apamin [Ligand Id: 2311] 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: 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]
There should be some charts here, you may need to enable JavaScript!
  • 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]
There should be some charts here, you may need to enable JavaScript!
  • KCa2.2 in Human [GtoPdb: 382] [UniProtKB: Q9H2S1]
  • KCa2.2 in Rat [GtoPdb: 382] [UniProtKB: P70604]
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
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 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]