Assay Detail
Functional
CHEMBL919394
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human opioid kappa receptor expressed in CHO cells assessed as inhibition of U-50488-stimulated [35S]GTP-gamma-S binding
6
Total Activities
6
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Pharmacological properties of bivalent ligands containing butorphan linked to nalbuphine, naltrexone, and naloxone at mu, delta, and kappa opioid receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 6.47 | 6.70 |
| Activity | 3 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL19019 | NALTREXONE | 4.0 | 1 | 6.70 |
| CHEMBL80 | NALOXONE | 4.0 | 1 | 6.50 |
| CHEMBL224671 | — | — | 1 | 6.22 |
| CHEMBL895 | NALBUPHINE | 4.0 | 1 | - |
| CHEMBL224014 | — | — | 1 | - |
| CHEMBL2113275 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL19019 | NALTREXONE | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL80 | NALOXONE | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL224671 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL895 | NALBUPHINE | Activity | - | — | - | |
| CHEMBL224014 | — | Activity | - | — | - | |
| CHEMBL2113275 | — | Activity | - | — | - |