Assay Detail
Binding
CHEMBL1046753
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Displacement of [3H]diprenorphine from human kappa opioid receptor expressed in CHO cells after 1 hr by liquid scintillation counting
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Pentapeptides displaying mu opioid receptor agonist and delta opioid receptor partial agonist/antagonist properties.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 9 | 7.98 | 8.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL572525 | — | — | 1 | 8.89 |
| CHEMBL583066 | — | — | 1 | 8.60 |
| CHEMBL583274 | — | — | 1 | 8.24 |
| CHEMBL583278 | — | — | 1 | 8.23 |
| CHEMBL583277 | — | — | 1 | 8.22 |
| CHEMBL583276 | — | — | 1 | 7.96 |
| CHEMBL583067 | — | — | 1 | 7.68 |
| CHEMBL583275 | — | — | 1 | 7.16 |
| CHEMBL572524 | — | — | 1 | 6.84 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL572525 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL583066 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL583274 | — | Ki | = | 5.8 | nM | 8.24 |
| CHEMBL583278 | — | Ki | = | 5.9 | nM | 8.23 |
| CHEMBL583277 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL583276 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL583067 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL583275 | — | Ki | = | 69.0 | nM | 7.16 |
| CHEMBL572524 | — | Ki | = | 145.0 | nM | 6.84 |