National Center for
4RX9: SYK Catalytic Domain Complexed with a Potent Pyrimidine Inhibitor
J. Med. Chem. (2015) 58 p.1950-1963
We describe the discovery of selective and potent Syk inhibitor 11, which exhibited favorable PK profiles in rat and dog and was found to be active in a collagen-induced arthritis model in rats. Compound 11 was selected for further profiling, but, unfortunately, in GLP toxicological studies it showed liver findings in rat and dog. Nevertheless, 11 could become a valuable tool compound to investigate the rich biology of Syk in vitro and in vivo.