Assay Detail
Binding
CHEMBL2382973
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Displacement of [3H]citalopram from human SERT expressed in HEK293 cell membranes
15
Total Activities
15
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
Conformationally restricted homotryptamines. Part 6: indole-5-cycloalkyl methylamines as selective serotonin reuptake inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 7.44 | 9.25 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL196468 | — | — | 1 | 9.25 |
| CHEMBL539470 | — | — | 1 | 8.96 |
| CHEMBL2380980 | — | — | 1 | 8.42 |
| CHEMBL2380975 | — | — | 1 | 8.37 |
| CHEMBL2380983 | — | — | 1 | 8.22 |
| CHEMBL2380971 | — | — | 1 | 7.75 |
| CHEMBL2380972 | — | — | 1 | 7.19 |
| CHEMBL2380979 | — | — | 1 | 7.01 |
| CHEMBL2380974 | — | — | 1 | 6.85 |
| CHEMBL2380976 | — | — | 1 | 6.70 |
| CHEMBL2380978 | — | — | 1 | 6.58 |
| CHEMBL2380973 | — | — | 1 | 6.52 |
| CHEMBL2380981 | — | — | 1 | 6.24 |
| CHEMBL2380977 | — | — | 1 | 6.15 |
| CHEMBL2380982 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL196468 | — | IC50 | = | 0.56 | nM | 9.25 |
| CHEMBL539470 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL2380980 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL2380975 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL2380983 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL2380971 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL2380972 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL2380979 | — | IC50 | = | 97.0 | nM | 7.01 |
| CHEMBL2380974 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL2380976 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL2380978 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL2380973 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL2380981 | — | IC50 | = | 570.0 | nM | 6.24 |
| CHEMBL2380977 | — | IC50 | = | 710.0 | nM | 6.15 |
| CHEMBL2380982 | — | IC50 | > | 1000.0 | nM | - |