Lanraplenib

Description: Lanraplenib (GS-9876) is a highly selective and orally active SYK inhibitor (IC50=9.5 nM) being developed for treating inflammatory diseases. It inhibits SYK activity in platelets via the glycoprotein VI (GPVI) receptor without prolonging bleeding time (BT) in monkeys or humans. Target: Syk. Smiles: Nc1cncc(n1)-c1cn2ccnc2c(Nc2ccc(cc2)N2CCN(CC2)C2COC2)n1. References: Di Paolo J, et al. FRI0049 Preclinical Characterization of GS-9876, A Novel, Oral SYK Inhibitor That Shows Efficacy in Multiple Established Rat Models of Collagen-Induced Arthritis.Annals of the Rheumatic Diseases 2016,75:443-444.