Assay Detail
Binding
CHEMBL880586
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [125I]RTI-55 dopamine transporter binding in rat striatal membrane
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Striatum |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Sodium-dependent dopamine transporter (CHEMBL338) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
The synthesis and biological evaluation of dopamine transporter inhibiting activity of substituted diphenylmethoxypiperidines.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 7.22 | 9.37 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL281594 | VANOXERINE | 3.0 | 1 | 9.37 |
| CHEMBL370627 | — | — | 1 | 7.90 |
| CHEMBL197857 | — | — | 1 | 7.66 |
| CHEMBL197615 | — | — | 1 | 7.36 |
| CHEMBL381247 | — | — | 1 | 7.30 |
| CHEMBL370805 | COCAINE | 4.0 | 1 | 6.98 |
| CHEMBL197858 | — | — | 1 | 6.81 |
| CHEMBL371067 | — | — | 1 | 6.58 |
| CHEMBL371224 | — | — | 1 | 6.56 |
| CHEMBL198172 | — | — | 1 | 6.53 |
| CHEMBL1492 | DIPHENYLPYRALINE | 4.0 | 1 | 6.38 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL281594 | VANOXERINE | IC50 | = | 0.43 | nM | 9.37 |
| CHEMBL370627 | — | IC50 | = | 12.5 | nM | 7.90 |
| CHEMBL197857 | — | IC50 | = | 22.1 | nM | 7.66 |
| CHEMBL197615 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL381247 | — | IC50 | = | 50.6 | nM | 7.30 |
| CHEMBL370805 | COCAINE | IC50 | = | 104.0 | nM | 6.98 |
| CHEMBL197858 | — | IC50 | = | 155.0 | nM | 6.81 |
| CHEMBL371067 | — | IC50 | = | 264.0 | nM | 6.58 |
| CHEMBL371224 | — | IC50 | = | 277.0 | nM | 6.56 |
| CHEMBL198172 | — | IC50 | = | 293.0 | nM | 6.53 |
| CHEMBL1492 | DIPHENYLPYRALINE | IC50 | = | 420.0 | nM | 6.38 |