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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主要な著者: 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
フォーマット: Artigo
言語:Inglês
出版事項: American Chemical Society 2011
オンライン･アクセス: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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