Assay Detail
Binding
CHEMBL757860
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of [3H]- naloxone binding to Opioid receptors in rat brain membrane in the absence of Na
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Publication
Synthesis of analogues of acetylmethadol and methadol as potential narcotic antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 10 | 7.20 | 8.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2107793 | ALPHACETYLMETHADOL | 2.0 | 1 | 8.92 |
| CHEMBL159659 | LEVOMETHADONE | 2.0 | 1 | 8.70 |
| CHEMBL2096625 | — | — | 1 | 8.22 |
| CHEMBL2105619 | BETACETYLMETHADOL | 2.0 | 1 | 7.82 |
| CHEMBL350719 | ESMETHADONE | 3.0 | 1 | 6.96 |
| CHEMBL171118 | — | — | 1 | 6.82 |
| CHEMBL159660 | ALPHAMETHADOL | 2.0 | 1 | 6.64 |
| CHEMBL355396 | — | — | 1 | 6.22 |
| CHEMBL1325 | — | — | 1 | 5.96 |
| CHEMBL367330 | — | — | 1 | 5.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2107793 | ALPHACETYLMETHADOL | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL159659 | LEVOMETHADONE | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL2096625 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL2105619 | BETACETYLMETHADOL | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL350719 | ESMETHADONE | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL171118 | — | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL159660 | ALPHAMETHADOL | Ki | = | 230.0 | nM | 6.64 |
| CHEMBL355396 | — | Ki | = | 600.0 | nM | 6.22 |
| CHEMBL1325 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL367330 | — | Ki | = | 2000.0 | nM | 5.70 |