α5IA [Ligand Id: 4095] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL306422
  • GABAA receptor α1 subunit/GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABA-A receptor; alpha-1/beta-3/gamma-2 in Human [ChEMBL: CHEMBL2094121] [GtoPdb: 404, 414, 412] [UniProtKB: P14867, P18507, P28472]
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  • GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABAA receptor α2 subunit/GABA-A receptor; alpha-2/beta-3/gamma-2 in Human [ChEMBL: CHEMBL2094130] [GtoPdb: 414, 412, 405] [UniProtKB: P18507, P28472, P47869]
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  • GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABAA receptor α3 subunit/GABA-A receptor; alpha-3/beta-3/gamma-2 in Human [ChEMBL: CHEMBL2094120] [GtoPdb: 414, 412, 406] [UniProtKB: P18507, P28472, P34903]
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  • GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABAA receptor α5 subunit/GABA-A receptor; alpha-5/beta-3/gamma-2 in Human [ChEMBL: CHEMBL2094122] [GtoPdb: 414, 412, 408] [UniProtKB: P18507, P28472, P31644]
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  • GABAA receptor α1 subunit/GABA receptor alpha-1 subunit in Human [ChEMBL: CHEMBL1962] [GtoPdb: 404] [UniProtKB: P14867]
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  • GABAA receptor α2 subunit/GABA receptor alpha-2 subunit in Human [ChEMBL: CHEMBL4956] [GtoPdb: 405] [UniProtKB: P47869]
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  • GABAA receptor α3 subunit/GABA receptor alpha-3 subunit in Human [ChEMBL: CHEMBL3026] [GtoPdb: 406] [UniProtKB: P34903]
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  • GABAA receptor α5 subunit/GABA receptor alpha-5 subunit in Human [ChEMBL: CHEMBL5112] [GtoPdb: 408] [UniProtKB: P31644]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
GABAA receptor α1 subunit/GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABA-A receptor; alpha-1/beta-3/gamma-2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094121] [GtoPdb: 404, 414, 412] [UniProtKB: P14867, P18507, P28472]
ChEMBL Displacement of [3H]-Ro- 15-1788 from human GABA-A alpha-1-beta-3-gamma-2 receptor subunits expressed in Xenopus oocytes B 9.06 pKi 0.88 nM Ki J Med Chem (2004) 47: 2176-2179 [PMID:15084116]
ChEMBL Displacement of [3H]-Ro- 15-1788 from human gamma-aminobutyric-acid GABA-A receptor alpha-1-beta-3-gamma-2 expressed in L(tk-) cells B 9.06 pKi 0.88 nM Ki J Med Chem (2004) 47: 5829-5832 [PMID:15537339]
GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABAA receptor α2 subunit/GABA-A receptor; alpha-2/beta-3/gamma-2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094130] [GtoPdb: 414, 412, 405] [UniProtKB: P18507, P28472, P47869]
ChEMBL Displacement of [3H]-Ro- 15-1788 from human GABA-A alpha-2-beta-3-gamma-2 receptor subunits expressed in Xenopus oocytes B 9.24 pKi 0.58 nM Ki J Med Chem (2004) 47: 2176-2179 [PMID:15084116]
ChEMBL Displacement of [3H]-Ro- 15-1788 from human gamma-aminobutyric-acid GABA-A receptor alpha-2-beta-3-gamma-2 expressed in L(tk-) cells B 9.24 pKi 0.58 nM Ki J Med Chem (2004) 47: 5829-5832 [PMID:15537339]
GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABAA receptor α3 subunit/GABA-A receptor; alpha-3/beta-3/gamma-2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094120] [GtoPdb: 414, 412, 406] [UniProtKB: P18507, P28472, P34903]
ChEMBL Displacement of [3H]-Ro- 15-1788 from human GABA-A alpha-3-beta-3-gamma-2 receptor subunits expressed in Xenopus oocytes B 9.21 pKi 0.61 nM Ki J Med Chem (2004) 47: 2176-2179 [PMID:15084116]
ChEMBL Displacement of [3H]-Ro- 15-1788 from human gamma-aminobutyric-acid GABA-A receptor alpha-3-beta-3-gamma-2 expressed in L(tk-) cells B 9.21 pKi 0.61 nM Ki J Med Chem (2004) 47: 5829-5832 [PMID:15537339]
GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABAA receptor α5 subunit/GABA-A receptor; alpha-5/beta-3/gamma-2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094122] [GtoPdb: 414, 412, 408] [UniProtKB: P18507, P28472, P31644]
ChEMBL Displacement of [3H]-Ro- 15-1788 from human GABA-A alpha-5-beta-3-gamma-2 receptor subunits expressed in Xenopus oocytes B 9.18 pKi 0.66 nM Ki J Med Chem (2004) 47: 2176-2179 [PMID:15084116]
ChEMBL Displacement of [3H]-Ro- 15-1788 from human gamma-aminobutyric-acid GABA-A receptor alpha-5-beta-3-gamma-2 expressed in L(tk-) cells B 9.18 pKi 0.66 nM Ki J Med Chem (2004) 47: 5829-5832 [PMID:15537339]
GABAA receptor α1 subunit/GABA receptor alpha-1 subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1962] [GtoPdb: 404] [UniProtKB: P14867]
ChEMBL Binding affinity to GABA-A alpha1 (unknown origin) B 9.06 pKi 0.88 nM Ki J Med Chem (2020) 63: 3425-3446 [PMID:31738537]
GABAA receptor α2 subunit/GABA receptor alpha-2 subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4956] [GtoPdb: 405] [UniProtKB: P47869]
ChEMBL Binding affinity to GABA-A alpha2 (unknown origin) B 9.24 pKi 0.58 nM Ki J Med Chem (2020) 63: 3425-3446 [PMID:31738537]
GABAA receptor α3 subunit/GABA receptor alpha-3 subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3026] [GtoPdb: 406] [UniProtKB: P34903]
ChEMBL Binding affinity to GABA-A alpha3 (unknown origin) B 9.21 pKi 0.61 nM Ki J Med Chem (2020) 63: 3425-3446 [PMID:31738537]
GABAA receptor α5 subunit/GABA receptor alpha-5 subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5112] [GtoPdb: 408] [UniProtKB: P31644]
ChEMBL Binding affinity to GABA-A alpha5 (unknown origin) B 9.18 pKi 0.66 nM Ki J Med Chem (2020) 63: 3425-3446 [PMID:31738537]

ChEMBL data shown on this page come from version 32:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]