Assay Detail
Binding
CHEMBL5581344
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-Citalopram from human SERT extracted from HEK293 cell membrane assessed as inhibition constant incubated for 60 mins by microbeta2 scintillation counter analysis
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Subcellular | Cell membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Dual 5-HT<sub>6</sub>/SERT ligands for mitigating neuropsychiatric symptoms of dementia exerting neuroprotection against amyloid-β toxicity, memory preservation, and antidepressant-like properties.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 33 | 7.79 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5591292 | — | — | 1 | 9.70 |
| CHEMBL490 | PAROXETINE | 4.0 | 1 | 9.22 |
| CHEMBL5595193 | — | — | 1 | 9.22 |
| CHEMBL1508 | ESCITALOPRAM | 4.0 | 1 | 9.00 |
| CHEMBL5591924 | — | — | 1 | 8.40 |
| CHEMBL5593858 | — | — | 1 | 8.40 |
| CHEMBL5595568 | — | — | 1 | 8.40 |
| CHEMBL5595885 | — | — | 1 | 8.30 |
| CHEMBL5595917 | — | — | 1 | 8.30 |
| CHEMBL5593795 | — | — | 1 | 8.15 |
| CHEMBL5595197 | — | — | 1 | 8.05 |
| CHEMBL5595546 | — | — | 1 | 8.05 |
| CHEMBL5592533 | — | — | 1 | 7.89 |
| CHEMBL5589768 | — | — | 1 | 7.82 |
| CHEMBL5593556 | — | — | 1 | 7.72 |
| CHEMBL5593156 | — | — | 1 | 7.68 |
| CHEMBL5594664 | — | — | 1 | 7.64 |
| CHEMBL5594857 | — | — | 1 | 7.51 |
| CHEMBL5593170 | — | — | 1 | 7.47 |
| CHEMBL5595457 | — | — | 1 | 7.38 |
| CHEMBL5592369 | — | — | 1 | 7.36 |
| CHEMBL5594446 | — | — | 1 | 7.31 |
| CHEMBL5594772 | — | — | 1 | 7.14 |
| CHEMBL5594193 | — | — | 1 | 7.12 |
| CHEMBL5593545 | — | — | 1 | 6.86 |
| CHEMBL5595216 | — | — | 1 | 6.81 |
| CHEMBL5592733 | — | — | 1 | 6.80 |
| CHEMBL5594351 | — | — | 1 | 6.72 |
| CHEMBL5592851 | — | — | 1 | 6.71 |
| CHEMBL5595898 | — | — | 1 | 6.65 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5591292 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL490 | PAROXETINE | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL5595193 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL1508 | ESCITALOPRAM | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL5591924 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL5593858 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL5595568 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL5595885 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL5595917 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL5593795 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL5595197 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL5595546 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL5592533 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL5589768 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL5593556 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL5593156 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL5594664 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL5594857 | — | Ki | = | 31.0 | nM | 7.51 |
| CHEMBL5593170 | — | Ki | = | 34.0 | nM | 7.47 |
| CHEMBL5595457 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL5592369 | — | Ki | = | 44.0 | nM | 7.36 |
| CHEMBL5594446 | — | Ki | = | 49.0 | nM | 7.31 |
| CHEMBL5594772 | — | Ki | = | 72.0 | nM | 7.14 |
| CHEMBL5594193 | — | Ki | = | 76.0 | nM | 7.12 |
| CHEMBL5593545 | — | Ki | = | 139.0 | nM | 6.86 |
| CHEMBL5595216 | — | Ki | = | 155.0 | nM | 6.81 |
| CHEMBL5592733 | — | Ki | = | 158.0 | nM | 6.80 |
| CHEMBL5594351 | — | Ki | = | 189.0 | nM | 6.72 |
| CHEMBL5592851 | — | Ki | = | 197.0 | nM | 6.71 |
| CHEMBL5595898 | — | Ki | = | 226.0 | nM | 6.65 |
| CHEMBL93240 | METITEPINE | Ki | - | — | - | |
| CHEMBL60264 | — | Ki | - | — | - | |
| CHEMBL6437 | MIANSERIN | Ki | - | — | - |