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BMS-813160: A Potent CCR2 and CCR5 Dual Antagonist Selected as a Clinical Candidate.

Authors:
Robert J Cherney Prakash Anjanappa Kumaravel Selvakumar Douglas G Batt Gregory D Brown Anne V Rose Ragini Vuppugalla Jing Chen Jian Pang Songmei Xu Melissa Yarde Andrew J Tebben Venkatram Reddy Paidi Mary Ellen Cvijic Arvind Mathur Joel C Barrish Sandhya Mandlekar Qihong Zhao Percy H Carter

ACS Med Chem Lett 2021 Nov 15;12(11):1753-1758. Epub 2021 Oct 15.

Bristol Myers Squibb Company, Research and Early Development, Princeton, New Jersey 08540-4000, United States.

BMS-813160 (compound ) was identified as a potent and selective CCR2/5 dual antagonist. Compound displayed good permeability at pH = 7.4 in PAMPA experiments and demonstrated excellent human liver microsome stability. Pharmacokinetic studies established that had excellent oral bioavailability and exhibited low clearance in dog and cyno. Compound 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 was selected as a clinical candidate.

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http://dx.doi.org/10.1021/acsmedchemlett.1c00373DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8591721PMC
November 2021

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