Assay Detail
Functional
CHEMBL4406543
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Agonist activity at human D3R expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 5 mins in presence of beta-adrenergic blocker propranolol and coelenterazine H by CAMYEL BRET assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| 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 | 7.77 | 8.46 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL59 | DOPAMINE | 4.0 | 1 | 8.46 |
| CHEMBL4476784 | — | — | 1 | 7.07 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL59 | DOPAMINE | EC50 | = | 3.5 | nM | 8.46 |
| CHEMBL4476784 | — | EC50 | = | 86.0 | nM | 7.07 |