Assay Detail
Binding
CHEMBL754622
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Binding affinity was determined towards opioid receptor kappa 1 using [3H]U-69593 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 | 8.16 | 9.74 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL56585 | CYCLAZOCINE | 2.0 | 1 | 9.74 |
| CHEMBL19019 | NALTREXONE | 4.0 | 1 | 9.51 |
| CHEMBL57628 | — | — | 1 | 9.31 |
| CHEMBL58646 | — | — | 1 | 9.28 |
| CHEMBL279968 | ETHYLKETOCYCLAZOCINE | — | 1 | 9.21 |
| CHEMBL60869 | — | — | 1 | 9.15 |
| CHEMBL56246 | — | — | 1 | 9.07 |
| CHEMBL299709 | — | — | 1 | 8.92 |
| CHEMBL298590 | — | — | 1 | 8.38 |
| CHEMBL59314 | — | — | 1 | 8.24 |
| CHEMBL56695 | — | — | 1 | 7.66 |
| CHEMBL56357 | — | — | 1 | 6.89 |
| CHEMBL293485 | — | — | 1 | 6.70 |
| CHEMBL293103 | — | — | 1 | 6.34 |
| CHEMBL56208 | — | — | 1 | 6.09 |
| CHEMBL299027 | — | — | 1 | 6.05 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL56585 | CYCLAZOCINE | Ki | = | 0.18 | nM | 9.74 |
| CHEMBL19019 | NALTREXONE | Ki | = | 0.31 | nM | 9.51 |
| CHEMBL57628 | — | Ki | = | 0.49 | nM | 9.31 |
| CHEMBL58646 | — | Ki | = | 0.53 | nM | 9.28 |
| CHEMBL279968 | ETHYLKETOCYCLAZOCINE | Ki | = | 0.62 | nM | 9.21 |
| CHEMBL60869 | — | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL56246 | — | Ki | = | 0.85 | nM | 9.07 |
| CHEMBL299709 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL298590 | — | Ki | = | 4.2 | nM | 8.38 |
| CHEMBL59314 | — | Ki | = | 5.8 | nM | 8.24 |
| CHEMBL56695 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL56357 | — | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL293485 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL293103 | — | Ki | = | 460.0 | nM | 6.34 |
| CHEMBL56208 | — | Ki | = | 820.0 | nM | 6.09 |
| CHEMBL299027 | — | Ki | = | 900.0 | nM | 6.05 |