Assay Detail
Binding
CHEMBL1038439
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Displacement of [125I]RTI-55 from human recombinant SERT expressed in HEK293 cells
8
Total Activities
8
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
Inhibition of serotonin and norepinephrine reuptake and inhibition of phosphodiesterase by multi-target inhibitors as potential agents for depression.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 8 | 7.29 | 8.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL336920 | (R)-DULOXETINE | — | 1 | 8.60 |
| CHEMBL594585 | R-NORDULOXETINE | — | 1 | 8.08 |
| CHEMBL595063 | (S)-NORDULOXETINE | — | 1 | 7.75 |
| CHEMBL596175 | — | — | 1 | 6.90 |
| CHEMBL370805 | COCAINE | 4.0 | 1 | 6.28 |
| CHEMBL596185 | — | — | 1 | 6.14 |
| CHEMBL440878 | — | — | 1 | - |
| CHEMBL463431 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL336920 | (R)-DULOXETINE | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL594585 | R-NORDULOXETINE | Ki | = | 8.3 | nM | 8.08 |
| CHEMBL595063 | (S)-NORDULOXETINE | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL596175 | — | Ki | = | 127.0 | nM | 6.90 |
| CHEMBL370805 | COCAINE | Ki | = | 525.0 | nM | 6.28 |
| CHEMBL596185 | — | Ki | = | 726.0 | nM | 6.14 |
| CHEMBL440878 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL463431 | — | Ki | > | 100000.0 | nM | - |