Assay Detail
Binding
CHEMBL4711027
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Displacement of [3H]-N-methylspiperone from human D3 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting method
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Structure-activity relationships for a series of (Bis(4-fluorophenyl)methyl)sulfinylethyl-aminopiperidines and -piperidine amines at the dopamine transporter: Bioisosteric replacement of the piperazine improves metabolic stability.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 15 | 5.60 | 6.37 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3916231 | — | — | 1 | 6.37 |
| CHEMBL3931765 | — | — | 1 | 6.32 |
| CHEMBL3918282 | — | — | 1 | 6.19 |
| CHEMBL4750607 | — | — | 1 | 6.16 |
| CHEMBL4798638 | — | — | 1 | 6.15 |
| CHEMBL4794406 | — | — | 1 | 6.04 |
| CHEMBL4636778 | — | — | 1 | 5.83 |
| CHEMBL4744824 | — | — | 1 | 5.60 |
| CHEMBL4791063 | — | — | 1 | 5.49 |
| CHEMBL4765081 | — | — | 1 | 5.47 |
| CHEMBL4741279 | — | — | 1 | 5.28 |
| CHEMBL4758774 | — | — | 1 | 5.26 |
| CHEMBL4750660 | — | — | 1 | 4.91 |
| CHEMBL4777080 | — | — | 1 | 4.55 |
| CHEMBL1373 | MODAFINIL | 4.0 | 1 | 4.41 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3916231 | — | Ki | = | 424.0 | nM | 6.37 |
| CHEMBL3931765 | — | Ki | = | 480.0 | nM | 6.32 |
| CHEMBL3918282 | — | Ki | = | 652.0 | nM | 6.19 |
| CHEMBL4750607 | — | Ki | = | 691.0 | nM | 6.16 |
| CHEMBL4798638 | — | Ki | = | 701.0 | nM | 6.15 |
| CHEMBL4794406 | — | Ki | = | 911.0 | nM | 6.04 |
| CHEMBL4636778 | — | Ki | = | 1470.0 | nM | 5.83 |
| CHEMBL4744824 | — | Ki | = | 2510.0 | nM | 5.60 |
| CHEMBL4791063 | — | Ki | = | 3260.0 | nM | 5.49 |
| CHEMBL4765081 | — | Ki | = | 3420.0 | nM | 5.47 |
| CHEMBL4741279 | — | Ki | = | 5230.0 | nM | 5.28 |
| CHEMBL4758774 | — | Ki | = | 5500.0 | nM | 5.26 |
| CHEMBL4750660 | — | Ki | = | 12400.0 | nM | 4.91 |
| CHEMBL4777080 | — | Ki | = | 28200.0 | nM | 4.55 |
| CHEMBL1373 | MODAFINIL | Ki | = | 39000.0 | nM | 4.41 |