Assay Detail
Binding
CHEMBL934280
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]DAMGO from rat mu opioid receptor expressed in mouse HN9.10 cells
13
Total Activities
7
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
A structure-activity relationship study and combinatorial synthetic approach of C-terminal modified bifunctional peptides that are delta/mu opioid receptor agonists and neurokinin 1 receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 7 | 7.98 | 9.19 |
| logIC50 | 6 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL271619 | — | — | 2 | 9.19 |
| CHEMBL200199 | BIPHALIN | — | 1 | 8.85 |
| CHEMBL406030 | — | — | 2 | 8.17 |
| CHEMBL438389 | — | — | 2 | 8.02 |
| CHEMBL261608 | — | — | 2 | 7.54 |
| CHEMBL272665 | — | — | 2 | 7.34 |
| CHEMBL261390 | — | — | 2 | 6.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL271619 | — | Ki | = | 0.65 | nM | 9.19 |
| CHEMBL200199 | BIPHALIN | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL406030 | — | Ki | = | 6.8 | nM | 8.17 |
| CHEMBL438389 | — | Ki | = | 9.5 | nM | 8.02 |
| CHEMBL261608 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL272665 | — | Ki | = | 46.0 | nM | 7.34 |
| CHEMBL261390 | — | Ki | = | 180.0 | nM | 6.75 |
| CHEMBL406030 | — | logIC50 | = | -7.8 | — | - |
| CHEMBL438389 | — | logIC50 | = | -7.7 | — | - |
| CHEMBL272665 | — | logIC50 | = | -7.0 | — | - |
| CHEMBL271619 | — | logIC50 | = | -8.9 | — | - |
| CHEMBL261608 | — | logIC50 | = | -7.2 | — | - |
| CHEMBL261390 | — | logIC50 | = | -6.4 | — | - |