Assay Detail
Functional
CHEMBL899316
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human kappa 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 | 8.28 | 9.49 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL300662 | — | — | 1 | 9.49 |
| CHEMBL238361 | — | — | 1 | 8.94 |
| CHEMBL238317 | — | — | 1 | 8.91 |
| CHEMBL238316 | — | — | 1 | 8.61 |
| CHEMBL19019 | NALTREXONE | 4.0 | 1 | 8.52 |
| CHEMBL236376 | — | — | 1 | 8.02 |
| CHEMBL237066 | — | — | 1 | 7.74 |
| CHEMBL236168 | — | — | 1 | 7.63 |
| CHEMBL236169 | — | — | 1 | 7.62 |
| CHEMBL236170 | — | — | 1 | 7.34 |
| CHEMBL238315 | — | — | 1 | - |
| CHEMBL438134 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL300662 | — | Ki | = | 0.32 | nM | 9.49 |
| CHEMBL238361 | — | Ki | = | 1.15 | nM | 8.94 |
| CHEMBL238317 | — | Ki | = | 1.22 | nM | 8.91 |
| CHEMBL238316 | — | Ki | = | 2.47 | nM | 8.61 |
| CHEMBL19019 | NALTREXONE | Ki | = | 2.99 | nM | 8.52 |
| CHEMBL236376 | — | Ki | = | 9.6 | nM | 8.02 |
| CHEMBL237066 | — | Ki | = | 18.41 | nM | 7.74 |
| CHEMBL236168 | — | Ki | = | 23.34 | nM | 7.63 |
| CHEMBL236169 | — | Ki | = | 24.15 | nM | 7.62 |
| CHEMBL236170 | — | Ki | = | 45.83 | nM | 7.34 |
| CHEMBL238315 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL438134 | — | Ki | > | 1000.0 | nM | - |