Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
 

 

Target Validation Information
TTD IDTTDC00193
Target NameNeuropeptide Y receptor type 1    
Type of TargetClinical trial target    
Drug Potency against TargetBenzylamine derivativeIC50 = 67 nM[1]
PD-160170Afinity = 48 nM[2]
PD-160170IC50 = 48 nM[3]
neuropeptide YIC50 = 1.2 nM[4]
N-arylpiperazine derivativeIC50 = 10 nM[5]
BMS-189323IC50 = 12 nM[5]
N-arylpiperazine derivativeIC50 = 14 nM[5]
N-arylpiperazine derivativeIC50 = 28 nM[5]
N-arylpiperazine derivativeIC50 = 3 nM[5]
N-arylpiperazine derivativeIC50 = 3 nM[5]
BMS-245782IC50 = 39 nM[5]
N-arylpiperazine derivativeIC50 = 4 nM[5]
N-arylpiperazine derivativeIC50 = 4 nM[5]
N-arylpiperazine derivativeIC50 = 5 nM[5]
ECONAZOLE NITRATEIC50 = 5146 nM[6]
N-arylpiperazine derivativeIC50 = 8 nM[5]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-oneKi < 1000 nM[7]
NEUROPEPTIDE-YKi = 0.5 nM[8]
BIBP-3226Ki = 1.3 nM[9]
AcPYY(22-36)Ki = 118 nM[10]
Pim[-Trp-Arg-Nva-Arg-Tyr-NH2]2Ki = 120 nM[11]
Adp[-Trp-Arg-Nva-Arg-Tyr-NH2]2Ki = 140 nM[11]
PYY(3-36)Ki = 21 nM[10]
LRHYLNLLTRQRY-NH2Ki = 210 nM[12]
H-[Trp-Arg-Nva-Arg-Tyr]2-NH2Ki = 220 nM[11]
N-arylpiperazine derivativeKi = 3.6 nM[5]
H-[Trp-Arg-Nva-Arg-Tyr]3-NH2Ki = 30 nM[11]
[Cys-Trp-Arg-Nva-Arg-Tyr-NH2]2Ki = 340 nM[11]
PYY(22-36)Ki = 390 nM[10]
Sub[-Tyr-Arg-Leu-Arg-Tyr-NH2]2Ki = 7.5 nM[11]
Sub[-Trp-Arg-Nva-Arg-Tyr-NH2]2Ki = 90 nM[11]
Action against Disease ModelBenzylamine derivativeThe original application reported that the benzylamine derivative 14 has potent Y1 affinity in SK-N-MC cells (IC50 = 67 nM).[13]
The Effect of Target Knockout, Knockdown or Genetic VariationsDecreased food intake decreased weight on ob/ob mice background[14]
Ref 1NPY-Ergic agents for the treatment of obesity. Drug Development Research. Volume 51 Issue 2, Pages 94 - 111 To Reference
Ref 2Curr Top Med Chem. 2007;7(17):1721-33.NPY Y1 and Y5 receptor selective antagonists as anti-obesity drugs. To Reference
Ref 3Pharmacol Biochem Behav. 2003 Mar;74(4):811-25.The glycine transporter-1 inhibitors NFPS and Org 24461: a pharmacological study. To Reference
Ref 4J 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. To Reference
Ref 5Bioorg Med Chem Lett. 2004 Dec 20;14(24):5975-8.Isosteric N-arylpiperazine replacements in a series of dihydropyridine NPY1 receptor antagonists. To Reference
Ref 6Bioorg Med Chem Lett. 2010 Dec 15;20(24):7331-6. Epub 2010 Oct 21.In silico identification and biochemical evaluation of novel inhibitors of NRH:quinone oxidoreductase 2 (NQO2). To Reference
Ref 7J 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. To Reference
Ref 8J 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. To Reference
Ref 9Bioorg Med Chem. 2010 Sep 1;18(17):6292-304. Epub 2010 Jul 16.N(G)-Acyl-argininamides as NPY Y(1) receptor antagonists: Influence of structurally diverse acyl substituents on stability and affinity. To Reference
Ref 10Bioorg Med Chem Lett. 2007 Jan 15;17(2):538-41. Epub 2006 Oct 7.Identification of selective neuropeptide Y2 peptide agonists. To Reference
Ref 11J 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. To Reference
Ref 12Bioorg 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. To Reference
Ref 13NPY-Ergic agents for the treatment of obesity. Drug Development Research. Volume 51 Issue 2, Pages 94 - 111 To Reference
Ref 14Obes Rev. 2006 Feb;7(1):89-108.Obesity drugs and their targets: correlation of mouse knockout phenotypes with drug effects in vivo. To Reference



 

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