Assay Detail
Binding
CHEMBL2433697
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]imipramin from human recombinant SERT over-expressed in HEK293 cells
7
Total Activities
7
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
Synthesis and biological evaluation of novel 3,4-diaryl lactam derivatives as triple reuptake inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 6.71 | 8.17 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL11 | IMIPRAMINE | 4.0 | 1 | 8.17 |
| CHEMBL41 | FLUOXETINE | 4.0 | 1 | 8.14 |
| CHEMBL2430680 | — | — | 1 | 7.07 |
| CHEMBL2430681 | — | — | 1 | 7.00 |
| CHEMBL2430699 | — | — | 1 | 6.01 |
| CHEMBL2430686 | — | — | 1 | 5.42 |
| CHEMBL2430700 | — | — | 1 | 5.19 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL11 | IMIPRAMINE | IC50 | = | 6.8 | nM | 8.17 |
| CHEMBL41 | FLUOXETINE | IC50 | = | 7.2 | nM | 8.14 |
| CHEMBL2430680 | — | IC50 | = | 85.6 | nM | 7.07 |
| CHEMBL2430681 | — | IC50 | = | 99.2 | nM | 7.00 |
| CHEMBL2430699 | — | IC50 | = | 965.4 | nM | 6.01 |
| CHEMBL2430686 | — | IC50 | = | 3757.0 | nM | 5.42 |
| CHEMBL2430700 | — | IC50 | = | 6451.0 | nM | 5.19 |