Assay Detail
Functional
CHEMBL5511973
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Agonist activity at human MOR expressed in CHO-K1 cells assessed as decrease in cAMP level incubated for 30 mins in presence of forskolin 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 |
|---|---|---|---|
| EC50 | 28 | 7.85 | 9.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL596 | FENTANYL | 4.0 | 1 | 9.68 |
| CHEMBL5568344 | — | — | 1 | 9.59 |
| CHEMBL5542870 | — | — | 1 | 9.57 |
| CHEMBL2364605 | CEBRANOPADOL | 3.0 | 1 | 9.49 |
| CHEMBL38874 | DAMGO | — | 1 | 9.48 |
| CHEMBL5523416 | — | — | 1 | 9.41 |
| CHEMBL5568330 | — | — | 1 | 9.21 |
| CHEMBL511142 | BUPRENORPHINE | 4.0 | 1 | 8.62 |
| CHEMBL4467777 | — | — | 1 | 8.54 |
| CHEMBL70 | MORPHINE | 4.0 | 1 | 8.12 |
| CHEMBL5523393 | — | — | 1 | 7.38 |
| CHEMBL5568271 | — | — | 1 | 7.07 |
| CHEMBL5517979 | — | — | 1 | 6.92 |
| CHEMBL5542571 | — | — | 1 | 6.91 |
| CHEMBL5568049 | — | — | 1 | 6.67 |
| CHEMBL5517852 | — | — | 1 | 6.59 |
| CHEMBL5560603 | — | — | 1 | 6.49 |
| CHEMBL5558566 | — | — | 1 | 6.41 |
| CHEMBL5557681 | — | — | 1 | 6.38 |
| CHEMBL5560034 | — | — | 1 | 6.29 |
| CHEMBL5560213 | — | — | 1 | 5.96 |
| CHEMBL80 | NALOXONE | 4.0 | 1 | - |
| CHEMBL19019 | NALTREXONE | 4.0 | 1 | - |
| CHEMBL300662 | — | — | 1 | - |
| CHEMBL3303774 | — | — | 1 | - |
| CHEMBL1773189 | — | — | 1 | - |
| CHEMBL1773188 | — | — | 1 | - |
| CHEMBL5559659 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL596 | FENTANYL | EC50 | = | 0.21 | nM | 9.68 |
| CHEMBL5568344 | — | EC50 | = | 0.26 | nM | 9.59 |
| CHEMBL5542870 | — | EC50 | = | 0.27 | nM | 9.57 |
| CHEMBL2364605 | CEBRANOPADOL | EC50 | = | 0.32 | nM | 9.49 |
| CHEMBL38874 | DAMGO | EC50 | = | 0.33 | nM | 9.48 |
| CHEMBL5523416 | — | EC50 | = | 0.39 | nM | 9.41 |
| CHEMBL5568330 | — | EC50 | = | 0.61 | nM | 9.21 |
| CHEMBL511142 | BUPRENORPHINE | EC50 | = | 2.37 | nM | 8.62 |
| CHEMBL4467777 | — | EC50 | = | 2.85 | nM | 8.54 |
| CHEMBL70 | MORPHINE | EC50 | = | 7.64 | nM | 8.12 |
| CHEMBL5523393 | — | EC50 | = | 41.26 | nM | 7.38 |
| CHEMBL5568271 | — | EC50 | = | 84.25 | nM | 7.07 |
| CHEMBL5517979 | — | EC50 | = | 121.73 | nM | 6.92 |
| CHEMBL5542571 | — | EC50 | = | 124.13 | nM | 6.91 |
| CHEMBL5568049 | — | EC50 | = | 213.35 | nM | 6.67 |
| CHEMBL5517852 | — | EC50 | = | 256.33 | nM | 6.59 |
| CHEMBL5560603 | — | EC50 | = | 324.8 | nM | 6.49 |
| CHEMBL5558566 | — | EC50 | = | 392.23 | nM | 6.41 |
| CHEMBL5557681 | — | EC50 | = | 421.17 | nM | 6.38 |
| CHEMBL5560034 | — | EC50 | = | 516.8 | nM | 6.29 |
| CHEMBL5560213 | — | EC50 | = | 1107.97 | nM | 5.96 |
| CHEMBL80 | NALOXONE | EC50 | - | — | - | |
| CHEMBL19019 | NALTREXONE | EC50 | - | — | - | |
| CHEMBL300662 | — | EC50 | - | — | - | |
| CHEMBL3303774 | — | EC50 | = | 0.004 | nM | - |
| CHEMBL1773189 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL1773188 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL5559659 | — | EC50 | > | 10000.0 | nM | - |