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PDGFRα kinase inhibitor 1 is a highly selective type II PDGFRα kinase inhibitor with IC50s of 132 nM and 6115 nM for PDGFRα and PDGFRβ, respectively[1].

PDGFRα kinase inhibitor 1 is a highly selective type II PDGFRα kinase inhibitor with IC50s of 132 nM and 6115 nM for PDGFRα and PDGFRβ, respectively[1]. PDGFRα kinase inhibitor 1 (CHMFL-PDGFR-159, Compound 15i) exhibits weak inhibition to DDR1 kinase (IC50: 2462±126 nM)[1].

PDGFRα: 132 nM (IC₅₀); PDGFRβ: 6115 nM (IC₅₀)

[1]. Wang Q, et al. Discovery of 4-((N-(2-(dimethylamino)ethyl)acrylamido)methyl)-N-(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)benzamide (CHMFL-PDGFR-159) as a highly selective type II PDGFRα kinase inhibitor for PDGFRα driving chronic eosinophilic leukemia. Eur J Med Chem. 2018 Apr 25;150:366-384.