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 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]