Assay Detail
Binding
CHEMBL881960
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of [3H]naloxone binding to opioid receptor in presence of NaCl
7
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Publication
Synthesis and biological evaluation of 14-alkoxymorphinans. 2. (-)-N-(cyclopropylmethyl)-4,14-dimethoxymorphinan-6-one, a selective mu opioid receptor antagonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 8.17 | 9.27 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1254682 | LEVALLORPHAN | 4.0 | 2 | 9.27 |
| CHEMBL19019 | NALTREXONE | 4.0 | 1 | 9.21 |
| CHEMBL80 | NALOXONE | 4.0 | 1 | 8.70 |
| CHEMBL322796 | CYPRODIME | — | 2 | 8.35 |
| CHEMBL290543 | — | — | 1 | 5.67 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1254682 | LEVALLORPHAN | IC50 | = | 0.54 | nM | 9.27 |
| CHEMBL19019 | NALTREXONE | IC50 | = | 0.62 | nM | 9.21 |
| CHEMBL1254682 | LEVALLORPHAN | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL80 | NALOXONE | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL322796 | CYPRODIME | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL322796 | CYPRODIME | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL290543 | — | IC50 | = | 2150.0 | nM | 5.67 |