Assay Detail
Binding
CHEMBL752653
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Evaluated for the binding affinity at kappa receptor
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Selective kappa-opioid agonists: synthesis and structure-activity relationships of piperidines incorporating on oxo-containing acyl group.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 21 | 7.95 | 9.19 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL433508 | — | — | 1 | 9.19 |
| CHEMBL117008 | — | — | 1 | 9.09 |
| CHEMBL118865 | SPIRADOLINE | 2.0 | 1 | 8.95 |
| CHEMBL117370 | — | — | 1 | 8.39 |
| CHEMBL326553 | — | — | 1 | 8.26 |
| CHEMBL117782 | — | — | 1 | 8.25 |
| CHEMBL326540 | — | — | 1 | 8.21 |
| CHEMBL333621 | — | — | 1 | 8.18 |
| CHEMBL116262 | — | — | 1 | 8.12 |
| CHEMBL332390 | — | — | 1 | 8.10 |
| CHEMBL117859 | — | — | 1 | 7.99 |
| CHEMBL115800 | — | — | 1 | 7.72 |
| CHEMBL119162 | — | — | 1 | 7.70 |
| CHEMBL116630 | — | — | 1 | 7.65 |
| CHEMBL326304 | — | — | 1 | 7.52 |
| CHEMBL331716 | — | — | 1 | 7.46 |
| CHEMBL119524 | — | — | 1 | 7.33 |
| CHEMBL324119 | — | — | 1 | 7.28 |
| CHEMBL119473 | — | — | 1 | 7.09 |
| CHEMBL70 | MORPHINE | 4.0 | 1 | 6.52 |
| CHEMBL326957 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL433508 | — | Ki | = | 0.64 | nM | 9.19 |
| CHEMBL117008 | — | Ki | = | 0.81 | nM | 9.09 |
| CHEMBL118865 | SPIRADOLINE | Ki | = | 1.13 | nM | 8.95 |
| CHEMBL117370 | — | Ki | = | 4.07 | nM | 8.39 |
| CHEMBL326553 | — | Ki | = | 5.44 | nM | 8.26 |
| CHEMBL117782 | — | Ki | = | 5.61 | nM | 8.25 |
| CHEMBL326540 | — | Ki | = | 6.24 | nM | 8.21 |
| CHEMBL333621 | — | Ki | = | 6.54 | nM | 8.18 |
| CHEMBL116262 | — | Ki | = | 7.6 | nM | 8.12 |
| CHEMBL332390 | — | Ki | = | 7.93 | nM | 8.10 |
| CHEMBL117859 | — | Ki | = | 10.3 | nM | 7.99 |
| CHEMBL115800 | — | Ki | = | 19.2 | nM | 7.72 |
| CHEMBL119162 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL116630 | — | Ki | = | 22.2 | nM | 7.65 |
| CHEMBL326304 | — | Ki | = | 30.4 | nM | 7.52 |
| CHEMBL331716 | — | Ki | = | 34.8 | nM | 7.46 |
| CHEMBL119524 | — | Ki | = | 47.0 | nM | 7.33 |
| CHEMBL324119 | — | Ki | = | 52.1 | nM | 7.28 |
| CHEMBL119473 | — | Ki | = | 80.3 | nM | 7.09 |
| CHEMBL70 | MORPHINE | Ki | = | 301.0 | nM | 6.52 |
| CHEMBL326957 | — | Ki | > | 100.0 | nM | - |