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. 2019 Dec 30;295(6):1565–1574. doi: 10.1074/jbc.RA119.011857

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© 2020 Scarneo et al.

Published under exclusive license by The American Society for Biochemistry and Molecular Biology, Inc.

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Figure 5. — Selectivity of HS-243 within the human kinome. a, kinome-wide screening of HS-243 against 468 human kinases. b, percentage of inhibition of top kinase hits from kinase screen (percentage of control from vehicle). c, dendrogram of human nononcogenic kinases show selectivity of HS-243 in the human kinome. The size of the dot is indicative of kinase potency. d, IC₅₀ values of top five kinases as determined by DiscoverX kinase assay. The data points represent means ± S.E. (n = 2). e, IC₅₀ values of HS-243 against IRAK-4, IRAK-1, TAK1, CLK4, and DYKR1B (n = 2).