Assay Detail
Binding
CHEMBL674429
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Binding affinity against dopamine transporter (DAT) by displacement of [3H]WIN-35428 in male wistar rats
9
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Sodium-dependent dopamine transporter (CHEMBL338) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Syntheses and binding studies of new [(aryl)(aryloxy)methyl]piperidine derivatives and related compounds as potential antidepressant drugs with high affinity for serotonin (5-HT) and norepinephrine (NE) transporters.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 9 | 6.64 | 7.35 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL781 | MAZINDOL | 4.0 | 1 | 7.35 |
| CHEMBL153093 | — | — | 1 | 6.96 |
| CHEMBL152141 | — | — | 1 | 6.95 |
| CHEMBL152935 | — | — | 2 | 6.79 |
| CHEMBL152254 | — | — | 2 | 6.60 |
| CHEMBL345277 | — | — | 1 | 6.42 |
| CHEMBL149641 | — | — | 1 | 6.28 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL781 | MAZINDOL | Ki | = | 44.3 | nM | 7.35 |
| CHEMBL153093 | — | Ki | = | 110.5 | nM | 6.96 |
| CHEMBL152141 | — | Ki | = | 112.8 | nM | 6.95 |
| CHEMBL152935 | — | Ki | = | 163.0 | nM | 6.79 |
| CHEMBL152254 | — | Ki | = | 253.4 | nM | 6.60 |
| CHEMBL345277 | — | Ki | = | 376.7 | nM | 6.42 |
| CHEMBL152935 | — | Ki | = | 461.3 | nM | 6.34 |
| CHEMBL149641 | — | Ki | = | 520.3 | nM | 6.28 |
| CHEMBL152254 | — | Ki | = | 821.0 | nM | 6.09 |