Assay Detail
Binding
CHEMBL905525
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]paroxetine from human cloned 5HTT receptor transfected in CHO cells
9
Total Activities
3
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 | Expert |
Target
Sodium-dependent serotonin transporter (CHEMBL228) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Tricyclic isoxazolines: identification of R226161 as a potential new antidepressant that combines potent serotonin reuptake inhibition and alpha2-adrenoceptor antagonism.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 9 | 8.19 | 8.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL318235 | — | — | 3 | 8.92 |
| CHEMBL226636 | — | — | 3 | 8.68 |
| CHEMBL390718 | — | — | 3 | 8.05 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL318235 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL318235 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL226636 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL318235 | — | Ki | = | 3.7 | nM | 8.43 |
| CHEMBL226636 | — | Ki | = | 5.6 | nM | 8.25 |
| CHEMBL390718 | — | Ki | = | 8.9 | nM | 8.05 |
| CHEMBL226636 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL390718 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL390718 | — | Ki | = | 79.0 | nM | 7.10 |