Assay Detail
Binding
CHEMBL4711026
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-N-methylspiperone from human D2L 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 | 5.56 | 7.11 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3918282 | — | — | 1 | 7.11 |
| CHEMBL3931765 | — | — | 1 | 6.53 |
| CHEMBL3916231 | — | — | 1 | 6.16 |
| CHEMBL4798638 | — | — | 1 | 5.64 |
| CHEMBL4794406 | — | — | 1 | 5.54 |
| CHEMBL4744824 | — | — | 1 | 5.54 |
| CHEMBL4750607 | — | — | 1 | 5.40 |
| CHEMBL4765081 | — | — | 1 | 5.22 |
| CHEMBL4758774 | — | — | 1 | 5.18 |
| CHEMBL4791063 | — | — | 1 | 5.13 |
| CHEMBL4741279 | — | — | 1 | 5.05 |
| CHEMBL4636778 | — | — | 1 | 4.92 |
| CHEMBL4750660 | — | — | 1 | 4.91 |
| CHEMBL1373 | MODAFINIL | 4.0 | 1 | - |
| CHEMBL4777080 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3918282 | — | Ki | = | 78.6 | nM | 7.11 |
| CHEMBL3931765 | — | Ki | = | 298.0 | nM | 6.53 |
| CHEMBL3916231 | — | Ki | = | 693.0 | nM | 6.16 |
| CHEMBL4798638 | — | Ki | = | 2270.0 | nM | 5.64 |
| CHEMBL4794406 | — | Ki | = | 2920.0 | nM | 5.54 |
| CHEMBL4744824 | — | Ki | = | 2900.0 | nM | 5.54 |
| CHEMBL4750607 | — | Ki | = | 4020.0 | nM | 5.40 |
| CHEMBL4765081 | — | Ki | = | 6070.0 | nM | 5.22 |
| CHEMBL4758774 | — | Ki | = | 6610.0 | nM | 5.18 |
| CHEMBL4791063 | — | Ki | = | 7440.0 | nM | 5.13 |
| CHEMBL4741279 | — | Ki | = | 8830.0 | nM | 5.05 |
| CHEMBL4636778 | — | Ki | = | 11900.0 | nM | 4.92 |
| CHEMBL4750660 | — | Ki | = | 12400.0 | nM | 4.91 |
| CHEMBL1373 | MODAFINIL | Ki | > | 100000.0 | nM | - |
| CHEMBL4777080 | — | Ki | = | 156000.0 | nM | - |