Assay Detail
Binding
CHEMBL758226
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Binding affinity was determined towards opioid receptor mu1 using [3H]DAMGO as radioligand
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. Part 2: 8-formamidocyclazocine analogues.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 16 | 8.03 | 9.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL19019 | NALTREXONE | 4.0 | 1 | 9.77 |
| CHEMBL56585 | CYCLAZOCINE | 2.0 | 1 | 9.49 |
| CHEMBL58646 | — | — | 1 | 9.39 |
| CHEMBL279968 | ETHYLKETOCYCLAZOCINE | — | 1 | 9.11 |
| CHEMBL57628 | — | — | 1 | 8.96 |
| CHEMBL60869 | — | — | 1 | 8.92 |
| CHEMBL56695 | — | — | 1 | 8.72 |
| CHEMBL56246 | — | — | 1 | 8.72 |
| CHEMBL59314 | — | — | 1 | 8.25 |
| CHEMBL299709 | — | — | 1 | 8.21 |
| CHEMBL298590 | — | — | 1 | 8.08 |
| CHEMBL56357 | — | — | 1 | 6.62 |
| CHEMBL293485 | — | — | 1 | 6.26 |
| CHEMBL56208 | — | — | 1 | 6.24 |
| CHEMBL293103 | — | — | 1 | 6.13 |
| CHEMBL299027 | — | — | 1 | 5.64 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL19019 | NALTREXONE | Ki | = | 0.17 | nM | 9.77 |
| CHEMBL56585 | CYCLAZOCINE | Ki | = | 0.32 | nM | 9.49 |
| CHEMBL58646 | — | Ki | = | 0.41 | nM | 9.39 |
| CHEMBL279968 | ETHYLKETOCYCLAZOCINE | Ki | = | 0.78 | nM | 9.11 |
| CHEMBL57628 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL60869 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL56695 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL56246 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL59314 | — | Ki | = | 5.6 | nM | 8.25 |
| CHEMBL299709 | — | Ki | = | 6.1 | nM | 8.21 |
| CHEMBL298590 | — | Ki | = | 8.3 | nM | 8.08 |
| CHEMBL56357 | — | Ki | = | 240.0 | nM | 6.62 |
| CHEMBL293485 | — | Ki | = | 550.0 | nM | 6.26 |
| CHEMBL56208 | — | Ki | = | 570.0 | nM | 6.24 |
| CHEMBL293103 | — | Ki | = | 740.0 | nM | 6.13 |
| CHEMBL299027 | — | Ki | = | 2300.0 | nM | 5.64 |