Assay Detail
Binding
CHEMBL4842937
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]citalopram from human SERT in HEK293 cells by Topcount scintillation analysis
24
Total Activities
24
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
Tuning the activity of known drugs via the introduction of halogen atoms, a case study of SERT ligands - Fluoxetine and fluvoxamine.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 24 | 7.21 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4869180 | — | — | 1 | 8.30 |
| CHEMBL4853402 | — | — | 1 | 8.05 |
| CHEMBL4868210 | — | — | 1 | 7.85 |
| CHEMBL4850522 | — | — | 1 | 7.82 |
| CHEMBL4853473 | — | — | 1 | 7.72 |
| CHEMBL4877693 | — | — | 1 | 7.68 |
| CHEMBL4853132 | — | — | 1 | 7.64 |
| CHEMBL4848149 | — | — | 1 | 7.64 |
| CHEMBL4850285 | — | — | 1 | 7.62 |
| CHEMBL41 | FLUOXETINE | 4.0 | 1 | 7.51 |
| CHEMBL4878382 | — | — | 1 | 7.51 |
| CHEMBL4876238 | — | — | 1 | 7.39 |
| CHEMBL4851108 | — | — | 1 | 7.28 |
| CHEMBL4864622 | — | — | 1 | 7.26 |
| CHEMBL4878448 | — | — | 1 | 7.21 |
| CHEMBL4848304 | — | — | 1 | 7.21 |
| CHEMBL4863405 | — | — | 1 | 7.18 |
| CHEMBL4874276 | — | — | 1 | 6.86 |
| CHEMBL4873814 | — | — | 1 | 6.70 |
| CHEMBL4863177 | — | — | 1 | 6.46 |
| CHEMBL814 | FLUVOXAMINE | 4.0 | 1 | 6.34 |
| CHEMBL4878226 | — | — | 1 | 6.26 |
| CHEMBL4865485 | — | — | 1 | 5.84 |
| CHEMBL4861511 | — | — | 1 | 5.79 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4869180 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL4853402 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL4868210 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL4850522 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL4853473 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL4877693 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL4853132 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL4848149 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL4850285 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL41 | FLUOXETINE | Ki | = | 31.0 | nM | 7.51 |
| CHEMBL4878382 | — | Ki | = | 31.0 | nM | 7.51 |
| CHEMBL4876238 | — | Ki | = | 41.0 | nM | 7.39 |
| CHEMBL4851108 | — | Ki | = | 52.0 | nM | 7.28 |
| CHEMBL4864622 | — | Ki | = | 55.0 | nM | 7.26 |
| CHEMBL4878448 | — | Ki | = | 62.0 | nM | 7.21 |
| CHEMBL4848304 | — | Ki | = | 61.0 | nM | 7.21 |
| CHEMBL4863405 | — | Ki | = | 66.0 | nM | 7.18 |
| CHEMBL4874276 | — | Ki | = | 137.0 | nM | 6.86 |
| CHEMBL4873814 | — | Ki | = | 202.0 | nM | 6.70 |
| CHEMBL4863177 | — | Ki | = | 349.0 | nM | 6.46 |
| CHEMBL814 | FLUVOXAMINE | Ki | = | 458.0 | nM | 6.34 |
| CHEMBL4878226 | — | Ki | = | 543.0 | nM | 6.26 |
| CHEMBL4865485 | — | Ki | = | 1458.0 | nM | 5.84 |
| CHEMBL4861511 | — | Ki | = | 1617.0 | nM | 5.79 |