Assay Detail
Binding
CHEMBL1024554
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Inhibition of [3H]DA uptake at human DAT expressed in HEK293 cells
42
Total Activities
34
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
4-Piperidines and 3-pyrrolidines as dual serotonin and noradrenaline reuptake inhibitors: design, synthesis and structure-activity relationships.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 42 | 6.44 | 8.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL549825 | — | — | 2 | 8.22 |
| CHEMBL563030 | — | — | 2 | 7.44 |
| CHEMBL550779 | — | — | 1 | 7.22 |
| CHEMBL559456 | — | — | 3 | 7.15 |
| CHEMBL541226 | — | — | 1 | 6.70 |
| CHEMBL559081 | — | — | 3 | 6.57 |
| CHEMBL551573 | — | — | 2 | 6.48 |
| CHEMBL552046 | — | — | 1 | 6.45 |
| CHEMBL150932 | — | — | 1 | 6.43 |
| CHEMBL564100 | — | — | 1 | 6.40 |
| CHEMBL540978 | — | — | 1 | 6.32 |
| CHEMBL1175 | DULOXETINE | 4.0 | 1 | 6.23 |
| CHEMBL562691 | — | — | 1 | 6.19 |
| CHEMBL563987 | — | — | 1 | 5.97 |
| CHEMBL563495 | — | — | 2 | 5.97 |
| CHEMBL562854 | — | — | 1 | 5.90 |
| CHEMBL550696 | — | — | 1 | 5.80 |
| CHEMBL556268 | — | — | 1 | 5.46 |
| CHEMBL562444 | — | — | 1 | 5.11 |
| CHEMBL560050 | — | — | 1 | - |
| CHEMBL550289 | — | — | 1 | - |
| CHEMBL549761 | — | — | 1 | - |
| CHEMBL551556 | — | — | 1 | - |
| CHEMBL563852 | — | — | 1 | - |
| CHEMBL556888 | — | — | 1 | - |
| CHEMBL562244 | — | — | 1 | - |
| CHEMBL562108 | — | — | 1 | - |
| CHEMBL549965 | — | — | 1 | - |
| CHEMBL563404 | — | — | 1 | - |
| CHEMBL560049 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL549825 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL563030 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL563030 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL550779 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL559456 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL549825 | — | IC50 | = | 99.0 | nM | 7.00 |
| CHEMBL559456 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL541226 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL559081 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL551573 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL552046 | — | IC50 | = | 353.0 | nM | 6.45 |
| CHEMBL150932 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL559456 | — | IC50 | = | 375.0 | nM | 6.43 |
| CHEMBL564100 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL540978 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL559081 | — | IC50 | = | 590.0 | nM | 6.23 |
| CHEMBL1175 | DULOXETINE | IC50 | = | 590.0 | nM | 6.23 |
| CHEMBL562691 | — | IC50 | = | 644.0 | nM | 6.19 |
| CHEMBL551573 | — | IC50 | = | 720.0 | nM | 6.14 |
| CHEMBL559081 | — | IC50 | = | 820.0 | nM | 6.09 |
| CHEMBL563495 | — | IC50 | = | 1060.0 | nM | 5.97 |
| CHEMBL563987 | — | IC50 | = | 1070.0 | nM | 5.97 |
| CHEMBL562854 | — | IC50 | = | 1270.0 | nM | 5.90 |
| CHEMBL563495 | — | IC50 | = | 1530.0 | nM | 5.82 |
| CHEMBL550696 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL556268 | — | IC50 | = | 3470.0 | nM | 5.46 |
| CHEMBL562444 | — | IC50 | = | 7830.0 | nM | 5.11 |
| CHEMBL564631 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL559654 | — | IC50 | > | 4000.0 | nM | - |
| CHEMBL551646 | — | IC50 | - | — | - | |
| CHEMBL560049 | — | IC50 | - | — | - | |
| CHEMBL550289 | — | IC50 | > | 4000.0 | nM | - |
| CHEMBL563404 | — | IC50 | - | — | - | |
| CHEMBL549761 | — | IC50 | > | 2920.0 | nM | - |
| CHEMBL551556 | — | IC50 | - | — | - | |
| CHEMBL563852 | — | IC50 | > | 40000.0 | nM | - |
| CHEMBL562244 | — | IC50 | > | 40000.0 | nM | - |
| CHEMBL560050 | — | IC50 | - | — | - | |
| CHEMBL549965 | — | IC50 | > | 4000.0 | nM | - |
| CHEMBL562108 | — | IC50 | - | — | - | |
| CHEMBL551443 | — | IC50 | - | — | - | |
| CHEMBL556888 | — | IC50 | - | — | - |