VU0506013 [Ligand Id: 14061] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL5420881 |
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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 | Positive allosteric modulation of YFP tagged human Y1 receptor transfected with COS-7 cells co-transfected with delta6Galphaqi4-myr measured after 24 hrs by calcium 2+ flux assay (Rvb = 64.6 pM ) | F | 10.32 | pEC50 | 0.05 | nM | EC50 | J Med Chem (2023) 66: 8745-8766 [PMID:37339079] |
| Y2 receptor/Neuropeptide Y receptor type 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4018] [GtoPdb: 306] [UniProtKB: P49146] | ||||||||
| ChEMBL | Positive allosteric modulation of YFP tagged human Y2 receptor transfected with COS-7 cells co-transfected with delta6Galphaqi4-myr measured after 24 hrs by calcium 2+ flux assay (Rvb = 16.9 pM ) | F | 10.79 | pEC50 | 0.02 | nM | EC50 | J Med Chem (2023) 66: 8745-8766 [PMID:37339079] |
| Y4 receptor/Neuropeptide Y receptor type 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4877] [GtoPdb: 307] [UniProtKB: P50391] | ||||||||
| ChEMBL | Displacement of K22-[TAMRA]-Nle-17,30-PP from human Nluc-Y4R transfected with COS-7 cells assessed as dissociation constant of K22-[TAMRA]-Nle-17,30-PP incubated for 5 mins followed by substrate addition by NanoBRET assay (Rvb = 32 nM ) | B | 7.51 | pKd | 31 | nM | Kd | J Med Chem (2023) 66: 8745-8766 [PMID:37339079] |
| ChEMBL | Displacement of K22-[TAMRA]-Nle-17,30-PP from human Nluc-tagged Y4R transfected with COS-7 cells assessed as inhibition constant of pancreatic polypeptide incubated for 5 mins followed by substrate addition by NanoBRET assay (Rvb = 2.7 nM ) | B | 8.36 | pKi | 4.4 | nM | Ki | J Med Chem (2023) 66: 8745-8766 [PMID:37339079] |
| GtoPdb | - | - | 6.9 | pEC50 | 125 | nM | EC50 | J Med Chem (2023) 66: 8745-8766 [PMID:37339079] |
| ChEMBL | Positive allosteric modulation of human Y4 receptor transfected with COS-7 cells co-transfected with delta6Galphaqi4-myr assessed as potentiation of pancreatic polypeptide EC20 response measured after 240 secs by calcium 2+ flux assay | F | 6.9 | pEC50 | 125.89 | nM | EC50 | J Med Chem (2023) 66: 8745-8766 [PMID:37339079] |
| ChEMBL | Positive allosteric modulation of human Y4 receptor transfected with COS-7 cells co-transfected with delta6Galphaqi4-myr assessed as potentiation of pancreatic polypeptide EC20 response measured after 240 secs by calcium 2+ flux assay | F | 6.9 | pEC50 | 125 | nM | EC50 | J Med Chem (2023) 66: 8745-8766 [PMID:37339079] |
| ChEMBL | Positive allosteric modulation of YFP tagged human Y4 receptor transfected with COS-7 cells co-transfected with delta6Galphaqi4-myr measured after 24 hrs by calcium 2+ flux assay (Rvb = 91.1 pM ) | F | 10.51 | pEC50 | 0.03 | nM | EC50 | J Med Chem (2023) 66: 8745-8766 [PMID:37339079] |
| Y4 receptor/Neuropeptide Y receptor type 4 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105736] [GtoPdb: 307] [UniProtKB: Q61041] | ||||||||
| ChEMBL | Positive allosteric modulation of mouse Y4 receptor transfected with COS-7 cells assessed as activation of G-protein signaling measured after 24 hrs by calcium 2+ flux assay | F | 10.15 | pEC50 | 0.07 | nM | EC50 | J Med Chem (2023) 66: 8745-8766 [PMID:37339079] |
| Y4 receptor/Neuropeptide Y receptor type 4 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4827] [GtoPdb: 307] [UniProtKB: Q63447] | ||||||||
| ChEMBL | Positive allosteric modulation of rat Y4 receptor transfected with COS-7 cells assessed as activation of G-protein signaling measured after 24 hrs by calcium 2+ flux assay | F | 9.51 | pEC50 | 0.31 | nM | EC50 | J Med Chem (2023) 66: 8745-8766 [PMID:37339079] |
| Y5 receptor/Neuropeptide Y receptor type 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4561] [GtoPdb: 308] [UniProtKB: Q15761] | ||||||||
| ChEMBL | Positive allosteric modulation of YFP tagged human Y5 receptor transfected with COS-7 cells co-transfected with delta6Galphaqi4-myr measured after 24 hrs by calcium 2+ flux assay (Rvb = 2.43 nM ) | F | 8.73 | pEC50 | 1.88 | nM | EC50 | J Med Chem (2023) 66: 8745-8766 [PMID:37339079] |
ChEMBL data shown on this page come from version 35:
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]
