Assay Detail
Binding
CHEMBL863612
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Inhibition of [3H]5-HT reuptake at 5HT 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 serotonin transporter (CHEMBL228) ↗| 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 | 7.68 | 8.41 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL214056 | — | — | 1 | 8.41 |
| CHEMBL534942 | — | — | 2 | 8.41 |
| CHEMBL213287 | — | — | 1 | 8.27 |
| CHEMBL1175 | DULOXETINE | 4.0 | 1 | 8.22 |
| CHEMBL377900 | — | — | 1 | 8.09 |
| CHEMBL540107 | — | — | 1 | 8.01 |
| CHEMBL378447 | — | — | 1 | 8.00 |
| CHEMBL211527 | — | — | 1 | 7.96 |
| CHEMBL212878 | — | — | 1 | 7.92 |
| CHEMBL377189 | — | — | 1 | 7.92 |
| CHEMBL214259 | — | — | 1 | 7.92 |
| CHEMBL213785 | — | — | 1 | 7.89 |
| CHEMBL534723 | — | — | 1 | 7.89 |
| CHEMBL386224 | — | — | 1 | 7.89 |
| CHEMBL378319 | — | — | 1 | 7.85 |
| CHEMBL214121 | — | — | 1 | 7.82 |
| CHEMBL41 | FLUOXETINE | 4.0 | 1 | 7.80 |
| CHEMBL214159 | — | — | 1 | 7.77 |
| CHEMBL425961 | — | — | 1 | 7.77 |
| CHEMBL384687 | — | — | 1 | 7.64 |
| CHEMBL209707 | — | — | 1 | 7.64 |
| CHEMBL214395 | — | — | 1 | 7.55 |
| CHEMBL211412 | — | — | 1 | 7.52 |
| CHEMBL214004 | — | — | 1 | 7.42 |
| CHEMBL210116 | — | — | 1 | 7.41 |
| CHEMBL213496 | — | — | 1 | 7.40 |
| CHEMBL212877 | — | — | 1 | 7.38 |
| CHEMBL213229 | — | — | 1 | 7.34 |
| CHEMBL213030 | — | — | 1 | 7.10 |
| CHEMBL376952 | — | — | 1 | 6.64 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL214056 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL534942 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL213287 | — | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL1175 | DULOXETINE | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL377900 | — | IC50 | = | 8.2 | nM | 8.09 |
| CHEMBL540107 | — | IC50 | = | 9.8 | nM | 8.01 |
| CHEMBL378447 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL211527 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL214259 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL377189 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL212878 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL386224 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL534723 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL534942 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL213785 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL378319 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL214121 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL41 | FLUOXETINE | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL214159 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL425961 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL384687 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL209707 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL214395 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL211412 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL214004 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL210116 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL213496 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL212877 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL213229 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL213030 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL376952 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL214003 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL14370 | REBOXETINE | IC50 | = | 590.0 | nM | 6.23 |