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 33:
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]
