carfentanil [Ligand Id: 10040] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL290429 ((4-carbomethoxy fentanyl), 4-carbomethoxyfentanyl, Carfentanil, Carfentanilo, 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 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]
