Benzothiophene containing Rho kinase inhibitors: Efficacy in an animal model of glaucoma

A benzothiophene containing Rho kinase inhibitor was identified in an ultra high-throughput enzymatic assay. SAR studies led to inhibitors with low nM enzymatic IC50s, low or sub-μM cellular EC50s in a novel label-free assay, and in vivo efficacy in a monkey model of ocular hypertension.