Discovery of INCB3284, a Potent, Selective, and Orally Bioavailable hCCR2 Antagonist

[Image: see text] We report the identification of 13 (INCB3284) as a potent human CCR2 (hCCR2) antagonist. INCB3284 exhibited an IC(50) of 3.7 nM in antagonism of monocyte chemoattractant protein-1 binding to hCCR2, an IC(50) of 4.7 nM in antagonism of chemotaxis activity, an IC(50) of 84 μM in inhi...

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Detalhes bibliográficos
Main Authors: Xue, Chu-Biao, Feng, Hao, Cao, Ganfeng, Huang, Taisheng, Glenn, Joseph, Anand, Rajan, Meloni, David, Zhang, Ke, Kong, Lingquan, Wang, Anlai, Zhang, Yingxin, Zheng, Changsheng, Xia, Michael, Chen, Lihua, Tanaka, Hiroyuki, Han, Qi, Robinson, D. J., Modi, Dilip, Storace, Lou, Shao, Lixin, Sharief, Vaqar, Li, Mei, Galya, Laurine G., Covington, Maryanne, Scherle, Peggy, Diamond, Sharon, Emm, Tom, Yeleswaram, Swamy, Contel, Nancy, Vaddi, Kris, Newton, Robert, Hollis, Greg, Friedman, Steven, Metcalf, Brian
Formato: Artigo
Idioma:Inglês
Publicado em: American Chemical Society 2011
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC4018154/
https://ncbi.nlm.nih.gov/pubmed/24900329
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/ml200030q
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