Assay Detail
Binding
CHEMBL4406593
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at RLuc8-fused human D3R Y365A mutant expressed in HEK293 cells co-expressing N-terminal Venus-tagged beta-arrestin2 and GRK3 assessed as induction of beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
3
Total Activities
3
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery, Optimization, and Characterization of ML417: A Novel and Highly Selective D3 Dopamine Receptor Agonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 2 | 6.88 | 7.48 |
| Activity | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL59 | DOPAMINE | 4.0 | 1 | 7.48 |
| CHEMBL4476784 | — | — | 1 | 6.28 |
| CHEMBL301265 | PRAMIPEXOLE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL59 | DOPAMINE | EC50 | = | 33.0 | nM | 7.48 |
| CHEMBL4476784 | — | EC50 | = | 520.0 | nM | 6.28 |
| CHEMBL301265 | PRAMIPEXOLE | Activity | - | — | - |