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    Bioorg Med Chem Lett. 2007 Jun 15;17(12):3339-43. Epub 2007 Apr 6.

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

    Johnson M, Li AR, Liu J, Fu Z, Zhu L, Miao S, Wang X, Xu Q, Huang A, Marcus A, Xu F, Ebsworth K, Sablan E, Danao J, Kumer J, Dairaghi D, Lawrence C, Sullivan T, Tonn G, Schall T, Collins T, Medina J.

    Amgen Inc., 1120 Veterans Boulevard, South San Francisco, CA 94080, USA.

    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.

    PMID: 17448658 [PubMed - indexed for MEDLINE]

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