Assay Detail
Binding
CHEMBL4276203
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Inhibition of [3H]serotonin uptake at human SERT expressed in HEK293 cells after 15 to 20 mins by microbeta scintillation counting method
15
Total Activities
15
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 systematic evaluation of 4-arylpiperazine- and 4-benzylpiperidine napthyl ethers as inhibitors of monoamine neurotransmitters reuptake.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 5.83 | 6.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1201066 | VENLAFAXINE HYDROCHLORIDE | 4.0 | 1 | 6.70 |
| CHEMBL4082902 | — | — | 1 | 6.24 |
| CHEMBL4278945 | — | — | 1 | 6.17 |
| CHEMBL4245867 | — | — | 1 | 6.13 |
| CHEMBL4283496 | — | — | 1 | 6.08 |
| CHEMBL4283917 | — | — | 1 | 6.00 |
| CHEMBL4295202 | — | — | 1 | 5.98 |
| CHEMBL4277619 | — | — | 1 | 5.97 |
| CHEMBL4286313 | — | — | 1 | 5.73 |
| CHEMBL4278059 | — | — | 1 | 5.55 |
| CHEMBL4282796 | — | — | 1 | 5.50 |
| CHEMBL4286186 | — | — | 1 | 5.37 |
| CHEMBL4290687 | — | — | 1 | 5.29 |
| CHEMBL4294090 | — | — | 1 | 4.97 |
| CHEMBL4288240 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1201066 | VENLAFAXINE HYDROCHLORIDE | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL4082902 | — | IC50 | = | 570.0 | nM | 6.24 |
| CHEMBL4278945 | — | IC50 | = | 680.0 | nM | 6.17 |
| CHEMBL4245867 | — | IC50 | = | 740.0 | nM | 6.13 |
| CHEMBL4283496 | — | IC50 | = | 830.0 | nM | 6.08 |
| CHEMBL4283917 | — | IC50 | = | 990.0 | nM | 6.00 |
| CHEMBL4295202 | — | IC50 | = | 1040.0 | nM | 5.98 |
| CHEMBL4277619 | — | IC50 | = | 1080.0 | nM | 5.97 |
| CHEMBL4286313 | — | IC50 | = | 1860.0 | nM | 5.73 |
| CHEMBL4278059 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL4282796 | — | IC50 | = | 3150.0 | nM | 5.50 |
| CHEMBL4286186 | — | IC50 | = | 4320.0 | nM | 5.37 |
| CHEMBL4290687 | — | IC50 | = | 5160.0 | nM | 5.29 |
| CHEMBL4294090 | — | IC50 | = | 10700.0 | nM | 4.97 |
| CHEMBL4288240 | — | IC50 | > | 10000.0 | nM | - |