ivacaftor [Ligand Id: 4342] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2010601 (Ivacaftor, Kalydeco, VX-770)
  • 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 Potentiation of CFTR G551D mutant (unknown origin) expressed in HEK293 cells incubated for 10 mins in presence of forskolin measured for 2 mins by YFP halide assay B 5.89 pEC50 1300 nM EC50 J Med Chem (2018) 61: 1425-1435 [PMID:29148763]
ChEMBL Potentiation of human CFTR F508del mutant in human bronchial epithelial cells by Ussing chambers recording technique B 6.63 pEC50 236 nM EC50 J. Med. Chem. (2014) 57: 9776-9795 [PMID:25441013]
ChEMBL Corrector activity at human bronchial epithelium CFTR F508del and G551D mutant assessed as increase in channel gating B 6.63 pEC50 236 nM EC50 J. Med. Chem. (2014) 57: 9774-9775 [PMID:25384240]
ChEMBL Potentiation of human CFTR F508del/G551D mutant in human bronchial epithelial cells by Ussing chambers recording technique B 7.66 pEC50 22 nM EC50 J. Med. Chem. (2014) 57: 9776-9795 [PMID:25441013]
ChEMBL Potentiation of human CFTR F508del mutant expressed in mouse NIH-3T3 cells after 30 mins by fluorescent voltage sensing optical assay B 8.52 pEC50 3 nM EC50 J. Med. Chem. (2014) 57: 9776-9795 [PMID:25441013]
ChEMBL Corrector activity at CFTR mutant (unknown origin) by phenotypic screening assay B 8.52 pEC50 3 nM EC50 J. Med. Chem. (2014) 57: 9774-9775 [PMID:25384240]
CYP2D6/Cytochrome P450 2D6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL289] [GtoPdb: 1329] [UniProtKB: P10635]
ChEMBL Inhibition of human ERG B 4.7 pIC50 >20000 nM IC50 J. Med. Chem. (2014) 57: 9776-9795 [PMID:25441013]

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, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos 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]