Assay Detail
Functional
CHEMBL5363871
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Partial 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
25
Total Activities
13
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 | 24 | 6.44 | 8.62 |
| Activity | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2443262 | OLICERIDINE | 4.0 | 2 | 8.62 |
| CHEMBL70 | MORPHINE | 4.0 | 2 | 7.92 |
| CHEMBL5418819 | — | — | 2 | 6.80 |
| CHEMBL5412995 | — | — | 2 | 6.56 |
| CHEMBL5404724 | — | — | 2 | 6.33 |
| CHEMBL5415842 | — | — | 2 | 6.22 |
| CHEMBL5397609 | — | — | 2 | 6.21 |
| CHEMBL5398913 | — | — | 2 | 6.05 |
| CHEMBL5412606 | — | — | 2 | 5.94 |
| CHEMBL5414796 | — | — | 2 | 5.74 |
| CHEMBL5434650 | — | — | 2 | 5.48 |
| CHEMBL5432993 | — | — | 2 | 5.46 |
| CHEMBL5395539 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2443262 | OLICERIDINE | EC50 | = | 2.399 | nM | 8.62 |
| CHEMBL2443262 | OLICERIDINE | EC50 | = | 2.4 | nM | 8.62 |
| CHEMBL70 | MORPHINE | EC50 | = | 12.1 | nM | 7.92 |
| CHEMBL70 | MORPHINE | EC50 | = | 12.02 | nM | 7.92 |
| CHEMBL5418819 | — | EC50 | = | 158.0 | nM | 6.80 |
| CHEMBL5418819 | — | EC50 | = | 158.49 | nM | 6.80 |
| CHEMBL5412995 | — | EC50 | = | 278.0 | nM | 6.56 |
| CHEMBL5412995 | — | EC50 | = | 275.42 | nM | 6.56 |
| CHEMBL5404724 | — | EC50 | = | 470.0 | nM | 6.33 |
| CHEMBL5404724 | — | EC50 | = | 467.74 | nM | 6.33 |
| CHEMBL5415842 | — | EC50 | = | 604.0 | nM | 6.22 |
| CHEMBL5415842 | — | EC50 | = | 602.56 | nM | 6.22 |
| CHEMBL5397609 | — | EC50 | = | 616.6 | nM | 6.21 |
| CHEMBL5397609 | — | EC50 | = | 611.0 | nM | 6.21 |
| CHEMBL5398913 | — | EC50 | = | 890.0 | nM | 6.05 |
| CHEMBL5398913 | — | EC50 | = | 891.25 | nM | 6.05 |
| CHEMBL5412606 | — | EC50 | = | 1159.0 | nM | 5.94 |
| CHEMBL5412606 | — | EC50 | = | 1148.15 | nM | 5.94 |
| CHEMBL5414796 | — | EC50 | = | 1810.0 | nM | 5.74 |
| CHEMBL5414796 | — | EC50 | = | 1819.7 | nM | 5.74 |
| CHEMBL5434650 | — | EC50 | = | 3314.0 | nM | 5.48 |
| CHEMBL5434650 | — | EC50 | = | 3311.31 | nM | 5.48 |
| CHEMBL5432993 | — | EC50 | = | 3467.37 | nM | 5.46 |
| CHEMBL5432993 | — | EC50 | = | 3447.0 | nM | 5.46 |
| CHEMBL5395539 | — | Activity | - | — | - |