Target Validation Information
TTD ID	T89213
Target Name	Neuropeptide Y receptor type 1 (NPY1R)
Type of Target	Clinical trial
Drug Potency against Target	PD-160170	Drug Info	Afinity = 48 nM	[8]
	4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one	Drug Info	Ki < 1000 nM	[7]
	AcPYY(22-36)	Drug Info	Ki = 118 nM	[3]
	Adp[-Trp-Arg-Nva-Arg-Tyr-NH2]2	Drug Info	Ki = 140 nM	[2]
	BMS-189323	Drug Info	IC50 = 12 nM	[1]
	BMS-245782	Drug Info	IC50 = 39 nM	[1]
	H-[Trp-Arg-Nva-Arg-Tyr]2-NH2	Drug Info	Ki = 220 nM	[2]
	H-[Trp-Arg-Nva-Arg-Tyr]3-NH2	Drug Info	Ki = 30 nM	[2]
	LRHYLNLLTRQRY-NH2	Drug Info	Ki = 210 nM	[4]
	NEUROPEPTIDE-Y	Drug Info	IC50 = 1.2 nM	[6]
	NEUROPEPTIDE-Y	Drug Info	Ki = 0.5 nM	[5]
	Pim[-Trp-Arg-Nva-Arg-Tyr-NH2]2	Drug Info	Ki = 120 nM	[2]
	PYY(22-36)	Drug Info	Ki = 390 nM	[3]
	Sub[-Trp-Arg-Nva-Arg-Tyr-NH2]2	Drug Info	Ki = 90 nM	[2]
	Sub[-Tyr-Arg-Leu-Arg-Tyr-NH2]2	Drug Info	Ki = 7.5 nM	[2]
	[Cys-Trp-Arg-Nva-Arg-Tyr-NH2]2	Drug Info	Ki = 340 nM	[2]
References
REF 1	Isosteric N-arylpiperazine replacements in a series of dihydropyridine NPY1 receptor antagonists. Bioorg Med Chem Lett. 2004 Dec 20;14(24):5975-8.
REF 2	Neuropeptide Y (NPY) Y4 receptor selective agonists based on NPY(32-36): development of an anorectic Y4 receptor selective agonist with picomolar a... J Med Chem. 2006 Apr 20;49(8):2661-5.
REF 3	Identification of selective neuropeptide Y2 peptide agonists. Bioorg Med Chem Lett. 2007 Jan 15;17(2):538-41.
REF 4	A long-acting selective neuropeptide Y2 receptor PEGylated peptide agonist reduces food intake in mice. Bioorg Med Chem Lett. 2007 Apr 1;17(7):1916-9.
REF 5	Guanidine-acylguanidine bioisosteric approach in the design of radioligands: synthesis of a tritium-labeled N(G)-propionylargininamide ([3H]-UR-MK1... J Med Chem. 2008 Dec 25;51(24):8168-72.
REF 6	5-OHKF and NorKA, depsipeptides from a Hawaiian collection of Bryopsis pennata: binding properties for NorKA to the human neuropeptide Y Y1 receptor. J Nat Prod. 2009 Dec;72(12):2172-6.
REF 7	Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 rec... J Med Chem. 2010 Sep 9;53(17):6386-97.
REF 8	NPY Y1 and Y5 receptor selective antagonists as anti-obesity drugs. Curr Top Med Chem. 2007;7(17):1721-33.

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