Assay Detail
Functional
CHEMBL5381014
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Partial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis
22
Total Activities
11
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 | 22 | 7.98 | 8.87 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2028019 | CARIPRAZINE | 4.0 | 2 | 8.87 |
| CHEMBL5431103 | — | — | 2 | 8.65 |
| CHEMBL5427695 | — | — | 2 | 8.39 |
| CHEMBL5437660 | — | — | 2 | 8.15 |
| CHEMBL5438081 | — | — | 2 | 8.00 |
| CHEMBL5403268 | — | — | 2 | 7.96 |
| CHEMBL5400528 | — | — | 2 | 7.93 |
| CHEMBL5435745 | — | — | 2 | 7.66 |
| CHEMBL5424897 | — | — | 2 | 7.58 |
| CHEMBL240773 | QUINPIROLE | 2.0 | 2 | 7.40 |
| CHEMBL59 | DOPAMINE | 4.0 | 2 | 7.18 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2028019 | CARIPRAZINE | EC50 | = | 1.34 | nM | 8.87 |
| CHEMBL2028019 | CARIPRAZINE | EC50 | = | 1.349 | nM | 8.87 |
| CHEMBL5431103 | — | EC50 | = | 2.239 | nM | 8.65 |
| CHEMBL5431103 | — | EC50 | = | 2.26 | nM | 8.65 |
| CHEMBL5427695 | — | EC50 | = | 4.074 | nM | 8.39 |
| CHEMBL5427695 | — | EC50 | = | 4.1 | nM | 8.39 |
| CHEMBL5437660 | — | EC50 | = | 7.079 | nM | 8.15 |
| CHEMBL5437660 | — | EC50 | = | 7.08 | nM | 8.15 |
| CHEMBL5438081 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5438081 | — | EC50 | = | 9.92 | nM | 8.00 |
| CHEMBL5403268 | — | EC50 | = | 11.02 | nM | 7.96 |
| CHEMBL5403268 | — | EC50 | = | 10.96 | nM | 7.96 |
| CHEMBL5400528 | — | EC50 | = | 11.75 | nM | 7.93 |
| CHEMBL5400528 | — | EC50 | = | 11.86 | nM | 7.93 |
| CHEMBL5435745 | — | EC50 | = | 21.88 | nM | 7.66 |
| CHEMBL5435745 | — | EC50 | = | 21.85 | nM | 7.66 |
| CHEMBL5424897 | — | EC50 | = | 26.3 | nM | 7.58 |
| CHEMBL5424897 | — | EC50 | = | 26.21 | nM | 7.58 |
| CHEMBL240773 | QUINPIROLE | EC50 | = | 39.81 | nM | 7.40 |
| CHEMBL240773 | QUINPIROLE | EC50 | = | 39.78 | nM | 7.40 |
| CHEMBL59 | DOPAMINE | EC50 | = | 66.07 | nM | 7.18 |
| CHEMBL59 | DOPAMINE | EC50 | = | 66.25 | nM | 7.18 |