Assay Detail
Functional
CHEMBL5511971
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Antagonist activity at human MOR expressed in CHO-K1 cells assessed as cAMP level preincubated for 15 mins followed by agonist addition and measured after 30 mins by HitHunter cAMP analysis
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Searching for Synthetic Opioid Rescue Agents: Identification of a Potent Opioid Agonist with Reduced Respiratory Depression.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 28 | 7.52 | 8.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL300662 | — | — | 1 | 8.68 |
| CHEMBL19019 | NALTREXONE | 4.0 | 1 | 7.94 |
| CHEMBL1773189 | — | — | 1 | 7.60 |
| CHEMBL80 | NALOXONE | 4.0 | 1 | 7.56 |
| CHEMBL1773188 | — | — | 1 | 6.72 |
| CHEMBL5559659 | — | — | 1 | 6.62 |
| CHEMBL38874 | DAMGO | — | 1 | - |
| CHEMBL70 | MORPHINE | 4.0 | 1 | - |
| CHEMBL5542870 | — | — | 1 | - |
| CHEMBL5568271 | — | — | 1 | - |
| CHEMBL5523416 | — | — | 1 | - |
| CHEMBL5568344 | — | — | 1 | - |
| CHEMBL2364605 | CEBRANOPADOL | 3.0 | 1 | - |
| CHEMBL3303774 | — | — | 1 | - |
| CHEMBL511142 | BUPRENORPHINE | 4.0 | 1 | - |
| CHEMBL4467777 | — | — | 1 | - |
| CHEMBL596 | FENTANYL | 4.0 | 1 | - |
| CHEMBL5517979 | — | — | 1 | - |
| CHEMBL5557681 | — | — | 1 | - |
| CHEMBL5560603 | — | — | 1 | - |
| CHEMBL5560034 | — | — | 1 | - |
| CHEMBL5542571 | — | — | 1 | - |
| CHEMBL5558566 | — | — | 1 | - |
| CHEMBL5517852 | — | — | 1 | - |
| CHEMBL5560213 | — | — | 1 | - |
| CHEMBL5568330 | — | — | 1 | - |
| CHEMBL5568049 | — | — | 1 | - |
| CHEMBL5523393 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL300662 | — | IC50 | = | 2.09 | nM | 8.68 |
| CHEMBL19019 | NALTREXONE | IC50 | = | 11.55 | nM | 7.94 |
| CHEMBL1773189 | — | IC50 | = | 24.94 | nM | 7.60 |
| CHEMBL80 | NALOXONE | IC50 | = | 27.45 | nM | 7.56 |
| CHEMBL1773188 | — | IC50 | = | 190.25 | nM | 6.72 |
| CHEMBL5559659 | — | IC50 | = | 242.03 | nM | 6.62 |
| CHEMBL38874 | DAMGO | IC50 | - | — | - | |
| CHEMBL70 | MORPHINE | IC50 | - | — | - | |
| CHEMBL5542870 | — | IC50 | - | — | - | |
| CHEMBL5568271 | — | IC50 | - | — | - | |
| CHEMBL5523416 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5568344 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2364605 | CEBRANOPADOL | IC50 | - | — | - | |
| CHEMBL3303774 | — | IC50 | - | — | - | |
| CHEMBL511142 | BUPRENORPHINE | IC50 | - | — | - | |
| CHEMBL4467777 | — | IC50 | - | — | - | |
| CHEMBL596 | FENTANYL | IC50 | - | — | - | |
| CHEMBL5517979 | — | IC50 | - | — | - | |
| CHEMBL5557681 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5560603 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5560034 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5542571 | — | IC50 | - | — | - | |
| CHEMBL5558566 | — | IC50 | - | — | - | |
| CHEMBL5517852 | — | IC50 | - | — | - | |
| CHEMBL5560213 | — | IC50 | - | — | - | |
| CHEMBL5568330 | — | IC50 | - | — | - | |
| CHEMBL5568049 | — | IC50 | - | — | - | |
| CHEMBL5523393 | — | IC50 | - | — | - |