MK-499 [Ligand Id: 2607] activity data from GtoPdb and ChEMBL

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL477015 (MK-499)
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 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]