Assay Detail
Binding
CHEMBL752148
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Activity was evaluated by inhibition of the binding of 1 nM [3H]U-69593 at Opioid receptor kappa 1 binding site
19
Total Activities
12
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
Asymmetric syntheses, opioid receptor affinities, and antinociceptive effects of 8-amino-5,9-methanobenzocyclooctenes, a new class of structural analogues of the morphine alkaloids.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 19 | 6.65 | 8.18 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL294226 | — | — | 3 | 8.18 |
| CHEMBL60270 | — | — | 1 | 7.76 |
| CHEMBL58059 | — | — | 1 | 7.29 |
| CHEMBL431947 | — | — | 2 | 7.21 |
| CHEMBL409026 | — | — | 2 | 6.96 |
| CHEMBL418460 | — | — | 1 | 6.67 |
| CHEMBL70 | MORPHINE | 4.0 | 1 | 6.48 |
| CHEMBL301421 | — | — | 2 | 6.39 |
| CHEMBL57879 | — | — | 2 | 6.36 |
| CHEMBL61644 | — | — | 1 | 6.10 |
| CHEMBL299460 | — | — | 2 | 5.54 |
| CHEMBL59840 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL294226 | — | Ki | = | 6.62 | nM | 8.18 |
| CHEMBL60270 | — | Ki | = | 17.2 | nM | 7.76 |
| CHEMBL58059 | — | Ki | = | 51.6 | nM | 7.29 |
| CHEMBL294226 | — | Ki | = | 53.1 | nM | 7.28 |
| CHEMBL431947 | — | Ki | = | 60.9 | nM | 7.21 |
| CHEMBL294226 | — | Ki | = | 80.8 | nM | 7.09 |
| CHEMBL409026 | — | Ki | = | 109.0 | nM | 6.96 |
| CHEMBL431947 | — | Ki | = | 123.0 | nM | 6.91 |
| CHEMBL418460 | — | Ki | = | 215.0 | nM | 6.67 |
| CHEMBL70 | MORPHINE | Ki | = | 330.0 | nM | 6.48 |
| CHEMBL301421 | — | Ki | = | 409.0 | nM | 6.39 |
| CHEMBL57879 | — | Ki | = | 440.0 | nM | 6.36 |
| CHEMBL57879 | — | Ki | = | 650.0 | nM | 6.19 |
| CHEMBL61644 | — | Ki | = | 795.0 | nM | 6.10 |
| CHEMBL299460 | — | Ki | = | 2900.0 | nM | 5.54 |
| CHEMBL299460 | — | Ki | = | 3800.0 | nM | 5.42 |
| CHEMBL301421 | — | Ki | = | 5960.0 | nM | 5.22 |
| CHEMBL409026 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL59840 | — | Ki | > | 10000.0 | nM | - |