Assay Detail
Binding
CHEMBL3095436
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Allosteric modulation at wild-type human SERT site S2 expressed in african green monkey COS7 cells assessed as inhibition of [3H]citalopram dissociation at 30 uM by scintillation counting analysis
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | COS-7 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sodium-dependent serotonin transporter (CHEMBL228) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Design and synthesis of 1-(3-(dimethylamino)propyl)-1-(4-fluorophenyl)-1,3-dihydroisobenzofuran-5-carbonitrile (citalopram) analogues as novel probes for the serotonin transporter S1 and S2 binding sites.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 5.37 | 5.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3094160 | — | — | 1 | 5.52 |
| CHEMBL1215762 | — | — | 1 | 5.47 |
| CHEMBL3094164 | — | — | 1 | 5.44 |
| CHEMBL1508 | ESCITALOPRAM | 4.0 | 1 | 5.34 |
| CHEMBL3094168 | — | — | 1 | 5.33 |
| CHEMBL3094159 | — | — | 1 | 5.31 |
| CHEMBL3094176 | — | — | 1 | 5.28 |
| CHEMBL3094161 | — | — | 1 | 5.24 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3094160 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL1215762 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL3094164 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL1508 | ESCITALOPRAM | IC50 | = | 4600.0 | nM | 5.34 |
| CHEMBL3094168 | — | IC50 | = | 4700.0 | nM | 5.33 |
| CHEMBL3094159 | — | IC50 | = | 4900.0 | nM | 5.31 |
| CHEMBL3094176 | — | IC50 | = | 5300.0 | nM | 5.28 |
| CHEMBL3094161 | — | IC50 | = | 5800.0 | nM | 5.24 |