Assay Detail
Binding
CHEMBL855467
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Displacement of [3H]DAMGO from mu opioid receptor in Wistar rat brain membrane
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Beta-methyl substitution of cyclohexylalanine in Dmt-Tic-Cha-Phe peptides results in highly potent delta opioid antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 10 | 6.36 | 7.26 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL376453 | — | — | 1 | 7.26 |
| CHEMBL415426 | — | — | 1 | 6.77 |
| CHEMBL218782 | — | — | 1 | 6.70 |
| CHEMBL375095 | — | — | 1 | 6.55 |
| CHEMBL218781 | — | — | 1 | 6.54 |
| CHEMBL269314 | — | — | 1 | 6.48 |
| CHEMBL375094 | — | — | 1 | 6.24 |
| CHEMBL219482 | — | — | 1 | 5.85 |
| CHEMBL191751 | — | — | 1 | 5.76 |
| CHEMBL2371935 | — | — | 1 | 5.44 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL376453 | — | Ki | = | 55.0 | nM | 7.26 |
| CHEMBL415426 | — | Ki | = | 170.0 | nM | 6.77 |
| CHEMBL218782 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL375095 | — | Ki | = | 280.0 | nM | 6.55 |
| CHEMBL218781 | — | Ki | = | 290.0 | nM | 6.54 |
| CHEMBL269314 | — | Ki | = | 330.0 | nM | 6.48 |
| CHEMBL375094 | — | Ki | = | 580.0 | nM | 6.24 |
| CHEMBL219482 | — | Ki | = | 1400.0 | nM | 5.85 |
| CHEMBL191751 | — | Ki | = | 1720.0 | nM | 5.76 |
| CHEMBL2371935 | — | Ki | = | 3600.0 | nM | 5.44 |