Target Validation Information
TTD ID	T06955
Target Name	C-C chemokine receptor type 4 (CCR4)
Type of Target	Successful
Drug Potency against Target	4-isopropyl-N-(naphthalen-1-yl)thiazol-2-amine	Drug Info	IC50 = 170 nM	[1]
	4-methyl-N-(naphthalen-1-yl)thiazol-2-amine	Drug Info	IC50 = 6400 nM	[1]
	4-tert-butyl-N-(2-isopropylphenyl)thiazol-2-amine	Drug Info	IC50 = 440 nM	[1]
	4-tert-butyl-N-(naphthalen-1-yl)oxazol-2-amine	Drug Info	IC50 = 80 nM	[1]
	4-tert-butyl-N-(naphthalen-1-yl)thiazol-2-amine	Drug Info	IC50 = 80 nM	[1]
	4-tert-butyl-N-m-tolylthiazol-2-amine	Drug Info	IC50 = 2000 nM	[1]
	4-tert-butyl-N-o-tolylthiazol-2-amine	Drug Info	IC50 = 900 nM	[1]
	4-tert-butyl-N-phenylthiazol-2-amine	Drug Info	IC50 = 4500 nM	[1]
	C-014C	Drug Info	IC50 = 13 nM	[3]
	Cenicriviroc	Drug Info	IC50 = 1100 nM	[2]
	N-(4-tert-butylthiazol-2-yl)-1H-indol-4-amine	Drug Info	IC50 = 490 nM	[1]
	N-(4-tert-butylthiazol-2-yl)isoquinolin-5-amine	Drug Info	IC50 = 1500 nM	[1]
	N-(4-tert-butylthiazol-2-yl)quinolin-5-amine	Drug Info	IC50 = 300 nM	[1]
	N-(naphthalen-1-yl)-4-neopentylthiazol-2-amine	Drug Info	IC50 = 220 nM	[1]
	N-(naphthalen-1-yl)-4-phenylthiazol-2-amine	Drug Info	IC50 = 5500 nM	[1]
Action against Disease Model	Mogamulizumab	Drug Info	Mogamuliz uMab reduced t uMor load via enhanced antibody-dependent cell cytotoxicity in preclinical studies and demonstrated promising efficacy in early clinical trials in patients with ATL. In addition, CCR4 also has a role in maintaining T-helper cell type 2 airways inflammation in asthma, and Amgen have acquired the rights to develop mogamuliz uMab for this indication andother non-oncology indications	[4]
References
REF 1	Optimization of 2-aminothiazole derivatives as CCR4 antagonists. Bioorg Med Chem Lett. 2006 May 15;16(10):2800-3.
REF 2	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 3	Discovery of potent CCR4 antagonists: Synthesis and structure-activity relationship study of 2,4-diaminoquinazolines. Bioorg Med Chem. 2008 Jul 15;16(14):7021-32.
REF 4	Mogamulizumab, a humanized mAb against C-C chemokine receptor 4 for the potential treatment of T-cell lymphomas and asthma. Curr Opin Mol Ther. 2010 Dec;12(6):770-9.

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