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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