Assay Detail
Functional
CHEMBL5381016
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
16
Total Activities
8
Compounds Tested
1
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
Dopamine D<sub>3</sub>/D<sub>2</sub> Receptor Ligands Based on Cariprazine for the Treatment of Psychostimulant Use Disorders That May Be Dual Diagnosed with Affective Disorders.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 16 | 8.39 | 8.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5431103 | — | — | 2 | 8.80 |
| CHEMBL5427695 | — | — | 2 | 8.79 |
| CHEMBL2028019 | CARIPRAZINE | 4.0 | 2 | 8.72 |
| CHEMBL240773 | QUINPIROLE | 2.0 | 2 | 8.59 |
| CHEMBL5403268 | — | — | 2 | 8.54 |
| CHEMBL5400528 | — | — | 2 | 8.22 |
| CHEMBL5438081 | — | — | 2 | 7.80 |
| CHEMBL5435745 | — | — | 2 | 7.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5431103 | — | EC50 | = | 1.585 | nM | 8.80 |
| CHEMBL5431103 | — | EC50 | = | 1.6 | nM | 8.80 |
| CHEMBL5427695 | — | EC50 | = | 1.622 | nM | 8.79 |
| CHEMBL5427695 | — | EC50 | = | 1.64 | nM | 8.79 |
| CHEMBL2028019 | CARIPRAZINE | EC50 | = | 1.905 | nM | 8.72 |
| CHEMBL2028019 | CARIPRAZINE | EC50 | = | 1.89 | nM | 8.72 |
| CHEMBL240773 | QUINPIROLE | EC50 | = | 2.57 | nM | 8.59 |
| CHEMBL240773 | QUINPIROLE | EC50 | = | 2.59 | nM | 8.59 |
| CHEMBL5403268 | — | EC50 | = | 2.884 | nM | 8.54 |
| CHEMBL5403268 | — | EC50 | = | 2.87 | nM | 8.54 |
| CHEMBL5400528 | — | EC50 | = | 6.026 | nM | 8.22 |
| CHEMBL5400528 | — | EC50 | = | 6.07 | nM | 8.22 |
| CHEMBL5438081 | — | EC50 | = | 15.85 | nM | 7.80 |
| CHEMBL5438081 | — | EC50 | = | 16.02 | nM | 7.79 |
| CHEMBL5435745 | — | EC50 | = | 19.95 | nM | 7.70 |
| CHEMBL5435745 | — | EC50 | = | 19.91 | nM | 7.70 |