CyPPA [Ligand Id: 2323] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL453730
  • KCa2.2 in Human [GtoPdb: 382] [UniProtKB: Q9H2S1]
  • KCa2.2/Small conductance calcium-activated potassium channel protein 2 in Rat [ChEMBL: CHEMBL2547] [GtoPdb: 382] [UniProtKB: P70604]
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  • KCa2.3 in Human [GtoPdb: 383] [UniProtKB: Q9UGI6]
  • KCa2.3/Small conductance calcium-activated potassium channel protein 3 in Rat [ChEMBL: CHEMBL3780] [GtoPdb: 383] [UniProtKB: P70605]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
KCa2.2 in Human [GtoPdb: 382] [UniProtKB: Q9H2S1]
GtoPdb - - 4.9 pEC50 - - - Br J Pharmacol (2007) 151: 655-65 [PMID:17486140]
KCa2.2/Small conductance calcium-activated potassium channel protein 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2547] [GtoPdb: 382] [UniProtKB: P70604]
ChEMBL Potentiation of rat KCa2.2a expressed in HEK293 cells at -90 mV holding potential measured at 1 to 2 days by patch clamp electrophysiology B 5.13 pEC50 7480 nM EC50 J Med Chem (2022) 65: 303-322 [PMID:34962403]
KCa2.3 in Human [GtoPdb: 383] [UniProtKB: Q9UGI6]
GtoPdb - - 5.3 pEC50 - - - Br J Pharmacol (2007) 151: 655-65 [PMID:17486140]
KCa2.3/Small conductance calcium-activated potassium channel protein 3 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3780] [GtoPdb: 383] [UniProtKB: P70605]
ChEMBL Displacement of [I125]apamine from Wistar rat recombinant SK3 channel expressed in HEK293 cells B 4.3 pKi >50000 nM Ki J Med Chem (2008) 51: 7625-7634 [PMID:18998663]

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]