dofetilide [Ligand Id: 2604] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL473 (Dofetilide, Tikosyn, UK-68798, UK-68,798)
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  • Kv10.1 in Human [GtoPdb: 570] [UniProtKB: O95259]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Binding affinity at hERG expressed in HEK293 cells by fluorescence polarization assay B 8.11 pKi 7.7 nM Ki J. Med. Chem. (2007) 50: 2931-2941 [PMID:17536794]
GtoPdb - - 8.19 pKi 6.4 nM Ki J Med Chem (2007) 50: 2931-41 [PMID:17536794]
ChEMBL Displacement of [3H]dofetilide from hERG expressed in HEK293 cells by SPA B 8.19 pKi 6.4 nM Ki J. Med. Chem. (2007) 50: 2931-2941 [PMID:17536794]
ChEMBL Blockade of the delayed rectifier K+ current (IKr) of guinea pig myocytes F 4.36 pIC50 44000 nM IC50 J. Med. Chem. (1995) 38: 2551-2556 [PMID:7629795]
ChEMBL Inhibition of human ERG expressed in CHO cells by patch clamp method B 5.84 pIC50 1460 nM IC50 Eur J Med Chem (2020) 199: 112395-112395 [PMID:32442850]
ChEMBL Inhibition of rapid delayed inward rectifying potassium current (IKr) in Chinese hamster ovary (CHO) cells stable expressing hERG measured using IonWorks Barracuda automated patch clamp platform F 6.2 pIC50 630.96 nM IC50 J Pharmacol Toxicol Methods (2014) 70: 246-254 [PMID:25087753]
ChEMBL Inhibition of human ERG B 6.7 pIC50 200 nM IC50 J Med Chem (2016) 59: 9489-9502 [PMID:27709945]
ChEMBL Inhibition of rapid delayed inward rectifying potassium current (IKr) in Chinese hamster ovary (CHO) K1 cells stably expressing hERG measured using IonWorks Quattro automated patch clamp platform F 6.9 pIC50 125.89 nM IC50 J Pharmacol Toxicol Methods (2014) 70: 246-254 [PMID:25087753]
ChEMBL Inhibition of human ERG channel in HEK293 cells by voltage-clamp method B 7.31 pIC50 48.98 nM IC50 Eur. J. Med. Chem. (2008) 43: 2479-2488 [PMID:18262683]
ChEMBL Inhibitory concentration against IKr potassium channel B 7.52 pIC50 30 nM IC50 Bioorg. Med. Chem. Lett. (2004) 14: 4771-4777 [PMID:15324906]
ChEMBL Inhibition of human ERG stably expressed in HEK293 cells B 7.82 pIC50 15 nM IC50 J Med Chem (2020) 63: 7186-7210 [PMID:32453591]
ChEMBL K+ channel blocking activity in human embryonic kidney cells expressing HERG Kv11.1 F 7.82 pIC50 15 nM IC50 J. Med. Chem. (2002) 45: 3844-3853 [PMID:12190308]
ChEMBL Inhibition of human ERG stably expressed in HEK293 cells by whole-cell manual patch clamp method B 7.89 pIC50 13 nM IC50 Eur J Med Chem (2020) 206: 112538-112538 [PMID:32927218]
ChEMBL Inhibition of human ERG in MCF7 cells B 7.91 pIC50 12.3 nM IC50 Eur. J. Med. Chem. (2009) 44: 1926-1932 [PMID:19110341]
ChEMBL Inhibition of K+ channel activity in CHO cells expressing HERG Kv11.1 B 8 pIC50 10 nM IC50 Bioorg. Med. Chem. Lett. (2003) 13: 1829-1835 [PMID:12729675]
ChEMBL Inhibition of rapid delayed inward rectifying potassium current (IKr) measured using manual patch clamp assay F 8 pIC50 10 nM IC50 J Pharmacol Toxicol Methods (2014) 70: 246-254 [PMID:25087753]
ChEMBL Inhibitory concentration against potassium channel HERG B 8 pIC50 10 nM IC50 Bioorg. Med. Chem. Lett. (2005) 15: 2886-2890 [PMID:15911273]
ChEMBL Inhibition of human Potassium channel HERG expressed in mammalian cells B 8 pIC50 10 nM IC50 Bioorg. Med. Chem. Lett. (2003) 13: 2773-2775 [PMID:12873512]
ChEMBL Inhibition of human ERG expressed in CHO cells by whole cell patch clamp technique B 8 pIC50 10 nM IC50 Bioorg. Med. Chem. (2008) 16: 6252-6260 [PMID:18448342]
ChEMBL Blockade of hERG expressed in HEK293 cells by whole-cell patch clamp method B 8.04 pIC50 9.2 nM IC50 J. Med. Chem. (2007) 50: 2931-2941 [PMID:17536794]
ChEMBL Inhibition of hERG K channel F 8.3 pIC50 5 nM IC50 Cardiovasc. Res. (2011) 91: 53-61 [PMID:21300721]
ChEMBL Displacement of [3H]astemizole from human ERG K+ channel expressed in HEK293 cells by scintillation spectrophotometric analysis B 8.39 pIC50 4.1 nM IC50 J. Med. Chem. (2013) 56: 2828-2840 [PMID:23473309]
Kv10.1 in Human [GtoPdb: 570] [UniProtKB: O95259]
GtoPdb - - 7.5 pIC50 - - - FEBS Lett (2006) 580: 5059-66 [PMID:16949586]

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, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños 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]