Assay Detail
Binding
CHEMBL3378814
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Displacement of [3H]Citolapram from human SERT expressed in HEK293E cells after 1 hr by liquid scintillation counting
21
Total Activities
21
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293E |
| 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 4-heteroaryl 1,2,3,4-tetrahydroisoquinolines as triple reuptake inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 7.42 | 8.36 |
| Ki | 2 | 6.64 | 6.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3323179 | — | — | 1 | 8.36 |
| CHEMBL3323183 | — | — | 1 | 8.35 |
| CHEMBL3323173 | — | — | 1 | 8.31 |
| CHEMBL3323174 | — | — | 1 | 8.28 |
| CHEMBL3323175 | — | — | 1 | 8.00 |
| CHEMBL3323089 | — | — | 1 | 7.62 |
| CHEMBL3323178 | — | — | 1 | 7.55 |
| CHEMBL3323093 | — | — | 1 | 7.54 |
| CHEMBL3323094 | — | — | 1 | 7.51 |
| CHEMBL3323097 | — | — | 1 | 7.46 |
| CHEMBL3323185 | — | — | 1 | 7.42 |
| CHEMBL3323096 | — | — | 1 | 7.40 |
| CHEMBL3323092 | — | — | 1 | 7.17 |
| CHEMBL3323095 | — | — | 1 | 7.16 |
| CHEMBL3323091 | — | — | 1 | 6.96 |
| CHEMBL3323099 | — | — | 1 | 6.89 |
| CHEMBL3323101 | — | — | 1 | 6.77 |
| CHEMBL3323088 | — | — | 1 | 6.64 |
| CHEMBL3323090 | — | — | 1 | 6.60 |
| CHEMBL3323187 | — | — | 1 | 5.60 |
| CHEMBL796 | METHYLPHENIDATE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3323179 | — | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL3323183 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL3323173 | — | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL3323174 | — | IC50 | = | 5.3 | nM | 8.28 |
| CHEMBL3323175 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3323089 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL3323178 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL3323093 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL3323094 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL3323097 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL3323185 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL3323096 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL3323092 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL3323095 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL3323091 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL3323099 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL3323101 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL3323088 | — | Ki | = | 230.0 | nM | 6.64 |
| CHEMBL3323090 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL3323187 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL796 | METHYLPHENIDATE | Ki | > | 10000.0 | nM | - |