2. Academic Validation
  3. Identification and initial evaluation of 4-N-aryl-[1,4]diazepane ureas as potent CXCR3 antagonists

Identification and initial evaluation of 4-N-aryl-[1,4]diazepane ureas as potent CXCR3 antagonists

  • Bioorg Med Chem Lett. 2006 Jan 1;16(1):200-3. doi: 10.1016/j.bmcl.2005.09.020.
Andrew G Cole 1,  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
Affiliations

Affiliation

  • 1 Pharmacopeia Drug Discovery, Inc., PO Box 5350, Princeton, NJ 08543, USA. acole@pcop.com
PMID: 16213722 DOI: 10.1016/j.bmcl.2005.09.020
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.

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