Assay Detail
Binding
CHEMBL4614036
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human DAT transiently expressed in COS7 cells assessed as reduction in [3H]-DA uptake measured after 5 mins by beta-scintillation counting method
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | COS-7 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sodium-dependent dopamine transporter (CHEMBL238) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
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 | 4 | 6.95 | 7.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4639814 | — | — | 1 | 7.96 |
| CHEMBL4636778 | — | — | 1 | 7.00 |
| CHEMBL4640372 | — | — | 1 | 6.57 |
| CHEMBL4634776 | — | — | 1 | 6.26 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4639814 | — | Ki | = | 11.1 | nM | 7.96 |
| CHEMBL4636778 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL4640372 | — | Ki | = | 268.0 | nM | 6.57 |
| CHEMBL4634776 | — | Ki | = | 552.0 | nM | 6.26 |