LY2603618
[(R)-1-(5-bromo-4-methyl-2-(2-(morpholin-2-yl)ethyl)phenyl)-3-(5-methylpyrazin-2-yl)urea]
is a potent and selective small molecule inhibitor of Checkpoint Kinase 1
(CHK1) protein kinase activity in vitro
(IC50 = 7 nM). Moreover, it shows no significant activity towards
CHK2 (IC50 = 12000 nM). LY2603618 showed an IC50 value
greater than 20 uM for a large number of kinases in a selectivity profiling
assay.
It carries the distinction of being the first selective CHK1 inhibitor to enter clinical cancer trials.
It carries the distinction of being the first selective CHK1 inhibitor to enter clinical cancer trials.
