Assay Detail
Binding
CHEMBL754913
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Inhibition of [3H]U-69593 binding to Opioid receptor kappa 1 of Chinese hamster ovary membrane
14
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cricetulus griseus |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
2-aminothiazole-derived opioids. Bioisosteric replacement of phenols.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 14 | 8.79 | 10.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL49269 | CYCLORPHAN | — | 1 | 10.47 |
| CHEMBL242756 | — | — | 1 | 10.31 |
| CHEMBL301160 | BUTORPHAN | — | 1 | 10.10 |
| CHEMBL59092 | — | — | 1 | 9.74 |
| CHEMBL48241 | — | — | 1 | 9.32 |
| CHEMBL301701 | — | — | 1 | 9.31 |
| CHEMBL390866 | — | — | 1 | 9.10 |
| CHEMBL592 | LEVORPHANOL | 4.0 | 1 | 8.64 |
| CHEMBL1766021 | — | — | 2 | 8.19 |
| CHEMBL56356 | — | — | 1 | 8.17 |
| CHEMBL299713 | — | — | 1 | 7.89 |
| CHEMBL70 | MORPHINE | 4.0 | 1 | 7.62 |
| CHEMBL294168 | — | — | 1 | 6.66 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL49269 | CYCLORPHAN | Ki | = | 0.034 | nM | 10.47 |
| CHEMBL242756 | — | Ki | = | 0.049 | nM | 10.31 |
| CHEMBL301160 | BUTORPHAN | Ki | = | 0.079 | nM | 10.10 |
| CHEMBL59092 | — | Ki | = | 0.18 | nM | 9.74 |
| CHEMBL48241 | — | Ki | = | 0.48 | nM | 9.32 |
| CHEMBL301701 | — | Ki | = | 0.49 | nM | 9.31 |
| CHEMBL390866 | — | Ki | = | 0.79 | nM | 9.10 |
| CHEMBL592 | LEVORPHANOL | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL1766021 | — | Ki | = | 6.4 | nM | 8.19 |
| CHEMBL56356 | — | Ki | = | 6.7 | nM | 8.17 |
| CHEMBL299713 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL70 | MORPHINE | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL1766021 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL294168 | — | Ki | = | 220.0 | nM | 6.66 |