neuropeptide Y [Ligand Id: 1504] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL438945 (Human neuropeptide y)
  • Y1 receptor/Neuropeptide Y receptor type 1 in Human [ChEMBL: CHEMBL4777] [GtoPdb: 305] [UniProtKB: P25929]
  • Y1 receptor in Rat [GtoPdb: 305] [UniProtKB: P21555]
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  • Y2 receptor/Neuropeptide Y receptor type 2 in Human [ChEMBL: CHEMBL4018] [GtoPdb: 306] [UniProtKB: P49146]
  • Y2 receptor in Rat [GtoPdb: 306] [UniProtKB: Q9ERC0]
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  • Y4 receptor/Neuropeptide Y receptor type 4 in Human [ChEMBL: CHEMBL4877] [GtoPdb: 307] [UniProtKB: P50391]
  • Y4 receptor in Rat [GtoPdb: 307] [UniProtKB: Q63447]
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  • Y5 receptor/Neuropeptide Y receptor type 5 in Human [ChEMBL: CHEMBL4561] [GtoPdb: 308] [UniProtKB: Q15761]
  • Y5 receptor in Rat [GtoPdb: 308] [UniProtKB: Q63634]
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  • PrRP receptor in Human [GtoPdb: 337] [UniProtKB: P49683]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Y1 receptor/Neuropeptide Y receptor type 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4777] [GtoPdb: 305] [UniProtKB: P25929]
ChEMBL Displacement of Cy5-pNPY from human Y1 receptor expressed in HEL cells after 90 to 120 mins by flow cytometry B 9.3 pKi 0.5 nM Ki J Med Chem (2013) 56: 8422-8431 [PMID:24090364]
ChEMBL Displacement of [125I]Peptide YY from neuropeptide Y receptor type 1 in human SK-N-MC cells after 60 mins B 9.68 pKi 0.21 nM Ki Bioorg Med Chem Lett (2013) 23: 1834-1838 [PMID:23403082]
ChEMBL Binding affinity to human neuropeptide Y receptor type 1 by radioligand displacement assay B 10.02 pKi 0.1 nM Ki Eur J Med Chem (2013) 63: 85-94 [PMID:23466604]
ChEMBL Displacement of [125I]-NPY from Y1 receptor in human MCF7 cells in presence of 1 uM BBN B 8.59 pIC50 2.6 nM IC50 Bioorg Med Chem Lett (2013) 23: 687-692 [PMID:23265893]
ChEMBL Inhibition of neuropeptide Y1 receptor in human SK-N-MC cells after 60 mins by scintillation counting B 8.92 pIC50 1.2 nM IC50 J Nat Prod (2009) 72: 2172-2176 [PMID:19916528]
ChEMBL Displacement of [125I]Peptide YY from neuropeptide Y receptor type 1 in human SK-N-MC cells after 60 mins B 9.66 pIC50 0.22 nM IC50 Bioorg Med Chem Lett (2013) 23: 1834-1838 [PMID:23403082]
ChEMBL Displacement of [125I]peptide YY from Y1 receptor in human SK-N-MC cells measured after 120 mins by scintillation counting method B 9.68 pIC50 0.21 nM IC50 Bioorg Med Chem (2017) 25: 471-482 [PMID:27876250]
ChEMBL Binding affinity to human neuropeptide Y receptor type 1 by radioligand displacement assay B 9.85 pIC50 0.14 nM IC50 Eur J Med Chem (2013) 63: 85-94 [PMID:23466604]
ChEMBL Binding affinity to human neuropeptide Y1 receptor by radioligand displacement assay B 10.15 pIC50 0.07 nM IC50 Bioorg Med Chem (2013) 21: 2764-2771 [PMID:23582449]
Y1 receptor in Rat [GtoPdb: 305] [UniProtKB: P21555]
GtoPdb - - 10.5 pKi - - - Peptides (1997) 18: 397-401 [PMID:9145427]
GtoPdb - - 8.8 pIC50 - - - Mol Pharmacol (1992) 41: 817-21 [PMID:1316999]
Y2 receptor/Neuropeptide Y receptor type 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4018] [GtoPdb: 306] [UniProtKB: P49146]
ChEMBL Displacement of Cy5-pNPY from human Y2 receptor expressed in CHO cells after 90 to 120 mins by flow cytometry B 9.1 pKi 0.8 nM Ki J Med Chem (2013) 56: 8422-8431 [PMID:24090364]
GtoPdb - - 9.5 pKi - - - Mol Pharmacol (1996) 49: 224-8 [PMID:8632753];
J Biol Chem (1995) 270: 26758-61 [PMID:7592910]
ChEMBL Binding affinity to human neuropeptide Y receptor type 2 by radioligand displacement assay B 10.12 pKi 0.08 nM Ki Eur J Med Chem (2013) 63: 85-94 [PMID:23466604]
ChEMBL Compound was evaluated for its inhibitory activity against Y2 receptor of rabbit kidney membrane B 9.3 pIC50 0.5 nM IC50 Bioorg Med Chem Lett (1993) 3: 937-942
ChEMBL Binding affinity to human neuropeptide Y receptor type 2 by radioligand displacement assay B 9.72 pIC50 0.19 nM IC50 Eur J Med Chem (2013) 63: 85-94 [PMID:23466604]
ChEMBL Binding affinity to human neuropeptide Y2 receptor by radioligand displacement assay B 10.05 pIC50 0.09 nM IC50 Bioorg Med Chem (2013) 21: 2764-2771 [PMID:23582449]
ChEMBL Displacement of [125I]peptide YY from Y2 receptor in human KAN-TS cells measured after 60 mins by scintillation counting method B 10.55 pIC50 0.03 nM IC50 Bioorg Med Chem (2017) 25: 471-482 [PMID:27876250]
Y2 receptor in Rat [GtoPdb: 306] [UniProtKB: Q9ERC0]
GtoPdb - - 9.4 pKi - - - Mol Pharmacol (2001) 60: 124-34 [PMID:11408607]
Y4 receptor/Neuropeptide Y receptor type 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4877] [GtoPdb: 307] [UniProtKB: P50391]
ChEMBL Displacement of Cy5-[K4]hPP from human Y4 receptor expressed in CHO cells after 90 to 120 mins by flow cytometry B 6.55 pKi 282 nM Ki J Med Chem (2013) 56: 8422-8431 [PMID:24090364]
GtoPdb - - 8 pKi - - - J Biol Chem (1995) 270: 29123-8 [PMID:7493937]
ChEMBL Agonist activity at human Y4 receptor expressed in sf9 cells assessed as hydrolysis of [gamma-33P]GTP after 2 mins by scintillation counting analysis B 6.38 pEC50 417 nM EC50 J Med Chem (2013) 56: 8422-8431 [PMID:24090364]
Y4 receptor in Rat [GtoPdb: 307] [UniProtKB: Q63447]
GtoPdb - - 6.4 pKi - - - Peptides (1997) 18: 609-12 [PMID:9210181]
GtoPdb - - 8.8 pKi - - - Peptides (1997) 18: 397-401 [PMID:9145427];
Peptides (1997) 18: 609-12 [PMID:9210181]
Y5 receptor/Neuropeptide Y receptor type 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4561] [GtoPdb: 308] [UniProtKB: Q15761]
ChEMBL Displacement of Cy5-pNPY from human Y5 receptor expressed in human HEC-1B cells after 90 to 120 mins by flow cytometry B 8.66 pKi 2.2 nM Ki J Med Chem (2013) 56: 8422-8431 [PMID:24090364]
GtoPdb - - 9.1 pKi - - - J Biol Chem (1996) 271: 26315-9 [PMID:8824284]
ChEMBL Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes. B 8.52 pIC50 3 nM IC50 J Med Chem (2000) 43: 346-350 [PMID:10669561]
Y5 receptor in Rat [GtoPdb: 308] [UniProtKB: Q63634]
GtoPdb - - 9.3 pKi - - - J Biol Chem (1996) 271: 26315-9 [PMID:8824284]
PrRP receptor in Human [GtoPdb: 337] [UniProtKB: P49683]
GtoPdb - - 5.4 pKi - - - Genomics (2005) 85: 688-703 [PMID:15885496]

ChEMBL data shown on this page come from version 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]