Assay Detail
Binding
CHEMBL3800924
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of wild-type human SERT expressed in HEK293 MSR cells assessed as [3H]-5-HT uptake preincubated for 30 mins followed addition of [3H]-5HT and compound for 10 mins by micro-scintillation counter
19
Total Activities
19
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 inhibitory evaluation of 3-linked imipramines for the exploration of the S2 site of the human serotonin transporter.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 19 | 5.86 | 7.51 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL11 | IMIPRAMINE | 4.0 | 1 | 7.51 |
| CHEMBL3797621 | — | — | 1 | 6.82 |
| CHEMBL3798035 | — | — | 1 | 6.66 |
| CHEMBL3797849 | — | — | 1 | 6.23 |
| CHEMBL3799668 | — | — | 1 | 6.22 |
| CHEMBL3799416 | — | — | 1 | 6.21 |
| CHEMBL3799596 | — | — | 1 | 6.00 |
| CHEMBL3799503 | — | — | 1 | 5.96 |
| CHEMBL3799795 | — | — | 1 | 5.96 |
| CHEMBL3799640 | — | — | 1 | 5.92 |
| CHEMBL3799072 | — | — | 1 | 5.82 |
| CHEMBL3799481 | — | — | 1 | 5.70 |
| CHEMBL3799011 | — | — | 1 | 5.46 |
| CHEMBL3798819 | — | — | 1 | 5.46 |
| CHEMBL3799319 | — | — | 1 | 5.23 |
| CHEMBL3799356 | — | — | 1 | 5.20 |
| CHEMBL3798279 | — | — | 1 | 5.19 |
| CHEMBL3800215 | — | — | 1 | 4.96 |
| CHEMBL3799131 | — | — | 1 | 4.89 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL11 | IMIPRAMINE | Ki | = | 31.0 | nM | 7.51 |
| CHEMBL3797621 | — | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL3798035 | — | Ki | = | 220.0 | nM | 6.66 |
| CHEMBL3797849 | — | Ki | = | 590.0 | nM | 6.23 |
| CHEMBL3799668 | — | Ki | = | 600.0 | nM | 6.22 |
| CHEMBL3799416 | — | Ki | = | 620.0 | nM | 6.21 |
| CHEMBL3799596 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL3799503 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL3799795 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL3799640 | — | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL3799072 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL3799481 | — | Ki | = | 2000.0 | nM | 5.70 |
| CHEMBL3799011 | — | Ki | = | 3500.0 | nM | 5.46 |
| CHEMBL3798819 | — | Ki | = | 3500.0 | nM | 5.46 |
| CHEMBL3799319 | — | Ki | = | 5900.0 | nM | 5.23 |
| CHEMBL3799356 | — | Ki | = | 6300.0 | nM | 5.20 |
| CHEMBL3798279 | — | Ki | = | 6500.0 | nM | 5.19 |
| CHEMBL3800215 | — | Ki | = | 11000.0 | nM | 4.96 |
| CHEMBL3799131 | — | Ki | = | 13000.0 | nM | 4.89 |