Assay Detail
Binding
CHEMBL757366
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Binding affinity using [3H]diprenorphine as the radioligand against wild-type Opioid receptor mu 1 in COS-7 cells
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cercopithecidae |
| Cell Type | COS-7 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Binding of norbinaltorphimine (norBNI) congeners to wild-type and mutant mu and kappa opioid receptors: molecular recognition loci for the pharmacophore and address components of kappa antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 7 | 7.41 | 9.57 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL281786 | DIPRENORPHINE | 2.0 | 1 | 9.57 |
| CHEMBL609747 | — | — | 1 | 7.40 |
| CHEMBL573214 | NORBINALTORPHIMINE | — | 1 | 7.16 |
| CHEMBL287752 | — | — | 1 | 6.99 |
| CHEMBL610524 | — | — | 1 | 6.78 |
| CHEMBL610523 | — | — | 1 | 6.56 |
| CHEMBL606959 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL281786 | DIPRENORPHINE | Ki | = | 0.27 | nM | 9.57 |
| CHEMBL609747 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL573214 | NORBINALTORPHIMINE | Ki | = | 70.0 | nM | 7.16 |
| CHEMBL287752 | — | Ki | = | 102.0 | nM | 6.99 |
| CHEMBL610524 | — | Ki | = | 165.0 | nM | 6.78 |
| CHEMBL610523 | — | Ki | = | 276.0 | nM | 6.56 |
| CHEMBL606959 | — | Ki | > | 1000.0 | nM | - |