Assay Detail
Functional
CHEMBL5363879
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Partial agonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins by BRET based GPA assay
16
Total Activities
12
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| 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 |
|---|---|---|---|
| Activity | 8 | - | - |
| EC50 | 8 | 7.50 | 8.01 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5414796 | — | — | 2 | 8.01 |
| CHEMBL5434650 | — | — | 2 | 7.60 |
| CHEMBL5418819 | — | — | 2 | 7.38 |
| CHEMBL5399270 | — | — | 2 | 7.01 |
| CHEMBL5432993 | — | — | 1 | - |
| CHEMBL5404724 | — | — | 1 | - |
| CHEMBL5412606 | — | — | 1 | - |
| CHEMBL5395539 | — | — | 1 | - |
| CHEMBL5398913 | — | — | 1 | - |
| CHEMBL5397609 | — | — | 1 | - |
| CHEMBL5412995 | — | — | 1 | - |
| CHEMBL5433458 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5414796 | — | EC50 | = | 9.772 | nM | 8.01 |
| CHEMBL5414796 | — | EC50 | = | 9.84 | nM | 8.01 |
| CHEMBL5434650 | — | EC50 | = | 25.12 | nM | 7.60 |
| CHEMBL5434650 | — | EC50 | = | 25.4 | nM | 7.59 |
| CHEMBL5418819 | — | EC50 | = | 41.69 | nM | 7.38 |
| CHEMBL5418819 | — | EC50 | = | 41.7 | nM | 7.38 |
| CHEMBL5399270 | — | EC50 | = | 97.72 | nM | 7.01 |
| CHEMBL5399270 | — | EC50 | = | 98.0 | nM | 7.01 |
| CHEMBL5432993 | — | Activity | - | — | - | |
| CHEMBL5404724 | — | Activity | - | — | - | |
| CHEMBL5412606 | — | Activity | - | — | - | |
| CHEMBL5395539 | — | Activity | - | — | - | |
| CHEMBL5398913 | — | Activity | - | — | - | |
| CHEMBL5397609 | — | Activity | - | — | - | |
| CHEMBL5412995 | — | Activity | - | — | - | |
| CHEMBL5433458 | — | Activity | - | — | - |