Assay Detail
Binding
CHEMBL1065654
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]spiperone from cloned dopamine D2L 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 | 7.68 | 8.43 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL602065 | — | — | 1 | 8.43 |
| CHEMBL599636 | — | — | 3 | 8.43 |
| CHEMBL599635 | — | — | 2 | 8.34 |
| CHEMBL457024 | — | — | 1 | 7.58 |
| CHEMBL599841 | — | — | 1 | 7.38 |
| CHEMBL273273 | 5-OH-DPAT | — | 1 | 7.23 |
| CHEMBL602264 | — | — | 1 | 7.07 |
| CHEMBL285755 | — | — | 1 | 6.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL602065 | — | Ki | = | 3.74 | nM | 8.43 |
| CHEMBL599636 | — | Ki | = | 3.75 | nM | 8.43 |
| CHEMBL599635 | — | Ki | = | 4.55 | nM | 8.34 |
| CHEMBL599636 | — | Ki | = | 13.8 | nM | 7.86 |
| CHEMBL599635 | — | Ki | = | 15.9 | nM | 7.80 |
| CHEMBL599636 | — | Ki | = | 20.7 | nM | 7.68 |
| CHEMBL457024 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL599841 | — | Ki | = | 41.4 | nM | 7.38 |
| CHEMBL273273 | 5-OH-DPAT | Ki | = | 58.8 | nM | 7.23 |
| CHEMBL602264 | — | Ki | = | 86.0 | nM | 7.07 |
| CHEMBL285755 | — | Ki | = | 202.0 | nM | 6.70 |