carfentanil [Ligand Id: 10040] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL290429 ((4-carbomethoxy fentanyl), 4-carbomethoxyfentanyl, Carfentanil, Carfentanyl, R 31833) |
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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 Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143] | ||||||||
| ChEMBL | Binding affinity against Opioid receptor delta 1 | B | 8.48 | pKi | 3.28 | nM | Ki | J Med Chem (2000) 43: 381-391 [PMID:10669565] |
| δ receptor/Delta opioid receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3222] [GtoPdb: 317] [UniProtKB: P32300] | ||||||||
| ChEMBL | Agonist activity at delta opioid receptor in mouse vas deferens assessed as inhibition of electrically-stimulated muscle contraction | B | 7.77 | pIC50 | 17 | nM | IC50 | Bioorg Med Chem (2014) 22: 4581-4586 [PMID:25129170] |
| δ receptor/Delta opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL269] [GtoPdb: 317] [UniProtKB: P33533] | ||||||||
| ChEMBL | Opioid receptor kappa 1 apparent binding constant from rat brain membranes using [3H]DADLE binding assay | B | 8.05 | pKi | 9 | nM | Ki | J Med Chem (1990) 33: 2456-2464 [PMID:2167979] |
| ChEMBL | Displacement of [3H]DSLET from delta opioid receptor in rat brain membranes | B | 8.48 | pKi | 3.3 | nM | Ki | Bioorg Med Chem (2014) 22: 4581-4586 [PMID:25129170] |
| δ receptor in Guinea pig [GtoPdb: 317] | ||||||||
| GtoPdb | Binding affinity-displacement of [3H]DPDPE in guinea pig whole brain | - | 8.48 | pKi | 3.28 | nM | Ki | Mol Pharmacol (1992) 41: 185-96 [PMID:1310142] |
| κ receptor/Kappa opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145] | ||||||||
| ChEMBL | Binding affinity against Opioid receptor kappa 1 | B | 7.37 | pKi | 43.1 | nM | Ki | J Med Chem (2000) 43: 381-391 [PMID:10669565] |
| Kappa opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3952] [UniProtKB: P41144] | ||||||||
| ChEMBL | Opioid receptor kappa 1 apparent binding constant from guinea pig cerebellum using [3H]diprenorphine binding assay | B | 7.04 | pKi | 92 | nM | Ki | J Med Chem (1990) 33: 2456-2464 [PMID:2167979] |
| ChEMBL | Displacement of [3H]U69593 from kappa opioid receptor in guinea pig brain membranes | B | 7.37 | pKi | 43 | nM | Ki | Bioorg Med Chem (2014) 22: 4581-4586 [PMID:25129170] |
| μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372] | ||||||||
| ChEMBL | Binding affinity against Opioid receptor mu 1 | B | 10.62 | pKi | 0.02 | nM | Ki | J Med Chem (2000) 43: 381-391 [PMID:10669565] |
| μ receptor/Mu opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL270] [GtoPdb: 319] [UniProtKB: P33535] | ||||||||
| ChEMBL | Inhibition of [3H]DAGO binding to rat brain membrane Opioid receptor mu 1 | B | 10.05 | pKi | 0.09 | nM | Ki | J Med Chem (1990) 33: 2456-2464 [PMID:2167979] |
| ChEMBL | Displacement of [3H]DAMGO from mu opioid receptor in rat brain membranes | B | 10.62 | pKi | 0.02 | nM | Ki | Bioorg Med Chem (2014) 22: 4581-4586 [PMID:25129170] |
| Mu opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4354] [UniProtKB: P97266] | ||||||||
| ChEMBL | Agonist activity at mu opioid receptor in guinea pig ileum assessed as inhibition of electrically-stimulated muscle contraction | B | 10.72 | pIC50 | 0.02 | nM | IC50 | Bioorg Med Chem (2014) 22: 4581-4586 [PMID:25129170] |
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]
