Assay Detail
Binding
CHEMBL1020017
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Inhibition of 5HT uptake at human SERT expressed in human JAR cells
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | JAR |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sodium-dependent serotonin transporter (CHEMBL228) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Structure-activity relationships of the cycloalkanol ethylamine scaffold: discovery of selective norepinephrine reuptake inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 6.32 | 8.03 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL41 | FLUOXETINE | 4.0 | 1 | 8.03 |
| CHEMBL637 | VENLAFAXINE | 4.0 | 1 | 7.51 |
| CHEMBL101055 | — | — | 1 | 7.06 |
| CHEMBL420644 | — | — | 1 | 6.91 |
| CHEMBL448953 | — | — | 1 | 6.81 |
| CHEMBL316862 | — | — | 1 | 6.75 |
| CHEMBL101899 | — | — | 1 | 6.54 |
| CHEMBL461095 | — | — | 1 | 6.39 |
| CHEMBL99653 | — | — | 1 | 6.27 |
| CHEMBL518195 | — | — | 1 | 5.92 |
| CHEMBL459644 | — | — | 1 | 5.82 |
| CHEMBL461707 | — | — | 1 | 5.57 |
| CHEMBL461705 | — | — | 1 | 5.30 |
| CHEMBL461706 | — | — | 1 | 5.21 |
| CHEMBL511347 | — | — | 1 | 4.73 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL41 | FLUOXETINE | IC50 | = | 9.4 | nM | 8.03 |
| CHEMBL637 | VENLAFAXINE | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL101055 | — | IC50 | = | 88.0 | nM | 7.06 |
| CHEMBL420644 | — | IC50 | = | 123.0 | nM | 6.91 |
| CHEMBL448953 | — | IC50 | = | 155.0 | nM | 6.81 |
| CHEMBL316862 | — | IC50 | = | 177.0 | nM | 6.75 |
| CHEMBL101899 | — | IC50 | = | 292.0 | nM | 6.54 |
| CHEMBL461095 | — | IC50 | = | 405.0 | nM | 6.39 |
| CHEMBL99653 | — | IC50 | = | 534.0 | nM | 6.27 |
| CHEMBL518195 | — | IC50 | = | 1214.0 | nM | 5.92 |
| CHEMBL459644 | — | IC50 | = | 1525.0 | nM | 5.82 |
| CHEMBL461707 | — | IC50 | = | 2669.0 | nM | 5.57 |
| CHEMBL461705 | — | IC50 | = | 4962.0 | nM | 5.30 |
| CHEMBL461706 | — | IC50 | = | 6102.0 | nM | 5.21 |
| CHEMBL511347 | — | IC50 | = | 18795.0 | nM | 4.73 |