CGS8216 [Ligand Id: 4156] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL19732 (CGS-8216)
  • 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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  • GABAA receptor α1 subunit/GABA receptor alpha-1 subunit in Human [ChEMBL: CHEMBL1962] [GtoPdb: 404] [UniProtKB: P14867]
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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]
GtoPdb - - 10.3 pKi 0.05 nM Ki J Med Chem (2000) 43: 71-95 [PMID:10633039]
ChEMBL Binding affinity for human recombinant gamma-aminobutyric-acid (GABA) A receptor alpha-1-beta-3-gamma-2 B 10.3 pKi 0.05 nM Ki J Med Chem (2000) 43: 71-95 [PMID:10633039]
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 10.1 pKi 0.08 nM Ki J Med Chem (2000) 43: 71-95 [PMID:10633039]
GtoPdb - - 10.1 pKi 0.08 nM Ki J Med Chem (2000) 43: 71-95 [PMID:10633039]
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]
GtoPdb - - 9.92 pKi 0.12 nM Ki J Med Chem (2000) 43: 71-95 [PMID:10633039]
ChEMBL Binding affinity for human recombinant gamma-aminobutyric-acid (GABA) A receptor alpha-3-beta-3-gamma-2 B 9.92 pKi 0.12 nM Ki J Med Chem (2000) 43: 71-95 [PMID:10633039]
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]
GtoPdb - - 9.6 pKi 0.25 nM Ki J Med Chem (2000) 43: 71-95 [PMID:10633039]
ChEMBL Binding affinity for human recombinant gamma-aminobutyric-acid (GABA) A receptor alpha-5-beta-3-gamma-2 B 9.6 pKi 0.25 nM Ki J Med Chem (2000) 43: 71-95 [PMID:10633039]
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 7.77 pKi 17 nM Ki J Med Chem (2000) 43: 71-95 [PMID:10633039]
GtoPdb - - 7.77 pKi 17 nM Ki
GABAA receptor π subunit/GABAA receptor δ subunit/GABAA receptor α1 subunit/GABAA receptor β1 subunit/GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABAA receptor α5 subunit/GABAA receptor α3 subunit/GABAA receptor α2 subunit/GABAA receptor β2 subunit/GABAA receptor α4 subunit/GABAA receptor ε subunit/GABAA receptor α6 subunit/GABAA receptor γ1 subunit/GABAA receptor γ3 subunit/GABAA receptor θ subunit/GABA-A receptor; anion channel in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2093872] [GtoPdb: 419, 416, 404, 410, 414, 412, 408, 406, 405, 411, 407, 417, 409, 413, 415, 418] [UniProtKB: O00591, O14764, P14867, P18505, P18507, P28472, P31644, P34903, P47869, P47870, P48169, P78334, Q16445, Q8N1C3, Q99928, Q9UN88]
GtoPdb - - 7.77 pKi 17 nM Ki
GtoPdb - - 9.6 pKi 0.25 nM Ki J Med Chem (2000) 43: 71-95 [PMID:10633039]
GtoPdb - - 9.92 pKi 0.12 nM Ki J Med Chem (2000) 43: 71-95 [PMID:10633039]
GtoPdb - - 10.1 pKi 0.08 nM Ki J Med Chem (2000) 43: 71-95 [PMID:10633039]
GtoPdb - - 10.3 pKi 0.05 nM Ki J Med Chem (2000) 43: 71-95 [PMID:10633039]
ChEMBL Inhibition on Benzodiazepine receptor B 9.4 pIC50 0.4 nM IC50 J Med Chem (1997) 40: 4360-4371 [PMID:9435905]
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 Binding affinity against Diazepam insensitive (DI) Gamma-aminobutyric acid A receptor B 7.34 pKi 46 nM Ki J Med Chem (1995) 38: 1679-1688 [PMID:7752192]
ChEMBL Displacement of [3H]-diazepam from GABA-A benzodiazepine receptor of rat cerebral cortex B 9.66 pKi 0.22 nM Ki J Med Chem (1987) 30: 454-455 [PMID:3029371]
ChEMBL Displacing potential to [3H]diazepam binding to benzodiazepine receptor in Wistar rat cerebral cortex B 9.66 pKi 0.22 nM Ki J Med Chem (1989) 32: 1213-1217 [PMID:2542554]
ChEMBL Displacement of [3H]diazepam from rat cerebral cortex benzodiazepine receptor B 9.66 pKi 0.22 nM Ki J Med Chem (1996) 39: 2844-2851 [PMID:8709114]
ChEMBL Binding affinity against benzodiazepine (BZ) receptor by displacing [3H]diazepam in cerebral cortex of Wistar rats B 9.66 pKi 0.22 nM Ki J Med Chem (1988) 31: 1738-1745 [PMID:2842502]
ChEMBL Binding affinity against Diazepam sensitive (DS) Gamma-aminobutyric acid A receptor in rat cerebellum. B 9.89 pKi 0.13 nM Ki J Med Chem (1995) 38: 1679-1688 [PMID:7752192]
ChEMBL Displacement of [3H]flunitrazepam from GABA-A Benzodiazepine receptor of rat forebrain B 8.36 pIC50 4.4 nM IC50 J Med Chem (1991) 34: 281-290 [PMID:1846920]
ChEMBL Displacement of [3H]flunitrazepam from GABA-A Benzodiazepine receptors in rat forebrain B 9.35 pIC50 0.45 nM IC50 J Med Chem (1991) 34: 2899-2906 [PMID:1680197]
ChEMBL In vitro inhibition of binding to GABA-A central benzodiazepine-receptor of rat brain B 9.4 pIC50 0.4 nM IC50 J Med Chem (1982) 25: 337-339 [PMID:6121916]
ChEMBL Concentration to inhibit [3H]flunitrazepam binding to rat cerebral cortical membrane B 9.4 pIC50 0.4 nM IC50 J Med Chem (1992) 35: 368-374 [PMID:1310121]
ChEMBL Inhibition of GABA-A benzodiazepine receptor B 9.4 pIC50 0.4 nM IC50 Bioorg Med Chem Lett (2000) 10: 2723-2726 [PMID:11133077]
ChEMBL In vitro inhibition of 3[H]Diazepam binding to Benzodiazepine receptor from rat cerebral cortical membranes B 9.4 pIC50 0.4 nM IC50 J Med Chem (1990) 33: 2343-2357 [PMID:2167977]
ChEMBL Binding affinity towards benzodiazepine receptor inverse agonist site by the displacement of [3H]diazepam in rat cerebral cortical membranes. B 9.4 pIC50 0.4 nM IC50 J Med Chem (1993) 36: 2929-2937 [PMID:8411009]
ChEMBL Binding affinity for rat benzodiazepine receptor inverse agonist site B 9.4 pIC50 0.4 nM IC50 J Med Chem (1996) 39: 2129-2140 [PMID:8667357]
ChEMBL Displacement of [3H]diazepam from GABA-A Benzodiazepine receptor of rat forebrain B 9.52 pIC50 0.3 nM IC50 J Med Chem (1991) 34: 281-290 [PMID:1846920]
ChEMBL Partial agonistic activity against specific binding of [3H]-Ro-15-1788 to GABA-A Benzodiazepine receptor in rat cortex B 9.89 pIC50 0.13 nM IC50 J Med Chem (1993) 36: 1669-1673 [PMID:8388472]
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 GABAA alpha-1-beta-2-gamma-2 receptor B 8.08 pKd 8.3 nM Kd J Med Chem (2008) 51: 3788-3803 [PMID:18537233]
GtoPdb - - 10.3 pKi 0.05 nM Ki J Med Chem (2000) 43: 71-95 [PMID:10633039]
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 GABAA alpha-5-beta-2-gamma-2 receptor B 6.7 pKd 200 nM Kd J Med Chem (2008) 51: 3788-3803 [PMID:18537233]
GtoPdb - - 9.6 pKi 0.25 nM Ki J Med Chem (2000) 43: 71-95 [PMID:10633039]

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]