Assay Detail
Binding
CHEMBL863614
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Inhibition of [3H]DA reuptake at DA transporter in HEK293 cells
30
Total Activities
29
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 | Expert |
Target
Sodium-dependent dopamine transporter (CHEMBL238) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Structure-activity relationships of N-substituted piperazine amine reuptake inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 30 | 5.75 | 6.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL384687 | — | — | 1 | 6.40 |
| CHEMBL1175 | DULOXETINE | 4.0 | 1 | 6.06 |
| CHEMBL214259 | — | — | 1 | 6.01 |
| CHEMBL213287 | — | — | 1 | 5.89 |
| CHEMBL534942 | — | — | 2 | 5.80 |
| CHEMBL213785 | — | — | 1 | 5.80 |
| CHEMBL214121 | — | — | 1 | 5.64 |
| CHEMBL41 | FLUOXETINE | 4.0 | 1 | 5.36 |
| CHEMBL378319 | — | — | 1 | 5.04 |
| CHEMBL386224 | — | — | 1 | - |
| CHEMBL214159 | — | — | 1 | - |
| CHEMBL214395 | — | — | 1 | - |
| CHEMBL378447 | — | — | 1 | - |
| CHEMBL211412 | — | — | 1 | - |
| CHEMBL213496 | — | — | 1 | - |
| CHEMBL377189 | — | — | 1 | - |
| CHEMBL210116 | — | — | 1 | - |
| CHEMBL213030 | — | — | 1 | - |
| CHEMBL214056 | — | — | 1 | - |
| CHEMBL214004 | — | — | 1 | - |
| CHEMBL377900 | — | — | 1 | - |
| CHEMBL376952 | — | — | 1 | - |
| CHEMBL213229 | — | — | 1 | - |
| CHEMBL212878 | — | — | 1 | - |
| CHEMBL14370 | REBOXETINE | 4.0 | 1 | - |
| CHEMBL534723 | — | — | 1 | - |
| CHEMBL425961 | — | — | 1 | - |
| CHEMBL540107 | — | — | 1 | - |
| CHEMBL211527 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL384687 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL1175 | DULOXETINE | IC50 | = | 870.0 | nM | 6.06 |
| CHEMBL214259 | — | IC50 | = | 970.0 | nM | 6.01 |
| CHEMBL213287 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL534942 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL213785 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL214121 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL534942 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL41 | FLUOXETINE | IC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL378319 | — | IC50 | = | 9200.0 | nM | 5.04 |
| CHEMBL214159 | — | IC50 | - | — | - | |
| CHEMBL214395 | — | IC50 | - | — | - | |
| CHEMBL378447 | — | IC50 | - | — | - | |
| CHEMBL211412 | — | IC50 | - | — | - | |
| CHEMBL213496 | — | IC50 | - | — | - | |
| CHEMBL377189 | — | IC50 | - | — | - | |
| CHEMBL210116 | — | IC50 | - | — | - | |
| CHEMBL213030 | — | IC50 | - | — | - | |
| CHEMBL214056 | — | IC50 | - | — | - | |
| CHEMBL214004 | — | IC50 | - | — | - | |
| CHEMBL386224 | — | IC50 | > | 4000.0 | nM | - |
| CHEMBL376952 | — | IC50 | - | — | - | |
| CHEMBL377900 | — | IC50 | > | 4000.0 | nM | - |
| CHEMBL212878 | — | IC50 | - | — | - | |
| CHEMBL213229 | — | IC50 | > | 4000.0 | nM | - |
| CHEMBL534723 | — | IC50 | > | 4000.0 | nM | - |
| CHEMBL14370 | REBOXETINE | IC50 | > | 25000.0 | nM | - |
| CHEMBL540107 | — | IC50 | > | 4000.0 | nM | - |
| CHEMBL425961 | — | IC50 | - | — | - | |
| CHEMBL211527 | — | IC50 | > | 4000.0 | nM | - |