bicuculline [Ligand Id: 2312] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL417990 (Bicuculline, (+)-Bicuculline)
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  • GABAA receptor γ1 subunit/GABA receptor gamma-1 subunit in Rat [ChEMBL: CHEMBL296] [GtoPdb: 413] [UniProtKB: P23574]
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  • KCa2.1 in Human [GtoPdb: 381] [UniProtKB: Q92952]
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  • KCa2.2 in Rat [GtoPdb: 382] [UniProtKB: P70604]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
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]
ChEMBL Binding affinity in vivo for gamma-aminobutyric-acid A receptor measured by its ability to displace [3H]-GABA agonist from rat brain preparations after iv injection. B 4.36 pIC50 44000 nM IC50 J Med Chem (1992) 35: 4092-4097 [PMID:1331456]
ChEMBL Displacement of [3H]GABA from gamma-aminobutyric-acid A (GABA-A) receptor B 4.82 pIC50 15000 nM IC50 J Med Chem (1992) 35: 1969-1977 [PMID:1317920]
ChEMBL Affinity for gamma-aminobutyric-acid A receptor measured by its ability to displace [3H]gabazine antagonist from rat brain preparations. F 5.21 pIC50 6200 nM IC50 J Med Chem (1992) 35: 4092-4097 [PMID:1331456]
GABAA receptor γ1 subunit/GABA receptor gamma-1 subunit in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL296] [GtoPdb: 413] [UniProtKB: P23574]
ChEMBL Percent displacement of [3H]GABA at Gamma-aminobutyric acid receptor in rat brain membranes at 0.01 uM B 5.42 pIC50 3800 nM IC50 J Med Chem (1980) 23: 1142-1144 [PMID:7420361]
KCa2.1 in Human [GtoPdb: 381] [UniProtKB: Q92952]
GtoPdb - - 4.8 pIC50 16000 nM IC50 Br J Pharmacol (2000) 129: 991-9 [PMID:10696100]
KCa2.2 in Rat [GtoPdb: 382] [UniProtKB: P70604]
GtoPdb - - 4.6 pIC50 - - - Br J Pharmacol (2000) 129: 991-9 [PMID:10696100]

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]