ChEMBL ligand: CHEMBL473 (Dofetilide, Tikosyn, UK-68,798, UK-68798)
Kv11.1/HERG in Human [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] There should be some charts here, you may need to enable JavaScript!
Kv10.1 in Human [GtoPdb: 570] [UniProtKB: O95259] There should be some charts here, you may need to enable JavaScript!

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 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]