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ChEMBL ligand: CHEMBL473 (Dofetilide, Tikosyn, UK-68798, UK-68,798) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos 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]