Assay Detail
Binding
CHEMBL3379355
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Displacement of [3H]WIN 35,428 from human DAT 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 dopamine transporter (CHEMBL238) ↗| 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 | 7.55 | 8.35 |
| Ki | 2 | 7.46 | 7.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3323096 | — | — | 1 | 8.35 |
| CHEMBL3323101 | — | — | 1 | 8.35 |
| CHEMBL3323179 | — | — | 1 | 8.28 |
| CHEMBL3323089 | — | — | 1 | 8.24 |
| CHEMBL3323175 | — | — | 1 | 8.16 |
| CHEMBL3323090 | — | — | 1 | 8.12 |
| CHEMBL3323174 | — | — | 1 | 8.05 |
| CHEMBL3323178 | — | — | 1 | 7.96 |
| CHEMBL3323173 | — | — | 1 | 7.92 |
| CHEMBL3323091 | — | — | 1 | 7.80 |
| CHEMBL796 | METHYLPHENIDATE | 4.0 | 1 | 7.47 |
| CHEMBL3323088 | — | — | 1 | 7.44 |
| CHEMBL3323097 | — | — | 1 | 7.42 |
| CHEMBL3323093 | — | — | 1 | 7.37 |
| CHEMBL3323092 | — | — | 1 | 7.29 |
| CHEMBL3323183 | — | — | 1 | 7.06 |
| CHEMBL3323095 | — | — | 1 | 6.72 |
| CHEMBL3323099 | — | — | 1 | 6.70 |
| CHEMBL3323185 | — | — | 1 | 6.24 |
| CHEMBL3323187 | — | — | 1 | 5.85 |
| CHEMBL3323094 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3323096 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL3323101 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL3323179 | — | IC50 | = | 5.3 | nM | 8.28 |
| CHEMBL3323089 | — | IC50 | = | 5.7 | nM | 8.24 |
| CHEMBL3323175 | — | IC50 | = | 6.9 | nM | 8.16 |
| CHEMBL3323090 | — | IC50 | = | 7.5 | nM | 8.12 |
| CHEMBL3323174 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3323178 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3323173 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3323091 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL796 | METHYLPHENIDATE | Ki | = | 34.0 | nM | 7.47 |
| CHEMBL3323088 | — | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL3323097 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL3323093 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL3323092 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL3323183 | — | IC50 | = | 88.0 | nM | 7.06 |
| CHEMBL3323095 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL3323099 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL3323185 | — | IC50 | = | 570.0 | nM | 6.24 |
| CHEMBL3323187 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL3323094 | — | IC50 | > | 300.0 | nM | - |