Assay Detail
Binding
CHEMBL1032747
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of [3H]dopamine uptake at human dopamine transporter expressed in mouse N2A cells by scintillation counting
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | N2a |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
Sodium-dependent dopamine transporter (CHEMBL238) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
A novel photoaffinity ligand for the dopamine transporter based on pyrovalerone.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 6.96 | 8.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL555491 | — | — | 1 | 8.15 |
| CHEMBL201960 | PYROVALERONE | 4.0 | 1 | 7.50 |
| CHEMBL553937 | — | — | 1 | 6.76 |
| CHEMBL558086 | — | — | 1 | 6.58 |
| CHEMBL894 | BUPROPION | 4.0 | 1 | 5.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL555491 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL201960 | PYROVALERONE | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL553937 | — | IC50 | = | 175.0 | nM | 6.76 |
| CHEMBL558086 | — | IC50 | = | 264.0 | nM | 6.58 |
| CHEMBL894 | BUPROPION | IC50 | = | 1567.0 | nM | 5.80 |