Assay Detail
Binding
CHEMBL903473
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Inhibition of [3H]DA from human DAT 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 dopamine transporter (CHEMBL238) ↗| 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 | 6.45 | 7.36 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL395931 | — | — | 1 | 7.36 |
| CHEMBL245880 | — | — | 1 | 7.05 |
| CHEMBL247340 | — | — | 1 | 6.94 |
| CHEMBL391806 | — | — | 1 | 6.91 |
| CHEMBL440230 | — | — | 1 | 6.90 |
| CHEMBL247341 | — | — | 1 | 6.71 |
| CHEMBL246920 | — | — | 1 | 6.69 |
| CHEMBL247733 | — | — | 1 | 6.14 |
| CHEMBL1175 | DULOXETINE | 4.0 | 1 | 6.06 |
| CHEMBL247538 | — | — | 1 | 6.01 |
| CHEMBL397392 | — | — | 1 | 5.92 |
| CHEMBL246519 | — | — | 1 | 5.92 |
| CHEMBL392016 | — | — | 1 | 5.83 |
| CHEMBL245482 | — | — | 1 | 5.80 |
| CHEMBL391143 | — | — | 1 | - |
| CHEMBL245492 | — | — | 1 | - |
| CHEMBL395408 | — | — | 1 | - |
| CHEMBL442272 | — | — | 1 | - |
| CHEMBL245687 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL395931 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL245880 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL247340 | — | IC50 | = | 115.0 | nM | 6.94 |
| CHEMBL391806 | — | IC50 | = | 122.0 | nM | 6.91 |
| CHEMBL440230 | — | IC50 | = | 125.0 | nM | 6.90 |
| CHEMBL247341 | — | IC50 | = | 196.0 | nM | 6.71 |
| CHEMBL246920 | — | IC50 | = | 206.0 | nM | 6.69 |
| CHEMBL247733 | — | IC50 | = | 727.0 | nM | 6.14 |
| CHEMBL1175 | DULOXETINE | IC50 | = | 870.0 | nM | 6.06 |
| CHEMBL247538 | — | IC50 | = | 968.0 | nM | 6.01 |
| CHEMBL397392 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL246519 | — | IC50 | = | 1190.0 | nM | 5.92 |
| CHEMBL392016 | — | IC50 | = | 1470.0 | nM | 5.83 |
| CHEMBL245482 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL391143 | — | IC50 | > | 4000.0 | nM | - |
| CHEMBL245492 | — | IC50 | > | 4000.0 | nM | - |
| CHEMBL395408 | — | IC50 | > | 4000.0 | nM | - |
| CHEMBL442272 | — | IC50 | > | 4000.0 | nM | - |
| CHEMBL245687 | — | IC50 | > | 4000.0 | nM | - |