enadoline [Ligand Id: 1646] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL318859 (CI-977, Enadolina, Enadoline) |
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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 | Inhibitory activity against Opioid receptor delta 1 in chinese Hamster Ovary (CHO) cell membranes was determined using [3H]naltrindole radioligand | B | 6 | pKi | >1000 | nM | Ki | J Med Chem (2003) 46: 5162-5170 [PMID:14613319] |
| κ receptor/Kappa opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145] | ||||||||
| GtoPdb | - | - | 9.2 | pKd | - | - | - | Mol Pharmacol (1996) 50: 977-84 [PMID:8863844] |
| ChEMBL | Inhibitory activity against Opioid receptor kappa 1 in chinese Hamster Ovary (CHO) cell membranes was determined using [3H]U-69593 radioligand | B | 9.57 | pKi | 0.27 | nM | Ki | J Med Chem (2003) 46: 5162-5170 [PMID:14613319] |
| GtoPdb | - | - | 9.6 | pKi | - | - | - |
J Med Chem (2003) 46: 5162-70 [PMID:14613319]; Br J Pharmacol (1990) 101: 183-9 [PMID:2178014] |
| ChEMBL | Inhibition of Opioid receptor kappa 1 as reduced contraction in electrically stimulated rabbit vas deferens | F | 8.48 | pEC50 | 3.3 | nM | EC50 | Bioorg Med Chem Lett (1997) 7: 291-296 |
| κ receptor/Kappa opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3614] [GtoPdb: 318] [UniProtKB: P34975] | ||||||||
| ChEMBL | Compound was evaluated for the inhibition of binding of [3H]U-69593 to cloned rat Opioid receptor kappa 1 expressed in CHO cell line | B | 10 | pKi | 0.1 | nM | Ki | Bioorg Med Chem Lett (1997) 7: 291-296 |
| μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372] | ||||||||
| ChEMBL | Inhibitory activity against Opioid receptor mu 1 in chinese Hamster Ovary (CHO) cells membranes was determined using [3H]-DAMGO radioligand | B | 7.66 | pKi | 22 | nM | Ki | J Med Chem (2003) 46: 5162-5170 [PMID:14613319] |
| μ receptor/Mu opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL270] [GtoPdb: 319] [UniProtKB: P33535] | ||||||||
| ChEMBL | Compound was evaluated for the inhibition of binding of [3H]DAGO to rat brain mu opioid receptor | B | 7.06 | pKi | 87.4 | nM | Ki | Bioorg Med Chem Lett (1997) 7: 291-296 |
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]
