picrotoxinin [Ligand Id: 2291] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL47244 (Picrotoxinin)
  • glycine receptor α2 subunit in Human [GtoPdb: 424] [UniProtKB: P23416]
  • glycine receptor α2 subunit/Glycine receptor subunit alpha-2 in Rat [ChEMBL: CHEMBL2328] [GtoPdb: 424] [UniProtKB: P22771]
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  • 5-HT3AB in Human [GtoPdb: 378]
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  • 5-HT3A in Human [GtoPdb: 379]
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  • glycine receptor α1 subunit in Human [GtoPdb: 423] [UniProtKB: P23415]
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  • glycine receptor α3 subunit in Human [GtoPdb: 425] [UniProtKB: O75311]
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  • glycine receptor β subunit in Human [GtoPdb: 427] [UniProtKB: P48167]
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  • Glycine Receptor (All subtypes) in Human [GtoPdb: 428]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
glycine receptor α2 subunit in Human [GtoPdb: 424] [UniProtKB: P23416]
GtoPdb - - 6.4 pIC50 410 nM IC50
glycine receptor α2 subunit/Glycine receptor subunit alpha-2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2328] [GtoPdb: 424] [UniProtKB: P22771]
ChEMBL Inhibition of rat alpha2 homomeric glycine receptor expressed in CHO cells assessed as inhibition of 300 uM glycine-elicited current by outside patch clamp technique B 5.62 pIC50 2400 nM IC50 J. Biol. Chem. (2007) 282: 16016-16035 [PMID:17405877]
5-HT3AB in Human [GtoPdb: 378]
GtoPdb - - 4.2 pIC50 63000 nM IC50 Neuropharmacology (2011) 60: 488-95 [PMID:21059362]
5-HT3A in Human [GtoPdb: 379]
GtoPdb - - 4.96 pIC50 11000 nM IC50 Mol. Pharmacol. (2011) 80: 183-90 [PMID:21505038]
glycine receptor α1 subunit in Human [GtoPdb: 423] [UniProtKB: P23415]
GtoPdb - - 5.3 pIC50 5100 nM IC50
glycine receptor α3 subunit in Human [GtoPdb: 425] [UniProtKB: O75311]
GtoPdb - - 6.4 pIC50 430 nM IC50
glycine receptor β subunit in Human [GtoPdb: 427] [UniProtKB: P48167]
GtoPdb - - 4.6 pIC50 27000 nM IC50
GtoPdb - - 5.1 pIC50 8900 nM IC50
Glycine Receptor (All subtypes) in Human [GtoPdb: 428]
GtoPdb - - 5.3 pIC50 - - - EMBO J. (1992) 11: 4305-11 [PMID:1385113];
J. Biol. Chem. (1995) 270: 13799-806 [PMID:7775436];
J. Neurochem. (2007) 103: 580-9 [PMID:17714449]

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]