Assay Detail
Functional
CHEMBL5511985
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Agonist activity at human KOR expressed in CHO-K1 cells assessed as decrease in cAMP level incubated for 30 mins in presence of forskolin by HitHunter cAMP analysis
13
Total Activities
13
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 | 13 | 7.39 | 9.27 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL290543 | — | — | 1 | 9.27 |
| CHEMBL3303774 | — | — | 1 | 8.44 |
| CHEMBL2364605 | CEBRANOPADOL | 3.0 | 1 | 6.78 |
| CHEMBL70 | MORPHINE | 4.0 | 1 | 6.46 |
| CHEMBL596 | FENTANYL | 4.0 | 1 | 6.01 |
| CHEMBL5523416 | — | — | 1 | - |
| CHEMBL5568344 | — | — | 1 | - |
| CHEMBL4467777 | — | — | 1 | - |
| CHEMBL5542870 | — | — | 1 | - |
| CHEMBL5568330 | — | — | 1 | - |
| CHEMBL340032 | DADLE | — | 1 | - |
| CHEMBL396460 | NOCICEPTIN | — | 1 | - |
| CHEMBL573214 | NORBINALTORPHIMINE | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL290543 | — | EC50 | = | 0.54 | nM | 9.27 |
| CHEMBL3303774 | — | EC50 | = | 3.65 | nM | 8.44 |
| CHEMBL2364605 | CEBRANOPADOL | EC50 | = | 166.02 | nM | 6.78 |
| CHEMBL70 | MORPHINE | EC50 | = | 345.67 | nM | 6.46 |
| CHEMBL596 | FENTANYL | EC50 | = | 987.35 | nM | 6.01 |
| CHEMBL5523416 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL5568344 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL4467777 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL5542870 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL5568330 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL340032 | DADLE | EC50 | - | — | - | |
| CHEMBL396460 | NOCICEPTIN | EC50 | - | — | - | |
| CHEMBL573214 | NORBINALTORPHIMINE | EC50 | - | — | - |