Assay Detail
Binding
CHEMBL925796
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Displacement of [3H]naloxone from human mu poioid receptor expressed in HEK293 cells
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Live cell monitoring of mu-opioid receptor-mediated G-protein activation reveals strong biological activity of close morphine biosynthetic precursors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 9 | 6.13 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL70 | MORPHINE | 4.0 | 1 | 8.40 |
| CHEMBL255467 | MORPHINONE | — | 1 | 6.84 |
| CHEMBL437602 | ORIPAVINE | — | 1 | 6.54 |
| CHEMBL257627 | CODEINONE | — | 1 | 6.34 |
| CHEMBL485 | CODEINE | 4.0 | 1 | 5.20 |
| CHEMBL403893 | THEBAINE | — | 1 | 5.13 |
| CHEMBL404097 | SALUTARIDINE | — | 1 | 4.46 |
| CHEMBL401501 | (R)-RETICULINE | — | 1 | - |
| CHEMBL255882 | SALUTARIDINOL | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL70 | MORPHINE | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL255467 | MORPHINONE | Ki | = | 146.0 | nM | 6.84 |
| CHEMBL437602 | ORIPAVINE | Ki | = | 286.0 | nM | 6.54 |
| CHEMBL257627 | CODEINONE | Ki | = | 459.0 | nM | 6.34 |
| CHEMBL485 | CODEINE | Ki | = | 6300.0 | nM | 5.20 |
| CHEMBL403893 | THEBAINE | Ki | = | 7400.0 | nM | 5.13 |
| CHEMBL404097 | SALUTARIDINE | Ki | = | 34600.0 | nM | 4.46 |
| CHEMBL401501 | (R)-RETICULINE | Ki | - | — | - | |
| CHEMBL255882 | SALUTARIDINOL | Ki | - | — | - |