Andrew G Cole,
Ilana L Stroke,
Marc-Raleigh Brescia,
Srilatha Simhadri,
Joan J Zhang,
Zahid Hussain,
Michael Snider,
Christopher Haskell, Sofia Ribeiro,
Kenneth C Appell,
Ian Henderson,
Maria L Webb
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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.
Bioorganic & Medicinal Chemistry Letters 02/2006; 16(1):200-3. · 2.55 Impact Factor
