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ChEMBL ligand: CHEMBL525408 (Apamin) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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]