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ID: ALA1148557
Journal: Bioorg Med Chem Lett
Title: Identification and initial evaluation of 4-N-aryl-[1,4]diazepane ureas as potent CXCR3 antagonists.
Authors: Cole AG, Stroke IL, Brescia MR, Simhadri S, Zhang JJ, Hussain Z, Snider M, Haskell C, Ribeiro S, Appell KC, Henderson I, Webb ML.
Abstract: The identification and evaluation of aryl-[1,4]diazepane ureas as functional antagonists of the chemokine receptor CXCR3 are described. Specific examples exhibit IC(50) values of approximately 60 nM in a calcium mobilization functional assay, and dose-dependently inhibit CXCR3 functional response to CXCL11 (interferon-inducible T-cell alpha chemoattractant/I-TAC) as measured by T-cell chemotaxis, with a potency of approximately 100 nM.
CiteXplore: 16213722