Assay Detail
Binding
CHEMBL4711029
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-Nisoxetine from NET in Sprague-Dawley rat frontal cortex membrane after 180 mins by microbeta scintillation counting method
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Frontal cortex |
| Subcellular | Membrane |
| Confidence | 0 — Uncurated / Unknown |
| 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 | 5.47 | 6.59 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4741279 | — | — | 1 | 6.59 |
| CHEMBL4750607 | — | — | 1 | 6.23 |
| CHEMBL4744824 | — | — | 1 | 6.04 |
| CHEMBL4791063 | — | — | 1 | 5.79 |
| CHEMBL3918282 | — | — | 1 | 5.08 |
| CHEMBL4750660 | — | — | 1 | 4.95 |
| CHEMBL4636778 | — | — | 1 | 4.94 |
| CHEMBL3916231 | — | — | 1 | 4.93 |
| CHEMBL4777080 | — | — | 1 | 4.64 |
| CHEMBL1373 | MODAFINIL | 4.0 | 1 | - |
| CHEMBL3931765 | — | — | 1 | - |
| CHEMBL4794406 | — | — | 1 | - |
| CHEMBL4758774 | — | — | 1 | - |
| CHEMBL4798638 | — | — | 1 | - |
| CHEMBL4765081 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4741279 | — | Ki | = | 258.0 | nM | 6.59 |
| CHEMBL4750607 | — | Ki | = | 585.0 | nM | 6.23 |
| CHEMBL4744824 | — | Ki | = | 920.0 | nM | 6.04 |
| CHEMBL4791063 | — | Ki | = | 1619.0 | nM | 5.79 |
| CHEMBL3918282 | — | Ki | = | 8240.0 | nM | 5.08 |
| CHEMBL4750660 | — | Ki | = | 11200.0 | nM | 4.95 |
| CHEMBL4636778 | — | Ki | = | 11500.0 | nM | 4.94 |
| CHEMBL3916231 | — | Ki | = | 11820.0 | nM | 4.93 |
| CHEMBL4777080 | — | Ki | = | 23000.0 | nM | 4.64 |
| CHEMBL1373 | MODAFINIL | Ki | > | 100000.0 | nM | - |
| CHEMBL3931765 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL4794406 | — | Ki | - | — | - | |
| CHEMBL4758774 | — | Ki | - | — | - | |
| CHEMBL4798638 | — | Ki | - | — | - | |
| CHEMBL4765081 | — | Ki | - | — | - |