Assay Detail
Binding
CHEMBL4614013
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]WIN35428 from DAT in Sprague-Dawley rat striatum membranes incubated for 120 mins by microbeta scintillation counting method
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Striatum |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sodium-dependent dopamine transporter (CHEMBL338) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Structure-Activity Relationships for a Series of (Bis(4-fluorophenyl)methyl)sulfinyl Alkyl Alicyclic Amines at the Dopamine Transporter: Functionalizing the Terminal Nitrogen Affects Affinity, Selectivity, and Metabolic Stability.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 29 | 7.46 | 8.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4642082 | — | — | 1 | 8.89 |
| CHEMBL4649604 | — | — | 1 | 8.87 |
| CHEMBL4647914 | — | — | 1 | 8.81 |
| CHEMBL4635958 | — | — | 1 | 8.76 |
| CHEMBL4635589 | — | — | 1 | 8.72 |
| CHEMBL4640772 | — | — | 1 | 8.70 |
| CHEMBL4648300 | — | — | 1 | 8.52 |
| CHEMBL4633748 | — | — | 1 | 8.44 |
| CHEMBL4643955 | — | — | 1 | 8.41 |
| CHEMBL4639814 | — | — | 1 | 8.17 |
| CHEMBL4643859 | — | — | 1 | 8.06 |
| CHEMBL4645184 | — | — | 1 | 7.93 |
| CHEMBL4636778 | — | — | 1 | 7.64 |
| CHEMBL4636336 | — | — | 1 | 7.63 |
| CHEMBL4647200 | — | — | 1 | 7.54 |
| CHEMBL4638977 | — | — | 1 | 7.42 |
| CHEMBL4640152 | — | — | 1 | 7.41 |
| CHEMBL4645855 | — | — | 1 | 7.39 |
| CHEMBL4647283 | — | — | 1 | 7.13 |
| CHEMBL4634934 | — | — | 1 | 7.04 |
| CHEMBL4640372 | — | — | 1 | 6.90 |
| CHEMBL4641869 | — | — | 1 | 6.74 |
| CHEMBL4634776 | — | — | 1 | 6.61 |
| CHEMBL4634263 | — | — | 1 | 6.35 |
| CHEMBL4648586 | — | — | 1 | 6.27 |
| CHEMBL4647526 | — | — | 1 | 6.11 |
| CHEMBL4643380 | — | — | 1 | 5.55 |
| CHEMBL4638203 | — | — | 1 | 5.29 |
| CHEMBL1373 | MODAFINIL | 4.0 | 1 | 5.09 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4642082 | — | Ki | = | 1.29 | nM | 8.89 |
| CHEMBL4649604 | — | Ki | = | 1.34 | nM | 8.87 |
| CHEMBL4647914 | — | Ki | = | 1.53 | nM | 8.81 |
| CHEMBL4635958 | — | Ki | = | 1.72 | nM | 8.76 |
| CHEMBL4635589 | — | Ki | = | 1.91 | nM | 8.72 |
| CHEMBL4640772 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL4648300 | — | Ki | = | 3.01 | nM | 8.52 |
| CHEMBL4633748 | — | Ki | = | 3.63 | nM | 8.44 |
| CHEMBL4643955 | — | Ki | = | 3.93 | nM | 8.41 |
| CHEMBL4639814 | — | Ki | = | 6.78 | nM | 8.17 |
| CHEMBL4643859 | — | Ki | = | 8.68 | nM | 8.06 |
| CHEMBL4645184 | — | Ki | = | 11.7 | nM | 7.93 |
| CHEMBL4636778 | — | Ki | = | 23.1 | nM | 7.64 |
| CHEMBL4636336 | — | Ki | = | 23.4 | nM | 7.63 |
| CHEMBL4647200 | — | Ki | = | 28.5 | nM | 7.54 |
| CHEMBL4638977 | — | Ki | = | 37.9 | nM | 7.42 |
| CHEMBL4640152 | — | Ki | = | 39.4 | nM | 7.41 |
| CHEMBL4645855 | — | Ki | = | 40.3 | nM | 7.39 |
| CHEMBL4647283 | — | Ki | = | 73.2 | nM | 7.13 |
| CHEMBL4634934 | — | Ki | = | 92.3 | nM | 7.04 |
| CHEMBL4640372 | — | Ki | = | 127.0 | nM | 6.90 |
| CHEMBL4641869 | — | Ki | = | 182.0 | nM | 6.74 |
| CHEMBL4634776 | — | Ki | = | 245.0 | nM | 6.61 |
| CHEMBL4634263 | — | Ki | = | 449.0 | nM | 6.35 |
| CHEMBL4648586 | — | Ki | = | 536.0 | nM | 6.27 |
| CHEMBL4647526 | — | Ki | = | 782.0 | nM | 6.11 |
| CHEMBL4643380 | — | Ki | = | 2830.0 | nM | 5.55 |
| CHEMBL4638203 | — | Ki | = | 5080.0 | nM | 5.29 |
| CHEMBL1373 | MODAFINIL | Ki | = | 8160.0 | nM | 5.09 |