Assay Detail
Binding
CHEMBL756528
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Concentration for 50% inhibition of [3H]naloxone (1 M) binding to opioid receptor in rat brain membrane was determined in the absence of NaCl
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Publication
Synthesis and biological evaluation of 14-alkoxymorphinans. 1. Highly potent opioid agonists in the series of (-)-14-methoxy-N-methylmorphinan-6-ones.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 9.70 | 10.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL963 | OXYMORPHONE | 4.0 | 1 | 10.89 |
| CHEMBL606711 | — | — | 1 | 10.70 |
| CHEMBL556578 | MORPHINE HYDROCHLORIDE | 3.0 | 1 | 10.30 |
| CHEMBL606767 | — | — | 1 | 10.07 |
| CHEMBL606820 | — | — | 1 | 9.70 |
| CHEMBL606643 | — | — | 1 | 9.70 |
| CHEMBL606770 | — | — | 1 | 9.70 |
| CHEMBL606769 | — | — | 1 | 9.52 |
| CHEMBL606644 | — | — | 1 | 9.52 |
| CHEMBL606768 | — | — | 1 | 9.30 |
| CHEMBL606707 | — | — | 1 | 9.30 |
| CHEMBL606819 | — | — | 1 | 9.12 |
| CHEMBL553032 | — | — | 1 | 9.10 |
| CHEMBL606771 | — | — | 1 | 8.85 |
| CHEMBL80 | NALOXONE | 4.0 | 1 | - |
| CHEMBL540269 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL963 | OXYMORPHONE | IC50 | = | 0.013 | nM | 10.89 |
| CHEMBL606711 | — | IC50 | = | 0.02 | nM | 10.70 |
| CHEMBL556578 | MORPHINE HYDROCHLORIDE | IC50 | = | 0.05 | nM | 10.30 |
| CHEMBL606767 | — | IC50 | = | 0.085 | nM | 10.07 |
| CHEMBL606820 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL606643 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL606770 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL606769 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL606644 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL606768 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL606707 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL606819 | — | IC50 | = | 0.75 | nM | 9.12 |
| CHEMBL553032 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL606771 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL80 | NALOXONE | IC50 | = | 0.009 | nM | - |
| CHEMBL540269 | — | IC50 | = | 0.003 | nM | - |