title: Discovery of small molecule benzimidazole antagonists of the chemokine receptor CXCR3.
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.
authors.affiliation: Abbott Bioresearch Center, 381 Plantation Street, Worcester, MA 01605, USA. martin.hayes@abbott.com
authors.forename: Martin E
authors.initials: ME
authors.lastname: Hayes
authors.forename: Grier A
authors.initials: GA
authors.lastname: Wallace
authors.forename: Pintipa
authors.initials: P
authors.lastname: Grongsaard
authors.forename: Agnieszka
authors.initials: A
authors.lastname: Bischoff
authors.forename: Dawn M
authors.initials: DM
authors.lastname: George
authors.forename: Wenyan
authors.initials: W
authors.lastname: Miao
authors.forename: Michael J
authors.initials: MJ
authors.lastname: McPherson
authors.forename: Robert H
authors.initials: RH
authors.lastname: Stoffel
authors.forename: David W
authors.initials: DW
authors.lastname: Green
authors.forename: Gregory P
authors.initials: GP
authors.lastname: Roth
mesh_terms: D001562:Benzimidazoles / Q000737:chemistry* / Q000494:pharmacology*; D015394:Molecular Structure; D054367:Receptors, CXCR3 / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
chemical_list: D001562:Benzimidazoles; C515187:CXCR3 protein, human; C515188:Cxcr3 protein, mouse; D054367:Receptors, CXCR3