Biarylsulfonamide CCR9 inhibitors for inflammatory bowel disease

Bioorg Med Chem Lett. 2015 Sep 1;25(17):3661-4. doi: 10.1016/j.bmcl.2015.06.046. Epub 2015 Jun 18.


Inflammatory bowel disease, including Crohn's disease and ulcerative colitis, affects millions of people worldwide. CCR9 has been shown to be a key chemokine receptor mediating the local inflammatory responses in the GI tract. The CCR9 inhibitor Vercirnon advanced to phase 3 clinical trials, but carries several liabilities which we sought to improve.

Keywords: CCR9; Crohn’s disease; IBD; Sulfonamide; Ulcerative colitis.

MeSH terms

  • Animals
  • Chemistry Techniques, Synthetic
  • Drug Evaluation, Preclinical / methods
  • Humans
  • Inflammatory Bowel Diseases / drug therapy*
  • Inhibitory Concentration 50
  • Mice
  • Receptors, CCR / antagonists & inhibitors*
  • Structure-Activity Relationship
  • Sulfonamides / chemistry*
  • Sulfonamides / pharmacology*


  • CC chemokine receptor 9
  • CCX282-B
  • Receptors, CCR
  • Sulfonamides