Assay Detail
Binding
CHEMBL1775935
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of NET in rat cerebral cortex assessed as [3H]norepinephrine accumulation
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Cerebral cortex |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
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 | 7.02 | 9.08 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL14370 | REBOXETINE | 4.0 | 1 | 9.08 |
| CHEMBL209808 | — | — | 1 | 7.59 |
| CHEMBL1773301 | — | — | 1 | 7.53 |
| CHEMBL211484 | — | — | 1 | 7.53 |
| CHEMBL211077 | — | — | 1 | 7.52 |
| CHEMBL1773297 | — | — | 1 | 7.42 |
| CHEMBL1773300 | — | — | 1 | 7.40 |
| CHEMBL1773298 | — | — | 1 | 7.33 |
| CHEMBL543876 | — | — | 1 | 7.31 |
| CHEMBL1773299 | — | — | 1 | 7.22 |
| CHEMBL41 | FLUOXETINE | 4.0 | 1 | 6.92 |
| CHEMBL1773296 | — | — | 1 | 6.80 |
| CHEMBL1773302 | — | — | 1 | 6.79 |
| CHEMBL1773305 | — | — | 1 | 6.65 |
| CHEMBL1773311 | — | — | 1 | 6.63 |
| CHEMBL1773303 | — | — | 1 | 6.53 |
| CHEMBL1773307 | — | — | 1 | 6.52 |
| CHEMBL1773309 | — | — | 1 | 6.45 |
| CHEMBL1773306 | — | — | 1 | 6.37 |
| CHEMBL1773310 | — | — | 1 | 6.33 |
| CHEMBL1773308 | — | — | 1 | 6.30 |
| CHEMBL1773304 | — | — | 1 | 6.26 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL14370 | REBOXETINE | Ki | = | 0.826 | nM | 9.08 |
| CHEMBL209808 | — | Ki | = | 25.5 | nM | 7.59 |
| CHEMBL1773301 | — | Ki | = | 29.3 | nM | 7.53 |
| CHEMBL211484 | — | Ki | = | 29.3 | nM | 7.53 |
| CHEMBL211077 | — | Ki | = | 30.5 | nM | 7.52 |
| CHEMBL1773297 | — | Ki | = | 38.5 | nM | 7.42 |
| CHEMBL1773300 | — | Ki | = | 39.6 | nM | 7.40 |
| CHEMBL1773298 | — | Ki | = | 47.2 | nM | 7.33 |
| CHEMBL543876 | — | Ki | = | 48.5 | nM | 7.31 |
| CHEMBL1773299 | — | Ki | = | 59.8 | nM | 7.22 |
| CHEMBL41 | FLUOXETINE | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL1773296 | — | Ki | = | 160.0 | nM | 6.80 |
| CHEMBL1773302 | — | Ki | = | 162.0 | nM | 6.79 |
| CHEMBL1773305 | — | Ki | = | 222.0 | nM | 6.65 |
| CHEMBL1773311 | — | Ki | = | 232.0 | nM | 6.63 |
| CHEMBL1773303 | — | Ki | = | 298.0 | nM | 6.53 |
| CHEMBL1773307 | — | Ki | = | 299.0 | nM | 6.52 |
| CHEMBL1773309 | — | Ki | = | 353.0 | nM | 6.45 |
| CHEMBL1773306 | — | Ki | = | 429.0 | nM | 6.37 |
| CHEMBL1773310 | — | Ki | = | 462.0 | nM | 6.33 |
| CHEMBL1773308 | — | Ki | = | 505.0 | nM | 6.30 |
| CHEMBL1773304 | — | Ki | = | 546.0 | nM | 6.26 |