Assay Detail
Binding
CHEMBL4011343
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human DAT expressed in HEK293 cell membranes assessed as reduction in [3H]-DA uptake incubated for 22 mins by micro beta scintillation counting analysis
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sodium-dependent dopamine transporter (CHEMBL238) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Scaffold Repurposing of Nucleosides (Adenosine Receptor Agonists): Enhanced Activity at the Human Dopamine and Norepinephrine Sodium Symporters.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 6.76 | 7.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL781 | MAZINDOL | 4.0 | 1 | 7.89 |
| CHEMBL2064645 | — | — | 1 | 7.04 |
| CHEMBL4093756 | — | — | 1 | 6.97 |
| CHEMBL4066973 | — | — | 1 | 6.90 |
| CHEMBL4071867 | — | — | 1 | 6.79 |
| CHEMBL3407785 | — | — | 1 | 6.64 |
| CHEMBL4071830 | — | — | 1 | 6.61 |
| CHEMBL3407784 | — | — | 1 | 6.60 |
| CHEMBL370805 | COCAINE | 4.0 | 1 | 6.56 |
| CHEMBL4092411 | — | — | 1 | 6.40 |
| CHEMBL4105127 | — | — | 1 | 5.94 |
| CHEMBL3612932 | — | — | 1 | - |
| CHEMBL4066427 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL781 | MAZINDOL | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL2064645 | — | IC50 | = | 92.0 | nM | 7.04 |
| CHEMBL4093756 | — | IC50 | = | 107.0 | nM | 6.97 |
| CHEMBL4066973 | — | IC50 | = | 127.0 | nM | 6.90 |
| CHEMBL4071867 | — | IC50 | = | 163.0 | nM | 6.79 |
| CHEMBL3407785 | — | IC50 | = | 229.0 | nM | 6.64 |
| CHEMBL4071830 | — | IC50 | = | 246.0 | nM | 6.61 |
| CHEMBL3407784 | — | IC50 | = | 253.0 | nM | 6.60 |
| CHEMBL370805 | COCAINE | IC50 | = | 274.0 | nM | 6.56 |
| CHEMBL4092411 | — | IC50 | = | 396.0 | nM | 6.40 |
| CHEMBL4105127 | — | IC50 | = | 1145.0 | nM | 5.94 |
| CHEMBL3612932 | — | IC50 | > | 8700.0 | nM | - |
| CHEMBL4066427 | — | IC50 | - | — | - |