Assay Detail
Functional
CHEMBL5511983
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Agonist activity at human DOR expressed in CHO-K1 cells assessed as decrease in cAMP level incubated for 30 mins in presence of forskolin by HitHunter cAMP analysis
11
Total Activities
11
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 | 11 | 8.05 | 10.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL340032 | DADLE | — | 1 | 10.40 |
| CHEMBL3303774 | — | — | 1 | 9.10 |
| CHEMBL5568330 | — | — | 1 | 8.76 |
| CHEMBL2364605 | CEBRANOPADOL | 3.0 | 1 | 8.42 |
| CHEMBL5542870 | — | — | 1 | 7.63 |
| CHEMBL4467777 | — | — | 1 | 6.96 |
| CHEMBL596 | FENTANYL | 4.0 | 1 | 6.82 |
| CHEMBL70 | MORPHINE | 4.0 | 1 | 6.28 |
| CHEMBL573214 | NORBINALTORPHIMINE | — | 1 | - |
| CHEMBL396460 | NOCICEPTIN | — | 1 | - |
| CHEMBL290543 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL340032 | DADLE | IC50 | = | 0.04 | nM | 10.40 |
| CHEMBL3303774 | — | IC50 | = | 0.79 | nM | 9.10 |
| CHEMBL5568330 | — | IC50 | = | 1.75 | nM | 8.76 |
| CHEMBL2364605 | CEBRANOPADOL | IC50 | = | 3.77 | nM | 8.42 |
| CHEMBL5542870 | — | IC50 | = | 23.51 | nM | 7.63 |
| CHEMBL4467777 | — | IC50 | = | 108.4 | nM | 6.96 |
| CHEMBL596 | FENTANYL | IC50 | = | 150.03 | nM | 6.82 |
| CHEMBL70 | MORPHINE | IC50 | = | 524.84 | nM | 6.28 |
| CHEMBL573214 | NORBINALTORPHIMINE | IC50 | - | — | - | |
| CHEMBL396460 | NOCICEPTIN | IC50 | - | — | - | |
| CHEMBL290543 | — | IC50 | - | — | - |