Assay Detail
Binding
CHEMBL1831837
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Inhibition of human SERT expressed in JAR cells assessed as serotonin uptake
16
Total Activities
16
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
Discovery of novel selective norepinephrine inhibitors: 1-(2-morpholin-2-ylethyl)-3-aryl-1,3-dihydro-2,1,3-benzothiadiazole 2,2-dioxides (WYE-114152).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 5.75 | 8.03 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL41 | FLUOXETINE | 4.0 | 1 | 8.03 |
| CHEMBL1830886 | — | — | 1 | 6.13 |
| CHEMBL1830891 | — | — | 1 | 6.09 |
| CHEMBL1828653 | — | — | 1 | 6.00 |
| CHEMBL1830878 | — | — | 1 | 5.99 |
| CHEMBL1830889 | — | — | 1 | 5.85 |
| CHEMBL1830877 | — | — | 1 | 5.75 |
| CHEMBL1830884 | — | — | 1 | 5.53 |
| CHEMBL1082458 | — | — | 1 | 5.47 |
| CHEMBL1830888 | — | — | 1 | 5.38 |
| CHEMBL1830876 | — | — | 1 | 5.29 |
| CHEMBL1830892 | — | — | 1 | 5.24 |
| CHEMBL1830885 | — | — | 1 | 5.19 |
| CHEMBL1830879 | — | — | 1 | 5.17 |
| CHEMBL1830890 | — | — | 1 | 5.08 |
| CHEMBL1830887 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL41 | FLUOXETINE | IC50 | = | 9.4 | nM | 8.03 |
| CHEMBL1830886 | — | IC50 | = | 749.0 | nM | 6.13 |
| CHEMBL1830891 | — | IC50 | = | 806.0 | nM | 6.09 |
| CHEMBL1828653 | — | IC50 | = | 992.0 | nM | 6.00 |
| CHEMBL1830878 | — | IC50 | = | 1030.0 | nM | 5.99 |
| CHEMBL1830889 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL1830877 | — | IC50 | = | 1775.0 | nM | 5.75 |
| CHEMBL1830884 | — | IC50 | = | 2983.0 | nM | 5.53 |
| CHEMBL1082458 | — | IC50 | = | 3380.0 | nM | 5.47 |
| CHEMBL1830888 | — | IC50 | = | 4128.0 | nM | 5.38 |
| CHEMBL1830876 | — | IC50 | = | 5100.0 | nM | 5.29 |
| CHEMBL1830892 | — | IC50 | = | 5790.0 | nM | 5.24 |
| CHEMBL1830885 | — | IC50 | = | 6410.0 | nM | 5.19 |
| CHEMBL1830879 | — | IC50 | = | 6770.0 | nM | 5.17 |
| CHEMBL1830890 | — | IC50 | = | 8347.0 | nM | 5.08 |
| CHEMBL1830887 | — | IC50 | - | — | - |