Assay Detail
Binding
CHEMBL929225
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Inhibition of [3H]5-HT uptake at human recombinant 5HT transporter expressed in HEK293 cells
23
Total Activities
23
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
Pyridyl-phenyl ether monoamine reuptake inhibitors: Impact of lipophilicity on dual SNRI pharmacology and off-target promiscuity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 7.89 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL401596 | — | — | 1 | 8.52 |
| CHEMBL403078 | — | — | 1 | 8.40 |
| CHEMBL256136 | — | — | 1 | 8.40 |
| CHEMBL257593 | — | — | 1 | 8.22 |
| CHEMBL256137 | — | — | 1 | 8.22 |
| CHEMBL256970 | — | — | 1 | 8.22 |
| CHEMBL402345 | — | — | 1 | 8.15 |
| CHEMBL260036 | — | — | 1 | 8.10 |
| CHEMBL247733 | — | — | 1 | 8.05 |
| CHEMBL402371 | — | — | 1 | 8.00 |
| CHEMBL402000 | — | — | 1 | 7.96 |
| CHEMBL403080 | — | — | 1 | 7.89 |
| CHEMBL256511 | — | — | 1 | 7.85 |
| CHEMBL258449 | — | — | 1 | 7.85 |
| CHEMBL403441 | — | — | 1 | 7.85 |
| CHEMBL260038 | — | — | 1 | 7.75 |
| CHEMBL256293 | — | — | 1 | 7.72 |
| CHEMBL403251 | — | — | 1 | 7.70 |
| CHEMBL256135 | — | — | 1 | 7.64 |
| CHEMBL260037 | — | — | 1 | 7.62 |
| CHEMBL259136 | — | — | 1 | 7.41 |
| CHEMBL257592 | — | — | 1 | 7.34 |
| CHEMBL260039 | — | — | 1 | 6.64 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL401596 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL403078 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL256136 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL257593 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL256137 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL256970 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL402345 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL260036 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL247733 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL402371 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL402000 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL403080 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL256511 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL258449 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL403441 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL260038 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL256293 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL403251 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL256135 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL260037 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL259136 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL257592 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL260039 | — | IC50 | = | 231.0 | nM | 6.64 |