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Discovery and optimization of a series of quinazolinone-derived antagonists of CXCR3 |
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| Authors: | Johnson Michael Li An-Rong Liu Jiwen Fu Zice Zhu Liusheng Miao Shichang Wang Xuemei Xu Qingge Huang Alan Marcus Andrew Xu Feng Ebsworth Karen Sablan Emmanuel Danao Jay Kumer Jeff Dairaghi Dan Lawrence Chris Sullivan Tim Tonn George Schall Thomas Collins Tassie Medina Julio |
| Institution: | Amgen Inc., 1120 Veterans Boulevard, South San Francisco, CA 94080, USA. |
| Abstract: | A series of quinazolinone-derived inhibitors of the CXCR3 receptor have been synthesized and their affinity for the receptor evaluated. Compounds were evaluated in a (125)I-IP10 displacement assay and in in vitro cell migration assays to IP10, ITAC, and MIG using human peripheral blood mononuclear cells. |
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