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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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Bibliografske podrobnosti
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
Format: Artigo
Jezik:Inglês
Izdano: American Chemical Society 2011
Online dostop: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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