Assay Detail
Functional
CHEMBL5363873
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at SNAP-tagged mouse MOR transfected in HEK293T cells coexpressing wild type Galpha-i2, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-i2 activation using coelenterazine as substrate incubated for 40 mins by BRET based GPA assay
6
Total Activities
3
Compounds Tested
1
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 | 6 | 7.23 | 8.48 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL38874 | DAMGO | — | 2 | 8.48 |
| CHEMBL5433458 | — | — | 2 | 7.14 |
| CHEMBL5399270 | — | — | 2 | 6.07 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL38874 | DAMGO | EC50 | = | 3.311 | nM | 8.48 |
| CHEMBL38874 | DAMGO | EC50 | = | 3.28 | nM | 8.48 |
| CHEMBL5433458 | — | EC50 | = | 72.44 | nM | 7.14 |
| CHEMBL5433458 | — | EC50 | = | 73.4 | nM | 7.13 |
| CHEMBL5399270 | — | EC50 | = | 851.14 | nM | 6.07 |
| CHEMBL5399270 | — | EC50 | = | 848.0 | nM | 6.07 |