Assay Detail
Binding
CHEMBL901089
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Displacement of [3H]diprenorphine from cloned human mu opioid receptor expressed in CHO cells
28
Total Activities
28
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 2.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 28 | 7.61 | 9.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL300662 | — | — | 1 | 9.82 |
| CHEMBL238361 | — | — | 1 | 9.77 |
| CHEMBL19019 | NALTREXONE | 4.0 | 1 | 9.06 |
| CHEMBL237295 | — | — | 1 | 8.30 |
| CHEMBL237066 | — | — | 1 | 8.13 |
| CHEMBL396636 | — | — | 1 | 8.12 |
| CHEMBL237073 | — | — | 1 | 8.00 |
| CHEMBL237718 | — | — | 1 | 7.95 |
| CHEMBL237506 | — | — | 1 | 7.93 |
| CHEMBL237934 | — | — | 1 | 7.92 |
| CHEMBL237716 | — | — | 1 | 7.92 |
| CHEMBL397148 | — | — | 1 | 7.80 |
| CHEMBL396637 | — | — | 1 | 7.74 |
| CHEMBL237505 | — | — | 1 | 7.68 |
| CHEMBL439038 | — | — | 1 | 7.61 |
| CHEMBL238156 | — | — | 1 | 7.38 |
| CHEMBL238157 | — | — | 1 | 7.38 |
| CHEMBL237294 | — | — | 1 | 7.04 |
| CHEMBL238363 | — | — | 1 | 6.89 |
| CHEMBL235155 | — | — | 1 | 6.75 |
| CHEMBL237071 | — | — | 1 | 6.73 |
| CHEMBL238364 | — | — | 1 | 6.67 |
| CHEMBL398089 | — | — | 1 | 6.63 |
| CHEMBL237293 | — | — | 1 | 6.39 |
| CHEMBL235154 | — | — | 1 | 6.18 |
| CHEMBL238362 | — | — | 1 | 6.00 |
| CHEMBL237072 | — | — | 1 | - |
| CHEMBL398090 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL300662 | — | Ki | = | 0.15 | nM | 9.82 |
| CHEMBL238361 | — | Ki | = | 0.17 | nM | 9.77 |
| CHEMBL19019 | NALTREXONE | Ki | = | 0.87 | nM | 9.06 |
| CHEMBL237295 | — | Ki | = | 5.05 | nM | 8.30 |
| CHEMBL237066 | — | Ki | = | 7.44 | nM | 8.13 |
| CHEMBL396636 | — | Ki | = | 7.55 | nM | 8.12 |
| CHEMBL237073 | — | Ki | = | 10.09 | nM | 8.00 |
| CHEMBL237718 | — | Ki | = | 11.14 | nM | 7.95 |
| CHEMBL237506 | — | Ki | = | 11.86 | nM | 7.93 |
| CHEMBL237934 | — | Ki | = | 11.93 | nM | 7.92 |
| CHEMBL237716 | — | Ki | = | 12.03 | nM | 7.92 |
| CHEMBL397148 | — | Ki | = | 15.95 | nM | 7.80 |
| CHEMBL396637 | — | Ki | = | 18.33 | nM | 7.74 |
| CHEMBL237505 | — | Ki | = | 20.81 | nM | 7.68 |
| CHEMBL439038 | — | Ki | = | 24.42 | nM | 7.61 |
| CHEMBL238156 | — | Ki | = | 42.03 | nM | 7.38 |
| CHEMBL238157 | — | Ki | = | 41.67 | nM | 7.38 |
| CHEMBL237294 | — | Ki | = | 91.49 | nM | 7.04 |
| CHEMBL238363 | — | Ki | = | 128.7 | nM | 6.89 |
| CHEMBL235155 | — | Ki | = | 179.0 | nM | 6.75 |
| CHEMBL237071 | — | Ki | = | 185.0 | nM | 6.73 |
| CHEMBL238364 | — | Ki | = | 215.87 | nM | 6.67 |
| CHEMBL398089 | — | Ki | = | 231.59 | nM | 6.63 |
| CHEMBL237293 | — | Ki | = | 405.8 | nM | 6.39 |
| CHEMBL235154 | — | Ki | = | 658.8 | nM | 6.18 |
| CHEMBL238362 | — | Ki | = | 1008.0 | nM | 6.00 |
| CHEMBL237072 | — | Ki | > | 3333.0 | nM | - |
| CHEMBL398090 | — | Ki | - | — | - |