Assay Detail
Binding
CHEMBL1050538
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]spiperone from human dopamine D3 receptor expressed in HEK293 cells
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Development of (S)-N6-(2-(4-(isoquinolin-1-yl)piperazin-1-yl)ethyl)-N6-propyl-4,5,6,7-tetrahydrobenzo[d]-thiazole-2,6-diamine and its analogue as a D3 receptor preferring agonist: potent in vivo activity in Parkinson's disease animal models.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 17 | 8.97 | 9.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL569977 | — | — | 1 | 9.72 |
| CHEMBL568801 | — | — | 1 | 9.40 |
| CHEMBL569322 | — | — | 1 | 9.36 |
| CHEMBL569747 | — | — | 1 | 9.36 |
| CHEMBL569746 | — | — | 1 | 9.24 |
| CHEMBL569003 | — | — | 1 | 9.16 |
| CHEMBL457025 | — | — | 1 | 9.08 |
| CHEMBL514885 | — | — | 1 | 9.04 |
| CHEMBL569107 | — | — | 1 | 8.92 |
| CHEMBL568822 | — | — | 1 | 8.90 |
| CHEMBL273273 | 5-OH-DPAT | — | 1 | 8.87 |
| CHEMBL456825 | — | — | 1 | 8.75 |
| CHEMBL571992 | — | — | 1 | 8.65 |
| CHEMBL301559 | — | — | 1 | 8.63 |
| CHEMBL577073 | — | — | 1 | 8.58 |
| CHEMBL570187 | — | — | 1 | 8.58 |
| CHEMBL570188 | — | — | 1 | 8.32 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL569977 | — | Ki | = | 0.19 | nM | 9.72 |
| CHEMBL568801 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL569322 | — | Ki | = | 0.441 | nM | 9.36 |
| CHEMBL569747 | — | Ki | = | 0.435 | nM | 9.36 |
| CHEMBL569746 | — | Ki | = | 0.57 | nM | 9.24 |
| CHEMBL569003 | — | Ki | = | 0.685 | nM | 9.16 |
| CHEMBL457025 | — | Ki | = | 0.825 | nM | 9.08 |
| CHEMBL514885 | — | Ki | = | 0.92 | nM | 9.04 |
| CHEMBL569107 | — | Ki | = | 1.21 | nM | 8.92 |
| CHEMBL568822 | — | Ki | = | 1.27 | nM | 8.90 |
| CHEMBL273273 | 5-OH-DPAT | Ki | = | 1.36 | nM | 8.87 |
| CHEMBL456825 | — | Ki | = | 1.77 | nM | 8.75 |
| CHEMBL571992 | — | Ki | = | 2.23 | nM | 8.65 |
| CHEMBL301559 | — | Ki | = | 2.35 | nM | 8.63 |
| CHEMBL577073 | — | Ki | = | 2.61 | nM | 8.58 |
| CHEMBL570187 | — | Ki | = | 2.65 | nM | 8.58 |
| CHEMBL570188 | — | Ki | = | 4.78 | nM | 8.32 |