2. Academic Validation
  3. Discovery and optimization of a series of quinazolinone-derived antagonists of CXCR3

Discovery and optimization of a series of quinazolinone-derived antagonists of CXCR3

  • Bioorg Med Chem Lett. 2007 Jun 15;17(12):3339-43. doi: 10.1016/j.bmcl.2007.03.106.
Michael Johnson 1,  An-Rong Li,  Jiwen Liu,  Zice Fu,  Liusheng Zhu,  Shichang Miao,  Xuemei Wang,  Qingge Xu,  Alan Huang,  Andrew Marcus,  Feng Xu,  Karen Ebsworth,  Emmanuel Sablan,  Jay Danao,  Jeff Kumer,  Dan Dairaghi,  Chris Lawrence,  Tim Sullivan,  George Tonn,  Thomas Schall,  Tassie Collins,  Julio Medina
Affiliations

Affiliation

  • 1 Amgen Inc., 1120 Veterans Boulevard, South San Francisco, CA 94080, USA.
PMID: 17448658 DOI: 10.1016/j.bmcl.2007.03.106
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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