Assay Detail
Binding
CHEMBL1045629
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Displacement of [3H]DPDPE from human delta opioid receptor expressed in HN9.10 cells
15
Total Activities
8
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
The biological activity and metabolic stability of peptidic bifunctional compounds that are opioid receptor agonists and neurokinin-1 receptor antagonists with a cystine moiety.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 8 | 8.59 | 9.18 |
| IC50 | 7 | 8.21 | 8.86 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL38874 | DAMGO | — | 2 | 9.18 |
| CHEMBL595972 | — | — | 2 | 9.18 |
| CHEMBL507340 | — | — | 2 | 9.18 |
| CHEMBL611926 | — | — | 2 | 8.89 |
| CHEMBL200199 | BIPHALIN | — | 1 | 8.59 |
| CHEMBL611924 | — | — | 2 | 8.30 |
| CHEMBL611925 | — | — | 2 | 8.11 |
| CHEMBL592969 | — | — | 2 | 7.27 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL38874 | DAMGO | Ki | = | 0.66 | nM | 9.18 |
| CHEMBL595972 | — | Ki | = | 0.66 | nM | 9.18 |
| CHEMBL507340 | — | Ki | = | 0.66 | nM | 9.18 |
| CHEMBL611926 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL595972 | — | IC50 | = | 1.38 | nM | 8.86 |
| CHEMBL38874 | DAMGO | IC50 | = | 1.445 | nM | 8.84 |
| CHEMBL507340 | — | IC50 | = | 1.445 | nM | 8.84 |
| CHEMBL200199 | BIPHALIN | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL611926 | — | IC50 | = | 2.692 | nM | 8.57 |
| CHEMBL611924 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL611925 | — | Ki | = | 7.8 | nM | 8.11 |
| CHEMBL611925 | — | IC50 | = | 15.49 | nM | 7.81 |
| CHEMBL611924 | — | IC50 | = | 22.39 | nM | 7.65 |
| CHEMBL592969 | — | Ki | = | 54.0 | nM | 7.27 |
| CHEMBL592969 | — | IC50 | = | 117.49 | nM | 6.93 |