Assay Detail
Binding
CHEMBL3801670
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human D3 receptor transfected in HEK293T cells by BRET based G0 activation assay
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK-293T |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Novel Analogues of (R)-5-(Methylamino)-5,6-dihydro-4H-imidazo[4,5,1-ij]quinolin-2(1H)-one (Sumanirole) Provide Clues to Dopamine D2/D3 Receptor Agonist Selectivity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 14 | 7.15 | 8.74 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL59 | DOPAMINE | 4.0 | 1 | 8.74 |
| CHEMBL434665 | — | — | 1 | 7.74 |
| CHEMBL26181 | — | — | 1 | 7.66 |
| CHEMBL3798803 | — | — | 1 | 7.59 |
| CHEMBL3797740 | — | — | 1 | 7.51 |
| CHEMBL3797209 | — | — | 1 | 7.29 |
| CHEMBL3799157 | — | — | 1 | 7.27 |
| CHEMBL3798179 | — | — | 1 | 7.03 |
| CHEMBL3800633 | — | — | 1 | 6.94 |
| CHEMBL3799626 | — | — | 1 | 6.90 |
| CHEMBL419792 | SUMANIROLE | 3.0 | 1 | 6.73 |
| CHEMBL3800165 | — | — | 1 | 5.85 |
| CHEMBL3799271 | — | — | 1 | 5.72 |
| CHEMBL240773 | QUINPIROLE | 2.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL59 | DOPAMINE | EC50 | = | 1.8 | nM | 8.74 |
| CHEMBL434665 | — | EC50 | = | 18.3 | nM | 7.74 |
| CHEMBL26181 | — | EC50 | = | 21.8 | nM | 7.66 |
| CHEMBL3798803 | — | EC50 | = | 25.6 | nM | 7.59 |
| CHEMBL3797740 | — | EC50 | = | 30.7 | nM | 7.51 |
| CHEMBL3797209 | — | EC50 | = | 51.9 | nM | 7.29 |
| CHEMBL3799157 | — | EC50 | = | 53.7 | nM | 7.27 |
| CHEMBL3798179 | — | EC50 | = | 94.3 | nM | 7.03 |
| CHEMBL3800633 | — | EC50 | = | 115.0 | nM | 6.94 |
| CHEMBL3799626 | — | EC50 | = | 125.0 | nM | 6.90 |
| CHEMBL419792 | SUMANIROLE | EC50 | = | 186.0 | nM | 6.73 |
| CHEMBL3800165 | — | EC50 | = | 1423.0 | nM | 5.85 |
| CHEMBL3799271 | — | EC50 | = | 1890.0 | nM | 5.72 |
| CHEMBL240773 | QUINPIROLE | EC50 | - | — | - |