[3H]BIBP3226 [Ligand Id: 3474] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL332347 (BIBP-3226)
  • NPFF1 receptor/Neuropeptide FF receptor 1 in Human [ChEMBL: CHEMBL5951] [GtoPdb: 300] [UniProtKB: Q9GZQ6]
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  • NPFF2 receptor/Neuropeptide FF receptor 2 in Human [ChEMBL: CHEMBL5952] [GtoPdb: 301] [UniProtKB: Q9Y5X5]
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  • Y1 receptor/Neuropeptide Y receptor type 1 in Human [ChEMBL: CHEMBL4777] [GtoPdb: 305] [UniProtKB: P25929]
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  • Y2 receptor/Neuropeptide Y receptor type 2 in Human [ChEMBL: CHEMBL4018] [GtoPdb: 306] [UniProtKB: P49146]
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  • Y4 receptor/Neuropeptide Y receptor type 4 in Human [ChEMBL: CHEMBL4877] [GtoPdb: 307] [UniProtKB: P50391]
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  • Y5 receptor/Neuropeptide Y receptor type 5 in Human [ChEMBL: CHEMBL4561] [GtoPdb: 308] [UniProtKB: Q15761]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
NPFF1 receptor/Neuropeptide FF receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5951] [GtoPdb: 300] [UniProtKB: Q9GZQ6]
ChEMBL Competitive antagonist activity at human NPFF1 receptor expressed in COS1 cells assessed as inhibition of NPVF-induced [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation counting F 7.68 pKd 20.89 nM Kd J. Med. Chem. (2012) 55: 6124-6136 [PMID:22708927]
ChEMBL Displacement of [3H]NPVF from human NPFF1 expressed in CHO cells by radioligand binding assay B 7.74 pKi 18 nM Ki J. Med. Chem. (2015) 58: 8834-8849 [PMID:26466164]
ChEMBL Binding affinity to human NPFF1 receptor expressed in CHO cells B 7.92 pKi 12 nM Ki J. Med. Chem. (2015) 58: 8834-8849 [PMID:26466164]
NPFF2 receptor/Neuropeptide FF receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5952] [GtoPdb: 301] [UniProtKB: Q9Y5X5]
ChEMBL Displacement of [3H]EYF from human NPFF2 expressed in CHO cells by radioligand binding assay B 6.6 pKi 250 nM Ki J. Med. Chem. (2015) 58: 8834-8849 [PMID:26466164]
ChEMBL Binding affinity to human NPFF2 receptor expressed in CHO cells B 7.08 pKi 84 nM Ki J. Med. Chem. (2015) 58: 8834-8849 [PMID:26466164]
ChEMBL Agonist activity at human NPFF2 receptor expressed in COS1 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation counting F 6.63 pEC50 233 nM EC50 J. Med. Chem. (2012) 55: 6124-6136 [PMID:22708927]
ChEMBL Agonist activity at human NPFF2 receptor F/Y7.35A mutant assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation counting F 6.95 pEC50 113 nM EC50 J. Med. Chem. (2012) 55: 6124-6136 [PMID:22708927]
Y1 receptor/Neuropeptide Y receptor type 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4777] [GtoPdb: 305] [UniProtKB: P25929]
ChEMBL Binding affinity to NPY1R in human SK-N-MC cells after 2 hrs by liquid scintillation counting assay B 8.68 pKd 2.1 nM Kd J. Med. Chem. (2015) 58: 8834-8849 [PMID:26466164]
GtoPdb - - 8.7 pKd 2.1 nM Kd
ChEMBL Binding affinity for Neuropeptide Y receptor type 1 expressed in AV-12 cells B 5.64 pKi 2315 nM Ki J. Med. Chem. (1997) 40: 3712-3714 [PMID:9371234]
ChEMBL Inhibition of binding of [125I]PYY radioligand to human neuropeptide Y1 receptor in SK-N-MC cell membrane B 7.83 pKi 14.9 nM Ki Bioorg. Med. Chem. Lett. (2002) 12: 379-382 [PMID:11814801]
ChEMBL Displacement of radiolabeled NPY from human Y1R expressed in human SK-N-MC cells B 8.29 pKi 5.1 nM Ki Bioorg. Med. Chem. (2011) 19: 2859-2878 [PMID:21493077]
ChEMBL Displacement of [3H]propionyl-pNPY from neuropeptide Y1 receptor in human SK-N-MC cells B 8.7 pKi 2 nM Ki J. Med. Chem. (2008) 51: 8168-8172 [PMID:19053784]
ChEMBL Displacement of [3H]UR-MK136 from NPY1R in human SK-N-MC cells by radioligand binding assay B 8.82 pKi 1.5 nM Ki J. Med. Chem. (2015) 58: 8834-8849 [PMID:26466164]
ChEMBL Displacement of [3H]propionyl-pNPY from NPY1R in HEL cells after 60 to 90 mins by flow cytometric analysis B 8.82 pKi 1.5 nM Ki J. Med. Chem. (2015) 58: 8834-8849 [PMID:26466164]
ChEMBL Displacement of [3H]UR-MK114 from neuropeptide Y1 receptor in human SK-N-MC cells B 8.82 pKi 1.5 nM Ki J. Med. Chem. (2008) 51: 8168-8172 [PMID:19053784]
ChEMBL Displacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cells B 8.89 pKi 1.3 nM Ki Bioorg. Med. Chem. (2011) 19: 2859-2878 [PMID:21493077]
ChEMBL Displacement of NG-([2,3-3H]propionyl)-BIBP-3226 from NPY Y1 receptor in human SK-N-MC cells B 8.89 pKi 1.3 nM Ki Bioorg. Med. Chem. (2008) 16: 9858-9866 [PMID:18851917]
ChEMBL Displacement of [3H]UR-MK114 from NPY1 receptor in human SK-N-MC cells B 8.89 pKi 1.3 nM Ki Bioorg. Med. Chem. (2010) 18: 6292-6304 [PMID:20688523]
ChEMBL Displacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cells B 8.89 pKi 1.3 nM Ki Bioorg. Med. Chem. (2013) 21: 6303-6322 [PMID:24074877]
ChEMBL Displacement of (R)-Na-Diphenylacetyl-Nomega[2-([2,3-3H]-propionylamino)ethyl]aminocarbonyl (4-hydroxybenzyl)-argininamide from NPY1R in human SK-N-MC cells by radioligand binding assay B 9 pKi 1 nM Ki J. Med. Chem. (2015) 58: 8834-8849 [PMID:26466164]
ChEMBL Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 5 mins by Fura-2 dye based spectrofluorimetric analysis B 7.79 pIC50 16.22 nM IC50 J. Med. Chem. (2015) 58: 8834-8849 [PMID:26466164]
ChEMBL Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 10 secs by Fura-2 dye based spectrofluorimetric analysis B 7.93 pIC50 11.75 nM IC50 J. Med. Chem. (2015) 58: 8834-8849 [PMID:26466164]
ChEMBL Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 10 mins by Fura-2 dye based spectrofluorimetric analysis B 7.99 pIC50 10.23 nM IC50 J. Med. Chem. (2015) 58: 8834-8849 [PMID:26466164]
ChEMBL Inhibition of neuropeptide Y1 receptor in human SK-N-MC cells after 60 mins by scintillation counting B 8.06 pIC50 8.8 nM IC50 J. Nat. Prod. (2009) 72: 2172-2176 [PMID:19916528]
ChEMBL Displacement of (R)-Na-Diphenylacetyl-Nomega[2-([2,3-3H]-propionylamino)ethyl]aminocarbonyl (4-hydroxybenzyl)-argininamide from NPY1R in human SK-N-MC cells B 8.4 pIC50 3.98 nM IC50 J. Med. Chem. (2015) 58: 8834-8849 [PMID:26466164]
ChEMBL Displacement of [3H]UR-MK114 from neuropeptide Y1 receptor in human SK-N-MC cells B 8.44 pIC50 3.63 nM IC50 J. Med. Chem. (2008) 51: 8168-8172 [PMID:19053784]
Y2 receptor/Neuropeptide Y receptor type 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4018] [GtoPdb: 306] [UniProtKB: P49146]
ChEMBL Affinity for human Neuropeptide Y receptor type 2 B 5 pKi >10000 nM Ki J. Med. Chem. (1997) 40: 3712-3714 [PMID:9371234]
Y4 receptor/Neuropeptide Y receptor type 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4877] [GtoPdb: 307] [UniProtKB: P50391]
ChEMBL Affinity for human Neuropeptide Y receptor type 4 B 5 pKi >10000 nM Ki J. Med. Chem. (1997) 40: 3712-3714 [PMID:9371234]
ChEMBL Binding affinity to human neuropeptide Y receptor type 4 receptor expressed in CHO cells using Cy5-[K4]-hPP by flow cytometric analysis B 5.3 pKi >5000 nM Ki Bioorg. Med. Chem. (2013) 21: 6303-6322 [PMID:24074877]
Y5 receptor/Neuropeptide Y receptor type 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4561] [GtoPdb: 308] [UniProtKB: Q15761]
ChEMBL Affinity for human Neuropeptide Y receptor type 5 B 5 pKi >10000 nM Ki J. Med. Chem. (1997) 40: 3712-3714 [PMID:9371234]

ChEMBL data shown on this page come from version 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]