Target Validation Information
TTD ID	T89988
Target Name	C-C chemokine receptor type 2 (CCR2)
Type of Target	Clinical trial
Drug Potency against Target	Aminoguanidine	Drug Info	IC50 = 5.6 nM
	INCB8696	Drug Info	IC50 = 10 nM	[3]
	RS-504393	Drug Info	IC50 = 89 nM	[2]
	Cenicriviroc	Drug Info	IC50 = 5.9 nM	[1]
Action against Disease Model	Aminoguanidine	Drug Info	INCB3284 exhibited an IC50 of 3.7 nM in antagonism of monocyte chemoattractant protein-1 binding to hCCR2, an IC50 of 4.7 nM in antagonism of chemotaxis activity, an IC50 of 84 |?M in inhibition of the hERG potassi uM current, a free fraction of 58% in protein binding, high selectivity over other chemokine receptors and G-protein-coupled receptors
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	Privileged structures: a useful concept for the rational design of new lead drug candidates. Mini Rev Med Chem. 2007 Nov;7(11):1108-19.
REF 3	Anti-chemokine small molecule drugs: a promising future Expert Opin Investig Drugs. 2010 Mar;19(3):345-55.

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