Assay Detail
Binding
CHEMBL673211
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Binding affinity at dopamine transporter from rat striatal membrane tissue by [3H]CFT displacement.
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Striatum |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Sodium-dependent dopamine transporter (CHEMBL338) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Structure-activity relationship studies of novel 4-[2-[bis(4-fluorophenyl)methoxy]ethyl]-1-(3-phenylpropyl)piperidine analogs: synthesis and biological evaluation at the dopamine and serotonin transporter sites.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 7.34 | 8.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL281594 | VANOXERINE | 3.0 | 1 | 8.22 |
| CHEMBL34032 | — | — | 1 | 8.01 |
| CHEMBL351215 | — | — | 1 | 7.97 |
| CHEMBL351595 | — | — | 1 | 7.92 |
| CHEMBL350100 | — | — | 1 | 7.89 |
| CHEMBL349281 | — | — | 1 | 7.87 |
| CHEMBL9329 | — | — | 1 | 7.84 |
| CHEMBL338733 | — | — | 1 | 7.82 |
| CHEMBL77867 | — | — | 1 | 7.78 |
| CHEMBL352272 | — | — | 1 | 7.70 |
| CHEMBL353797 | — | — | 1 | 7.19 |
| CHEMBL166122 | — | — | 1 | 6.97 |
| CHEMBL422018 | — | — | 1 | 6.94 |
| CHEMBL162006 | — | — | 1 | 6.90 |
| CHEMBL350372 | — | — | 1 | 6.80 |
| CHEMBL166072 | — | — | 1 | 6.59 |
| CHEMBL165740 | — | — | 1 | 6.51 |
| CHEMBL165657 | — | — | 1 | 6.42 |
| CHEMBL415747 | — | — | 1 | 6.15 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL281594 | VANOXERINE | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL34032 | — | IC50 | = | 9.7 | nM | 8.01 |
| CHEMBL351215 | — | IC50 | = | 10.6 | nM | 7.97 |
| CHEMBL351595 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL350100 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL349281 | — | IC50 | = | 13.5 | nM | 7.87 |
| CHEMBL9329 | — | IC50 | = | 14.5 | nM | 7.84 |
| CHEMBL338733 | — | IC50 | = | 15.2 | nM | 7.82 |
| CHEMBL77867 | — | IC50 | = | 16.7 | nM | 7.78 |
| CHEMBL352272 | — | IC50 | = | 19.9 | nM | 7.70 |
| CHEMBL353797 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL166122 | — | IC50 | = | 108.0 | nM | 6.97 |
| CHEMBL422018 | — | IC50 | = | 115.0 | nM | 6.94 |
| CHEMBL162006 | — | IC50 | = | 126.0 | nM | 6.90 |
| CHEMBL350372 | — | IC50 | = | 159.0 | nM | 6.80 |
| CHEMBL166072 | — | IC50 | = | 255.0 | nM | 6.59 |
| CHEMBL165740 | — | IC50 | = | 311.0 | nM | 6.51 |
| CHEMBL165657 | — | IC50 | = | 382.0 | nM | 6.42 |
| CHEMBL415747 | — | IC50 | = | 702.0 | nM | 6.15 |