- Advanced search
- Immuno Portal
- Malaria Portal
Synonyms: Kalydeco® | VX-770
ivacaftor is an approved drug (FDA and EMA (2012))
Compound class: Synthetic organic
Comment: Ivacaftor is a cystic fibrosis transmembrane conductance regulator (CFTR) potentiator, the net effect of which is increased chloride channel opening.
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
View more information in the IUPHAR Pharmacology Education Project: ivacaftor
1. Eckford PD, Li C, Ramjeesingh M, Bear CE. (2012)
Cystic fibrosis transmembrane conductance regulator (CFTR) potentiator VX-770 (ivacaftor) opens the defective channel gate of mutant CFTR in a phosphorylation-dependent but ATP-independent manner.
J Biol Chem, 287 (44): 36639-49. [PMID:22942289]
2. Van Goor F, Hadida S, Grootenhuis PD, Burton B, Cao D, Neuberger T, Turnbull A, Singh A, Joubran J, Hazlewood A et al.. (2009)
Rescue of CF airway epithelial cell function in vitro by a CFTR potentiator, VX-770.
Proc Natl Acad Sci USA, 106 (44): 18825-30. [PMID:19846789]