CTOP [Ligand Id: 1674] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL507214 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| δ receptor/Delta opioid receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3222] [GtoPdb: 317] [UniProtKB: P32300] | ||||||||
| ChEMBL | Antagonist activity against delta opioid receptor in mouse vas deference assessed as effect on DPDPE-induced response | F | 4.87 | pIC50 | 13500 | nM | IC50 | J Med Chem (2008) 51: 5866-5870 [PMID:18800771] |
| δ receptor/Delta opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL269] [GtoPdb: 317] [UniProtKB: P33533] | ||||||||
| ChEMBL | Displacement of [3H]DSLET from DOR in rat brain membrane measured after 2 hrs | B | 6.59 | pKi | 258 | nM | Ki | J Med Chem (2016) 59: 9243-9254 [PMID:27676089] |
| ChEMBL | Inhibition of [3H]-DPDPE binding to Opioid receptor delta 1 of rat brain membranes | B | 4.87 | pIC50 | 13500 | nM | IC50 | J Med Chem (1986) 29: 2370-2375 [PMID:2878079] |
| Kappa opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3952] [UniProtKB: P41144] | ||||||||
| ChEMBL | Displacement of [3H]U69,593 from KOR in guinea pig brain membrane measured after 2 hrs | B | 4.83 | pKi | 14900 | nM | Ki | J Med Chem (2016) 59: 9243-9254 [PMID:27676089] |
| MC1 receptor/Melanocortin receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3795] [GtoPdb: 282] [UniProtKB: Q01726] | ||||||||
| ChEMBL | Effective concentration required for maximum agonist response at melanocortin 1 receptor from frog skin. | F | 7 | pEC50 | 100 | nM | EC50 | J Med Chem (2004) 47: 1514-1526 [PMID:14998337] |
| μ receptor in Human [GtoPdb: 319] [UniProtKB: P35372] | ||||||||
| GtoPdb | - | - | 9.7 | pKi | - | - | - |
Mol Pharmacol (1994) 45: 330-4 [PMID:8114680]; Life Sci (1986) 38: 2221-9 [PMID:2872570] |
| μ receptor/Mu opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL270] [GtoPdb: 319] [UniProtKB: P33535] | ||||||||
| ChEMBL | Displacement of [3H]DAMGO from MOR in rat brain membrane measured after 2 hrs | B | 8.89 | pKi | 1.3 | nM | Ki | J Med Chem (2016) 59: 9243-9254 [PMID:27676089] |
| ChEMBL | Compound was evaluated for the inhibition of binding of [3H]naloxone toOpioid receptor mu 1 of rat brain membranes | B | 8.55 | pIC50 | 2.8 | nM | IC50 | J Med Chem (1986) 29: 2370-2375 [PMID:2878079] |
| Mu opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4354] [UniProtKB: P97266] | ||||||||
| ChEMBL | Antagonist activity against mu opioid receptor in guinea pig ileum assessed as effect on TAPP-induced response | F | 8.55 | pIC50 | 2.8 | nM | IC50 | J Med Chem (2008) 51: 5866-5870 [PMID:18800771] |
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]
