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Assays for the Identification of Novel Antivirals against Bluetongue Virus
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BMS-813160: A Potent CCR2 and CCR5 Dual Antagonist Selected as a Clinical Candidate
Robert J Cherney1, Prakash Anjanappa2, Kumaravel Selvakumar2
1Bristol Myers Squibb Company, Research and Early Development, Princeton, New Jersey 08540-4000, United States.
Abstract:
BMS-813160 (compound 3) was identified as a potent and selective CCR2/5 dual antagonist. Compound 3 displayed good permeability at pH = 7.4 in PAMPA experiments and demonstrated excellent human liver microsome stability. Pharmacokinetic studies established that 3 had excellent oral bioavailability and exhibited low clearance in dog and cyno. Compound 3 was also studied in the mouse thioglycollate-induced peritonitis model, which confirmed its ability to inhibit the migration of inflammatory monocytes and macrophages. As a result of this profile, compound 3 was selected as a clinical candidate.
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