Assay Detail
Binding
CHEMBL758068
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Compound was evaluated for the inhibition of [3H]- naloxone binding to Opioid receptors in rat brain membrane in the presence of Na
9
Total Activities
9
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 of analogues of acetylmethadol and methadol as potential narcotic antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 9 | 6.09 | 8.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2107793 | ALPHACETYLMETHADOL | 2.0 | 1 | 8.47 |
| CHEMBL159659 | LEVOMETHADONE | 2.0 | 1 | 7.11 |
| CHEMBL2096625 | — | — | 1 | 6.72 |
| CHEMBL2105619 | BETACETYLMETHADOL | 2.0 | 1 | 6.35 |
| CHEMBL171118 | — | — | 1 | 5.70 |
| CHEMBL350719 | ESMETHADONE | 3.0 | 1 | 5.50 |
| CHEMBL355396 | — | — | 1 | 5.30 |
| CHEMBL1325 | — | — | 1 | 5.17 |
| CHEMBL367330 | — | — | 1 | 4.52 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2107793 | ALPHACETYLMETHADOL | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL159659 | LEVOMETHADONE | Ki | = | 77.0 | nM | 7.11 |
| CHEMBL2096625 | — | Ki | = | 190.0 | nM | 6.72 |
| CHEMBL2105619 | BETACETYLMETHADOL | Ki | = | 450.0 | nM | 6.35 |
| CHEMBL171118 | — | Ki | = | 2000.0 | nM | 5.70 |
| CHEMBL350719 | ESMETHADONE | Ki | = | 3200.0 | nM | 5.50 |
| CHEMBL355396 | — | Ki | = | 5000.0 | nM | 5.30 |
| CHEMBL1325 | — | Ki | = | 6800.0 | nM | 5.17 |
| CHEMBL367330 | — | Ki | = | 30000.0 | nM | 4.52 |