Assay Detail
Functional
CHEMBL899317
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Antagonist activity at human delta 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 | 7.82 | 9.04 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL238317 | — | — | 1 | 9.04 |
| CHEMBL238361 | — | — | 1 | 9.01 |
| CHEMBL300662 | — | — | 1 | 8.92 |
| CHEMBL236376 | — | — | 1 | 8.54 |
| CHEMBL19019 | NALTREXONE | 4.0 | 1 | 7.96 |
| CHEMBL237066 | — | — | 1 | 7.64 |
| CHEMBL238316 | — | — | 1 | 7.27 |
| CHEMBL236168 | — | — | 1 | 6.89 |
| CHEMBL236169 | — | — | 1 | 6.67 |
| CHEMBL236170 | — | — | 1 | 6.30 |
| CHEMBL238315 | — | — | 1 | - |
| CHEMBL438134 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL238317 | — | Ki | = | 0.92 | nM | 9.04 |
| CHEMBL238361 | — | Ki | = | 0.97 | nM | 9.01 |
| CHEMBL300662 | — | Ki | = | 1.19 | nM | 8.92 |
| CHEMBL236376 | — | Ki | = | 2.86 | nM | 8.54 |
| CHEMBL19019 | NALTREXONE | Ki | = | 11.06 | nM | 7.96 |
| CHEMBL237066 | — | Ki | = | 23.14 | nM | 7.64 |
| CHEMBL238316 | — | Ki | = | 54.15 | nM | 7.27 |
| CHEMBL236168 | — | Ki | = | 128.07 | nM | 6.89 |
| CHEMBL236169 | — | Ki | = | 211.63 | nM | 6.67 |
| CHEMBL236170 | — | Ki | = | 495.99 | nM | 6.30 |
| CHEMBL238315 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL438134 | — | Ki | > | 1000.0 | nM | - |