Assay Detail
Binding
CHEMBL948024
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-citalopram from human SERT expressed in HEK293 cell membrane
13
Total Activities
13
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
The synthesis of bivalent 2beta-carbomethoxy-3beta-(3,4-dichlorophenyl)-8-heterobicyclo[3.2.1]octanes as probes for proximal binding sites on the dopamine and serotonin transporters.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 7.18 | 8.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL42553 | — | — | 1 | 8.60 |
| CHEMBL227757 | — | — | 1 | 8.52 |
| CHEMBL390929 | — | — | 1 | 8.33 |
| CHEMBL271707 | — | — | 1 | 7.77 |
| CHEMBL399740 | — | — | 1 | 7.51 |
| CHEMBL255140 | — | — | 1 | 7.28 |
| CHEMBL257482 | — | — | 1 | 7.25 |
| CHEMBL256046 | — | — | 1 | 6.97 |
| CHEMBL403660 | — | — | 1 | 6.85 |
| CHEMBL401554 | — | — | 1 | 6.39 |
| CHEMBL270659 | — | — | 1 | 6.23 |
| CHEMBL407902 | — | — | 1 | 6.00 |
| CHEMBL279331 | — | — | 1 | 5.66 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL42553 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL227757 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL390929 | — | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL271707 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL399740 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL255140 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL257482 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL256046 | — | IC50 | = | 106.0 | nM | 6.97 |
| CHEMBL403660 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL401554 | — | IC50 | = | 405.0 | nM | 6.39 |
| CHEMBL270659 | — | IC50 | = | 593.0 | nM | 6.23 |
| CHEMBL407902 | — | IC50 | = | 992.0 | nM | 6.00 |
| CHEMBL279331 | — | IC50 | = | 2200.0 | nM | 5.66 |