Assay Detail
Functional
CHEMBL832936
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of [3H]dopamine uptake in HEK293 cells expressing human dopamine transporter
5
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Sodium-dependent dopamine transporter (CHEMBL238) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis and pharmacology of ethylphenidate enantiomers: the human transesterification metabolite of methylphenidate and ethanol.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 6.92 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1722 | METHYLPHENIDATE HYDROCHLORIDE | 4.0 | 1 | 7.70 |
| CHEMBL2093958 | — | — | 2 | 7.57 |
| CHEMBL534479 | — | — | 1 | 7.02 |
| CHEMBL370805 | COCAINE | 4.0 | 1 | 6.54 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1722 | METHYLPHENIDATE HYDROCHLORIDE | IC50 | = | 19.9 | nM | 7.70 |
| CHEMBL2093958 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL534479 | — | IC50 | = | 95.0 | nM | 7.02 |
| CHEMBL370805 | COCAINE | IC50 | = | 289.0 | nM | 6.54 |
| CHEMBL2093958 | — | IC50 | = | 1730.0 | nM | 5.76 |