Assay Detail
Functional
CHEMBL5377679
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Agonist activity at mu-opioid receptor (unknown origin)
10
Total Activities
10
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
A Novel Bifunctional μOR Agonist and σ<sub>1</sub>R Antagonist with Potent Analgesic Responses and Reduced Adverse Effects.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 8 | 7.13 | 8.72 |
| Ki | 2 | 9.66 | 9.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5082165 | — | — | 1 | 9.66 |
| CHEMBL596 | FENTANYL | 4.0 | 1 | 8.72 |
| CHEMBL70 | MORPHINE | 4.0 | 1 | 7.68 |
| CHEMBL5179132 | — | — | 1 | 7.31 |
| CHEMBL4781352 | — | — | 1 | 7.28 |
| CHEMBL5086571 | — | — | 1 | 6.74 |
| CHEMBL4461774 | — | — | 1 | 6.71 |
| CHEMBL172155 | — | — | 1 | 6.31 |
| CHEMBL4439908 | — | — | 1 | 6.28 |
| CHEMBL5287561 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5082165 | — | Ki | = | 0.22 | nM | 9.66 |
| CHEMBL596 | FENTANYL | EC50 | = | 1.9 | nM | 8.72 |
| CHEMBL70 | MORPHINE | EC50 | = | 21.0 | nM | 7.68 |
| CHEMBL5179132 | — | EC50 | = | 49.0 | nM | 7.31 |
| CHEMBL4781352 | — | EC50 | = | 52.0 | nM | 7.28 |
| CHEMBL5086571 | — | EC50 | = | 183.0 | nM | 6.74 |
| CHEMBL4461774 | — | EC50 | = | 195.0 | nM | 6.71 |
| CHEMBL172155 | — | EC50 | = | 490.0 | nM | 6.31 |
| CHEMBL4439908 | — | EC50 | = | 523.0 | nM | 6.28 |
| CHEMBL5287561 | — | Ki | < | 100.0 | nM | - |