Assay Detail
Binding
CHEMBL3635647
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Displacement of [3H]diprenorphine from rat mu-opioid receptor expressed in C6 cell membrane for 1 hr by liquid scintillation counting analysis
16
Total Activities
16
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
Further Optimization and Evaluation of Bioavailable, Mixed-Efficacy μ-Opioid Receptor (MOR) Agonists/δ-Opioid Receptor (DOR) Antagonists: Balancing MOR and DOR Affinities.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 16 | 10.13 | 10.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3634251 | — | — | 1 | 10.92 |
| CHEMBL3634258 | — | — | 1 | 10.52 |
| CHEMBL3634250 | — | — | 1 | 10.52 |
| CHEMBL3634252 | — | — | 1 | 10.40 |
| CHEMBL3634249 | — | — | 1 | 10.37 |
| CHEMBL3634248 | — | — | 1 | 10.35 |
| CHEMBL3634257 | — | — | 1 | 10.30 |
| CHEMBL3634256 | — | — | 1 | 10.30 |
| CHEMBL3634254 | — | — | 1 | 10.22 |
| CHEMBL3634253 | — | — | 1 | 10.22 |
| CHEMBL2322562 | — | — | 1 | 10.11 |
| CHEMBL3634247 | — | — | 1 | 9.89 |
| CHEMBL2322563 | — | — | 1 | 9.80 |
| CHEMBL2322568 | — | — | 1 | 9.66 |
| CHEMBL3634255 | — | — | 1 | 9.41 |
| CHEMBL2322561 | — | — | 1 | 9.12 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3634251 | — | Ki | = | 0.012 | nM | 10.92 |
| CHEMBL3634258 | — | Ki | = | 0.03 | nM | 10.52 |
| CHEMBL3634250 | — | Ki | = | 0.03 | nM | 10.52 |
| CHEMBL3634252 | — | Ki | = | 0.04 | nM | 10.40 |
| CHEMBL3634249 | — | Ki | = | 0.043 | nM | 10.37 |
| CHEMBL3634248 | — | Ki | = | 0.045 | nM | 10.35 |
| CHEMBL3634257 | — | Ki | = | 0.05 | nM | 10.30 |
| CHEMBL3634256 | — | Ki | = | 0.05 | nM | 10.30 |
| CHEMBL3634254 | — | Ki | = | 0.06 | nM | 10.22 |
| CHEMBL3634253 | — | Ki | = | 0.06 | nM | 10.22 |
| CHEMBL2322562 | — | Ki | = | 0.078 | nM | 10.11 |
| CHEMBL3634247 | — | Ki | = | 0.13 | nM | 9.89 |
| CHEMBL2322563 | — | Ki | = | 0.16 | nM | 9.80 |
| CHEMBL2322568 | — | Ki | = | 0.22 | nM | 9.66 |
| CHEMBL3634255 | — | Ki | = | 0.39 | nM | 9.41 |
| CHEMBL2322561 | — | Ki | = | 0.76 | nM | 9.12 |