Assay Detail
Binding
CHEMBL4011341
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Enhancing of [3H]mazindol binding to recombinant human DAT expressed in HEK293 cell membranes preincubated for 10 mins followed by radioligand addition measured after 90 mins by micro beta scintillation counting analysis
23
Total Activities
13
Compounds Tested
2
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 |
|---|---|---|---|
| EC50 | 13 | 6.49 | 6.91 |
| Activity | 10 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4066973 | — | — | 2 | 6.91 |
| CHEMBL2064645 | — | — | 2 | 6.89 |
| CHEMBL3407784 | — | — | 2 | 6.88 |
| CHEMBL4093756 | — | — | 2 | 6.57 |
| CHEMBL4071830 | — | — | 2 | 6.51 |
| CHEMBL4105127 | — | — | 2 | 6.27 |
| CHEMBL4071867 | — | — | 2 | 6.26 |
| CHEMBL4092411 | — | — | 2 | 6.07 |
| CHEMBL3407785 | — | — | 2 | 6.06 |
| CHEMBL3612932 | — | — | 2 | - |
| CHEMBL4066427 | — | — | 1 | - |
| CHEMBL370805 | COCAINE | 4.0 | 1 | - |
| CHEMBL781 | MAZINDOL | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4066973 | — | EC50 | = | 124.0 | nM | 6.91 |
| CHEMBL2064645 | — | EC50 | = | 128.0 | nM | 6.89 |
| CHEMBL3407784 | — | EC50 | = | 131.0 | nM | 6.88 |
| CHEMBL4093756 | — | EC50 | = | 267.0 | nM | 6.57 |
| CHEMBL4071830 | — | EC50 | = | 308.0 | nM | 6.51 |
| CHEMBL4105127 | — | EC50 | = | 535.0 | nM | 6.27 |
| CHEMBL4071867 | — | EC50 | = | 550.0 | nM | 6.26 |
| CHEMBL4092411 | — | EC50 | = | 860.0 | nM | 6.07 |
| CHEMBL3407785 | — | EC50 | = | 870.0 | nM | 6.06 |
| CHEMBL3612932 | — | EC50 | - | — | - | |
| CHEMBL4066427 | — | EC50 | - | — | - | |
| CHEMBL3407784 | — | Activity | = | 403.0 | % | - |
| CHEMBL3407785 | — | Activity | = | 369.0 | % | - |
| CHEMBL2064645 | — | Activity | = | 438.0 | % | - |
| CHEMBL4071867 | — | Activity | = | 405.0 | % | - |
| CHEMBL3612932 | — | Activity | - | — | - | |
| CHEMBL4066973 | — | Activity | = | 540.0 | % | - |
| CHEMBL4093756 | — | Activity | = | 455.0 | % | - |
| CHEMBL4071830 | — | Activity | = | 520.0 | % | - |
| CHEMBL4105127 | — | Activity | = | 347.0 | % | - |
| CHEMBL4092411 | — | Activity | = | 269.0 | % | - |
| CHEMBL370805 | COCAINE | EC50 | - | — | - | |
| CHEMBL781 | MAZINDOL | EC50 | - | — | - |