bicuculline [Ligand Id: 2312] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL417990 ((+)-Bicuculline, Bicuculline) |
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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 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]
