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TargetGABA-A receptor; alpha-5/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:  4.20E+5nMAssay 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
PubMed
TargetGABA-A receptor; alpha-5/beta-3/gamma-2(Human)
The Royal Danish School of Pharmacy

Curated by ChEMBL
LigandPNGBDBM50000106(Piperidine-4-carboxylic acid | Piperidine-4-carbox...)
Affinity DataEC50:  6.90E+5nMAssay 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
PubMed
TargetGABA-A receptor; alpha-5/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:  7.50E+4nMAssay 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
PubMed
TargetGABA-A receptor; alpha-5/beta-3/gamma-2(Human)
The Royal Danish School of Pharmacy

Curated by ChEMBL
LigandPNGBDBM50100946(piperidine-4-seleninic acid | Piperidine-4-selenic...)
Affinity DataEC50:  4.20E+5nMAssay 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
PubMed
TargetGABA-A receptor; alpha-5/beta-3/gamma-2(Human)
The Royal Danish School of Pharmacy

Curated by ChEMBL
LigandPNGBDBM50100943(3-Amino-propane-1-selenic acid | CHEMBL41065)
Affinity DataEC50:  1.90E+6nMAssay 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
PubMed
TargetGABA-A receptor; alpha-5/beta-3/gamma-2(Human)
The Royal Danish School of Pharmacy

Curated by ChEMBL
LigandPNGBDBM50087272(CHEMBL34155 | P4S | Piperidine-4-sulfonic acid | P...)
Affinity DataEC50:  2.00E+4nMAssay 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
PubMed
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)
TargetGABA-A receptor; alpha-5/beta-3/gamma-2(Human)
The Royal Danish School of Pharmacy

Curated by ChEMBL
LigandPNGBDBM50100944(Piperidin-4-yl-phosphinic acid | CHEMBL291079)
Affinity DataEC50:  2.60E+5nMAssay 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
PubMed
TargetGABA-A receptor; alpha-5/beta-3/gamma-2(Human)
The Royal Danish School of Pharmacy

Curated by ChEMBL
LigandPNGBDBM50110704(3-(2-Hydroxy-ethylsulfanyl)-6,6-dimethyl-1-thiazol...)
Affinity DataEC50:  0.700nMAssay Description:Inverse agonist activity at GABAA alpha5beta3gamma2 in Homo sapiens (human) L(tk-) cells by patch clamp assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/25/2014
Entry Details Article

LigandPNGBDBM50120773(8-(2-Fluoro-benzoyl)-2-(2-fluoro-phenyl)-6,7,8,9-t...)
Affinity DataEC50:  346nMAssay Description:Effective concentration against Gamma-aminobutyric acid A receptor, alpha 5More 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:  291nMAssay Description:Effective concentration against Gamma-aminobutyric acid A receptor, alpha 5More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
LigandPNGBDBM50120792(8-Benzyl-2-p-tolyl-6,7,8,9-tetrahydro-5H-1,3a,5,8-...)
Affinity DataEC50:  650nMAssay Description:Effective concentration against Gamma-aminobutyric acid A receptor, alpha 5More 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:  323nMAssay Description:Effective concentration against Gamma-aminobutyric acid A receptor, alpha 5More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
LigandPNGBDBM50120791(8-Cyclohexylmethyl-2-(2-fluoro-phenyl)-6,7,8,9-tet...)
Affinity DataEC50:  231nMAssay Description:Effective concentration against Gamma-aminobutyric acid A receptor, alpha 5More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
LigandPNGBDBM50120808(2-(2-Fluoro-phenyl)-8-(4-methyl-benzoyl)-6,7,8,9-t...)
Affinity DataEC50:  90nMAssay Description:Effective concentration against Gamma-aminobutyric acid A receptor, alpha 5More 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:  38nMAssay Description:Effective concentration against Gamma-aminobutyric acid A receptor, alpha 5More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
LigandPNGBDBM50120798(2-(2-Fluoro-phenyl)-8-(3H-imidazol-4-ylmethyl)-6,7...)
Affinity DataEC50:  439nMAssay Description:Effective concentration against Gamma-aminobutyric acid A receptor, alpha 5More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
LigandPNGBDBM50120799(8-(3,4-Difluoro-benzoyl)-2-(2-fluoro-phenyl)-6,7,8...)
Affinity DataEC50:  491nMAssay Description:Effective concentration against Gamma-aminobutyric acid A receptor, alpha 5More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
LigandPNGBDBM26266(Ambien | CHEMBL911 | ZPM | N,N-dimethyl-2-[6-methy...)
Affinity DataEC50: >3.00E+3nMAssay Description:Effective concentration against Gamma-aminobutyric acid A receptor, alpha 5More 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:  111nMAssay Description:Effective concentration against Gamma-aminobutyric acid A receptor, alpha 5More 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:  375nMAssay Description:Effective concentration against Gamma-aminobutyric acid A receptor, alpha 5More 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:  10nMAssay Description:Effective concentration against Gamma-aminobutyric acid A receptor, alpha 5More 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:  112nMAssay Description:Effective concentration against Gamma-aminobutyric acid A receptor, alpha 5More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
LigandPNGBDBM50120780(2-(2-Fluoro-phenyl)-4-oxo-5,6,7,9-tetrahydro-4H-1,...)
Affinity DataEC50:  1.00E+3nMAssay Description:Effective concentration against Gamma-aminobutyric acid A receptor, alpha 5More 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:  94nMAssay Description:Effective concentration against Gamma-aminobutyric acid A receptor, alpha 5More 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:  74nMAssay Description:Effective concentration against Gamma-aminobutyric acid A receptor, alpha 5More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetGABA-A receptor; alpha-5/beta-3/gamma-2(Human)
The Royal Danish School of Pharmacy

Curated by ChEMBL
LigandPNGBDBM50144861(3-(5-Methyl-isoxazol-3-yl)-6-(pyridin-2-ylmethoxy)...)
Affinity DataEC50:  2.5nMAssay Description:Effective concentration against human Alpha-5-beta-3-gamma-2 GABA-A receptor was determinedMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetGABA-A receptor; alpha-5/beta-3/gamma-2(Human)
The Royal Danish School of Pharmacy

Curated by ChEMBL
LigandPNGBDBM50000766(CHEMBL12 | DIAZEPAM | US9271961, Diazepam)
Affinity DataEC50:  45nMAssay Description:Binding affinity to human alpha5beta3gamma2 GABA receptor expressed in Xenopus laevis oocytesMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/20/2011
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
LigandPNGBDBM50065229(4-Ethyl-6,7-dimethoxy-9H-carbazole-3-carboxylic ac...)
Affinity DataEC50:  3nMAssay Description:Binding affinity to human alpha5beta3gamma2 GABA receptor expressed in Xenopus laevis oocytesMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/20/2011
Entry Details Article
PubMed
TargetGABA-A receptor; alpha-5/beta-3/gamma-2(Human)
The Royal Danish School of Pharmacy

Curated by ChEMBL
LigandPNGBDBM50332376(4-Amino-N-propyl-8-(pyrimidin-2-yl)cinnoline-3-car...)
Affinity DataEC50:  1.13E+3nMAssay Description:Binding affinity to human alpha5beta3gamma2 GABA receptor expressed in Xenopus laevis oocytesMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/20/2011
Entry Details Article
PubMed
TargetGABA-A receptor; alpha-5/beta-3/gamma-2(Human)
The Royal Danish School of Pharmacy

Curated by ChEMBL
LigandPNGBDBM50332375(4-Amino-8-(5-(azetidine-1-carbonyl)pyridin-3-yl)-N...)
Affinity DataEC50:  455nMAssay Description:Binding affinity to human alpha5beta3gamma2 GABA receptor expressed in Xenopus laevis oocytesMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/20/2011
Entry Details Article
PubMed
TargetGABA-A receptor; alpha-5/beta-3/gamma-2(Human)
The Royal Danish School of Pharmacy

Curated by ChEMBL
LigandPNGBDBM50332374(9-Amino-2-cyclobutyl-5-(pyrimidin-2-yl)-2,3-dihydr...)
Affinity DataEC50:  206nMAssay Description:Binding affinity to human alpha5beta3gamma2 GABA receptor expressed in Xenopus laevis oocytesMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/20/2011
Entry Details Article
PubMed
LigandPNGBDBM50049736(8-Ethynyl-5-methyl-6-oxo-5,6-dihydro-4H-2,5,10b-tr...)
Affinity DataEC50:  9.80E+3nMAssay Description:Activity at alpha-5-beta-3-gamma-2 GABAA receptor expressed in Xenopus oocytes assessed as inhibition in GABA-induced current by voltage clamp assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/17/2012
Entry Details Article
PubMed
LigandPNGBDBM50243981(CHEMBL453066 | Beta CCM | Methyl Beta-carboline-3 ...)
Affinity DataKd:  58nMAssay Description:Binding affinity to GABAA alpha-5-beta-2-gamma-2 receptorMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/17/2012
Entry Details Article
PubMed
LigandPNGBDBM50001765(Halcion | CHEMBL646 | 8-chloro-6-(2-chlorophenyl)-...)
Affinity DataKd:  4nMAssay Description:Binding affinity to GABAA alpha-5-beta-2-gamma-2 receptorMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/17/2012
Entry Details Article
PubMed
LigandPNGBDBM50000766(CHEMBL12 | DIAZEPAM | US9271961, Diazepam)
Affinity DataKd:  23nMAssay Description:Binding affinity to GABAA alpha-5-beta-2-gamma-2 receptorMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/17/2012
Entry Details Article
PubMedPDB3D3D Structure (crystal)
LigandPNGBDBM50083894(7-Ethynyl-1-methyl-5-phenyl-1,3-dihydro-benzo[e][1...)
Affinity DataKd:  7nMAssay Description:Binding affinity to GABAA alpha-5-beta-2-gamma-2 receptorMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/17/2012
Entry Details Article
PubMed
LigandPNGBDBM25878(Flunitrazepam | [3H]Rohypnol | 5-(2-fluorophenyl)-...)
Affinity DataKd:  3nMAssay Description:Binding affinity to GABAA alpha-5-beta-2-gamma-2 receptorMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/17/2012
Entry Details Article
PubMed
LigandPNGBDBM50244120(tert-butyl 4-methyl-5-oxo-7-(2-(trimethylsilyl)eth...)
Affinity DataKd:  58nMAssay Description:Binding affinity to GABAA alpha-5-beta-2-gamma-2 receptorMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/17/2012
Entry Details Article
PubMed
LigandPNGBDBM50244119(ethyl 4-methyl-5-oxo-7-(2-(trimethylsilyl)ethynyl)...)
Affinity DataKd:  5nMAssay Description:Binding affinity to GABAA alpha-5-beta-2-gamma-2 receptorMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/17/2012
Entry Details Article
PubMed
LigandPNGBDBM50244118(ethyl 12-oxo-15-[2-(trimethylsilyl)ethynyl]-2,4,11...)
Affinity DataKd:  4nMAssay Description:Binding affinity to GABAA alpha-5-beta-2-gamma-2 receptorMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/17/2012
Entry Details Article
PubMed
LigandPNGBDBM50067419(RY-066 | ethyl 9-oxo-7-(2-trimethylsilyl-1-ethynyl...)
Affinity DataKd:  2.60nMAssay Description:Binding affinity to GABAA alpha-5-beta-2-gamma-2 receptorMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/17/2012
Entry Details Article
PubMed
LigandPNGBDBM50244074(ethyl 7-azido-4-methyl-5-oxo-4,5-dihydroimidazo[1,...)
Affinity DataKd:  3.80nMAssay Description:Binding affinity to GABAA alpha-5-beta-2-gamma-2 receptorMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/17/2012
Entry Details Article
PubMed
LigandPNGBDBM50244073(ethyl 7-fluoro-4-methyl-5-oxo-1,3a,4,5-tetrahydroi...)
Affinity DataKd:  0.5nMAssay Description:Binding affinity to GABAA alpha-5-beta-2-gamma-2 receptorMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/17/2012
Entry Details Article
PubMed
LigandPNGBDBM50244072(8-Ethyl-5-methyl-6-oxo-3a,4,5,6-tetrahydro-1H-2,5,...)
Affinity DataKd:  1.5nMAssay Description:Binding affinity to GABAA alpha-5-beta-2-gamma-2 receptorMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/17/2012
Entry Details Article
PubMed
LigandPNGBDBM84956(2-(4-Methoxy-phenyl)-2,5-dihydro-pyrazolo[4,3-c]qu...)
Affinity DataKd:  5nMAssay Description:Binding affinity to GABAA alpha-5-beta-2-gamma-2 receptorMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/17/2012
Entry Details Article
PubMed
LigandPNGBDBM84957(CHEMBL20042 | CGS 9896)
Affinity DataKd:  40nMAssay Description:Binding affinity to GABAA alpha-5-beta-2-gamma-2 receptorMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/17/2012
Entry Details Article
PubMed
LigandPNGBDBM50017009(CHEMBL19732 | 2-Phenyl-2,5-dihydro-pyrazolo[4,3-c]...)
Affinity DataKd:  200nMAssay Description:Binding affinity to GABAA alpha-5-beta-2-gamma-2 receptorMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/17/2012
Entry Details Article
PubMed
LigandPNGBDBM50244037(3-propoxy-9H-pyrido[3,4-b]indole | CHEMBL499814)
Affinity DataKd:  591nMAssay Description:Binding affinity to GABAA alpha-5-beta-2-gamma-2 receptorMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/17/2012
Entry Details Article
PubMed
LigandPNGBDBM50244036(CHEMBL509197 | Beta-CCT | tert-butyl 9H-pyrido[3,4...)
Affinity DataKd:  111nMAssay Description:Binding affinity to GABAA alpha-5-beta-2-gamma-2 receptorMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/17/2012
Entry Details Article
PubMed
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