RPR260243 [Ligand Id: 7657] 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: CHEMBL406931 (RPR-260243)
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 Activation of human ERG1 isoform 1 expressed in Xenopus laevis oocytes assessed as increase in peak tail current magnitude by two electrode voltage clamp technique B 4.82 pEC50 15000 nM EC50 Proc Natl Acad Sci U S A (2007) 104: 13827-13832 [PMID:17693551]
ChEMBL Activation of human ERG1 isoform 1 expressed in Xenopus laevis oocytes assessed as shifting of voltage dependence of inactivation towards positive potentials by two electrode voltage clamp technique B 5.1 pEC50 8000 nM EC50 Proc Natl Acad Sci U S A (2007) 104: 13827-13832 [PMID:17693551]

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]