Assay Detail
Binding
CHEMBL1647747
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Inhibition of [3H]dopamine uptake at human DAT expressed in mouse N2A cells
9
Total Activities
9
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 | Autocuration |
Target
Sodium-dependent dopamine transporter (CHEMBL238) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Azido-iodo-N-benzyl derivatives of threo-methylphenidate (Ritalin, Concerta): Rational design, synthesis, pharmacological evaluation, and dopamine transporter photoaffinity labeling.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 6.20 | 7.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1253735 | — | — | 1 | 7.96 |
| CHEMBL1641691 | — | — | 1 | 7.85 |
| CHEMBL827 | DEXMETHYLPHENIDATE | 4.0 | 1 | 6.81 |
| CHEMBL1641694 | — | — | 1 | 5.91 |
| CHEMBL1641695 | — | — | 1 | 5.74 |
| CHEMBL1641697 | — | — | 1 | 5.57 |
| CHEMBL1641692 | — | — | 1 | 5.56 |
| CHEMBL1641696 | — | — | 1 | 5.33 |
| CHEMBL1641693 | — | — | 1 | 5.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1253735 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL1641691 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL827 | DEXMETHYLPHENIDATE | IC50 | = | 156.0 | nM | 6.81 |
| CHEMBL1641694 | — | IC50 | = | 1232.0 | nM | 5.91 |
| CHEMBL1641695 | — | IC50 | = | 1828.0 | nM | 5.74 |
| CHEMBL1641697 | — | IC50 | = | 2696.0 | nM | 5.57 |
| CHEMBL1641692 | — | IC50 | = | 2764.0 | nM | 5.56 |
| CHEMBL1641696 | — | IC50 | = | 4627.0 | nM | 5.33 |
| CHEMBL1641693 | — | IC50 | = | 7966.0 | nM | 5.10 |