Assay Detail
Functional
CHEMBL753803
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Apparent binding affinity of compound was determined by antagonism towards Opioid receptor kappa 1 in [35S]GTP-gamma-S, binding assay in guinea pig caudate
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Cavia porcellus |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Identification of opioid ligands possessing mixed micro agonist/delta antagonist activity among pyridomorphinans derived from naloxone, oxymorphone, and hydromorphone [correction of hydropmorphone].
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 6 | 7.51 | 8.06 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL567175 | NALTRINDOLE | — | 1 | 8.06 |
| CHEMBL610261 | — | — | 1 | 7.95 |
| CHEMBL611685 | — | — | 1 | 6.51 |
| CHEMBL611434 | — | — | 1 | - |
| CHEMBL611435 | — | — | 1 | - |
| CHEMBL611438 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL567175 | NALTRINDOLE | Ki | = | 8.8 | nM | 8.06 |
| CHEMBL610261 | — | Ki | = | 11.2 | nM | 7.95 |
| CHEMBL611685 | — | Ki | = | 308.0 | nM | 6.51 |
| CHEMBL611434 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL611435 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL611438 | — | Ki | = | 767.0 | — | - |