Assay Detail
Binding
CHEMBL755007
Review assay metadata, readout intent, target linkage, and publication context from the same page.
inhibition of 1.0 nM [3H]- DAGO binding to guinea pig brain membrane opioid receptor mu
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Electrophilic opioid ligands. Oxygen tethered alpha-methylene-gamma-lactone, acrylate, isothiocyanate, and epoxide derivatives of 6 beta-naltrexol.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 8.57 | 9.14 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL19019 | NALTREXONE | 4.0 | 1 | 9.14 |
| CHEMBL350384 | BREMAZOCINE | 2.0 | 1 | 8.74 |
| CHEMBL140278 | — | — | 1 | 8.66 |
| CHEMBL78932 | — | — | 1 | 8.66 |
| CHEMBL2310843 | — | — | 1 | 8.64 |
| CHEMBL76023 | — | — | 1 | 8.60 |
| CHEMBL310785 | — | — | 1 | 8.55 |
| CHEMBL311912 | — | — | 1 | 8.54 |
| CHEMBL80531 | — | — | 1 | 8.47 |
| CHEMBL80434 | — | — | 1 | 8.46 |
| CHEMBL78796 | — | — | 1 | 8.38 |
| CHEMBL80 | NALOXONE | 4.0 | 1 | 8.05 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL19019 | NALTREXONE | IC50 | = | 0.73 | nM | 9.14 |
| CHEMBL350384 | BREMAZOCINE | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL140278 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL78932 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL2310843 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL76023 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL310785 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL311912 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL80531 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL80434 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL78796 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL80 | NALOXONE | IC50 | = | 8.9 | nM | 8.05 |