lumacaftor [Ligand Id: 7481] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2103870 (VRT 826809, VX 809, VRT-826809, VX-809, Lumacaftor)
  • CFTR/Cystic fibrosis transmembrane conductance regulator in Human [ChEMBL: CHEMBL4051] [GtoPdb: 707] [UniProtKB: P13569]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
CFTR/Cystic fibrosis transmembrane conductance regulator in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4051] [GtoPdb: 707] [UniProtKB: P13569]
ChEMBL Corrector activity at human CFTR F508 deletion mutant expressed in FRT cells incubated for 25 mins with forskolin by YFP-based fluorescence analysis relative to control B 5.59 pEC50 2600 nM EC50 J. Med. Chem. (2015) 58: 9697-9711 [PMID:26561003]
ChEMBL Corrector activity at CFTR F508-del mutant (unknown origin) B 5.59 pEC50 2600 nM EC50 Eur J Med Chem (2018) 144: 179-200 [PMID:29272749]
ChEMBL Corrector activity at CFTR F508-del mutant (unknown origin) expressed in human CFBE41o cells harboring HS-YFP preincubated for 24 hrs followed by forskolin/genistein stimulation for 30 mins by fluorescence assay B 5.59 pEC50 2570.4 nM EC50 Eur J Med Chem (2018) 144: 179-200 [PMID:29272749]
GtoPdb EC50 determined by measuring F508del-CFTR (expressed in FRT cells) activity (I influx; wih co-expression of a fluorescent YFP halide sensor) in the presence of increasing doses of test compound. - 5.59 pEC50 2600 nM EC50 J. Med. Chem. (2015) 58: 9697-711 [PMID:26561003]

ChEMBL data shown on this page come from version 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños 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]