Assay Detail
Binding
CHEMBL2330684
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Displacement of [3H]diprenorphine from rat DOR expressed in rat C6 cells after 1 hr by liquid scintillation counting analysis
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Cell Type | C6 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Opioid peptidomimetics: leads for the design of bioavailable mixed efficacy μ opioid receptor (MOR) agonist/δ opioid receptor (DOR) antagonist ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 10 | 7.56 | 8.39 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2322563 | — | — | 1 | 8.39 |
| CHEMBL2322561 | — | — | 1 | 8.22 |
| CHEMBL2322560 | — | — | 1 | 8.05 |
| CHEMBL2322568 | — | — | 1 | 8.03 |
| CHEMBL2322562 | — | — | 1 | 8.00 |
| CHEMBL2322564 | — | — | 1 | 7.25 |
| CHEMBL2322566 | — | — | 1 | 7.18 |
| CHEMBL2322565 | — | — | 1 | 6.92 |
| CHEMBL70 | MORPHINE | 4.0 | 1 | 6.77 |
| CHEMBL2322567 | — | — | 1 | 6.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2322563 | — | Ki | = | 4.1 | nM | 8.39 |
| CHEMBL2322561 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL2322560 | — | Ki | = | 8.9 | nM | 8.05 |
| CHEMBL2322568 | — | Ki | = | 9.4 | nM | 8.03 |
| CHEMBL2322562 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL2322564 | — | Ki | = | 56.0 | nM | 7.25 |
| CHEMBL2322566 | — | Ki | = | 66.0 | nM | 7.18 |
| CHEMBL2322565 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL70 | MORPHINE | Ki | = | 171.0 | nM | 6.77 |
| CHEMBL2322567 | — | Ki | = | 180.0 | nM | 6.75 |