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Synonyms: AB-1010 | AB1010 | Masican® (proposed trade name)
Compound class: Synthetic organic
Comment: Using the trade name Masivet, this compound has been used for several years to treat mast cell tumours in dogs . It is a receptor tyrosine kinase (RTK) inhibitor, with inhibitory activity at the cKIT, platelet derived growth factor receptor (PDGFR) and fibroblast growth factor receptor (FGFR) RTKs .
SARS-CoV-2: Using X-ray crystallography, masitinib has been shown to bind (non-covalently) into the catalytic site of the SARS-CoV-2 3CL protease (Mpro) , which corresponds with detection of in vitro Mpro inhibitory activity. It does not bind to the other viral protease PLpro.
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.✖
|Masitinib has completed Phase 3 clinical trials for asthma and rheumatoid arthritis, but the outcomes from these trials have not been published. Results from Phase 2 NCT00842270 in asthma , and Phase 2a NCT00831922 in rheumatoid arthritis , were reported in 2009 .|
||EMA orphan drug for mastocytosis.|