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ID: ALA1141624

Journal: Bioorg Med Chem Lett

Title: Discovery of small molecule benzimidazole antagonists of the chemokine receptor CXCR3.

Authors: Hayes ME, Wallace GA, Grongsaard P, Bischoff A, George DM, Miao W, McPherson MJ, Stoffel RH, Green DW, Roth GP.

Abstract: High-throughput screening identified a low molecular weight antagonist of CXCR3 displaying micromolar activity in a membrane filtration-binding assay. Systematic modification of the benzimidazole core and tethered acetophenone moiety established tractable SAR of analogs with improved physicochemical properties and sub-micromolar activity across both human and murine receptors.

CiteXplore: 18242988

DOI: 10.1016/j.bmcl.2008.01.074