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Synonyms: compound 15 [PMID: 31059256] | example 1156 [WO2014151616A1] | LXH-254 | LXH254
Compound class: Synthetic organic
Comment: Naporafenib (LXH254) is an investigational, potent, selective and orally bioavailable RAF inhibitor that was designed to target RAS mutant cancers, i.e.those that harbour genetic alterations in the RAS-RAF-MEK-ERK (MAPK) pathway . It is one of the compounds claimed in Novartis' patent WO2014151616A1 . Naporafenib is a Type-2 kinase inhibitor that binds the DFG-out conformation of the kinase.
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. Aversa R, Barsanti PA, Burger M, Dillon MP, Dipesa A, Hu C, Lou Y, Nishiguchi G, Pan Y, Polyakov V et al.. (2014)
Biaryl amide compounds as kinase inhibitors.
Patent number: WO2014151616A1. Assignee: Novartis. Priority date: 14/03/2013. Publication date: 25/09/2014.
2. Ramurthy S, Taft BR, Aversa RJ, Barsanti PA, Burger MT, Lou Y, Nishiguchi GA, Rico A, Setti L, Smith A et al.. (2020)
Design and Discovery of N-(3-(2-(2-Hydroxyethoxy)-6-morpholinopyridin-4-yl)-4-methylphenyl)-2-(trifluoromethyl)isonicotinamide, a Selective, Efficacious, and Well-Tolerated RAF Inhibitor Targeting RAS Mutant Cancers: The Path to the Clinic.
J Med Chem, 63 (5): 2013-2027. [PMID:31059256]