Assay Detail
Binding
CHEMBL3800925
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human SERT W103A mutant 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 |
|---|---|---|---|
| IC50 | 19 | 6.44 | 8.59 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL11 | IMIPRAMINE | 4.0 | 1 | 8.59 |
| CHEMBL3798035 | — | — | 1 | 7.40 |
| CHEMBL3797621 | — | — | 1 | 7.22 |
| CHEMBL3799356 | — | — | 1 | 6.57 |
| CHEMBL3799596 | — | — | 1 | 6.55 |
| CHEMBL3799668 | — | — | 1 | 6.55 |
| CHEMBL3799795 | — | — | 1 | 6.52 |
| CHEMBL3797849 | — | — | 1 | 6.47 |
| CHEMBL3799503 | — | — | 1 | 6.46 |
| CHEMBL3798279 | — | — | 1 | 6.38 |
| CHEMBL3799072 | — | — | 1 | 6.36 |
| CHEMBL3799481 | — | — | 1 | 6.25 |
| CHEMBL3799640 | — | — | 1 | 6.22 |
| CHEMBL3799416 | — | — | 1 | 6.21 |
| CHEMBL3799319 | — | — | 1 | 6.08 |
| CHEMBL3799011 | — | — | 1 | 6.03 |
| CHEMBL3799131 | — | — | 1 | 5.80 |
| CHEMBL3800215 | — | — | 1 | 5.39 |
| CHEMBL3798819 | — | — | 1 | 5.32 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL11 | IMIPRAMINE | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL3798035 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL3797621 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL3799356 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL3799596 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL3799668 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL3799795 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL3797849 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL3799503 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL3798279 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL3799072 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL3799481 | — | IC50 | = | 560.0 | nM | 6.25 |
| CHEMBL3799640 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL3799416 | — | IC50 | = | 610.0 | nM | 6.21 |
| CHEMBL3799319 | — | IC50 | = | 840.0 | nM | 6.08 |
| CHEMBL3799011 | — | IC50 | = | 940.0 | nM | 6.03 |
| CHEMBL3799131 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL3800215 | — | IC50 | = | 4100.0 | nM | 5.39 |
| CHEMBL3798819 | — | IC50 | = | 4800.0 | nM | 5.32 |