Target Validation Information
TTD ID	T09960
Target Name	C-C chemokine receptor type 5 (CCR5)
Type of Target	Successful
Drug Potency against Target	Maraviroc	Drug Info	IC50 = 0.7 nM	[12]
	GW873140	Drug Info	IC50 = 0.6 nM	[12]
	INCB9471	Drug Info	IC50 < 13 nM
	SCH-C	Drug Info	IC50 = 0.69 nM	[11]
	Vicriviroc	Drug Info	Ki = 4 nM	[12]
	Tak-220	Drug Info	IC50 = 3.5 nM	[10]
	TAK-779	Drug Info	Ki = 1.1 nM	[11]
	(2-(4-chlorobenzyloxy)-5-bromophenyl)methanamine	Drug Info	IC50 = 1700 nM	[7]
	4-(2-(4-chlorobenzyloxy)-5-bromobenzyl)morpholine	Drug Info	IC50 = 1000 nM	[6]
	ANIBAMINE	Drug Info	IC50 = 1000 nM	[1]
	Cenicriviroc	Drug Info	IC90 = 0.81 nM	[4]
	GT-1282	Drug Info	IC50 = 64 nM	[8]
	Maraviroc	Drug Info	IC90 < 10 nM	[3]
	N-(2-(4-chlorobenzyloxy)-5-bromobenzyl)ethanamine	Drug Info	IC50 = 1100 nM	[7]
	NIFEVIROC	Drug Info	IC50 = 2.9 nM	[9]
	SCH-210971	Drug Info	IC50 = 1200 nM	[5]
	VARIECOLIN	Drug Info	IC50 = 9000 nM	[2]
References
REF 1	Isolation and structure of antagonists of chemokine receptor (CCR5). J Nat Prod. 2004 Jun;67(6):1036-8.
REF 2	Inhibition of the human chemokine receptor CCR5 by variecolin and variecolol and isolation of four new variecolin analogues, emericolins A-D, from ... J Nat Prod. 2004 Oct;67(10):1681-4.
REF 3	New approaches toward anti-HIV chemotherapy. J Med Chem. 2005 Mar 10;48(5):1297-313.
REF 4	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 5	Chemokine receptor CCR-5 inhibitors produced by Chaetomium globosum. J Nat Prod. 2006 Jul;69(7):1025-8.
REF 6	CCR5 receptor antagonists: discovery and SAR study of guanylhydrazone derivatives. Bioorg Med Chem Lett. 2007 Jan 1;17(1):231-4.
REF 7	CCR5 receptor antagonists: discovery and SAR of novel 4-hydroxypiperidine derivatives. Bioorg Med Chem Lett. 2007 Apr 1;17(7):1883-7.
REF 8	Reduced cardiac side-effect potential by introduction of polar groups: discovery of NIBR-1282, an orally bioavailable CCR5 antagonist which is acti... Bioorg Med Chem Lett. 2008 Mar 15;18(6):2000-5.
REF 9	Studies on the structure-activity relationship of 1,3,3,4-tetra-substituted pyrrolidine embodied CCR5 receptor antagonists. Part 2: Discovery of hi... Bioorg Med Chem Lett. 2010 Sep 1;20(17):5334-6.
REF 10	Anticancer activities of histone deacetylase inhibitors. Nat Rev Drug Discov. 2006 Sep;5(9):769-84.
REF 11	Chemokine receptor-directed agents as novel anti-HIV-1 therapies. Curr Top Med Chem. 2004;4(10):1017-33.
REF 12	An update in the development of HIV entry inhibitors. Curr Top Med Chem. 2007;7(13):1273-89.

If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.