Assay Detail
Binding
CHEMBL1775933
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of DAT in rat striatum assessed as [3H]dopamine accumulation
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Striatum |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sodium-dependent dopamine transporter (CHEMBL338) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Further structure-activity relationship studies on 4-((((3S,6S)-6-benzhydryltetrahydro-2H-pyran-3-yl)amino)methyl)phenol: identification of compounds with triple uptake inhibitory activity as potential antidepressant agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 22 | 7.08 | 7.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1773301 | — | — | 1 | 7.80 |
| CHEMBL543876 | — | — | 1 | 7.79 |
| CHEMBL1773310 | — | — | 1 | 7.55 |
| CHEMBL1773297 | — | — | 1 | 7.50 |
| CHEMBL211484 | — | — | 1 | 7.43 |
| CHEMBL211077 | — | — | 1 | 7.38 |
| CHEMBL1773298 | — | — | 1 | 7.38 |
| CHEMBL1773300 | — | — | 1 | 7.37 |
| CHEMBL1773303 | — | — | 1 | 7.27 |
| CHEMBL1773304 | — | — | 1 | 7.14 |
| CHEMBL209808 | — | — | 1 | 7.07 |
| CHEMBL1773305 | — | — | 1 | 6.97 |
| CHEMBL1773299 | — | — | 1 | 6.96 |
| CHEMBL1773306 | — | — | 1 | 6.90 |
| CHEMBL1773307 | — | — | 1 | 6.86 |
| CHEMBL1773309 | — | — | 1 | 6.84 |
| CHEMBL1773302 | — | — | 1 | 6.84 |
| CHEMBL1773296 | — | — | 1 | 6.70 |
| CHEMBL1773308 | — | — | 1 | 6.68 |
| CHEMBL1773311 | — | — | 1 | 6.33 |
| CHEMBL41 | FLUOXETINE | 4.0 | 1 | 5.96 |
| CHEMBL14370 | REBOXETINE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1773301 | — | Ki | = | 15.9 | nM | 7.80 |
| CHEMBL543876 | — | Ki | = | 16.2 | nM | 7.79 |
| CHEMBL1773310 | — | Ki | = | 28.3 | nM | 7.55 |
| CHEMBL1773297 | — | Ki | = | 31.3 | nM | 7.50 |
| CHEMBL211484 | — | Ki | = | 37.4 | nM | 7.43 |
| CHEMBL211077 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL1773298 | — | Ki | = | 41.4 | nM | 7.38 |
| CHEMBL1773300 | — | Ki | = | 43.2 | nM | 7.37 |
| CHEMBL1773303 | — | Ki | = | 54.0 | nM | 7.27 |
| CHEMBL1773304 | — | Ki | = | 71.8 | nM | 7.14 |
| CHEMBL209808 | — | Ki | = | 85.2 | nM | 7.07 |
| CHEMBL1773305 | — | Ki | = | 106.0 | nM | 6.97 |
| CHEMBL1773299 | — | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL1773306 | — | Ki | = | 125.0 | nM | 6.90 |
| CHEMBL1773307 | — | Ki | = | 137.0 | nM | 6.86 |
| CHEMBL1773309 | — | Ki | = | 145.0 | nM | 6.84 |
| CHEMBL1773302 | — | Ki | = | 145.0 | nM | 6.84 |
| CHEMBL1773296 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL1773308 | — | Ki | = | 209.0 | nM | 6.68 |
| CHEMBL1773311 | — | Ki | = | 473.0 | nM | 6.33 |
| CHEMBL41 | FLUOXETINE | Ki | = | 1092.0 | nM | 5.96 |
| CHEMBL14370 | REBOXETINE | Ki | - | — | - |