Assay Detail
Binding
CHEMBL4233796
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human SERT expressed in HEK293 cells assessed as reduction in [3H]5-HT uptake by micro beta scintillation counting analysis
28
Total Activities
28
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 | Autocuration |
Target
Sodium-dependent serotonin transporter (CHEMBL228) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Design, synthesis and docking study of 4-arylpiperazine carboxamides as monoamine neurotransmitters reuptake inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 28 | 6.01 | 6.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1201066 | VENLAFAXINE HYDROCHLORIDE | 4.0 | 1 | 6.70 |
| CHEMBL4250965 | — | — | 1 | 6.64 |
| CHEMBL4240379 | — | — | 1 | 6.64 |
| CHEMBL4244291 | — | — | 1 | 6.56 |
| CHEMBL4243340 | — | — | 1 | 6.55 |
| CHEMBL4237635 | — | — | 1 | 6.40 |
| CHEMBL4239115 | — | — | 1 | 6.34 |
| CHEMBL4243862 | — | — | 1 | 6.26 |
| CHEMBL4240083 | — | — | 1 | 6.13 |
| CHEMBL4245867 | — | — | 1 | 6.13 |
| CHEMBL4248022 | — | — | 1 | 6.00 |
| CHEMBL4251399 | — | — | 1 | 5.93 |
| CHEMBL4243712 | — | — | 1 | 5.88 |
| CHEMBL4247254 | — | — | 1 | 5.37 |
| CHEMBL4248596 | — | — | 1 | 5.35 |
| CHEMBL4241632 | — | — | 1 | 5.16 |
| CHEMBL4247932 | — | — | 1 | 5.16 |
| CHEMBL4249668 | — | — | 1 | 5.02 |
| CHEMBL4250502 | — | — | 1 | - |
| CHEMBL4246682 | — | — | 1 | - |
| CHEMBL4237739 | — | — | 1 | - |
| CHEMBL4245408 | — | — | 1 | - |
| CHEMBL4248092 | — | — | 1 | - |
| CHEMBL4238362 | — | — | 1 | - |
| CHEMBL4237912 | — | — | 1 | - |
| CHEMBL4242062 | — | — | 1 | - |
| CHEMBL4237546 | — | — | 1 | - |
| CHEMBL4247560 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1201066 | VENLAFAXINE HYDROCHLORIDE | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL4250965 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL4240379 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL4244291 | — | IC50 | = | 273.0 | nM | 6.56 |
| CHEMBL4243340 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL4237635 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL4239115 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL4243862 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL4240083 | — | IC50 | = | 741.4 | nM | 6.13 |
| CHEMBL4245867 | — | IC50 | = | 740.0 | nM | 6.13 |
| CHEMBL4248022 | — | IC50 | = | 1010.0 | nM | 6.00 |
| CHEMBL4251399 | — | IC50 | = | 1170.0 | nM | 5.93 |
| CHEMBL4243712 | — | IC50 | = | 1320.0 | nM | 5.88 |
| CHEMBL4247254 | — | IC50 | = | 4270.0 | nM | 5.37 |
| CHEMBL4248596 | — | IC50 | = | 4460.0 | nM | 5.35 |
| CHEMBL4241632 | — | IC50 | = | 6940.0 | nM | 5.16 |
| CHEMBL4247932 | — | IC50 | = | 6850.0 | nM | 5.16 |
| CHEMBL4249668 | — | IC50 | = | 9640.0 | nM | 5.02 |
| CHEMBL4250502 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4246682 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4237739 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4245408 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4248092 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4238362 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4237912 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4242062 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4237546 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4247560 | — | IC50 | > | 10000.0 | nM | - |