Target Validation Information
TTD ID	T02752
Target Name	C-C chemokine receptor type 3 (CCR3)
Type of Target	Discontinued
Drug Potency against Target	Bertilimumab	Drug Info	IC50 = 0.009 uM	[4]
	YM-344031	Drug Info	IC50 = 3 nM	[3]
	Cenicriviroc	Drug Info	IC50 = 2400 nM	[1]
Action against Disease Model	Bertilimumab	Drug Info	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.	[2]
References
REF 1	Highly potent and orally active CCR5 antagonists as anti-HIV-1 agents: synthesis and biological activities of 1-benzazocine derivatives containing ... J Med Chem. 2006 Mar 23;49(6):2037-48.
REF 2	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.
REF 3	In vitro and in vivo characterization of a novel CCR3 antagonist, YM-344031. Biochem Biophys Res Commun. 2006 Jan 27;339(4):1217-23.
REF 4	Competitive Gly/NMDA receptor antagonists. Curr Top Med Chem. 2006;6(8):809-21.

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