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. 2020 Apr 21;15(4):e0231877. doi: 10.1371/journal.pone.0231877

Fig 1. Molecular structure and In Vitro profile of INCB054828.

Fig 1

(A) Molecular structure of INCB054828. (B) Potency of INCB054828 against FGFR kinases. Activity of recombinant human enzymes was assayed as described at the Michaelis–Menten constant (Km) ATP for each enzyme. The mean IC50 and S.D. for 6 (FGFR4) or 8 (FGFR1, FGFR2, FGFR3, KDR) independent experiments using multiple lots of inhibitor is reported. (C) Selectivity profile of INCB054828. Biochemical IC50 values of INCB054828 for 56 kinases. Small gray circles indicate tested kinases with IC50 >10,000 nM. Among non-FGFRs, KDR and c-KIT were the only kinases inhibited with an IC50 value <1,000 nM.