Assay Detail
Binding
CHEMBL749650
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of [3H]-DAMGO binding to Opioid receptor mu 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 | 8.50 | 10.21 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL49269 | CYCLORPHAN | — | 1 | 10.21 |
| CHEMBL592 | LEVORPHANOL | 4.0 | 1 | 9.68 |
| CHEMBL301160 | BUTORPHAN | — | 1 | 9.64 |
| CHEMBL59092 | — | — | 1 | 9.49 |
| CHEMBL70 | MORPHINE | 4.0 | 1 | 9.06 |
| CHEMBL1766021 | — | — | 2 | 8.96 |
| CHEMBL242756 | — | — | 1 | 8.82 |
| CHEMBL48241 | — | — | 1 | 8.48 |
| CHEMBL390866 | — | — | 1 | 8.15 |
| CHEMBL301701 | — | — | 1 | 8.08 |
| CHEMBL294168 | — | — | 1 | 7.52 |
| CHEMBL56356 | — | — | 1 | 7.32 |
| CHEMBL299713 | — | — | 1 | 6.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL49269 | CYCLORPHAN | Ki | = | 0.062 | nM | 10.21 |
| CHEMBL592 | LEVORPHANOL | Ki | = | 0.21 | nM | 9.68 |
| CHEMBL301160 | BUTORPHAN | Ki | = | 0.23 | nM | 9.64 |
| CHEMBL59092 | — | Ki | = | 0.32 | nM | 9.49 |
| CHEMBL70 | MORPHINE | Ki | = | 0.88 | nM | 9.06 |
| CHEMBL1766021 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL242756 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL48241 | — | Ki | = | 3.3 | nM | 8.48 |
| CHEMBL390866 | — | Ki | = | 7.1 | nM | 8.15 |
| CHEMBL301701 | — | Ki | = | 8.3 | nM | 8.08 |
| CHEMBL294168 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL56356 | — | Ki | = | 48.0 | nM | 7.32 |
| CHEMBL1766021 | — | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL299713 | — | Ki | = | 200.0 | nM | 6.70 |