Compile Data Set for Download or QSAR
Report error Found 37 Enz. Inhib. hit(s) for PDB: 6X3T
TargetGamma-aminobutyric acid receptor subunit alpha-1(Human)
Merck Sharp and Dohme Research Laboratories

Curated by PDSP Ki Database
LigandPNGBDBM24183(4-amino-n-[2,3-3H]butyric acid | cid_119 | Gamma-A...)
Affinity DataKi:  21.4nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/1/2012
Entry Details
PubMedPDB3D3D Structure (crystal)
LigandPNGBDBM24183(4-amino-n-[2,3-3H]butyric acid | cid_119 | Gamma-A...)
Affinity DataIC50: 22nMAssay Description:Inhibitory effect was measured for [3H]GABA-uptake from rat synaptosomal membraneMore 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-2(Human)
Merck Sharp and Dohme Research Laboratories

Curated by PDSP Ki Database
LigandPNGBDBM24183(4-amino-n-[2,3-3H]butyric acid | cid_119 | Gamma-A...)
Affinity DataKi:  22.9nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/1/2012
Entry Details
PubMedPDB3D3D Structure (crystal)
TargetGamma-aminobutyric acid receptor subunit alpha-1(Human)
Merck Sharp and Dohme Research Laboratories

Curated by PDSP Ki Database
LigandPNGBDBM24183(4-amino-n-[2,3-3H]butyric acid | cid_119 | Gamma-A...)
Affinity DataKi:  57.5nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/1/2012
Entry Details
PubMedPDB3D3D Structure (crystal)
TargetGamma-aminobutyric acid receptor subunit alpha-1(Human)
Merck Sharp and Dohme Research Laboratories

Curated by PDSP Ki Database
LigandPNGBDBM24183(4-amino-n-[2,3-3H]butyric acid | cid_119 | Gamma-A...)
Affinity DataKi:  77.6nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/1/2012
Entry Details
PubMedPDB3D3D Structure (crystal)
TargetGamma-aminobutyric acid receptor subunit alpha-5/beta-2/gamma-2(Human)
University of Copenhagen

Curated by ChEMBL
LigandPNGBDBM24183(4-amino-n-[2,3-3H]butyric acid | cid_119 | Gamma-A...)
Affinity DataEC50:  230nMAssay Description:Agonist activity at recombinant human GABA-A alpha5beta2gamma2S receptor transiently expressed in human tsA201 cells incubated for 30 mins and measur...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/24/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetGamma-aminobutyric acid receptor subunit alpha-5/beta-2/gamma-2(Human)
University of Copenhagen

Curated by ChEMBL
LigandPNGBDBM24183(4-amino-n-[2,3-3H]butyric acid | cid_119 | Gamma-A...)
Affinity DataEC50:  234nMAssay Description:Agonist activity at recombinant human GABA-A alpha5beta2gamma2S receptor transiently expressed in human tsA201 cells incubated for 30 mins and measur...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/24/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetGamma-aminobutyric acid receptor subunit alpha-2/beta-2/gamma-2(Human)
University of Copenhagen

Curated by ChEMBL
LigandPNGBDBM24183(4-amino-n-[2,3-3H]butyric acid | cid_119 | Gamma-A...)
Affinity DataEC50:  650nMAssay Description:Agonist activity at human GABAAalpha2beta2gamma2S receptor expressed in tsA-201cells by FLIPR membrane potential blue assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/27/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetGamma-aminobutyric acid receptor subunit alpha-2/beta-2/gamma-2(Human)
University of Copenhagen

Curated by ChEMBL
LigandPNGBDBM24183(4-amino-n-[2,3-3H]butyric acid | cid_119 | Gamma-A...)
Affinity DataEC50:  661nMAssay Description:Agonist activity at human GABAAalpha2beta2gamma2S receptor expressed in tsA-201cells by FLIPR membrane potential blue assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/27/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetGamma-aminobutyric acid receptor subunit alpha-3/beta-2/gamma-2(Human)
University of Copenhagen

Curated by ChEMBL
LigandPNGBDBM24183(4-amino-n-[2,3-3H]butyric acid | cid_119 | Gamma-A...)
Affinity DataEC50:  912nMAssay Description:Agonist activity at human GABAAalpha3beta2gamma2S receptor expressed in tsA-201cells by FLIPR membrane potential blue assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/27/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetGamma-aminobutyric acid receptor subunit alpha-3/beta-2/gamma-2(Human)
University of Copenhagen

Curated by ChEMBL
LigandPNGBDBM24183(4-amino-n-[2,3-3H]butyric acid | cid_119 | Gamma-A...)
Affinity DataEC50:  920nMAssay Description:Agonist activity at human GABAAalpha3beta2gamma2S receptor expressed in tsA-201cells by FLIPR membrane potential blue assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/27/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetGamma-aminobutyric acid receptor subunit alpha-6/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:  1.50E+3nMAssay Description:Effective agonist dose for human Gamma-aminobutyric acid A receptor alpha-6-beta-3-gamma-2More 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-2/gamma-2(Human)
University of Copenhagen

Curated by ChEMBL
LigandPNGBDBM24183(4-amino-n-[2,3-3H]butyric acid | cid_119 | Gamma-A...)
Affinity DataEC50:  1.78E+3nMAssay Description:Agonist activity at human GABAAalpha1beta2gamma2S receptor expressed in tsA-201cells by FLIPR membrane potential blue assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/27/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetGamma-aminobutyric acid receptor subunit alpha-1/beta-2/gamma-2(Human)
University of Copenhagen

Curated by ChEMBL
LigandPNGBDBM24183(4-amino-n-[2,3-3H]butyric acid | cid_119 | Gamma-A...)
Affinity DataEC50:  1.80E+3nMAssay Description:Agonist activity at human GABAAalpha1beta2gamma2S receptor expressed in tsA-201cells by FLIPR membrane potential blue assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/27/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetGamma-aminobutyric acid receptor subunit alpha-1/beta-2/gamma-2(Human)
University of Copenhagen

Curated by ChEMBL
LigandPNGBDBM50058046(propofol | CHEMBL526)
Affinity DataEC50:  2.00E+3nMAssay Description:Potentiation of GABA responses at human Gamma-aminobutyric acid A receptor alpha-1-beta-2-gamma-2More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/20/2013
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetGABA-A receptor; alpha-5/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:  3.00E+3nMAssay Description:Effective agonist dose for human Gamma-aminobutyric acid A receptor alpha-5-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-4/beta-2/gamma-2(Human)
University of Copenhagen

Curated by ChEMBL
LigandPNGBDBM24183(4-amino-n-[2,3-3H]butyric acid | cid_119 | Gamma-A...)
Affinity DataEC50:  3.70E+3nMAssay Description:Agonist activity at recombinant human GABA-A alpha4beta2gamma2S receptor transiently expressed in human tsA201 cells incubated for 30 mins and measur...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/24/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetGamma-aminobutyric acid receptor subunit alpha-1/beta-2/gamma-2(Human)
University of Copenhagen

Curated by ChEMBL
LigandPNGBDBM24183(4-amino-n-[2,3-3H]butyric acid | cid_119 | Gamma-A...)
Affinity DataEC50:  3.70E+3nMAssay Description:Agonist activity at recombinant human GABA-A alpha1beta2gamma2S receptor transiently expressed in human tsA201 cells incubated for 30 mins and measur...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/24/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetGamma-aminobutyric acid receptor subunit alpha-4/beta-2/gamma-2(Human)
University of Copenhagen

Curated by ChEMBL
LigandPNGBDBM24183(4-amino-n-[2,3-3H]butyric acid | cid_119 | Gamma-A...)
Affinity DataEC50:  3.72E+3nMAssay Description:Agonist activity at recombinant human GABA-A alpha4beta2gamma2S receptor transiently expressed in human tsA201 cells incubated for 30 mins and measur...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/24/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetGamma-aminobutyric acid receptor subunit alpha-1/beta-2/gamma-2(Human)
University of Copenhagen

Curated by ChEMBL
LigandPNGBDBM24183(4-amino-n-[2,3-3H]butyric acid | cid_119 | Gamma-A...)
Affinity DataEC50:  3.80E+3nMAssay Description:Agonist activity at recombinant human GABA-A alpha1beta2gamma2S receptor transiently expressed in human tsA201 cells incubated for 30 mins and measur...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/24/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetGamma-aminobutyric acid receptor subunit alpha-1/beta-3/gamma-2(Human)
Organon Research and Development Group

Curated by ChEMBL
LigandPNGBDBM50058046(propofol | CHEMBL526)
Affinity DataEC50:  4.10E+3nMAssay Description:GABA-modulatory action compound was evaluated on Oocytes expressing recombinant human alpha-1-beta-3-gamma-2L GABA A receptor at concentrations of >=...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/25/2012
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetGamma-aminobutyric acid receptor subunit alpha-1/beta-3/gamma-2(Human)
Organon Research and Development Group

Curated by ChEMBL
LigandPNGBDBM50058046(propofol | CHEMBL526)
Affinity DataEC50:  5.40E+3nMAssay Description:Positive allosteric modulation of GABAA alpha1beta3gamma2L in HEK cell plasma membrane assessed as increase in [3H]muscimol binding measured after 10...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/24/2022
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetGamma-aminobutyric acid receptor subunit alpha-1/beta-3/gamma-2(Human)
Organon Research and Development Group

Curated by ChEMBL
LigandPNGBDBM50058046(propofol | CHEMBL526)
Affinity DataIC50: 8.00E+3nMAssay Description:Inhibition of [3H]azietomidate labelling of GABAA alpha1beta3gamma2L (unknown origin) expressed in Xenopus laevis oocytes assessed as reduction in ph...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/24/2022
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetGABA A receptor alpha-1/beta-1/gamma-2(Human)
Università

Curated by ChEMBL
LigandPNGBDBM50058046(propofol | CHEMBL526)
Affinity DataEC50:  8.00E+3nMAssay Description:Modulation of GABA-induced chloride currents in Xenopus laevis oocytes expressing human alpha-1-beta-1-gamma-2 GABA-A receptor subunitsMore 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-2/gamma-2(Human)
University of Copenhagen

Curated by ChEMBL
LigandPNGBDBM50058046(propofol | CHEMBL526)
Affinity DataEC50:  1.00E+4nMAssay Description:Direct activation of human Gamma-aminobutyric acid A receptor alpha-1-beta-2-gamma-2More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/20/2013
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetGamma-aminobutyric acid receptor subunit alpha-1(Rat)
Johannes Gutenberg University

Curated by ChEMBL
LigandPNGBDBM24183(4-amino-n-[2,3-3H]butyric acid | cid_119 | Gamma-A...)
Affinity DataEC50:  1.00E+4nMAssay Description:Activity at rat wild type GABAA alpha-1-beta-2 receptor expressed in Xenopus laevis oocytes at -60 mV by Two-Electrode voltage clamp methodMore data for this Ligand-Target Pair
In Depth
Date in BDB:
1/11/2010
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetGamma-aminobutyric acid receptor subunit alpha-2/beta-2/gamma-2(Human)
University of Copenhagen

Curated by ChEMBL
LigandPNGBDBM50058046(propofol | CHEMBL526)
Affinity DataEC50:  1.12E+4nMAssay Description:Effective concentration against GABA-evoked chloride currents mediated by human Gamma-aminobutyric acid GABA-A receptor alpha2-beta2-gamma2L expresse...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/4/2012
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetGamma-aminobutyric acid receptor subunit alpha-3/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:  2.80E+4nMAssay Description:Agonist activity on human Gamma-aminobutyric acid A receptor alpha-3-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)
Organon Research and Development Group

Curated by ChEMBL
LigandPNGBDBM50058046(propofol | CHEMBL526)
Affinity DataIC50: 3.20E+4nMAssay Description:Inhibition of [3H]pTFD-di-iPr-BnOH labelling of GABAA alpha1beta3gamma2L (unknown origin) expressed in Xenopus laevis oocytes assessed as reduction i...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/24/2022
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetGABA-A receptor; alpha-2/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:  4.00E+4nMAssay Description:Agonist activity on human Gamma-aminobutyric acid A receptor alpha-2-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-2/gamma-2(Human)
University of Copenhagen

Curated by ChEMBL
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)
TargetGamma-aminobutyric acid receptor subunit alpha-1/beta-3/gamma-2(Human)
Organon Research and Development Group

Curated by ChEMBL
LigandPNGBDBM50058046(propofol | CHEMBL526)
Affinity DataIC50: 4.40E+4nMAssay Description:Inhibition of [3H]R-mTFD-MPAB labelling of GABAA alpha1beta3gamma2L (unknown origin) expressed in Xenopus laevis oocytes assessed as reduction in pho...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/24/2022
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetGABA A receptor alpha-1/beta-1/gamma-2(Human)
Università

Curated by ChEMBL
LigandPNGBDBM50058046(propofol | CHEMBL526)
Affinity DataEC50:  4.40E+4nMAssay Description:Direct activation of chloride current in Xenopus laevis oocytes expressing human alpha-1-beta-1-gamma-2 GABA-A receptor subunitsMore 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)
Organon Research and Development Group

Curated by ChEMBL
LigandPNGBDBM50058046(propofol | CHEMBL526)
Affinity DataEC50:  5.00E+4nMAssay Description:GABA-mimetic action on Oocytes expressing human alpha-1-beta-3-gamma-2L GABA-A receptor subunits at >=100 uMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/25/2012
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetGABA A receptor alpha-4/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:  5.00E+4nMAssay Description:Effective agonist dose for human Gamma-aminobutyric acid A receptor alpha-4-beta-3-gamma-2More 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-2/gamma-2(Human)
University of Copenhagen

Curated by ChEMBL
LigandPNGBDBM24183(4-amino-n-[2,3-3H]butyric acid | cid_119 | Gamma-A...)
Affinity DataEC50:  5.10E+4nMAssay Description:Partial agonist activity at GABAAalpha1beta2gamma2s receptor (unknown origin) expressed in Xenopus laevis oocytes assessed as induction of chloride c...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/4/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetGamma-aminobutyric acid receptor subunit alpha-1/beta-3/gamma-2(Human)
Organon Research and Development Group

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)