Assay Detail
Binding
CHEMBL1001385
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]citalopram from human SERT expressed in HEK293 cells
9
Total Activities
9
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
3-(4-(6-Fluoroalkoxy-3,4-dihydroisoquinoline-2(1H)-yl)cyclohexyl)-1H-indole-5-carbonitriles for SERT imaging: chemical synthesis, evaluation in vitro and radiofluorination.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 9 | 8.05 | 9.38 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL490 | PAROXETINE | 4.0 | 1 | 9.38 |
| CHEMBL22183 | — | — | 1 | 9.14 |
| CHEMBL294481 | — | — | 1 | 8.39 |
| CHEMBL549 | CITALOPRAM | 4.0 | 1 | 8.36 |
| CHEMBL54465 | — | — | 1 | 8.35 |
| CHEMBL449277 | — | — | 1 | 8.21 |
| CHEMBL293583 | — | — | 1 | 7.13 |
| CHEMBL55505 | — | — | 1 | 7.04 |
| CHEMBL477587 | — | — | 1 | 6.49 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL490 | PAROXETINE | Ki | = | 0.42 | nM | 9.38 |
| CHEMBL22183 | — | Ki | = | 0.73 | nM | 9.14 |
| CHEMBL294481 | — | Ki | = | 4.1 | nM | 8.39 |
| CHEMBL549 | CITALOPRAM | Ki | = | 4.38 | nM | 8.36 |
| CHEMBL54465 | — | Ki | = | 4.51 | nM | 8.35 |
| CHEMBL449277 | — | Ki | = | 6.16 | nM | 8.21 |
| CHEMBL293583 | — | Ki | = | 73.7 | nM | 7.13 |
| CHEMBL55505 | — | Ki | = | 90.7 | nM | 7.04 |
| CHEMBL477587 | — | Ki | = | 327.0 | nM | 6.49 |