Target Validation Information
TTD ID	T20331
Target Name	Neuropeptide Y receptor type 5 (NPY5R)
Type of Target	Discontinued
Drug Potency against Target	CGP71683A	Drug Info	IC50 = 1.4 nM	[4]
	NPY5RA-972	Drug Info	IC50 = 3 nM	[6]
	2,4,4-triphenylimidazoline	Drug Info	IC50 = 54 nM	[3]
	AR-129330	Drug Info	IC50 = 2700 nM	[2]
	FR-226928	Drug Info	IC50 = 16 nM	[1]
	FR-230481	Drug Info	IC50 = 0.54 nM	[1]
	FR-233118	Drug Info	IC50 = 0.7 nM	[1]
	FR-73966	Drug Info	IC50 = 53 nM	[1]
Action against Disease Model	CGP71683A	Drug Info	CGP71683A alone induced cell death in a time- and dose-dependent manner in Y5R-expressing cells. The stimulation of MDA MB-231 cell migration by NPY is inhibited by CGP71683A	[5]
References
REF 1	Novel potent antagonists of human neuropeptide Y Y5 receptors. Part 3: 7-methoxy-1-hydroxy-1-substituted tetraline derivatives. Bioorg Med Chem Lett. 2002 Mar 11;12(5):799-802.
REF 2	Lead optimization of 4-(dimethylamino)quinazolines, potent and selective antagonists for the melanin-concentrating hormone receptor 1. Bioorg Med Chem Lett. 2005 Sep 1;15(17):3853-6.
REF 3	Discovery of substituted 2,4,4-triarylimidazoline derivatives as potent and selective neuropeptide Y Y5 receptor antagonists. Bioorg Med Chem Lett. 2009 Mar 15;19(6):1670-4.
REF 4	NPY Y1 and Y5 receptor selective antagonists as anti-obesity drugs. Curr Top Med Chem. 2007;7(17):1721-33.
REF 5	Neuropeptide Y Y5 receptor promotes cell growth through extracellular signal-regulated kinase signaling and cyclic AMP inhibition in a human breast cancer cell line. Mol Cancer Res. 2010 Apr;8(4):604-14.
REF 6	Binding and cAMP studies of melanotropin peptides with the cloned human peripheral melanocortin receptor, hMC1R. Biochem Biophys Res Commun. 1994 Nov 15;204(3):1137-42.

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