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ChEMBL ligand: CHEMBL477015 (MK-499) |
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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 | Displacement of [35S]MK499 from human ERG expressed in HEK293 cells | B | 6.17 | pIC50 | 670 | nM | IC50 | J Med Chem (2010) 53: 4028-4037 [PMID:20423086] |
ChEMBL | Inhibition of human ERG channel in HEK293 cells by voltage-clamp method | B | 7.67 | pIC50 | 21.38 | nM | IC50 | Eur J Med Chem (2008) 43: 2479-2488 [PMID:18262683] |
Kv10.1 in Human [GtoPdb: 570] [UniProtKB: O95259] | ||||||||
GtoPdb | - | - | 6 | pIC50 | - | - | - |
FEBS Lett (2006) 580: 5059-66 [PMID:16949586]; Mol Pharmacol (2004) 65: 1120-9 [PMID:15102940] |
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]