Assay Detail
Binding
CHEMBL901090
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]diprenorphine from cloned human kappa 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 | 6.64 | 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 |
| CHEMBL238156 | — | — | 1 | 7.21 |
| CHEMBL396637 | — | — | 1 | 7.14 |
| CHEMBL237718 | — | — | 1 | 7.11 |
| CHEMBL237506 | — | — | 1 | 6.97 |
| CHEMBL396636 | — | — | 1 | 6.97 |
| CHEMBL237716 | — | — | 1 | 6.93 |
| CHEMBL237066 | — | — | 1 | 6.87 |
| CHEMBL237295 | — | — | 1 | 6.73 |
| CHEMBL237934 | — | — | 1 | 6.50 |
| CHEMBL238363 | — | — | 1 | 6.44 |
| CHEMBL237073 | — | — | 1 | 6.44 |
| CHEMBL237071 | — | — | 1 | 6.25 |
| CHEMBL238157 | — | — | 1 | 6.15 |
| CHEMBL397148 | — | — | 1 | 5.91 |
| CHEMBL235155 | — | — | 1 | 5.67 |
| CHEMBL398089 | — | — | 1 | 5.62 |
| CHEMBL237293 | — | — | 1 | 5.54 |
| CHEMBL238364 | — | — | 1 | 5.49 |
| CHEMBL237072 | — | — | 1 | 5.44 |
| CHEMBL237294 | — | — | 1 | - |
| CHEMBL235154 | — | — | 1 | - |
| CHEMBL238362 | — | — | 1 | - |
| CHEMBL398090 | — | — | 1 | - |
| CHEMBL237505 | — | — | 1 | - |
| CHEMBL439038 | — | — | 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 |
| CHEMBL238156 | — | Ki | = | 61.65 | nM | 7.21 |
| CHEMBL396637 | — | Ki | = | 71.62 | nM | 7.14 |
| CHEMBL237718 | — | Ki | = | 78.09 | nM | 7.11 |
| CHEMBL237506 | — | Ki | = | 105.88 | nM | 6.97 |
| CHEMBL396636 | — | Ki | = | 105.95 | nM | 6.97 |
| CHEMBL237716 | — | Ki | = | 116.41 | nM | 6.93 |
| CHEMBL237066 | — | Ki | = | 136.26 | nM | 6.87 |
| CHEMBL237295 | — | Ki | = | 187.97 | nM | 6.73 |
| CHEMBL237934 | — | Ki | = | 318.95 | nM | 6.50 |
| CHEMBL238363 | — | Ki | = | 359.89 | nM | 6.44 |
| CHEMBL237073 | — | Ki | = | 360.6 | nM | 6.44 |
| CHEMBL237071 | — | Ki | = | 555.9 | nM | 6.25 |
| CHEMBL238157 | — | Ki | = | 703.78 | nM | 6.15 |
| CHEMBL397148 | — | Ki | = | 1221.0 | nM | 5.91 |
| CHEMBL235155 | — | Ki | = | 2150.0 | nM | 5.67 |
| CHEMBL398089 | — | Ki | = | 2428.17 | nM | 5.62 |
| CHEMBL237293 | — | Ki | = | 2873.0 | nM | 5.54 |
| CHEMBL238364 | — | Ki | = | 3254.0 | nM | 5.49 |
| CHEMBL237072 | — | Ki | = | 3606.0 | nM | 5.44 |
| CHEMBL237294 | — | Ki | > | 4897.0 | nM | - |
| CHEMBL235154 | — | Ki | > | 5000.0 | nM | - |
| CHEMBL238362 | — | Ki | > | 5000.0 | nM | - |
| CHEMBL398090 | — | Ki | - | — | - | |
| CHEMBL237505 | — | Ki | - | — | - | |
| CHEMBL439038 | — | Ki | - | — | - |