Assay Detail
Binding
CHEMBL925795
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Activation of human mu opioid receptor expressed in HEK293a cells co-expressing YFP-labelled alphai1 and CFP-labelled beta1gamma2 Gi subunits assessed as Gi protein activation by fluorescence resonance energy transfer
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293-A |
| 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 |
|---|---|---|---|
| EC50 | 9 | 6.26 | 8.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL70 | MORPHINE | 4.0 | 1 | 8.22 |
| CHEMBL255467 | MORPHINONE | — | 1 | 7.55 |
| CHEMBL437602 | ORIPAVINE | — | 1 | 6.56 |
| CHEMBL257627 | CODEINONE | — | 1 | 6.53 |
| CHEMBL403893 | THEBAINE | — | 1 | 5.25 |
| CHEMBL485 | CODEINE | 4.0 | 1 | 5.21 |
| CHEMBL404097 | SALUTARIDINE | — | 1 | 4.49 |
| CHEMBL401501 | (R)-RETICULINE | — | 1 | - |
| CHEMBL255882 | SALUTARIDINOL | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL70 | MORPHINE | EC50 | = | 6.0 | nM | 8.22 |
| CHEMBL255467 | MORPHINONE | EC50 | = | 28.0 | nM | 7.55 |
| CHEMBL437602 | ORIPAVINE | EC50 | = | 277.0 | nM | 6.56 |
| CHEMBL257627 | CODEINONE | EC50 | = | 294.0 | nM | 6.53 |
| CHEMBL403893 | THEBAINE | EC50 | = | 5600.0 | nM | 5.25 |
| CHEMBL485 | CODEINE | EC50 | = | 6100.0 | nM | 5.21 |
| CHEMBL404097 | SALUTARIDINE | EC50 | = | 32500.0 | nM | 4.49 |
| CHEMBL401501 | (R)-RETICULINE | EC50 | - | — | - | |
| CHEMBL255882 | SALUTARIDINOL | EC50 | - | — | - |