Assay Detail
Binding
CHEMBL747232
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Binding affinity using [3H]diprenorphine as the radioligand against E297A mutant Opioid receptor kappa 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 | 7.89 | 9.42 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL281786 | DIPRENORPHINE | 2.0 | 1 | 9.42 |
| CHEMBL573214 | NORBINALTORPHIMINE | — | 1 | 7.89 |
| CHEMBL610523 | — | — | 1 | 7.77 |
| CHEMBL609747 | — | — | 1 | 7.40 |
| CHEMBL287752 | — | — | 1 | 6.98 |
| CHEMBL606959 | — | — | 1 | - |
| CHEMBL610524 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL281786 | DIPRENORPHINE | Ki | = | 0.38 | nM | 9.42 |
| CHEMBL573214 | NORBINALTORPHIMINE | Ki | = | 12.8 | nM | 7.89 |
| CHEMBL610523 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL609747 | — | Ki | = | 39.6 | nM | 7.40 |
| CHEMBL287752 | — | Ki | = | 104.0 | nM | 6.98 |
| CHEMBL606959 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL610524 | — | Ki | > | 1000.0 | nM | - |