L838417 [Ligand Id: 4241] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL373250 (L-838417)
  • 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: 404414412] [UniProtKB: P14867P18507P28472]
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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: 414412405] [UniProtKB: P18507P28472P47869]
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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: 414412406] [UniProtKB: P18507P28472P34903]
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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: 414412408] [UniProtKB: P18507P28472P31644]
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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: 404414412] [UniProtKB: P14867P18507P28472]
ChEMBL Displacement of [3H]-Ro15-1788 from human recombinant GABAA alpha1 in combination with beta-3-gamma-2 expressed in L(tk-) cells B 9.1 pKi 0.8 nM Ki J. Med. Chem. (2006) 49: 35-38 [PMID:16392789]
ChEMBL Displacement of [3H]-flumazenil from human GABAA alpha1beta3gamma2 expressed in Ltk cells B 9.1 pKi 0.79 nM Ki J Med Chem (2020) 63: 3425-3446 [PMID:31738537]
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: 414412405] [UniProtKB: P18507P28472P47869]
ChEMBL Displacement of [3H]-Ro15-1788 from human recombinant GABAA alpha2 in combination with beta3gamma2 expressed in L(tk-) cells B 9.15 pKi 0.7 nM Ki J. Med. Chem. (2006) 49: 35-38 [PMID:16392789]
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: 414412406] [UniProtKB: P18507P28472P34903]
ChEMBL Displacement of [3H]Ro-151788 from human recombinant GABAA alpha3 in combination with beta3gamma2 expressed in L(tk-) cells B 9.15 pKi 0.7 nM Ki J. Med. Chem. (2006) 49: 35-38 [PMID:16392789]
ChEMBL Displacement of [3H]-flumazenil from human GABAA alpha3beta3gamma2 expressed in Ltk cells B 9.17 pKi 0.67 nM Ki J Med Chem (2020) 63: 3425-3446 [PMID:31738537]
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: 414412408] [UniProtKB: P18507P28472P31644]
ChEMBL Displacement of [3H]Ro-151788 from human recombinant GABAA alpha5 in combination with beta3gamma2 expressed in L(tk-) cells B 8.64 pKi 2.3 nM Ki J. Med. Chem. (2006) 49: 35-38 [PMID:16392789]
ChEMBL Displacement of [3H]-flumazenil from human GABAA alpha5beta3gamma2 expressed in Ltk cells B 8.65 pKi 2.25 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 Positive allosteric modulation of GABAA alpha2 (unknown origin) B 9.15 pKi 0.7 nM Ki J. Med. Chem. (2013) 56: 593-624 [PMID:23121096]
GABAA receptor α3 subunit/GABA receptor alpha-3 subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3026] [GtoPdb: 406] [UniProtKB: P34903]
ChEMBL Positive allosteric modulation of GABAA alpha3 (unknown origin) B 9.15 pKi 0.7 nM Ki J. Med. Chem. (2013) 56: 593-624 [PMID:23121096]
GABAA receptor α5 subunit/GABA receptor alpha-5 subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5112] [GtoPdb: 408] [UniProtKB: P31644]
ChEMBL Positive allosteric modulation of GABAA alpha5 (unknown origin) B 8.64 pKi 2.3 nM Ki J. Med. Chem. (2013) 56: 593-624 [PMID:23121096]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]