ZK93423 [Ligand Id: 4346] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1518572 (ZK-93423)
  • 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 γ2 subunit/GABAA receptor β3 subunit/GABAA receptor α6 subunit/GABA-A receptor; alpha-6/beta-3/gamma-2 in Human [ChEMBL: CHEMBL2095190] [GtoPdb: 414, 412, 409] [UniProtKB: P18507, P28472, Q16445]
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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 Binding affinity for human recombinant gamma-aminobutyric-acid (GABA) A receptor alpha-1-beta-3-gamma-2 B 8.39 pKi 4.1 nM Ki J Med Chem (2000) 43: 71-95 [PMID:10633039]
ChEMBL Binding affinity measured using LtK- cell membranes expressing GABA alpha-1-beta-3-gamma-2 receptor B 8.39 pKi 4.1 nM Ki J Med Chem (1998) 41: 2537-2552 [PMID:9651158]
GtoPdb - - 9 pKi 1 nM Ki J Med Chem (1998) 41: 2537-52 [PMID:9651158]
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 Binding affinity to human recombinant gamma-aminobutyric-acid (GABA) A receptor alpha-2-beta-3-gamma-2 B 8.38 pKi 4.2 nM Ki J Med Chem (2000) 43: 71-95 [PMID:10633039]
ChEMBL Binding affinity measured using LtK- cell membranes expressing GABA alpha-2-beta-3-gamma-2 receptor B 8.38 pKi 4.2 nM Ki J Med Chem (1998) 41: 2537-2552 [PMID:9651158]
GtoPdb - - 8.4 pKi 4.2 nM Ki J Med Chem (1998) 41: 2537-52 [PMID:9651158]
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 Binding affinity for human recombinant gamma-aminobutyric-acid (GABA) A receptor alpha-3-beta-3-gamma-2 B 8.22 pKi 6 nM Ki J Med Chem (2000) 43: 71-95 [PMID:10633039]
ChEMBL Binding affinity measured using LtK- cell membranes expressing GABA alpha-3-beta-3-gamma-2 receptor B 8.22 pKi 6 nM Ki J Med Chem (1998) 41: 2537-2552 [PMID:9651158]
GtoPdb - - 8.4 pKi 4.5 nM Ki J Med Chem (1998) 41: 2537-52 [PMID:9651158]
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 Binding affinity for human recombinant gamma-aminobutyric-acid (GABA) A receptor alpha-5-beta-3-gamma-2 B 8.35 pKi 4.5 nM Ki J Med Chem (2000) 43: 71-95 [PMID:10633039]
ChEMBL Binding affinity measured using LtK- cell membranes expressing Gamma-aminobutyric acid A receptor alpha-5-beta-3-gamma-2 B 8.35 pKi 4.5 nM Ki J Med Chem (1998) 41: 2537-2552 [PMID:9651158]
GtoPdb - - 8.4 pKi 4.5 nM Ki J Med Chem (1998) 41: 2537-52 [PMID:9651158]
GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABAA receptor α6 subunit/GABA-A receptor; alpha-6/beta-3/gamma-2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2095190] [GtoPdb: 414, 412, 409] [UniProtKB: P18507, P28472, Q16445]
ChEMBL Binding affinity for human recombinant gamma-aminobutyric-acid (GABA) A receptor alpha-6-beta-3-gamma-2 B 6 pKi >1000 nM Ki J Med Chem (2000) 43: 71-95 [PMID:10633039]
ChEMBL Binding affinity measured using LtK- cell membranes expressing Gamma-aminobutyric acid A receptor alpha-6-beta-3-gamma-2 B 6 pKi >1000 nM Ki J Med Chem (1998) 41: 2537-2552 [PMID:9651158]
GABAA receptor π subunit/GABAA receptor β1 subunit/GABAA receptor δ subunit/GABAA receptor γ2 subunit/GABAA receptor α5 subunit/GABAA receptor α3 subunit/GABAA receptor γ1 subunit/GABAA receptor α2 subunit/GABAA receptor α4 subunit/GABAA receptor γ3 subunit/GABAA receptor α6 subunit/GABAA receptor α1 subunit/GABAA receptor β3 subunit/GABAA receptor β2 subunit/GABAA receptor ε subunit in Human [GtoPdb: 419, 410, 416, 414, 408, 406, 413, 405, 407, 415, 409, 404, 412, 411, 417] [UniProtKB: O00591, P18505, O14764, P18507, P31644, P34903, Q8N1C3, P47869, P48169, Q99928, Q16445, P14867, P28472, P47870, P78334]
GtoPdb - - 8.4 pKi 4.2 nM Ki J Med Chem (1998) 41: 2537-52 [PMID:9651158]
GtoPdb - - 8.4 pKi 4.5 nM Ki J Med Chem (1998) 41: 2537-52 [PMID:9651158]
GtoPdb - - 8.4 pKi 4.5 nM Ki J Med Chem (1998) 41: 2537-52 [PMID:9651158]
GtoPdb - - 9 pKi 1 nM Ki J Med Chem (1998) 41: 2537-52 [PMID:9651158]
GABAA receptor π subunit/GABAA receptor β1 subunit/GABAA receptor δ subunit/GABAA receptor γ2 subunit/GABAA receptor α5 subunit/GABAA receptor α3 subunit/GABAA receptor γ1 subunit/GABAA receptor α2 subunit/GABAA receptor α4 subunit/GABAA receptor γ3 subunit/GABAA receptor α6 subunit/GABAA receptor α1 subunit/GABAA receptor β3 subunit/GABAA receptor β2 subunit/GABAA receptor ε subunit/GABA-A receptor; anion channel in Rat (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL1907607] [GtoPdb: 419, 410, 416, 414, 408, 406, 413, 405, 407, 415, 409, 404, 412, 411, 417] [UniProtKB: O09028, P15431, P18506, P18508, P19969, P20236, P23574, P23576, P28471, P28473, P30191, P62813, P63079, P63138, Q91ZM7, Q9ES14]
ChEMBL In vitro inhibitory concentration of compound against benzodiazepine receptor from rat cerebral cortex using [3H]- flunitrazepam was evaluated B 8.3 pIC50 5 nM IC50 J Med Chem (1994) 37: 745-757 [PMID:8145224]
ChEMBL Effect on [3H]flunitrazepam binding to Benzodiazepine receptor B 9 pIC50 1 nM IC50 J Med Chem (1991) 34: 1754-1756 [PMID:1674542]
ChEMBL Displacement of [3H]flunitrazepam from GABA-A Benzodiazepine receptor of rat brain cortical membranes B 9 pIC50 1 nM IC50 J Med Chem (1998) 41: 2537-2552 [PMID:9651158]
ChEMBL Inhibition of [3H]-Ro- 15-1788 binding to GABA-A benzodiazepine receptor in rat brain membrane B 9 pIC50 1 nM IC50 J Med Chem (1995) 38: 950-957 [PMID:7699711]
ChEMBL In vitro inhibition of [3H]flunitrazepam binding to GABA-A Benzodiazepine receptor of rat cerebral cortex membranes B 9 pIC50 1 nM IC50 J Med Chem (1990) 33: 1062-1069 [PMID:1968513]

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]