Assay Detail
Functional
CHEMBL779644
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Concentration of drug required to inhibit the stereospecific binding of [3H]-naloxone (5 nM) to homogenates of rat brain minus cerebellum in the absence of 100 mM NaCl
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Confidence | 1 — Organism |
| Curated By | Intermediate |
Publication
5-Aryl-3-azabicyclo[3.2.0]heptan-6-one ketals, compounds with morphine-like analgesic activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 6.72 | 8.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1254682 | LEVALLORPHAN | 4.0 | 1 | 8.05 |
| CHEMBL80 | NALOXONE | 4.0 | 1 | 7.34 |
| CHEMBL346515 | — | — | 1 | 7.21 |
| CHEMBL2096625 | — | — | 1 | 7.13 |
| CHEMBL485 | CODEINE | 4.0 | 1 | 5.58 |
| CHEMBL156381 | — | — | 1 | 5.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1254682 | LEVALLORPHAN | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL80 | NALOXONE | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL346515 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL2096625 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL485 | CODEINE | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL156381 | — | IC50 | = | 9924.0 | nM | 5.00 |