamma-2(Human)
The Royal Danish School of Pharmacy

Curated by ChEMBL
LigandPNGBDBM50000106(Piperidine-4-carboxylic acid | Piperidine-4-carbox...)
Affinity DataEC50:  6.20E+5nMAssay Description:Effective agonist dose for human Gamma-aminobutyric acid A receptor alpha-1-beta-3-gamma-2 expressed in Xenopus oocytesMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetGamma-aminobutyric acid receptor subunit alpha-1/beta-3/gamma-2(Human)
The Royal Danish School of Pharmacy

Curated by ChEMBL
LigandPNGBDBM50032955(1,2,3,6-Tetrahydro-pyridine-4-carboxylic acid | CH...)
Affinity DataEC50:  1.60E+5nMAssay Description:Effective agonist dose for human Gamma-aminobutyric acid A receptor alpha-1-beta-3-gamma-2 expressed in Xenopus oocytesMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetGamma-aminobutyric acid receptor subunit alpha-1/beta-3/gamma-2(Human)
The Royal Danish School of Pharmacy

Curated by ChEMBL
LigandPNGBDBM50100943(3-Amino-propane-1-selenic acid | CHEMBL41065)
Affinity DataEC50:  1.40E+6nMAssay Description:Effective agonist dose for human Gamma-aminobutyric acid A receptor alpha-1-beta-3-gamma-2 expressed in Xenopus oocytesMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetGamma-aminobutyric acid receptor subunit alpha-1/beta-3/gamma-2(Human)
The Royal Danish School of Pharmacy

Curated by ChEMBL
LigandPNGBDBM50100946(piperidine-4-seleninic acid | Piperidine-4-selenic...)
Affinity DataEC50:  2.00E+5nMAssay Description:Effective agonist dose for human Gamma-aminobutyric acid A receptor alpha-1-beta-3-gamma-2 expressed in Xenopus oocytesMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetGamma-aminobutyric acid receptor subunit alpha-1/beta-3/gamma-2(Human)
The Royal Danish School of Pharmacy

Curated by ChEMBL
LigandPNGBDBM50087272(CHEMBL34155 | P4S | Piperidine-4-sulfonic acid | P...)
Affinity DataEC50:  4.00E+4nMAssay Description:Effective agonist dose for human Gamma-aminobutyric acid A receptor alpha-1-beta-3-gamma-2 expressed in Xenopus oocytesMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetGamma-aminobutyric acid receptor subunit alpha-1/beta-3/gamma-2(Human)
The Royal Danish School of Pharmacy

Curated by ChEMBL
LigandPNGBDBM24183(4-amino-n-[2,3-3H]butyric acid | cid_119 | Gamma-A...)
Affinity DataEC50:  8.00E+4nMAssay Description:Effective agonist dose for human Gamma-aminobutyric acid A receptor alpha-1-beta-3-gamma-2 expressed in Xenopus oocytesMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetGamma-aminobutyric acid receptor subunit alpha-1/beta-3/gamma-2(Human)
The Royal Danish School of Pharmacy

Curated by ChEMBL
LigandPNGBDBM50100944(Piperidin-4-yl-phosphinic acid | CHEMBL291079)
Affinity DataEC50:  2.70E+5nMAssay Description:Effective agonist dose for human Gamma-aminobutyric acid A receptor alpha-1-beta-3-gamma-2 expressed in Xenopus oocytesMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
LigandPNGBDBM50454517(CHEMBL3137984)
Affinity DataEC50: >5.00E+4nMAssay Description:Potentiation of GABA-activated currents in Xenopus oocytes expressing cloned human alpha-1-beta-2-gamma-2L subunits of GABA-A receptorMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/4/2012
Entry Details Article
PubMed
LigandPNGBDBM50454499(CHEMBL3137990)
Affinity DataEC50:  390nMAssay Description:Potentiation of GABA-activated currents in Xenopus oocytes expressing cloned human alpha-1-beta-2-gamma-2L subunits of GABA-A receptorMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/4/2012
Entry Details Article
PubMed
LigandPNGBDBM50055963(1-[(3R,5R,10S,13S,17S)-3-(4-Acetyl-phenylethynyl)-...)
Affinity DataEC50:  6.60nMAssay Description:Steroid potentiation of 5% GABA responses in Xenopus oocytes expressing human alpha-1-beta-2-gamma-2L subunits of GABA-A receptorMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
LigandPNGBDBM50454526(CHEMBL3138293)
Affinity DataEC50:  31nMAssay Description:Steroid potentiation of 5% GABA responses in Xenopus oocytes expressing human alpha-1-beta-2-gamma-2L subunits of GABA-A receptorMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
LigandPNGBDBM50454529(CHEMBL3138315)
Affinity DataEC50: >1.00E+3nMAssay Description:Steroid potentiation of 5% GABA responses in Xenopus oocytes expressing human alpha-1-beta-2-gamma-2L subunits of GABA-A receptorMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
LigandPNGBDBM50055953(1-[(3R,5R,10S,13S,17S)-3-Hydroxy-3-(2-hydroxy-phen...)
Affinity DataEC50:  340nMAssay Description:Steroid potentiation of 5% GABA responses in Xenopus oocytes expressing human alpha-1-beta-2-gamma-2L subunits of GABA-A receptorMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
LigandPNGBDBM50454528(CHEMBL3138292)
Affinity DataEC50: >1.00E+3nMAssay Description:Steroid potentiation of 5% GABA responses in Xenopus oocytes expressing human alpha-1-beta-2-gamma-2L subunits of GABA-A receptorMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
LigandPNGBDBM50454527(CHEMBL3138291)
Affinity DataEC50:  18nMAssay Description:Steroid potentiation of 5% GABA responses in Xenopus oocytes expressing human alpha-1-beta-2-gamma-2L subunits of GABA-A receptorMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
LigandPNGBDBM50454531(CHEMBL3138433)
Affinity DataEC50:  8.20nMAssay Description:Steroid potentiation of 5% GABA responses in Xenopus oocytes expressing human alpha-1-beta-2-gamma-2L subunits of GABA-A receptorMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
LigandPNGBDBM50215531(2-chloro-alpha-[[(4-chlorophenyl)amino]methylene]-...)
Affinity DataEC50:  34nMAssay Description:Activity at human GABAA alpha-1-beta-2-gamma-2L expressed in Xenopus oocytes assessed as potentiation of GABA currentsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
LigandPNGBDBM24183(4-amino-n-[2,3-3H]butyric acid | cid_119 | Gamma-A...)
Affinity DataEC50:  4.30E+4nMAssay Description:Agonist activity at GABA alpha-1-beta-2-gamma-2 receptor expressed in HEK293 cells by Whole-cell patch-clamp techniqueMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMedPDB3D3D Structure (crystal)
LigandPNGBDBM50218536(4(5)-(carboxymethyl)-5(4)-methylimidazole | CHEMBL...)
Affinity DataEC50: >1.00E+6nMAssay Description:Agonist activity at GABA alpha-1-beta-2-gamma-2 receptor expressed in HEK293 cells by Whole-cell patch-clamp techniqueMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
LigandPNGBDBM85712(1H-imidazol-4-ylacetic acid | NSC_96215 | CAS_645-...)
Affinity DataEC50:  1.38E+5nMAssay Description:Agonist activity at GABA alpha-1-beta-2-gamma-2 receptor expressed in HEK293 cells by Whole-cell patch-clamp techniqueMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
LigandPNGBDBM50125935(CHEMBL681 | R(+)-etomidate | Amidate | (R)-1-(1-ph...)
Affinity DataEC50:  1.20E+3nMAssay Description:Ability to enhance currents from alpha-1-beta-2-gamma-2L-subunit of GABA receptor elicited by low concentrations of GABAMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/30/2012
Entry Details Article
PubMedPDB3D3D Structure (crystal)
LigandPNGBDBM50125936(3-((R)-1-Phenyl-ethyl)-3H-imidazole-4-carboxylic a...)
Affinity DataEC50:  3.70E+4nMAssay Description:Direct activation of Gamma-aminobutyric acid A receptor in the absence of GABAMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/30/2012
Entry Details Article
PubMed
LigandPNGBDBM50125939(3-((S)-1-Phenyl-ethyl)-3H-imidazole-4-carboxylic a...)
Affinity DataEC50:  2.00E+4nMAssay Description:Enhancement of currents elicited by GABA at EC5 (6-12 uM)More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/30/2012
Entry Details Article
PubMed
LigandPNGBDBM50125935(CHEMBL681 | R(+)-etomidate | Amidate | (R)-1-(1-ph...)
Affinity DataEC50:  6.40E+4nMAssay Description:Direct activation of Gamma-aminobutyric acid A receptor in the absence of GABAMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/30/2012
Entry Details Article
PubMedPDB3D3D Structure (crystal)
LigandPNGBDBM50125936(3-((R)-1-Phenyl-ethyl)-3H-imidazole-4-carboxylic a...)
Affinity DataEC50:  2.00E+3nMAssay Description:Enhancement of currents elicited by GABA at EC5 (6-12 uM)More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/30/2012
Entry Details Article
PubMed
LigandPNGBDBM50125937(CHEMBL279678 | 3-((S)-1-Phenyl-ethyl)-3H-imidazole...)
Affinity DataEC50:  4.70E+4nMAssay Description:Enhancement of currents elicited by GABA at EC5 (6-12 uM)More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/30/2012
Entry Details Article
PubMed
LigandPNGBDBM50125935(CHEMBL681 | R(+)-etomidate | Amidate | (R)-1-(1-ph...)
Affinity DataEC50:  2.50E+3nMAssay Description:Enhancement of currents elicited by GABA at EC5 (6-12 uM)More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/30/2012
Entry Details Article
PubMedPDB3D3D Structure (crystal)
LigandPNGBDBM50125936(3-((R)-1-Phenyl-ethyl)-3H-imidazole-4-carboxylic a...)
Affinity DataEC50:  1.20E+3nMAssay Description:Ability to enhance currents from alpha-1-beta-2-gamma-2L-subunit of GABA receptor elicited by low concentrations of GABAMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/30/2012
Entry Details Article
PubMed
LigandPNGBDBM50120772(2-(2-Fluoro-phenyl)-8-propionyl-6,7,8,9-tetrahydro...)
Affinity DataEC50:  95nMAssay Description:Effective concentration against gamma-aminobutyric acid (GABA) A receptor, alpha 1More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
LigandPNGBDBM50120771(8-Benzyl-2-(2-thiophen-2-yl-phenyl)-6,7,8,9-tetrah...)
Affinity DataEC50:  208nMAssay Description:Effective concentration against gamma-aminobutyric acid (GABA) A receptor, alpha 1More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
LigandPNGBDBM50120786(8-Benzyl-2-(3-methoxy-phenyl)-6,7,8,9-tetrahydro-5...)
Affinity DataEC50:  81nMAssay Description:Effective concentration against gamma-aminobutyric acid (GABA) A receptor, alpha 1More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
LigandPNGBDBM50120789(8-Benzyl-2-(4-fluoro-phenyl)-6,7,8,9-tetrahydro-5H...)
Affinity DataEC50:  136nMAssay Description:Effective concentration against gamma-aminobutyric acid (GABA) A receptor, alpha 1More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
LigandPNGBDBM50120790(8-Benzyl-2-(2,5-difluoro-phenyl)-6,7,8,9-tetrahydr...)
Affinity DataEC50:  36nMAssay Description:Effective concentration against gamma-aminobutyric acid (GABA) A receptor, alpha 1More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
LigandPNGBDBM50120777(8-(3-Fluoro-benzoyl)-2-(2-fluoro-phenyl)-6,7,8,9-t...)
Affinity DataEC50:  69nMAssay Description:Effective concentration against gamma-aminobutyric acid (GABA) A receptor, alpha 1More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
LigandPNGBDBM50120776(8-Benzyl-2-(2,4-difluoro-phenyl)-6,7,8,9-tetrahydr...)
Affinity DataEC50:  92nMAssay Description:Effective concentration against gamma-aminobutyric acid (GABA) A receptor, alpha 1More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
LigandPNGBDBM50120795(2-(2-Fluoro-phenyl)-8-(2-methyl-benzoyl)-6,7,8,9-t...)
Affinity DataEC50:  544nMAssay Description:Effective concentration against gamma-aminobutyric acid (GABA) A receptor, alpha 1More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
LigandPNGBDBM50120779(8-(4-Fluoro-benzoyl)-2-(2-fluoro-phenyl)-6,7,8,9-t...)
Affinity DataEC50:  41nMAssay Description:Effective concentration against gamma-aminobutyric acid (GABA) A receptor, alpha 1More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
LigandPNGBDBM50120805(2-(2-Fluoro-phenyl)-8-propenyl-6,7,8,9-tetrahydro-...)
Affinity DataEC50:  170nMAssay Description:Effective concentration against gamma-aminobutyric acid (GABA) A receptor, alpha 1More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
LigandPNGBDBM50120781(8-Benzyl-2-(3-fluoro-phenyl)-6,7,8,9-tetrahydro-5H...)
Affinity DataEC50:  120nMAssay Description:Effective concentration against gamma-aminobutyric acid (GABA) A receptor, alpha 1More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
LigandPNGBDBM50001728(CHEMBL661 | 8-chloro-1-methyl-6-phenyl-4H-[1,2,4]t...)
Affinity DataEC50:  37nMAssay Description:Effective concentration against gamma-aminobutyric acid (GABA) A receptor, alpha 1More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
LigandPNGBDBM50120774(2-(2-Fluoro-phenyl)-8-(4-methoxy-benzoyl)-6,7,8,9-...)
Affinity DataEC50:  2.20E+3nMAssay Description:Effective concentration against gamma-aminobutyric acid (GABA) A receptor, alpha 1More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
LigandPNGBDBM50120788(8-Butyl-2-(2-fluoro-phenyl)-6,7,8,9-tetrahydro-5H-...)
Affinity DataEC50:  258nMAssay Description:Effective concentration against gamma-aminobutyric acid (GABA) A receptor, alpha 1More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
LigandPNGBDBM50120783(8-Benzyl-2-(2-fluoro-phenyl)-6,7,8,9-tetrahydro-5H...)
Affinity DataEC50:  18nMAssay Description:Effective concentration against gamma-aminobutyric acid (GABA) A receptor, alpha 1More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
LigandPNGBDBM50120794(2-(2-Fluoro-phenyl)-8-thiophen-2-ylmethyl-6,7,8,9-...)
Affinity DataEC50:  107nMAssay Description:Effective concentration against gamma-aminobutyric acid (GABA) A receptor, alpha 1More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
LigandPNGBDBM50120773(8-(2-Fluoro-benzoyl)-2-(2-fluoro-phenyl)-6,7,8,9-t...)
Affinity DataEC50:  93nMAssay Description:Effective concentration against gamma-aminobutyric acid (GABA) A receptor, alpha 1More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
LigandPNGBDBM50120793(8-Cyclopropylmethyl-2-(2-fluoro-phenyl)-6,7,8,9-te...)
Affinity DataEC50:  135nMAssay Description:Effective concentration against gamma-aminobutyric acid (GABA) A receptor, alpha 1More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
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