Assay Detail
Binding
CHEMBL935203
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Displacement of [3H]DPDPE from human delta 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 | Homo sapiens |
| 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 |
|---|---|---|---|
| EC50 | 7 | 7.59 | 8.59 |
| logIC50 | 6 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL200199 | BIPHALIN | — | 1 | 8.59 |
| CHEMBL271619 | — | — | 2 | 8.00 |
| CHEMBL406030 | — | — | 2 | 7.51 |
| CHEMBL261608 | — | — | 2 | 7.51 |
| CHEMBL261390 | — | — | 2 | 7.30 |
| CHEMBL438389 | — | — | 2 | 7.14 |
| CHEMBL272665 | — | — | 2 | 7.11 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL200199 | BIPHALIN | EC50 | = | 2.6 | nM | 8.59 |
| CHEMBL271619 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL406030 | — | EC50 | = | 31.0 | nM | 7.51 |
| CHEMBL261608 | — | EC50 | = | 31.0 | nM | 7.51 |
| CHEMBL261390 | — | EC50 | = | 50.0 | nM | 7.30 |
| CHEMBL438389 | — | EC50 | = | 72.0 | nM | 7.14 |
| CHEMBL272665 | — | EC50 | = | 77.0 | nM | 7.11 |
| CHEMBL261390 | — | logIC50 | = | -7.0 | — | - |
| CHEMBL406030 | — | logIC50 | = | -6.5 | — | - |
| CHEMBL438389 | — | logIC50 | = | -6.8 | — | - |
| CHEMBL272665 | — | logIC50 | = | -6.8 | — | - |
| CHEMBL271619 | — | logIC50 | = | -7.7 | — | - |
| CHEMBL261608 | — | logIC50 | = | -7.2 | — | - |