Assay Detail
Binding
CHEMBL2020717
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]DAMGO from mu opioid receptor in mouse whole brain without cerebellum
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis of new opioid derivatives with a propellane skeleton and their pharmacology. Part 2: Propellane derivatives with an amide side chain.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 14 | 7.64 | 9.37 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL490665 | NALFURAFINE HYDROCHLORIDE | 4.0 | 1 | 9.37 |
| CHEMBL2017141 | — | — | 1 | 8.91 |
| CHEMBL2017142 | — | — | 1 | 8.66 |
| CHEMBL2017144 | — | — | 1 | 7.91 |
| CHEMBL2017151 | — | — | 1 | 7.91 |
| CHEMBL2017143 | — | — | 1 | 7.50 |
| CHEMBL2017152 | — | — | 1 | 7.47 |
| CHEMBL2017153 | — | — | 1 | 7.45 |
| CHEMBL2017147 | — | — | 1 | 7.27 |
| CHEMBL2017145 | — | — | 1 | 7.10 |
| CHEMBL2017148 | — | — | 1 | 7.09 |
| CHEMBL2017146 | — | — | 1 | 6.97 |
| CHEMBL2017149 | — | — | 1 | 6.95 |
| CHEMBL2017150 | — | — | 1 | 6.34 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL490665 | NALFURAFINE HYDROCHLORIDE | Ki | = | 0.431 | nM | 9.37 |
| CHEMBL2017141 | — | Ki | = | 1.23 | nM | 8.91 |
| CHEMBL2017142 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL2017144 | — | Ki | = | 12.2 | nM | 7.91 |
| CHEMBL2017151 | — | Ki | = | 12.4 | nM | 7.91 |
| CHEMBL2017143 | — | Ki | = | 31.9 | nM | 7.50 |
| CHEMBL2017152 | — | Ki | = | 33.9 | nM | 7.47 |
| CHEMBL2017153 | — | Ki | = | 35.9 | nM | 7.45 |
| CHEMBL2017147 | — | Ki | = | 54.1 | nM | 7.27 |
| CHEMBL2017145 | — | Ki | = | 79.7 | nM | 7.10 |
| CHEMBL2017148 | — | Ki | = | 80.8 | nM | 7.09 |
| CHEMBL2017146 | — | Ki | = | 106.0 | nM | 6.97 |
| CHEMBL2017149 | — | Ki | = | 112.0 | nM | 6.95 |
| CHEMBL2017150 | — | Ki | = | 453.0 | nM | 6.34 |