Assay Detail
Functional
CHEMBL1065658
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Agonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of 4-(4-(2-((5-Hydroxy-1,2,3,4-tetrahydronaphthalen-2-yl)(propyl)amino)ethyl)piperazin-1-yl)quinolin-8-ol and its analogues as highly potent dopamine D2/D3 agonists and as iron chelator: in vivo activity indicates potential application in symptomatic and neuroprotective therapy for Parkinson's disease.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 4 | 8.56 | 9.13 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL599635 | — | — | 1 | 9.13 |
| CHEMBL599636 | — | — | 1 | 8.80 |
| CHEMBL59 | DOPAMINE | 4.0 | 1 | 8.32 |
| CHEMBL589 | ROPINIROLE | 4.0 | 1 | 7.99 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL599635 | — | EC50 | = | 0.74 | nM | 9.13 |
| CHEMBL599636 | — | EC50 | = | 1.58 | nM | 8.80 |
| CHEMBL59 | DOPAMINE | EC50 | = | 4.76 | nM | 8.32 |
| CHEMBL589 | ROPINIROLE | EC50 | = | 10.3 | nM | 7.99 |