Sunday, November 13, 2016

Drugs in Clinical Pipeline: LY2603618 | Kinase Inhibitors | Checkpoint Kinase 1 (CHK1) Inhibitor | Cancer Drug

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.
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