[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 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]