Assay Detail
Functional
CHEMBL4015818
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Agonist activity at human D2S receptor expressed in HEK293T cell membranes coexpressing Galphao1 assessed as induction of nucleotide exchange preincubated for 30 mins followed by addition of [35S]GTPgammaS measured after 30 mins by [35S]GTPgammaS binding assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK-293T |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Hydroxy-Substituted Heteroarylpiperazines: Novel Scaffolds for β-Arrestin-Biased D2R Agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 11 | 7.05 | 8.49 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1303 | ROTIGOTINE | 4.0 | 1 | 8.49 |
| CHEMBL4102628 | — | — | 1 | 7.17 |
| CHEMBL4064742 | — | — | 1 | 7.11 |
| CHEMBL4091507 | — | — | 1 | 7.05 |
| CHEMBL301265 | PRAMIPEXOLE | 4.0 | 1 | 7.00 |
| CHEMBL1112 | ARIPIPRAZOLE | 4.0 | 1 | 6.89 |
| CHEMBL59 | DOPAMINE | 4.0 | 1 | 6.70 |
| CHEMBL240773 | QUINPIROLE | 2.0 | 1 | 6.57 |
| CHEMBL589 | ROPINIROLE | 4.0 | 1 | 6.48 |
| CHEMBL4084690 | — | — | 1 | - |
| CHEMBL2165126 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1303 | ROTIGOTINE | EC50 | = | 3.2 | nM | 8.49 |
| CHEMBL4102628 | — | EC50 | = | 67.0 | nM | 7.17 |
| CHEMBL4064742 | — | EC50 | = | 78.0 | nM | 7.11 |
| CHEMBL4091507 | — | EC50 | = | 90.0 | nM | 7.05 |
| CHEMBL301265 | PRAMIPEXOLE | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL1112 | ARIPIPRAZOLE | EC50 | = | 130.0 | nM | 6.89 |
| CHEMBL59 | DOPAMINE | EC50 | = | 200.0 | nM | 6.70 |
| CHEMBL240773 | QUINPIROLE | EC50 | = | 270.0 | nM | 6.57 |
| CHEMBL589 | ROPINIROLE | EC50 | = | 330.0 | nM | 6.48 |
| CHEMBL4084690 | — | EC50 | > | 5000.0 | nM | - |
| CHEMBL2165126 | — | EC50 | > | 5000.0 | nM | - |