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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 31:
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]