Discovery of small molecule benzimidazole antagonists of the chemokine receptor CXCR3
ME Hayes, GA Wallace, P Grongsaard… - Bioorganic & medicinal …, 2008 - Elsevier
ME Hayes, GA Wallace, P Grongsaard, A Bischoff, DM George, W Miao, MJ McPherson…
Bioorganic & medicinal chemistry letters, 2008•ElsevierHigh-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.
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.
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.
Elsevier