Discovery of INCB8761/PF-4136309, a Potent, Selective, and Orally Bioavailable CCR2 Antagonist

[Image: see text] We report the discovery of a new (S)-3-aminopyrrolidine series of CCR2 antagonists. Structure–activity relationship studies on this new series led to the identification of 17 (INCB8761/PF-4136309) that exhibited potent CCR2 antagonistic activity, high selectivity, weak hERG activit...

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Main Authors: Xue, Chu-Biao, Wang, Anlai, Han, Qi, Zhang, Yingxin, Cao, Ganfeng, Feng, Hao, Huang, Taisheng, Zheng, Changsheng, Xia, Michael, Zhang, Ke, Kong, Lingquan, Glenn, Joseph, Anand, Rajan, Meloni, David, Robinson, D. J., Shao, Lixin, Storace, Lou, Li, Mei, Hughes, Robert O., Devraj, Rajesh, Morton, Philip A., Rogier, D. Joseph, Covington, Maryanne, Scherle, Peggy, Diamond, Sharon, Emm, Tom, Yeleswaram, Swamy, Contel, Nancy, Vaddi, Kris, Newton, Robert, Hollis, Greg, Metcalf, Brian
Formato: Artigo
Idioma:Inglês
Publicado em: American Chemical Society 2011
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC4018168/
https://ncbi.nlm.nih.gov/pubmed/24900280
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/ml200199c
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