Assay Detail
Binding
CHEMBL753769
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of 0.5 nM [3H]- Bremazocine binding to Opioid receptor mu 1 of bovine striatum membrane
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Bos taurus |
| Tissue | Striatum |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Electrophilic alpha-methylene-gamma-lactone and isothiocyanate opioid ligands related to etorphine.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 7.88 | 9.49 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3038194 | — | — | 1 | 9.49 |
| CHEMBL350384 | BREMAZOCINE | 2.0 | 1 | 9.30 |
| CHEMBL2021332 | — | — | 1 | 9.12 |
| CHEMBL3038199 | — | — | 1 | 9.00 |
| CHEMBL281786 | DIPRENORPHINE | 2.0 | 1 | 8.85 |
| CHEMBL80 | NALOXONE | 4.0 | 1 | 8.30 |
| CHEMBL3038197 | — | — | 1 | 8.21 |
| CHEMBL3038193 | — | — | 1 | 7.47 |
| CHEMBL2021335 | — | — | 1 | 7.20 |
| CHEMBL3038198 | — | — | 1 | 6.77 |
| CHEMBL3038195 | — | — | 1 | 6.49 |
| CHEMBL2021333 | — | — | 1 | 6.36 |
| CHEMBL3038196 | — | — | 1 | 5.94 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3038194 | — | IC50 | = | 0.32 | nM | 9.49 |
| CHEMBL350384 | BREMAZOCINE | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL2021332 | — | IC50 | = | 0.76 | nM | 9.12 |
| CHEMBL3038199 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL281786 | DIPRENORPHINE | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL80 | NALOXONE | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3038197 | — | IC50 | = | 6.2 | nM | 8.21 |
| CHEMBL3038193 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL2021335 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL3038198 | — | IC50 | = | 171.0 | nM | 6.77 |
| CHEMBL3038195 | — | IC50 | = | 323.0 | nM | 6.49 |
| CHEMBL2021333 | — | IC50 | = | 434.0 | nM | 6.36 |
| CHEMBL3038196 | — | IC50 | = | 1160.0 | nM | 5.94 |