Assay Detail
Binding
CHEMBL902422
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Inhibition of [3H]5-HT from human SERT expressed in HEK293 cells
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 | Intermediate |
Target
Sodium-dependent serotonin transporter (CHEMBL228) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
N-Benzyl-N-(tetrahydro-2H-pyran-4-yl)pyrrolidin-3-amines as selective dual serotonin/noradrenaline reuptake inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 7.90 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL440230 | — | — | 1 | 8.52 |
| CHEMBL395931 | — | — | 1 | 8.40 |
| CHEMBL391806 | — | — | 1 | 8.30 |
| CHEMBL247340 | — | — | 1 | 8.30 |
| CHEMBL246920 | — | — | 1 | 8.22 |
| CHEMBL1175 | DULOXETINE | 4.0 | 1 | 8.22 |
| CHEMBL245482 | — | — | 1 | 8.10 |
| CHEMBL247733 | — | — | 1 | 8.05 |
| CHEMBL245880 | — | — | 1 | 8.00 |
| CHEMBL247538 | — | — | 1 | 7.96 |
| CHEMBL247341 | — | — | 1 | 7.96 |
| CHEMBL391143 | — | — | 1 | 7.89 |
| CHEMBL392016 | — | — | 1 | 7.82 |
| CHEMBL246519 | — | — | 1 | 7.82 |
| CHEMBL442272 | — | — | 1 | 7.68 |
| CHEMBL245492 | — | — | 1 | 7.62 |
| CHEMBL397392 | — | — | 1 | 7.54 |
| CHEMBL395408 | — | — | 1 | 7.37 |
| CHEMBL245687 | — | — | 1 | 6.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL440230 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL395931 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL391806 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL247340 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL246920 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL1175 | DULOXETINE | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL245482 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL247733 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL245880 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL247538 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL247341 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL391143 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL392016 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL246519 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL442272 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL245492 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL397392 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL395408 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL245687 | — | IC50 | = | 400.0 | nM | 6.40 |