Identify novel inhibitors of MLCK,by detecting substrate phosphorylation using HTRF as a readout
Here we present the synthesis and biological activity of a series of 7-substituted-1-(3-bromophenylamino)isoquinoline-4-carbonitriles as inhibitors of myosin light chain kinase (MLCK) and the epidermal growth factor receptor kinase (EGFR). The inhibitory effect of these molecules was found to be dependent on the nature of the substituents at the 7-position of the isoquinoline scaffold.
Bioorg Med Chem. 2011;19(1):429-39.