tert-butylphenoxycyclohexanol [Ligand Id: 12607] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL3559801 |
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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 human C-terminal eYFP-fused human NY1 receptor expressed in African green monkey COS7 cells co-expressing delta6Galphaqi4-myr assessed as potentiation of neuropeptide Y-mediated Ca2+ flux by measuring pancreatic polypeptide EC50 at 30 uM treated at 20 secs post baseline detection followed by addition of neuropeptide Y after 140 secs by Fluo2-AM fluorescent dye-based assay (Rvb = 10.3 +/- 0.1 No_unit) | F | 10.4 | pEC50 | 0.04 | nM | EC50 | J Med Chem (2017) 60: 7605-7612 [PMID:28795803] |
| Y2 receptor/Neuropeptide Y receptor type 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4018] [GtoPdb: 306] [UniProtKB: P49146] | ||||||||
| ChEMBL | Positive allosteric modulation of human C-terminal eYFP-fused human NY2 receptor expressed in African green monkey COS7 cells co-expressing delta6Galphaqi4-myr assessed as potentiation of neuropeptide Y-mediated Ca2+ flux by measuring pancreatic polypeptide EC50 at 30 uM treated at 20 secs post baseline detection followed by addition of neuropeptide Y after 140 secs by Fluo2-AM fluorescent dye-based assay (Rvb = 10 +/- 0.1 No_unit) | F | 10.2 | pEC50 | 0.06 | nM | EC50 | J Med Chem (2017) 60: 7605-7612 [PMID:28795803] |
| Y4 receptor/Neuropeptide Y receptor type 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4877] [GtoPdb: 307] [UniProtKB: P50391] | ||||||||
| ChEMBL | Effect on neuropeptide Y-mediated displacement of 125I-pancreatic polypeptide from human C-terminal eYFP-tagged NY4 receptor expressed in HEK293 cell membranes assessed as neuropeptide Y pKi at 30 uM after 5 hrs by by scintillation counting (Rvb = 7.9 +/- 0.2 No_unit) | B | 8.2 | pKi | 6.31 | nM | Ki | J Med Chem (2017) 60: 7605-7612 [PMID:28795803] |
| ChEMBL | Effect on peptide YY-mediated displacement of 125I-pancreatic polypeptide from human C-terminal eYFP-tagged NY4 receptor expressed in HEK293 cell membranes assessed as peptide YY pKi at 30 uM after 5 hrs by by scintillation counting (Rvb = 8 +/- 0.2 No_unit) | B | 8.2 | pKi | 6.31 | nM | Ki | J Med Chem (2017) 60: 7605-7612 [PMID:28795803] |
| ChEMBL | Effect on pancreatic polypeptide-mediated displacement of 125I-pancreatic polypeptide from human C-terminal eYFP-tagged NY4 receptor expressed in HEK293 cell membranes assessed as pancreatic polypeptide pKi at 30 uM after 5 hrs by by scintillation counting (Rvb = 10.2 +/- 0.1 No_unit) | B | 10.2 | pKi | 0.06 | nM | Ki | J Med Chem (2017) 60: 7605-7612 [PMID:28795803] |
| ChEMBL | Positive allosteric modulation of human C-terminal eYFP-fused human NY4 receptor expressed in African green monkey COS7 cells co-expressing delta6Galphaqi4-myr assessed as potentiation of pancreatic polypeptide-mediated Ca2+ flux treated at 20 secs post baseline detection followed by addition of pancreatic polypeptide after 140 secs by Fluo2-AM fluorescent dye based-assay | F | 5.29 | pEC50 | 5100 | nM | EC50 | J Med Chem (2017) 60: 7605-7612 [PMID:28795803] |
| ChEMBL | Positive allosteric modulation of human C-terminal eYFP-fused human NY4 receptor expressed in African green monkey COS7 cells co-expressing delta6Galphaqi4-myr assessed as potentiation of pancreatic polypeptide-mediated Ca2+ flux treated at 20 secs post baseline detection followed by addition of pancreatic polypeptide after 140 secs by Fluo2-AM fluorescent dye based-assay | F | 5.3 | pEC50 | 5011.87 | nM | EC50 | J Med Chem (2017) 60: 7605-7612 [PMID:28795803] |
| ChEMBL | Positive allosteric modulation of human C-terminal eYFP-tagged NY4 receptor expressed in HEK293 cells assessed as potentiation of peptide YY-induced arrestin 3 recruitment by measuring peptide YY EC50 at 30 uM after 30 mins by BRET assay (Rvb = 1600 nM) | B | 6.07 | pEC50 | 845 | nM | EC50 | J Med Chem (2017) 60: 7605-7612 [PMID:28795803] |
| ChEMBL | Positive allosteric modulation of human C-terminal eYFP-tagged NY4 receptor expressed in HEK293 cells assessed as potentiation of peptide YY-induced arrestin 3 recruitment by measuring peptide YY pEC50 at 30 uM after 30 mins by BRET assay (Rvb = 5.8 +/- 0.20 No_unit) | B | 6.1 | pEC50 | 794.33 | nM | EC50 | J Med Chem (2017) 60: 7605-7612 [PMID:28795803] |
| ChEMBL | Positive allosteric modulation of human C-terminal eYFP-tagged NY4 receptor expressed in HEK293 cells assessed as potentiation of neuropeptide Y-induced arrestin 3 recruitment by measuring neuropeptide Y EC50 at 30 uM after 30 mins by BRET assay (Rvb = 1380 nM) | B | 6.35 | pEC50 | 443 | nM | EC50 | J Med Chem (2017) 60: 7605-7612 [PMID:28795803] |
| ChEMBL | Positive allosteric modulation of human C-terminal eYFP-tagged NY4 receptor expressed in HEK293 cells assessed as potentiation of neuropeptide Y-induced arrestin 3 recruitment by measuring neuropeptide Y pEC50 at 30 uM after 30 mins by BRET assay (Rvb = 5.9 +/- 0.15 No_unit) | B | 6.4 | pEC50 | 398.11 | nM | EC50 | J Med Chem (2017) 60: 7605-7612 [PMID:28795803] |
| ChEMBL | Positive allosteric modulation of human C-terminal eYFP-tagged NY4 receptor expressed in HEK293 cells assessed as potentiation of pancreatic polypeptide-induced arrestin 3 recruitment by measuring pancreatic polypeptide EC50 at 30 uM after 30 mins by BRET assay (Rvb = 5.6 nM) | B | 8.35 | pEC50 | 4.5 | nM | EC50 | J Med Chem (2017) 60: 7605-7612 [PMID:28795803] |
| ChEMBL | Positive allosteric modulation of human C-terminal eYFP-tagged NY4 receptor expressed in HEK293 cells assessed as potentiation of pancreatic polypeptide-induced arrestin 3 recruitment by measuring pancreatic polypeptide pEC50 at 30 uM after 30 mins by BRET assay (Rvb = 8.3 +/- 0.12 No_unit) | B | 8.4 | pEC50 | 3.98 | nM | EC50 | J Med Chem (2017) 60: 7605-7612 [PMID:28795803] |
| ChEMBL | Positive allosteric modulation of human NY4 receptor expressed in African green monkey COS7 cells co-expressing delta6Galphaqi4-myr assessed as potentiation of peptide YY induced-calcium flux by measuring peptide YY pEC50 at 30 uM treated at 20 secs post baseline detection followed by addition of peptide YY after 140 secs by Fluo2-AM fluorescent dye based-assay (Rvb = 8.6 +/- 0.08 No_unit) | F | 9.3 | pEC50 | 0.5 | nM | EC50 | J Med Chem (2017) 60: 7605-7612 [PMID:28795803] |
| ChEMBL | Positive allosteric modulation of human NY4 receptor expressed in African green monkey COS7 cells co-expressing delta6Galphaqi4-myr assessed as potentiation of peptide YY induced-calcium flux by measuring peptide YY EC50 at 30 uM treated at 20 secs post baseline detection followed by addition of peptide YY after 140 secs by Fluo2-AM fluorescent dye based-assay (Rvb = 2.6 nM) | F | 9.3 | pEC50 | 0.5 | nM | EC50 | J Med Chem (2017) 60: 7605-7612 [PMID:28795803] |
| ChEMBL | Positive allosteric modulation of human NY4 receptor expressed in African green monkey COS7 cells co-expressing delta6Galphaqi4-myr assessed as potentiation of neuropeptide Y induced-calcium flux by measuring neuropeptide Y EC50 at 30 uM treated at 20 secs post baseline detection followed by addition of neuropeptide Y after 140 secs by Fluo2-AM fluorescent dye based-assay (Rvb = 5.2 nM) | F | 9.4 | pEC50 | 0.4 | nM | EC50 | J Med Chem (2017) 60: 7605-7612 [PMID:28795803] |
| ChEMBL | Positive allosteric modulation of human NY4 receptor expressed in African green monkey COS7 cells co-expressing delta6Galphaqi4-myr assessed as potentiation of neuropeptide Y induced-calcium flux by measuring neuropeptide Y pEC50 at 30 uM treated at 20 secs post baseline detection followed by addition of neuropeptide Y after 140 secs by Fluo2-AM fluorescent dye based-assay (Rvb = 8.3 +/- 0.04 No_unit) | F | 9.4 | pEC50 | 0.4 | nM | EC50 | J Med Chem (2017) 60: 7605-7612 [PMID:28795803] |
| ChEMBL | Positive allosteric modulation of human NY4 receptor expressed in African green monkey COS7 cells co-expressing delta6Galphaqi4-myr assessed as potentiation of pancreatic polypeptide induced-calcium flux by measuring pancreatic polypeptide pEC50 at 30 uM treated at 20 secs post baseline detection followed by addition of pancreatic polypeptide after 140 secs by Fluo2-AM fluorescent dye based-assay (Rvb = 10 +/- 0.04 No_unit) | F | 10.4 | pEC50 | 0.04 | nM | EC50 | J Med Chem (2017) 60: 7605-7612 [PMID:28795803] |
| ChEMBL | Positive allosteric modulation of human NY4 receptor expressed in African green monkey COS7 cells co-expressing delta6Galphaqi4-myr assessed as potentiation of pancreatic polypeptide induced-calcium flux by measuring pancreatic polypeptide EC50 at 30 uM treated at 20 secs post baseline detection followed by addition of pancreatic polypeptide after 140 secs by Fluo2-AM fluorescent dye based-assay (Rvb = 0.1 nM) | F | 10.52 | pEC50 | 0.03 | nM | EC50 | J Med Chem (2017) 60: 7605-7612 [PMID:28795803] |
| Y5 receptor/Neuropeptide Y receptor type 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4561] [GtoPdb: 308] [UniProtKB: Q15761] | ||||||||
| ChEMBL | Positive allosteric modulation of human C-terminal eYFP-fused human NY5 receptor expressed in African green monkey COS7 cells co-expressing delta6Galphaqi4-myr assessed as potentiation of neuropeptide Y-mediated Ca2+ flux by measuring pancreatic polypeptide EC50 at 30 uM treated at 20 secs post baseline detection followed by addition of neuropeptide Y after 140 secs by Fluo2-AM fluorescent dye-based assay (Rvb = 8.5 +/- 0.1 No_unit) | F | 8.5 | pEC50 | 3.16 | nM | EC50 | J Med Chem (2017) 60: 7605-7612 [PMID:28795803] |
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]
