Target Validation Information | |||||
---|---|---|---|---|---|
Target ID | T02752 | ||||
Target Name | C-C chemokine receptor type 3 | ||||
Target Type | Research |
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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 552416 | Contribution 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 552568 | In 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 552602 | Competitive Gly/NMDA receptor antagonists. Curr Top Med Chem. 2006;6(8):809-21. | ||||
Ref 528083 | J 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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