Assay Detail
Binding
CHEMBL3801674
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Agonist activity at recombinant human D3 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometry
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHOp |
| 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 | 7.51 | 9.09 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL434665 | — | — | 1 | 9.09 |
| CHEMBL59 | DOPAMINE | 4.0 | 1 | 8.57 |
| CHEMBL240773 | QUINPIROLE | 2.0 | 1 | 8.48 |
| CHEMBL3797209 | — | — | 1 | 8.43 |
| CHEMBL3799626 | — | — | 1 | 7.92 |
| CHEMBL3800633 | — | — | 1 | 7.71 |
| CHEMBL3798803 | — | — | 1 | 7.66 |
| CHEMBL3798179 | — | — | 1 | 7.28 |
| CHEMBL3800165 | — | — | 1 | 7.25 |
| CHEMBL3797740 | — | — | 1 | 6.83 |
| CHEMBL3799157 | — | — | 1 | 6.75 |
| CHEMBL419792 | SUMANIROLE | 3.0 | 1 | 6.17 |
| CHEMBL3799271 | — | — | 1 | 5.47 |
| CHEMBL26181 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL434665 | — | EC50 | = | 0.81 | nM | 9.09 |
| CHEMBL59 | DOPAMINE | EC50 | = | 2.7 | nM | 8.57 |
| CHEMBL240773 | QUINPIROLE | EC50 | = | 3.3 | nM | 8.48 |
| CHEMBL3797209 | — | EC50 | = | 3.7 | nM | 8.43 |
| CHEMBL3799626 | — | EC50 | = | 11.9 | nM | 7.92 |
| CHEMBL3800633 | — | EC50 | = | 19.6 | nM | 7.71 |
| CHEMBL3798803 | — | EC50 | = | 22.0 | nM | 7.66 |
| CHEMBL3798179 | — | EC50 | = | 53.0 | nM | 7.28 |
| CHEMBL3800165 | — | EC50 | = | 56.1 | nM | 7.25 |
| CHEMBL3797740 | — | EC50 | = | 148.0 | nM | 6.83 |
| CHEMBL3799157 | — | EC50 | = | 178.0 | nM | 6.75 |
| CHEMBL419792 | SUMANIROLE | EC50 | = | 669.0 | nM | 6.17 |
| CHEMBL3799271 | — | EC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL26181 | — | EC50 | - | — | - |