Target Validation Information
Target ID T02752
Target Name C-C chemokine receptor type 3
Target Type
Research
Drug Potency against Target YM-344031 Drug Info IC50 = 3 nM [552568]
Bertilimumab Drug Info IC50 = 0.009 uM [552602]
Cenicriviroc Drug Info IC50 = 2400 nM [528083]
Action against Disease Model Bertilimumab Chemotactic activity was significantly increased by an eosinophil chemoattractant in all asthmatic groups relative to healthy subjects (p < 0.05) and was significantly inhibitedby CAT-213 (100 nM) in subjects with moderate and severe asthma, with median inhibition of 52% (p < 0.05), 78% (p < 0.0001), and 86% (p < 0.0001), respectively, in samples representing stable-moderate, unstable-moderate, and severe asthma. [552416] Drug Info
The Effect of Target Knockout, Knockdown or Genetic Variations To further define the co-stimulatory signals mediated by chemokine receptor 3 (CCR3), an eotaxin-1 receptor, effects of CCR3 blockade were tested with an allergic conjunctivitismodel and in ex vivo isolated connective tissue-type mast cells. Our results show that CCR3 blockade significantly suppresses allergen-mediated hypersensitivity reactions as well as IgE-mediated mastcell degranulation [552416]
References
Ref 552416Contribution of eotaxin-1 to eosinophil chemotactic activity of moderate and severe asthmatic sputum. Am J Respir Crit Care Med. 2004 May 15;169(10):1110-7. Epub 2004 Mar 4.
Ref 552568In vitro and in vivo characterization of a novel CCR3 antagonist, YM-344031. Biochem Biophys Res Commun. 2006 Jan 27;339(4):1217-23. Epub 2005 Dec 5.
Ref 552602Competitive Gly/NMDA receptor antagonists. Curr Top Med Chem. 2006;6(8):809-21.
Ref 528083J Med Chem. 2006 Mar 23;49(6):2037-48.Highly potent and orally active CCR5 antagonists as anti-HIV-1 agents: synthesis and biological activities of 1-benzazocine derivatives containing a sulfoxide moiety.

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