CPK20 [Ligand Id: 14038] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL4476393
  • KNa1.1/Potassium channel subfamily T member 1 in Human [ChEMBL: CHEMBL4739688] [GtoPdb: 385] [UniProtKB: Q5JUK3]
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  • KNa1.2/Potassium channel subfamily T member 2 in Human [ChEMBL: CHEMBL4739693] [GtoPdb: 386] [UniProtKB: Q6UVM3]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
KNa1.1/Potassium channel subfamily T member 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4739688] [GtoPdb: 385] [UniProtKB: Q5JUK3]
ChEMBL Inhibition of human KCNT1 (98 to 354 residues) expressed in CHO cells assessed as reduction in thallium fluorescent signal incubated for 15 mins followed by LOX addition measured after 15 mins by FluxOR green dye based fluorescence analysis B 5.19 pIC50 6400 nM IC50 J Med Chem (2024) 67: 9124-9149 [PMID:38782404]
ChEMBL Inhibition of human KCNT1 (98 to 354 residues) expressed in CHO cells at +60 mV holding potential by whole-cell patch clamp electrophysiology method B 6.68 pIC50 210 nM IC50 J Med Chem (2024) 67: 9124-9149 [PMID:38782404]
GtoPdb - - 6.7 pIC50 200 nM IC50 J Med Chem (2024) 67: 9124-9149 [PMID:38782404]
KNa1.2/Potassium channel subfamily T member 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4739693] [GtoPdb: 386] [UniProtKB: Q6UVM3]
ChEMBL Inhibition of human KCNT2 expressed in HEK cells at +60 mV holding potential by whole-cell patch clamp electrophysiology method B 5.9 pIC50 1270 nM IC50 J Med Chem (2024) 67: 9124-9149 [PMID:38782404]
GtoPdb - - 5.9 pIC50 1270 nM IC50 J Med Chem (2024) 67: 9124-9149 [PMID:38782404]

ChEMBL data shown on this page come from version 36:

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]