Assay Detail
Binding
CHEMBL4396183
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H] imipramine from human recombinant 5-HT transporter measured after 60 mins by scintillation counter method
6
Total Activities
3
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sodium-dependent serotonin transporter (CHEMBL228) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Multi-targeting protein-protein interaction inhibitors: Evolution of macrocyclic ligands with embedded carbohydrates (MECs) to improve selectivity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 3 | 7.10 | 8.72 |
| IC50 | 3 | 6.76 | 8.39 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL11 | IMIPRAMINE | 4.0 | 2 | 8.72 |
| CHEMBL4579120 | — | — | 2 | 5.47 |
| CHEMBL4562303 | — | — | 2 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL11 | IMIPRAMINE | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL11 | IMIPRAMINE | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL4579120 | — | Ki | = | 3400.0 | nM | 5.47 |
| CHEMBL4579120 | — | IC50 | = | 7400.0 | nM | 5.13 |
| CHEMBL4562303 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL4562303 | — | IC50 | > | 100000.0 | nM | - |