apamin [Ligand Id: 2311] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL525408 (Apamin)
  • KCa2.1/Small conductance calcium-activated potassium channel protein 1 in Human [ChEMBL: CHEMBL2369] [GtoPdb: 381] [UniProtKB: Q92952]
  • KCa2.1/Small conductance calcium-activated potassium channel protein 1 in Rat [ChEMBL: CHEMBL3743] [GtoPdb: 381] [UniProtKB: P70606]
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  • KCa2.3/Small conductance calcium-activated potassium channel protein 3 in Human [ChEMBL: CHEMBL3381] [GtoPdb: 383] [UniProtKB: Q9UGI6]
  • KCa2.3 in Rat [GtoPdb: 383] [UniProtKB: P70605]
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  • KCa2.2 in Human [GtoPdb: 382] [UniProtKB: Q9H2S1]
  • 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
KCa2.1/Small conductance calcium-activated potassium channel protein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2369] [GtoPdb: 381] [UniProtKB: Q92952]
GtoPdb - - 8.48 pIC50 3.3 nM IC50 Br. J. Pharmacol. (2000) 129: 627-30 [PMID:10683185];
Toxicon (2004) 43: 933-49 [PMID:15208027];
Br. J. Pharmacol. (2000) 129: 991-9 [PMID:10696100]
ChEMBL Displacement of radiolabeled apamin from calcium-activated SK channel B 10.85 pIC50 0.01 nM IC50 J. Med. Chem. (2008) 51: 7094-7098 [PMID:18983139]
KCa2.1/Small conductance calcium-activated potassium channel protein 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3743] [GtoPdb: 381] [UniProtKB: P70606]
ChEMBL Inhibition of rat SK Calcium channel B 10.62 pIC50 0.02 nM IC50 Bioorg. Med. Chem. (2010) 18: 7675-7699 [PMID:20875743]
KCa2.3/Small conductance calcium-activated potassium channel protein 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3381] [GtoPdb: 383] [UniProtKB: Q9UGI6]
GtoPdb - - 9.1 pIC50 0.8 nM IC50 Neuropharmacology (2001) 40: 772-83 [PMID:11369031];
Mol. Pharmacol. (2004) 65: 788-801 [PMID:14978258]
ChEMBL Inhibition of Kca2.3 channel expressed in HEK293 cells by thallium flux assay B 9.77 pIC50 0.17 nM IC50 Bioorg. Med. Chem. Lett. (2008) 18: 5694-5697 [PMID:18824351]
ChEMBL Inhibition of Kca2.3 channel expressed in HEK293 cells by thallium flux assay B 9.77 pIC50 0.17 nM IC50 Bioorg. Med. Chem. Lett. (2008) 18: 5316-5319 [PMID:18774291]
ChEMBL Inhibition of Kca2.3 channel expressed in HEK293 cells by electrophysiology assay B 10.19 pIC50 0.06 nM IC50 Bioorg. Med. Chem. Lett. (2008) 18: 5694-5697 [PMID:18824351]
ChEMBL Inhibition of Kca2.3 channel expressed in HEK293 cells by electrophysiology assay B 10.19 pIC50 0.06 nM IC50 Bioorg. Med. Chem. Lett. (2008) 18: 5316-5319 [PMID:18774291]
KCa2.3 in Rat [GtoPdb: 383] [UniProtKB: P70605]
GtoPdb - - 9.2 pIC50 - - - Am. J. Physiol., Cell Physiol. (2001) 280: C836-42 [PMID:11245600];
J. Physiol. (Lond.) (2001) 535: 323-34 [PMID:11533126]
KCa2.2 in Human [GtoPdb: 382] [UniProtKB: Q9H2S1]
GtoPdb - - 9.4 pKd 0.3 nM Kd FEBS Lett. (2000) 469: 196-202 [PMID:10713270]
KCa2.2 in Rat [GtoPdb: 382] [UniProtKB: P70604]
GtoPdb - - 10.2 pIC50 - - - Science (1996) 273: 1709-14 [PMID:8781233];
Br. J. Pharmacol. (2000) 129: 991-9 [PMID:10696100]

ChEMBL data shown on this page come from version 25:

A.P. Bento, A. Gaulton, A. Hersey, et al. (2014). The ChEMBL bioactivity database: an update. Nucl. Acids Res. Database Issue. 42 D1083-D1090. [PMID:24214965]