Assay Detail
Binding
CHEMBL1065655
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Displacement of [3H]spiperone from cloned dopamine D3 receptor expressed in HEK cells
11
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | HEK293 |
| Confidence | 8 — Homologous 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 |
|---|---|---|---|
| Ki | 11 | 8.80 | 9.73 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL602065 | — | — | 1 | 9.73 |
| CHEMBL599635 | — | — | 2 | 9.09 |
| CHEMBL457024 | — | — | 1 | 9.08 |
| CHEMBL599636 | — | — | 3 | 8.89 |
| CHEMBL273273 | 5-OH-DPAT | — | 1 | 8.87 |
| CHEMBL285755 | — | — | 1 | 8.63 |
| CHEMBL599841 | — | — | 1 | 8.43 |
| CHEMBL602264 | — | — | 1 | 8.25 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL602065 | — | Ki | = | 0.186 | nM | 9.73 |
| CHEMBL599635 | — | Ki | = | 0.818 | nM | 9.09 |
| CHEMBL457024 | — | Ki | = | 0.825 | nM | 9.08 |
| CHEMBL599635 | — | Ki | = | 1.27 | nM | 8.90 |
| CHEMBL599636 | — | Ki | = | 1.28 | nM | 8.89 |
| CHEMBL273273 | 5-OH-DPAT | Ki | = | 1.36 | nM | 8.87 |
| CHEMBL599636 | — | Ki | = | 1.35 | nM | 8.87 |
| CHEMBL285755 | — | Ki | = | 2.35 | nM | 8.63 |
| CHEMBL599841 | — | Ki | = | 3.71 | nM | 8.43 |
| CHEMBL602264 | — | Ki | = | 5.57 | nM | 8.25 |
| CHEMBL599636 | — | Ki | = | 7.73 | nM | 8.11 |