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Miscellaneous (18)

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Abstract #26623 Published in IGR 12-3

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

Davis RL; Kahraman M; Prins TJ; Beaver Y; Cook TG; Cramp J; Cayanan CS; Gardiner EMM; McLaughlin MA; Clark AF
Bioorganic and Medicinal Chemistry Letters 2010; 20: 3361-3366

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We identified a new benzothiophene containing Rho kinase inhibitor scaffold in an ultra high-throughput enzymatic activity screen. SAR studies, driven by a novel label-free cellular impedance assay, were used to derive 39, which substantially reduced intraocular pressure in a monkey model of glaucoma-associated ocular hypertension.

R.L. Davis. Kalypsys, Inc., 10420 Wateridge Circle, San Diego, CA 92121, United States. rdavis@kalypsys.com

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Classification:

11.14 Investigational drugs; pharmacological experiments (Part of: 11 Medical treatment)
5.2 Primates (Part of: 5 Experimental glaucoma; animal models)

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