Assay Detail
Binding
CHEMBL898267
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Displacement of [3H]bremazocine from human delta 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 | 7.19 | 8.94 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL238361 | — | — | 1 | 8.94 |
| CHEMBL238317 | — | — | 1 | 8.73 |
| CHEMBL300662 | — | — | 1 | 8.32 |
| CHEMBL236376 | — | — | 1 | 8.07 |
| CHEMBL19019 | NALTREXONE | 4.0 | 1 | 7.79 |
| CHEMBL237066 | — | — | 1 | 7.15 |
| CHEMBL238280 | — | — | 1 | 6.67 |
| CHEMBL238283 | — | — | 1 | 6.17 |
| CHEMBL396392 | — | — | 1 | 6.14 |
| CHEMBL238305 | — | — | 1 | 5.62 |
| CHEMBL238282 | — | — | 1 | 5.46 |
| CHEMBL236395 | — | — | 1 | - |
| CHEMBL236391 | — | — | 1 | - |
| CHEMBL236392 | — | — | 1 | - |
| CHEMBL236393 | — | — | 1 | - |
| CHEMBL236394 | — | — | 1 | - |
| CHEMBL399814 | — | — | 1 | - |
| CHEMBL238281 | — | — | 1 | - |
| CHEMBL235560 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL238361 | — | Ki | = | 1.16 | nM | 8.94 |
| CHEMBL238317 | — | Ki | = | 1.88 | nM | 8.73 |
| CHEMBL300662 | — | Ki | = | 4.82 | nM | 8.32 |
| CHEMBL236376 | — | Ki | = | 8.54 | nM | 8.07 |
| CHEMBL19019 | NALTREXONE | Ki | = | 16.31 | nM | 7.79 |
| CHEMBL237066 | — | Ki | = | 70.21 | nM | 7.15 |
| CHEMBL238280 | — | Ki | = | 214.73 | nM | 6.67 |
| CHEMBL238283 | — | Ki | = | 673.58 | nM | 6.17 |
| CHEMBL396392 | — | Ki | = | 718.45 | nM | 6.14 |
| CHEMBL238305 | — | Ki | = | 2414.41 | nM | 5.62 |
| CHEMBL238282 | — | Ki | = | 3458.36 | nM | 5.46 |
| CHEMBL236395 | — | Ki | > | 5000.0 | nM | - |
| CHEMBL236391 | — | Ki | > | 5000.0 | nM | - |
| CHEMBL236392 | — | Ki | > | 5000.0 | nM | - |
| CHEMBL236393 | — | Ki | > | 5000.0 | nM | - |
| CHEMBL236394 | — | Ki | > | 5000.0 | nM | - |
| CHEMBL399814 | — | Ki | > | 5000.0 | nM | - |
| CHEMBL238281 | — | Ki | > | 5000.0 | nM | - |
| CHEMBL235560 | — | Ki | > | 5000.0 | nM | - |