zaleplon [Ligand Id: 4345] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1521 (CL 284,846, CL-284846, L-846, L846, LJC 10846, LJC-10846, SKP-1041, Sonata, ZAL-846, Zaleplon, Zaleplon civ, Zerene)
  • GABAA receptor α1 subunit/GABAA receptor γ2 subunit/GABAA receptor β2 subunit/GABA-A receptor; alpha-1/beta-2/gamma-2 in Human [ChEMBL: CHEMBL2095172] [GtoPdb: 404414411] [UniProtKB: P14867P18507P47870]
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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 β3 subunit/GABAA receptor α5 subunit/GABAA receptor γ3 subunit/Gamma-aminobutyric acid receptor subunit alpha-5/beta-3/gamma-3 in Human [ChEMBL: CHEMBL3885577] [GtoPdb: 412408415] [UniProtKB: P28472P31644Q99928]
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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 β2 subunit/GABA-A receptor; alpha-1/beta-2/gamma-2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2095172] [GtoPdb: 404414411] [UniProtKB: P14867P18507P47870]
ChEMBL Modulation of human GABA-A alpha1beta2gamma2 expressed in xenopus oocytes assessed as potentiation of GABA-evoked chloride currents B 6.54 pEC50 290 nM EC50 J Med Chem (2013) 56: 593-624 [PMID:23121096]
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 Modulation of human GABAA alpha2beta3gamma2 expressed in xenopus oocytes assessed as potentiation of GABA-evoked chloride currents B 5.79 pEC50 1630 nM EC50 J Med Chem (2013) 56: 593-624 [PMID:23121096]
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 Modulation of human GABAA alpha3beta3gamma2 expressed in xenopus oocytes assessed as potentiation of GABA-evoked chloride currents B 6 pEC50 >1000 nM EC50 J Med Chem (2013) 56: 593-624 [PMID:23121096]
GABAA receptor β3 subunit/GABAA receptor α5 subunit/GABAA receptor γ3 subunit/Gamma-aminobutyric acid receptor subunit alpha-5/beta-3/gamma-3 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3885577] [GtoPdb: 412408415] [UniProtKB: P28472P31644Q99928]
ChEMBL Modulation of human GABAA alpha5beta3gamma3 expressed in xenopus oocytes assessed as potentiation of GABA-evoked chloride currents B 6 pEC50 >1000 nM EC50 J Med Chem (2013) 56: 593-624 [PMID:23121096]

ChEMBL data shown on this page come from version 33:

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]