Target Validation Information
Target ID T89213
Target Name Neuropeptide Y receptor type 1
Target Type
Research
Drug Potency against Target PD-160170 Drug Info Afinity = 48 nM [552749]
Pim[-Trp-Arg-Nva-Arg-Tyr-NH2]2 Drug Info Ki = 120 nM [528136]
H-[Trp-Arg-Nva-Arg-Tyr]2-NH2 Drug Info Ki = 220 nM [528136]
Sub[-Trp-Arg-Nva-Arg-Tyr-NH2]2 Drug Info Ki = 90 nM [528136]
PYY(22-36) Drug Info Ki = 390 nM [528484]
BMS-189323 Drug Info IC50 = 12 nM [527291]
H-[Trp-Arg-Nva-Arg-Tyr]3-NH2 Drug Info Ki = 30 nM [528136]
Neuropeptide Y Drug Info IC50 = 1.2 nM [530519]
NEUROPEPTIDE-Y Drug Info Ki = 0.5 nM [529844]
AcPYY(22-36) Drug Info Ki = 118 nM [528484]
[Cys-Trp-Arg-Nva-Arg-Tyr-NH2]2 Drug Info Ki = 340 nM [528136]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one Drug Info Ki < 1000 nM [531079]
Sub[-Tyr-Arg-Leu-Arg-Tyr-NH2]2 Drug Info Ki = 7.5 nM [528136]
Adp[-Trp-Arg-Nva-Arg-Tyr-NH2]2 Drug Info Ki = 140 nM [528136]
BMS-245782 Drug Info IC50 = 39 nM [527291]
LRHYLNLLTRQRY-NH2 Drug Info Ki = 210 nM [528667]
The Effect of Target Knockout, Knockdown or Genetic Variations Decreased food intake decreased weight on ob/ob mice background [552749]
References
Ref 552749NPY Y1 and Y5 receptor selective antagonists as anti-obesity drugs. Curr Top Med Chem. 2007;7(17):1721-33.
Ref 528136J Med Chem. 2006 Apr 20;49(8):2661-5.Neuropeptide Y (NPY) Y4 receptor selective agonists based on NPY(32-36): development of an anorectic Y4 receptor selective agonist with picomolar affinity.
Ref 528136J Med Chem. 2006 Apr 20;49(8):2661-5.Neuropeptide Y (NPY) Y4 receptor selective agonists based on NPY(32-36): development of an anorectic Y4 receptor selective agonist with picomolar affinity.
Ref 528136J Med Chem. 2006 Apr 20;49(8):2661-5.Neuropeptide Y (NPY) Y4 receptor selective agonists based on NPY(32-36): development of an anorectic Y4 receptor selective agonist with picomolar affinity.
Ref 528484Bioorg Med Chem Lett. 2007 Jan 15;17(2):538-41. Epub 2006 Oct 7.Identification of selective neuropeptide Y2 peptide agonists.
Ref 527291Bioorg Med Chem Lett. 2004 Dec 20;14(24):5975-8.Isosteric N-arylpiperazine replacements in a series of dihydropyridine NPY1 receptor antagonists.
Ref 528136J Med Chem. 2006 Apr 20;49(8):2661-5.Neuropeptide Y (NPY) Y4 receptor selective agonists based on NPY(32-36): development of an anorectic Y4 receptor selective agonist with picomolar affinity.
Ref 530519J Nat Prod. 2009 Dec;72(12):2172-6.5-OHKF and NorKA, depsipeptides from a Hawaiian collection of Bryopsis pennata: binding properties for NorKA to the human neuropeptide Y Y1 receptor.
Ref 529844J Med Chem. 2008 Dec 25;51(24):8168-72.Guanidine-acylguanidine bioisosteric approach in the design of radioligands: synthesis of a tritium-labeled N(G)-propionylargininamide ([3H]-UR-MK114) as a highly potent and selective neuropeptide Y Y1 receptor antagonist.
Ref 528484Bioorg Med Chem Lett. 2007 Jan 15;17(2):538-41. Epub 2006 Oct 7.Identification of selective neuropeptide Y2 peptide agonists.
Ref 528136J Med Chem. 2006 Apr 20;49(8):2661-5.Neuropeptide Y (NPY) Y4 receptor selective agonists based on NPY(32-36): development of an anorectic Y4 receptor selective agonist with picomolar affinity.
Ref 531079J Med Chem. 2010 Sep 9;53(17):6386-97.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 receptor agonist with unprecedented selectivity and procognitive potential.
Ref 528136J Med Chem. 2006 Apr 20;49(8):2661-5.Neuropeptide Y (NPY) Y4 receptor selective agonists based on NPY(32-36): development of an anorectic Y4 receptor selective agonist with picomolar affinity.
Ref 528136J Med Chem. 2006 Apr 20;49(8):2661-5.Neuropeptide Y (NPY) Y4 receptor selective agonists based on NPY(32-36): development of an anorectic Y4 receptor selective agonist with picomolar affinity.
Ref 527291Bioorg Med Chem Lett. 2004 Dec 20;14(24):5975-8.Isosteric N-arylpiperazine replacements in a series of dihydropyridine NPY1 receptor antagonists.
Ref 528667Bioorg Med Chem Lett. 2007 Apr 1;17(7):1916-9. Epub 2007 Jan 24.A long-acting selective neuropeptide Y2 receptor PEGylated peptide agonist reduces food intake in mice.

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