Zobrazeno 1 - 6
of 6
pro vyhledávání: '"Robinson, Darius J."'
Autor:
Brian Metcalf, Sharon Diamond, Taisheng Huang, Lixin Shao, Swamy Yeleswaram, D. Joseph Rogier, Greg Hollis, Michael Xia, Ke Zhang, Ganfeng Cao, Nancy Contel, Lingquan Kong, Peggy Scherle, Maryanne Covington, Tom Emm, Robert Hughes, Joseph Glenn, Robert C. Newton, Kris Vaddi, Changsheng Zheng, Lou Storace, Chu-Biao Xue, Rajan Anand, Hao Feng, Meloni David, Anlai Wang, Mei Li, Philip A. Morton, Robinson Darius J, Qi Han, Rajesh V. Devraj, Yingxin Zhang
Publikováno v:
ACS Medicinal Chemistry Letters. 2:913-918
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, hig
Autor:
Greg Hollis, Changsheng Zheng, Hao Feng, Mei Li, Peggy Scherle, Taisheng Huang, Joseph Glenn, Chu-Biao Xue, Kris Vaddi, Lixin Shao, Brian Metcalf, Tom Emm, Nancy Contel, Ke Zhang, Ganfeng Cao, Dilip P. Modi, Lou Storace, Anlai Wang, Sharon Diamond, Robert C. Newton, Chen Lihua, Steven Friedman, Rajan Anand, Vaqar Sharief, Lingquan Kong, Hiroyuki Tanaka, Meloni David, Maryanne Covington, Michael Xia, Laurine G. Galya, Robinson Darius J, Qi Han, Swamy Yeleswaram, Yingxin Zhang
Publikováno v:
ACS medicinal chemistry letters. 2(6)
We report the identification of 13 (INCB3284) as a potent human CCR2 (hCCR2) antagonist. INCB3284 exhibited an IC50 of 3.7 nM in antagonism of monocyte chemoattractant protein-1 binding to hCCR2, an IC50 of 4.7 nM in antagonism of chemotaxis activity
Autor:
Taisheng Huang, Michael Xia, Rajan Anand, Swamy Yeleswaram, Carrie Brodmerkel, Meloni David, Hao Feng, Maryanne Covington, Kris Vaddi, Sharon Diamond, Chu-Biao Xue, Anlai Wang, Ke Zhang, Ganfeng Cao, Brian Metcalf, Robinson Darius J, Lou Storace, Qi Han, Mei Li, Ling Kong, Peggy Scherle, Joseph Glenn, Lixin Shao, Robert C. Newton, Yingxin Zhang, Changsheng Zheng, Steven Friedman, Greg Hollis
Publikováno v:
Bioorganicmedicinal chemistry letters. 20(24)
Rational design based on a pharmacophore of CCR2 antagonists reported in the literature identified lead compound 9a with potent inhibitory activity against human CCR2 (hCCR2) but moderate activity against murine CCR2 (mCCR2). Modification on 9a led t
Autor:
Winters, Michael P., Robinson, Darius J., Khine, Hnin Hnin, Pullen, Steven S., Woska, Joseph R., Jr., Raymond, Ernest L., Sellati, Rosemarie, Cywin, Charles L., Snow, Roger J., Kashem, Mohammed A., Wolak, John P., King, Josephine, Kaplita, Paul V., Liu, Lisa H., Farrell, Thomas M., DesJarlais, Renee, Roth, Gregory P., Takahashi, Hidenori, Moriarty, Kevin J.
Publikováno v:
In Bioorganic & Medicinal Chemistry Letters 2008 18(20):5541-5544
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Publikováno v:
In Tetrahedron Letters 1994 35(25):4271-4274