Assay Detail
Binding
CHEMBL753521
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of 0.5 nM [3H]bremazocine from guinea pig brain membrane opioid receptor kappa with 100 nM DAGO and 100 nM DPDPE
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 | 7.71 | 8.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL350384 | BREMAZOCINE | 2.0 | 1 | 8.92 |
| CHEMBL19019 | NALTREXONE | 4.0 | 1 | 8.02 |
| CHEMBL80434 | — | — | 1 | 7.77 |
| CHEMBL311912 | — | — | 1 | 7.77 |
| CHEMBL140278 | — | — | 1 | 7.70 |
| CHEMBL76023 | — | — | 1 | 7.68 |
| CHEMBL310785 | — | — | 1 | 7.60 |
| CHEMBL80531 | — | — | 1 | 7.55 |
| CHEMBL2310843 | — | — | 1 | 7.47 |
| CHEMBL78796 | — | — | 1 | 7.36 |
| CHEMBL78932 | — | — | 1 | 7.32 |
| CHEMBL80 | NALOXONE | 4.0 | 1 | 7.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL350384 | BREMAZOCINE | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL19019 | NALTREXONE | IC50 | = | 9.5 | nM | 8.02 |
| CHEMBL80434 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL311912 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL140278 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL76023 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL310785 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL80531 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL2310843 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL78796 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL78932 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL80 | NALOXONE | IC50 | = | 50.0 | nM | 7.30 |