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

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL417990 (Bicuculline, (+)-Bicuculline)
  • 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 [ChEMBL: CHEMBL2093872] [GtoPdb: 419416404410414412408406405411407417409413415418] [UniProtKB: O00591O14764P14867P18505P18507P28472P31644P34903P47869P47870P48169P78334Q16445Q8N1C3Q99928Q9UN88]
  • This target only has 0 pki data point
1 CHEMBL417990_lig_chart_1 GABA-A receptor; anion channel Human
There should be some charts here, you may need to enable JavaScript!
  • GABAA receptor γ1 subunit/GABA receptor gamma-1 subunit in Rat [ChEMBL: CHEMBL296] [GtoPdb: 413] [UniProtKB: P23574]
  • This target only has 0 pki data point
2 CHEMBL417990_lig_chart_2 GABA receptor gamma-1 subunit Rat
There should be some charts here, you may need to enable JavaScript!
  • KCa2.1 in Human [GtoPdb: 381] [UniProtKB: Q92952]
  • This target only has 0 pki data point
3 CHEMBL417990_lig_chart_3 KCa2.1 Human
There should be some charts here, you may need to enable JavaScript!
  • KCa2.2 in Rat [GtoPdb: 382] [UniProtKB: P70604]
  • This target only has 0 pki data point
4 CHEMBL417990_lig_chart_4 KCa2.2 Rat
There should be some charts here, you may need to enable JavaScript!
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: 419416404410414412408406405411407417409413415418] [UniProtKB: O00591O14764P14867P18505P18507P28472P31644P34903P47869P47870P48169P78334Q16445Q8N1C3Q99928Q9UN88]
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 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos 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]