Assay Detail
Binding
CHEMBL5055012
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-citalopram from human SERT expressed in HEK cell membrane assessed as inhibition constant by radioligand binding assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK |
| Subcellular | Cell membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sodium-dependent serotonin transporter (CHEMBL228) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
C-terminal modified Enkephalin-like tetrapeptides with enhanced affinities at the kappa opioid receptor and monoamine transporters.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 8 | 6.01 | 8.04 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL629 | AMITRIPTYLINE | 4.0 | 1 | 8.04 |
| CHEMBL5089012 | — | — | 1 | 6.06 |
| CHEMBL5077561 | — | — | 1 | 6.00 |
| CHEMBL5090705 | — | — | 1 | 5.75 |
| CHEMBL5078669 | — | — | 1 | 5.64 |
| CHEMBL5081245 | — | — | 1 | 5.60 |
| CHEMBL5091642 | — | — | 1 | 4.96 |
| CHEMBL5086370 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL629 | AMITRIPTYLINE | Ki | = | 9.2 | nM | 8.04 |
| CHEMBL5089012 | — | Ki | = | 880.0 | nM | 6.06 |
| CHEMBL5077561 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL5090705 | — | Ki | = | 1800.0 | nM | 5.75 |
| CHEMBL5078669 | — | Ki | = | 2300.0 | nM | 5.64 |
| CHEMBL5081245 | — | Ki | = | 2500.0 | nM | 5.60 |
| CHEMBL5091642 | — | Ki | = | 11000.0 | nM | 4.96 |
| CHEMBL5086370 | — | Ki | > | 10000.0 | nM | - |