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

Robert L. Davis,Mehmet Kahraman,Thomas J. Prins,Yan Beaver,Travis G. Cook,Jessica Cramp,Charmagne S. Cayanan,Elisabeth M.M. Gardiner,Marsha A. McLaughlin,Abbot F. Clark,Mark R. Hellberg,Andrew K. Shiau,Stewart A. Noble,Allen J. Borchardt

Bioorganic & Medicinal Chemistry Letters（2010）

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摘要

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.

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关键词

ROCK,Rho,Kinase,Adhesion,Impedance,Benzothiophene,ATP competitive,Inhibitor,Glaucoma

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