Assay Detail
Binding
CHEMBL754075
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of 0.5 nM [3H]bremazocine binding to guinea pig brain membrane opioid receptors
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
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 | 7.94 | 8.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL350384 | BREMAZOCINE | 2.0 | 1 | 8.82 |
| CHEMBL19019 | NALTREXONE | 4.0 | 1 | 8.24 |
| CHEMBL311912 | — | — | 1 | 7.96 |
| CHEMBL76023 | — | — | 1 | 7.96 |
| CHEMBL80434 | — | — | 1 | 7.92 |
| CHEMBL2310843 | — | — | 1 | 7.92 |
| CHEMBL140278 | — | — | 1 | 7.89 |
| CHEMBL310785 | — | — | 1 | 7.85 |
| CHEMBL78932 | — | — | 1 | 7.82 |
| CHEMBL80531 | — | — | 1 | 7.75 |
| CHEMBL78796 | — | — | 1 | 7.72 |
| CHEMBL80 | NALOXONE | 4.0 | 1 | 7.37 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL350384 | BREMAZOCINE | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL19019 | NALTREXONE | IC50 | = | 5.7 | nM | 8.24 |
| CHEMBL311912 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL76023 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL80434 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL2310843 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL140278 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL310785 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL78932 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL80531 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL78796 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL80 | NALOXONE | IC50 | = | 43.0 | nM | 7.37 |