Assay Detail
Binding
CHEMBL863613
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Inhibition of [3H]NA reuptake at NA transporter in HEK293 cells
33
Total Activities
32
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 noradrenaline transporter (CHEMBL222) ↗| 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 | 33 | 7.33 | 8.06 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL214003 | — | — | 1 | 8.06 |
| CHEMBL14370 | REBOXETINE | 4.0 | 1 | 7.96 |
| CHEMBL213229 | — | — | 1 | 7.82 |
| CHEMBL534723 | — | — | 1 | 7.80 |
| CHEMBL386224 | — | — | 1 | 7.80 |
| CHEMBL1175 | DULOXETINE | 4.0 | 1 | 7.72 |
| CHEMBL534942 | — | — | 2 | 7.72 |
| CHEMBL540107 | — | — | 1 | 7.72 |
| CHEMBL213496 | — | — | 1 | 7.68 |
| CHEMBL213287 | — | — | 1 | 7.66 |
| CHEMBL214395 | — | — | 1 | 7.66 |
| CHEMBL214121 | — | — | 1 | 7.60 |
| CHEMBL214159 | — | — | 1 | 7.55 |
| CHEMBL378447 | — | — | 1 | 7.42 |
| CHEMBL213030 | — | — | 1 | 7.35 |
| CHEMBL384687 | — | — | 1 | 7.32 |
| CHEMBL378319 | — | — | 1 | 7.12 |
| CHEMBL212877 | — | — | 1 | 7.12 |
| CHEMBL214259 | — | — | 1 | 7.09 |
| CHEMBL213785 | — | — | 1 | 7.03 |
| CHEMBL214056 | — | — | 1 | 7.00 |
| CHEMBL377900 | — | — | 1 | 6.92 |
| CHEMBL377189 | — | — | 1 | 6.92 |
| CHEMBL211412 | — | — | 1 | 6.89 |
| CHEMBL210116 | — | — | 1 | 6.47 |
| CHEMBL41 | FLUOXETINE | 4.0 | 1 | 5.28 |
| CHEMBL211527 | — | — | 1 | - |
| CHEMBL214004 | — | — | 1 | - |
| CHEMBL376952 | — | — | 1 | - |
| CHEMBL212878 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL214003 | — | IC50 | = | 8.8 | nM | 8.06 |
| CHEMBL14370 | REBOXETINE | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL213229 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL534723 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL386224 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL1175 | DULOXETINE | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL534942 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL540107 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL213496 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL213287 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL214395 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL214121 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL214159 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL378447 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL213030 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL384687 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL534942 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL378319 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL212877 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL214259 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL213785 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL214056 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL377900 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL377189 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL211412 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL210116 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL41 | FLUOXETINE | IC50 | = | 5200.0 | nM | 5.28 |
| CHEMBL209707 | — | IC50 | > | 400.0 | nM | - |
| CHEMBL425961 | — | IC50 | > | 400.0 | nM | - |
| CHEMBL212878 | — | IC50 | > | 400.0 | nM | - |
| CHEMBL376952 | — | IC50 | > | 400.0 | nM | - |
| CHEMBL214004 | — | IC50 | > | 400.0 | nM | - |
| CHEMBL211527 | — | IC50 | > | 400.0 | nM | - |