Assay Detail
Binding
CHEMBL3270686
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Displacement of [3H]R-(+)-7-OHDPAT from dopamine D3 receptor in Sprague-Dawley rat ventral striatum after 90 mins
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Ventral striatum |
| 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 | 13 | 7.33 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2203405 | — | — | 1 | 9.40 |
| CHEMBL540612 | — | — | 1 | 8.92 |
| CHEMBL3265067 | — | — | 1 | 8.57 |
| CHEMBL3265063 | — | — | 1 | 8.34 |
| CHEMBL3265064 | — | — | 1 | 7.72 |
| CHEMBL3265065 | — | — | 1 | 7.55 |
| CHEMBL3265062 | — | — | 1 | 7.36 |
| CHEMBL1081023 | — | — | 1 | 7.34 |
| CHEMBL3265061 | — | — | 1 | 6.97 |
| CHEMBL3265066 | — | — | 1 | 6.34 |
| CHEMBL3265059 | — | — | 1 | 5.93 |
| CHEMBL3265060 | — | — | 1 | 5.92 |
| CHEMBL3989843 | TRANYLCYPROMINE | 4.0 | 1 | 4.89 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2203405 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL540612 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL3265067 | — | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL3265063 | — | Ki | = | 4.6 | nM | 8.34 |
| CHEMBL3265064 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL3265065 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL3265062 | — | Ki | = | 44.0 | nM | 7.36 |
| CHEMBL1081023 | — | Ki | = | 46.0 | nM | 7.34 |
| CHEMBL3265061 | — | Ki | = | 108.0 | nM | 6.97 |
| CHEMBL3265066 | — | Ki | = | 457.0 | nM | 6.34 |
| CHEMBL3265059 | — | Ki | = | 1171.0 | nM | 5.93 |
| CHEMBL3265060 | — | Ki | = | 1195.0 | nM | 5.92 |
| CHEMBL3989843 | TRANYLCYPROMINE | Ki | = | 12793.0 | nM | 4.89 |