Jul 2026
Discovery of a Potent, Orally Bioavailable Small-Molecule Inhibitor of Wildtype KIT with Exceptionally High Kinome Selectivity.
A highly selective small-molecule KIT inhibitor is described that exhibits excellent broad kinome selectivity, with a selectivity score of S(50%) = 0.003, demonstrated promising in vivo therapeutic efficacy in an SCF-driven acute cutaneous anaphylaxis model in rodents.
Karen Y. Chen, Shiwei Qu, Xue-Lei Yan et al.
· Journal of Medicinal Chemist... · 1 citation