Assay Detail
Functional
CHEMBL899315
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| 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 | 12 | 8.91 | 10.37 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL300662 | — | — | 1 | 10.37 |
| CHEMBL238361 | — | — | 1 | 10.15 |
| CHEMBL238317 | — | — | 1 | 9.82 |
| CHEMBL236376 | — | — | 1 | 9.36 |
| CHEMBL19019 | NALTREXONE | 4.0 | 1 | 9.23 |
| CHEMBL237066 | — | — | 1 | 8.65 |
| CHEMBL238316 | — | — | 1 | 8.39 |
| CHEMBL236168 | — | — | 1 | 7.78 |
| CHEMBL236169 | — | — | 1 | 7.73 |
| CHEMBL236170 | — | — | 1 | 7.65 |
| CHEMBL238315 | — | — | 1 | - |
| CHEMBL438134 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL300662 | — | Ki | = | 0.043 | nM | 10.37 |
| CHEMBL238361 | — | Ki | = | 0.07 | nM | 10.15 |
| CHEMBL238317 | — | Ki | = | 0.15 | nM | 9.82 |
| CHEMBL236376 | — | Ki | = | 0.44 | nM | 9.36 |
| CHEMBL19019 | NALTREXONE | Ki | = | 0.59 | nM | 9.23 |
| CHEMBL237066 | — | Ki | = | 2.25 | nM | 8.65 |
| CHEMBL238316 | — | Ki | = | 4.09 | nM | 8.39 |
| CHEMBL236168 | — | Ki | = | 16.56 | nM | 7.78 |
| CHEMBL236169 | — | Ki | = | 18.47 | nM | 7.73 |
| CHEMBL236170 | — | Ki | = | 22.26 | nM | 7.65 |
| CHEMBL238315 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL438134 | — | Ki | > | 1000.0 | nM | - |