Assay Detail
Binding
CHEMBL2389183
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Displacement of [3H]citalopram from human SERT transfected in HEK293 cells after 3 hrs by Wallac counting analysis
14
Total Activities
9
Compounds Tested
2
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
Discovery of a potent, dual serotonin and norepinephrine reuptake inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 9 | 8.97 | 9.68 |
| IC50 | 5 | 8.20 | 8.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2386163 | — | — | 2 | 9.68 |
| CHEMBL2386164 | — | — | 1 | 9.64 |
| CHEMBL1175 | DULOXETINE | 4.0 | 2 | 9.62 |
| CHEMBL2386166 | — | — | 1 | 9.12 |
| CHEMBL2386165 | — | — | 1 | 9.08 |
| CHEMBL2386162 | — | — | 1 | 8.72 |
| CHEMBL259209 | MILNACIPRAN | 4.0 | 2 | 8.19 |
| CHEMBL637 | VENLAFAXINE | 4.0 | 2 | 7.96 |
| CHEMBL1118 | DESVENLAFAXINE | 4.0 | 2 | 7.82 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2386163 | — | Ki | = | 0.21 | nM | 9.68 |
| CHEMBL2386163 | — | Ki | = | 0.22 | nM | 9.66 |
| CHEMBL2386164 | — | Ki | = | 0.23 | nM | 9.64 |
| CHEMBL1175 | DULOXETINE | Ki | = | 0.24 | nM | 9.62 |
| CHEMBL2386166 | — | Ki | = | 0.75 | nM | 9.12 |
| CHEMBL2386165 | — | Ki | = | 0.84 | nM | 9.08 |
| CHEMBL2386162 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL1175 | DULOXETINE | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL259209 | MILNACIPRAN | Ki | = | 6.5 | nM | 8.19 |
| CHEMBL637 | VENLAFAXINE | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL1118 | DESVENLAFAXINE | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL1118 | DESVENLAFAXINE | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL259209 | MILNACIPRAN | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL637 | VENLAFAXINE | IC50 | > | 20.0 | nM | - |