Assay Detail
Binding
CHEMBL3270691
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]N-methylspiperone from human dopamine D3 receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting analysis
10
Total Activities
10
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 | Autocuration |
Publication
Tranylcypromine substituted cis-hydroxycyclobutylnaphthamides as potent and selective dopamine D₃ receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 10 | 8.46 | 9.87 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL8946 | ETICLOPRIDE | 2.0 | 1 | 9.87 |
| CHEMBL267932 | MESPIPERONE | 2.0 | 1 | 9.58 |
| CHEMBL1627305 | — | — | 1 | 8.73 |
| CHEMBL3265063 | — | — | 1 | 8.58 |
| CHEMBL3265067 | — | — | 1 | 8.55 |
| CHEMBL1255588 | — | — | 1 | 8.19 |
| CHEMBL242644 | — | — | 1 | 8.17 |
| CHEMBL8809 | RACLOPRIDE | 2.0 | 1 | 7.87 |
| CHEMBL3265064 | — | — | 1 | 7.66 |
| CHEMBL3265065 | — | — | 1 | 7.42 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL8946 | ETICLOPRIDE | Ki | = | 0.134 | nM | 9.87 |
| CHEMBL267932 | MESPIPERONE | Ki | = | 0.265 | nM | 9.58 |
| CHEMBL1627305 | — | Ki | = | 1.88 | nM | 8.73 |
| CHEMBL3265063 | — | Ki | = | 2.61 | nM | 8.58 |
| CHEMBL3265067 | — | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL1255588 | — | Ki | = | 6.39 | nM | 8.19 |
| CHEMBL242644 | — | Ki | = | 6.7 | nM | 8.17 |
| CHEMBL8809 | RACLOPRIDE | Ki | = | 13.4 | nM | 7.87 |
| CHEMBL3265064 | — | Ki | = | 22.1 | nM | 7.66 |
| CHEMBL3265065 | — | Ki | = | 37.9 | nM | 7.42 |