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ChEMBL ligand: CHEMBL332347 (BIBP-3226) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 32:
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]