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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  • TAS2R14 in Human [GtoPdb: 668] [UniProtKB: Q9NYV8]
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  • TAS2R46 in Human [GtoPdb: 679] [UniProtKB: P59540]
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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]
TAS2R14 in Human [GtoPdb: 668] [UniProtKB: Q9NYV8]
GtoPdb - - 4.74 pEC50 18000 nM EC50 Biochem Biophys Res Commun (2004) 319: 479-85 [PMID:15178431]
TAS2R46 in Human [GtoPdb: 679] [UniProtKB: P59540]
GtoPdb - - 4.15 pEC50 70000 nM EC50 J Agric Food Chem (2007) 55: 6236-43 [PMID:17595105]

ChEMBL data shown on this page come from version 33:

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]