dofetilide [Ligand Id: 2604] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL473 (Dofetilide, Tikosyn, UK-68,798, UK-68798) |
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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 34:
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]
