Assay Detail
Binding
CHEMBL5047397
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of SERT (unknown origin) in HEK293 cells assessed as inhibition of 5-HT reuptake by spectrophotometric analysis
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sodium-dependent serotonin transporter (CHEMBL228) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
The novel therapeutic strategy of vilazodone-donepezil chimeras as potent triple-target ligands for the potential treatment of Alzheimer's disease with comorbid depression.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 26 | 7.61 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL439849 | VILAZODONE | 4.0 | 1 | 9.40 |
| CHEMBL549 | CITALOPRAM | 4.0 | 1 | 8.24 |
| CHEMBL5080984 | — | — | 1 | 8.08 |
| CHEMBL5075438 | — | — | 1 | 8.07 |
| CHEMBL5076406 | — | — | 1 | 8.05 |
| CHEMBL5088281 | — | — | 1 | 7.92 |
| CHEMBL5094829 | — | — | 1 | 7.83 |
| CHEMBL5080857 | — | — | 1 | 7.80 |
| CHEMBL5088919 | — | — | 1 | 7.79 |
| CHEMBL5089999 | — | — | 1 | 7.74 |
| CHEMBL5088143 | — | — | 1 | 7.70 |
| CHEMBL5082250 | — | — | 1 | 7.53 |
| CHEMBL5071820 | — | — | 1 | 7.49 |
| CHEMBL5087445 | — | — | 1 | 7.47 |
| CHEMBL5080308 | — | — | 1 | 7.45 |
| CHEMBL5069928 | — | — | 1 | 7.44 |
| CHEMBL5082836 | — | — | 1 | 7.40 |
| CHEMBL5086036 | — | — | 1 | 7.39 |
| CHEMBL5087923 | — | — | 1 | 7.26 |
| CHEMBL5086121 | — | — | 1 | 7.12 |
| CHEMBL5082360 | — | — | 1 | 7.12 |
| CHEMBL5087922 | — | — | 1 | 6.94 |
| CHEMBL5090651 | — | — | 1 | 6.80 |
| CHEMBL5076277 | — | — | 1 | 6.55 |
| CHEMBL5087351 | — | — | 1 | - |
| CHEMBL5088060 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL439849 | VILAZODONE | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL549 | CITALOPRAM | IC50 | = | 5.81 | nM | 8.24 |
| CHEMBL5080984 | — | IC50 | = | 8.25 | nM | 8.08 |
| CHEMBL5075438 | — | IC50 | = | 8.41 | nM | 8.07 |
| CHEMBL5076406 | — | IC50 | = | 8.81 | nM | 8.05 |
| CHEMBL5088281 | — | IC50 | = | 12.09 | nM | 7.92 |
| CHEMBL5094829 | — | IC50 | = | 14.87 | nM | 7.83 |
| CHEMBL5080857 | — | IC50 | = | 15.86 | nM | 7.80 |
| CHEMBL5088919 | — | IC50 | = | 16.2 | nM | 7.79 |
| CHEMBL5089999 | — | IC50 | = | 18.36 | nM | 7.74 |
| CHEMBL5088143 | — | IC50 | = | 20.13 | nM | 7.70 |
| CHEMBL5082250 | — | IC50 | = | 29.22 | nM | 7.53 |
| CHEMBL5071820 | — | IC50 | = | 32.26 | nM | 7.49 |
| CHEMBL5087445 | — | IC50 | = | 33.51 | nM | 7.47 |
| CHEMBL5080308 | — | IC50 | = | 35.69 | nM | 7.45 |
| CHEMBL5069928 | — | IC50 | = | 36.03 | nM | 7.44 |
| CHEMBL5082836 | — | IC50 | = | 39.92 | nM | 7.40 |
| CHEMBL5086036 | — | IC50 | = | 41.15 | nM | 7.39 |
| CHEMBL5087923 | — | IC50 | = | 54.52 | nM | 7.26 |
| CHEMBL5086121 | — | IC50 | = | 75.24 | nM | 7.12 |
| CHEMBL5082360 | — | IC50 | = | 76.5 | nM | 7.12 |
| CHEMBL5087922 | — | IC50 | = | 114.1 | nM | 6.94 |
| CHEMBL5090651 | — | IC50 | = | 159.1 | nM | 6.80 |
| CHEMBL5076277 | — | IC50 | = | 284.55 | nM | 6.55 |
| CHEMBL5087351 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL5088060 | — | IC50 | > | 1000.0 | nM | - |