Assay Detail
Binding
CHEMBL899319
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]diprenorphine from human kappa opioid receptor expressed in CHO cells in presence of high sodium by SPA
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Structure-activity relationship studies of carboxamido-biaryl ethers as opioid receptor antagonists (OpRAs). Part 1.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 19 | 7.25 | 8.33 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL300662 | — | — | 1 | 8.33 |
| CHEMBL19019 | NALTREXONE | 4.0 | 1 | 8.28 |
| CHEMBL238361 | — | — | 1 | 8.08 |
| CHEMBL238317 | — | — | 1 | 7.82 |
| CHEMBL236376 | — | — | 1 | 7.16 |
| CHEMBL237066 | — | — | 1 | 6.87 |
| CHEMBL238280 | — | — | 1 | 5.94 |
| CHEMBL238283 | — | — | 1 | 5.55 |
| CHEMBL238282 | — | — | 1 | - |
| CHEMBL399814 | — | — | 1 | - |
| CHEMBL238305 | — | — | 1 | - |
| CHEMBL236391 | — | — | 1 | - |
| CHEMBL236392 | — | — | 1 | - |
| CHEMBL236393 | — | — | 1 | - |
| CHEMBL396392 | — | — | 1 | - |
| CHEMBL238281 | — | — | 1 | - |
| CHEMBL236395 | — | — | 1 | - |
| CHEMBL236394 | — | — | 1 | - |
| CHEMBL235560 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL300662 | — | Ki | = | 4.68 | nM | 8.33 |
| CHEMBL19019 | NALTREXONE | Ki | = | 5.28 | nM | 8.28 |
| CHEMBL238361 | — | Ki | = | 8.38 | nM | 8.08 |
| CHEMBL238317 | — | Ki | = | 15.04 | nM | 7.82 |
| CHEMBL236376 | — | Ki | = | 69.27 | nM | 7.16 |
| CHEMBL237066 | — | Ki | = | 136.26 | nM | 6.87 |
| CHEMBL238280 | — | Ki | = | 1147.5 | nM | 5.94 |
| CHEMBL238283 | — | Ki | = | 2808.74 | nM | 5.55 |
| CHEMBL238282 | — | Ki | > | 5000.0 | nM | - |
| CHEMBL399814 | — | Ki | > | 5000.0 | nM | - |
| CHEMBL238305 | — | Ki | > | 5000.0 | nM | - |
| CHEMBL236391 | — | Ki | > | 5000.0 | nM | - |
| CHEMBL236392 | — | Ki | > | 5000.0 | nM | - |
| CHEMBL236393 | — | Ki | > | 5000.0 | nM | - |
| CHEMBL396392 | — | Ki | > | 5000.0 | nM | - |
| CHEMBL238281 | — | Ki | > | 5000.0 | nM | - |
| CHEMBL236395 | — | Ki | > | 5000.0 | nM | - |
| CHEMBL236394 | — | Ki | > | 5000.0 | nM | - |
| CHEMBL235560 | — | Ki | > | 5000.0 | nM | - |