Assay Detail
Functional
CHEMBL5363875
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Partial agonist activity at Rluc8 fused mouse MOR transfected in HEK293T cells coexpressing wild type GRK2 assessed as arrestin-3 recruitment using coelenterazine as substrate incubated for 40 mins by BRET assay
15
Total Activities
10
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Mus musculus |
| Cell Type | HEK293T |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Pharmacological and Physicochemical Properties Optimization for Dual-Target Dopamine D<sub>3</sub> (D<sub>3</sub>R) and μ-Opioid (MOR) Receptor Ligands as Potentially Safer Analgesics.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 10 | 6.39 | 7.49 |
| Activity | 5 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2443262 | OLICERIDINE | 4.0 | 2 | 7.49 |
| CHEMBL70 | MORPHINE | 4.0 | 2 | 6.68 |
| CHEMBL5418819 | — | — | 2 | 6.33 |
| CHEMBL5412995 | — | — | 2 | 6.06 |
| CHEMBL5397609 | — | — | 2 | 5.38 |
| CHEMBL5432993 | — | — | 1 | - |
| CHEMBL5434650 | — | — | 1 | - |
| CHEMBL5414796 | — | — | 1 | - |
| CHEMBL5404724 | — | — | 1 | - |
| CHEMBL5395539 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2443262 | OLICERIDINE | EC50 | = | 32.36 | nM | 7.49 |
| CHEMBL2443262 | OLICERIDINE | EC50 | = | 32.5 | nM | 7.49 |
| CHEMBL70 | MORPHINE | EC50 | = | 208.93 | nM | 6.68 |
| CHEMBL70 | MORPHINE | EC50 | = | 207.0 | nM | 6.68 |
| CHEMBL5418819 | — | EC50 | = | 467.74 | nM | 6.33 |
| CHEMBL5418819 | — | EC50 | = | 470.0 | nM | 6.33 |
| CHEMBL5412995 | — | EC50 | = | 870.96 | nM | 6.06 |
| CHEMBL5412995 | — | EC50 | = | 876.0 | nM | 6.06 |
| CHEMBL5397609 | — | EC50 | = | 4168.69 | nM | 5.38 |
| CHEMBL5397609 | — | EC50 | = | 4206.0 | nM | 5.38 |
| CHEMBL5432993 | — | Activity | - | — | - | |
| CHEMBL5434650 | — | Activity | - | — | - | |
| CHEMBL5414796 | — | Activity | - | — | - | |
| CHEMBL5404724 | — | Activity | - | — | - | |
| CHEMBL5395539 | — | Activity | - | — | - |