Submission Details

Design Rationale:

Paper suggests it inhibits MPro with an IC50 of ca. 3 uM. " an alternative explanation is that masitinib exerts its antiviral effect through inhibition of tyrosine kinases, two lines of evidence argue against it: first, our drug-repurposing screen included multiple other tyrosine kinase inhibitors that inhibit the same kinases with equal or better affinities than masitinib and which did not significantly inhibit OC43 infection (table S3)." Second, multiple CRISPR-mediated screens showed that knock-out of these tyrosine kinases did not affect SARS-CoV-2 and other coronaviruses infection (37–39). Nevertheless, it is possible that the inhibition of one or more tyrosine kinases by masitinib contributes to its antiviral activity." "In addition to its direct antiviral effect described here, masitinib has been shown to decrease airway inflammation and improve lung functions in a feline model of asthma (40)."

Other Notes:

worth a punt at seeing if it cocrystallises? Might unearth novel binding?