ChEMBL ligand: CHEMBL473 (Dofetilida, Dofetilide, Tikosyn, UK-68,798, UK-68798)
Kv11.1/Voltage-gated inwardly rectifying potassium channel KCNH2 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/Voltage-gated inwardly rectifying potassium channel KCNH2 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	hERG Inhibition Activity Assay: 1. CHO-hERG cells which have been incubated overnight were added with sample buffer and incubated for 90 minutes at room temperature in darkness.2. The sample buffer was removed and assay buffer was added.3. The compound is added to the cell plate and incubated for 20 minutes in darkness.4. Cell plate was placed into FDSS. The fluorescence signal was recorded every second for 10 seconds. Exciting buffer was added to the cells at the 10th second and the fluorescence signal was recorded every second for 180 seconds5. Data were processed.	B	7.05	pIC50	90	nM	IC50	US-10167299-B2. 1-(3-aminopropyl) substituted cyclic amine compounds, preparation method therefor, and pharmaceutical compositions and uses thereof (2019)
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	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	B	7.82	pIC50	15	nM	IC50	J Med Chem (2020) 63: 7186-7210 [PMID:32453591]
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 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 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	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 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	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 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]