Assay Detail
Binding
CHEMBL3821818
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Inhibition of human SERT expressed in CHO cells assessed as [3H]-5-hydroxytryptamine reuptake incubated for 20 mins measured after 30 mins by topcount method
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sodium-dependent serotonin transporter (CHEMBL228) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Design, synthesis, and biological evaluation of a novel series of peripheral-selective noradrenaline reuptake inhibitors - Part 3.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 7.05 | 7.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3818117 | — | — | 1 | 7.92 |
| CHEMBL3817915 | — | — | 1 | 7.57 |
| CHEMBL3818901 | — | — | 1 | 7.27 |
| CHEMBL3818471 | — | — | 1 | 7.17 |
| CHEMBL3819243 | — | — | 1 | 7.10 |
| CHEMBL3818953 | — | — | 1 | 7.07 |
| CHEMBL3819009 | — | — | 1 | 6.92 |
| CHEMBL3819201 | — | — | 1 | 6.89 |
| CHEMBL3818345 | — | — | 1 | 6.42 |
| CHEMBL3818946 | — | — | 1 | 6.14 |
| CHEMBL3593402 | — | — | 1 | - |
| CHEMBL3819441 | — | — | 1 | - |
| CHEMBL3818596 | — | — | 1 | - |
| CHEMBL3819217 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3818117 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3817915 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL3818901 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL3818471 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL3819243 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL3818953 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL3819009 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL3819201 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL3818345 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL3818946 | — | IC50 | = | 730.0 | nM | 6.14 |
| CHEMBL3593402 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL3819441 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL3818596 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL3819217 | — | IC50 | > | 1000.0 | nM | - |