Discovery of a Potent and Orally Bioavailable CCR2 and CCR5 Dual Antagonist

This report describes the discovery of a potent, orally bioavailable CC chemokine receptor 2 (CCR2) antagonist which, while optimized for CCR2 potency, also had potent CC chemokine receptor 5 (CCR5) activity.

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Bibliographic Details
Published inACS medicinal chemistry letters Vol. 1; no. 1; pp. 14 - 18
Main Authors Pasternak, Alexander, Goble, Stephen D, Struthers, Mary, Vicario, Pasquale P, Ayala, Julia M, Di Salvo, Jerry, Kilburn, Ruth, Wisniewski, Thomas, DeMartino, Julie A, Mills, Sander G, Yang, Lihu
Format Journal Article
LanguageEnglish
Published American Chemical Society 08.04.2010
Subjects
Letter
chemokine, dual antagonist
CCR5
CCR2
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Summary:This report describes the discovery of a potent, orally bioavailable CC chemokine receptor 2 (CCR2) antagonist which, while optimized for CCR2 potency, also had potent CC chemokine receptor 5 (CCR5) activity.
ISSN:1948-5875
1948-5875
DOI:10.1021/ml900009d