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 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]