Assay Detail
Binding
CHEMBL891361
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]DAMGO from mu opioid receptor in rat brain P2 synaptosome
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Transformation of mu-opioid receptor agonists into biologically potent mu-opioid receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 11 | 8.41 | 10.27 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL412923 | — | — | 1 | 10.27 |
| CHEMBL412924 | — | — | 1 | 9.59 |
| CHEMBL412922 | — | — | 1 | 9.35 |
| CHEMBL316446 | ENDOMORPHIN-1 | — | 1 | 9.25 |
| CHEMBL333357 | ENDOMORPHIN 2 | — | 1 | 8.88 |
| CHEMBL397177 | — | — | 1 | 8.34 |
| CHEMBL396506 | — | — | 1 | 8.16 |
| CHEMBL232303 | — | — | 1 | 7.91 |
| CHEMBL397176 | — | — | 1 | 7.88 |
| CHEMBL266988 | — | — | 1 | 6.89 |
| CHEMBL412921 | — | — | 1 | 5.98 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL412923 | — | Ki | = | 0.054 | nM | 10.27 |
| CHEMBL412924 | — | Ki | = | 0.26 | nM | 9.59 |
| CHEMBL412922 | — | Ki | = | 0.45 | nM | 9.35 |
| CHEMBL316446 | ENDOMORPHIN-1 | Ki | = | 0.56 | nM | 9.25 |
| CHEMBL333357 | ENDOMORPHIN 2 | Ki | = | 1.33 | nM | 8.88 |
| CHEMBL397177 | — | Ki | = | 4.6 | nM | 8.34 |
| CHEMBL396506 | — | Ki | = | 6.94 | nM | 8.16 |
| CHEMBL232303 | — | Ki | = | 12.4 | nM | 7.91 |
| CHEMBL397176 | — | Ki | = | 13.1 | nM | 7.88 |
| CHEMBL266988 | — | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL412921 | — | Ki | = | 1045.0 | nM | 5.98 |