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Synonyms: GSK 2126458 | GSK-2126458 | GSK2126458
Compound class: Synthetic organic
Comment: Omipalisib (GSK2126458) is a potent dual inhibitor of phosphoinositide 3-kinase α (PI3Kα) and the mammalian target of rapamycin (mTOR). It is compound 1 in . It was originally developed for anti-proliferative activity in cancer, but has been repositioned as a potential idiopathic pulmonary fibrosis (IPF) therapy .
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.✖
1. Knight SD, Adams ND, Burgess JL, Chaudhari AM, Darcy MG, Donatelli CA, Luengo JI, Newlander KA, Parrish CA, Ridgers LH et al.. (2010)
Discovery of GSK2126458, a Highly Potent Inhibitor of PI3K and the Mammalian Target of Rapamycin.
ACS Med Chem Lett, 1 (1): 39-43. [PMID:24900173]
2. Mercer PF, Woodcock HV, Eley JD, Platé M, Sulikowski MG, Durrenberger PF, Franklin L, Nanthakumar CB, Man Y, Genovese F et al.. (2016)
Exploration of a potent PI3 kinase/mTOR inhibitor as a novel anti-fibrotic agent in IPF.
Thorax, 71 (8): 701-11. [PMID:27103349]