Assay Detail
Binding
CHEMBL3379356
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]Nisoxetine from human NET 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 noradrenaline transporter (CHEMBL222) ↗| 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 | 7.65 | 8.89 |
| Ki | 2 | 7.30 | 8.12 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3323173 | — | — | 1 | 8.89 |
| CHEMBL3323089 | — | — | 1 | 8.59 |
| CHEMBL3323178 | — | — | 1 | 8.54 |
| CHEMBL3323174 | — | — | 1 | 8.30 |
| CHEMBL3323090 | — | — | 1 | 8.28 |
| CHEMBL3323175 | — | — | 1 | 8.26 |
| CHEMBL3323101 | — | — | 1 | 8.22 |
| CHEMBL3323088 | — | — | 1 | 8.12 |
| CHEMBL3323096 | — | — | 1 | 8.00 |
| CHEMBL3323092 | — | — | 1 | 7.82 |
| CHEMBL3323093 | — | — | 1 | 7.66 |
| CHEMBL3323183 | — | — | 1 | 7.64 |
| CHEMBL3323099 | — | — | 1 | 7.28 |
| CHEMBL3323094 | — | — | 1 | 7.16 |
| CHEMBL3323185 | — | — | 1 | 6.96 |
| CHEMBL3323097 | — | — | 1 | 6.89 |
| CHEMBL796 | METHYLPHENIDATE | 4.0 | 1 | 6.47 |
| CHEMBL3323095 | — | — | 1 | 6.46 |
| CHEMBL3323187 | — | — | 1 | 5.04 |
| CHEMBL3323091 | — | — | 1 | - |
| CHEMBL3323179 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3323173 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL3323089 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL3323178 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL3323174 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3323090 | — | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL3323175 | — | IC50 | = | 5.5 | nM | 8.26 |
| CHEMBL3323101 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3323088 | — | Ki | = | 7.6 | nM | 8.12 |
| CHEMBL3323096 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3323092 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3323093 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL3323183 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL3323099 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL3323094 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL3323185 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL3323097 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL796 | METHYLPHENIDATE | Ki | = | 340.0 | nM | 6.47 |
| CHEMBL3323095 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL3323187 | — | IC50 | = | 9100.0 | nM | 5.04 |
| CHEMBL3323091 | — | IC50 | < | 1.0 | nM | - |
| CHEMBL3323179 | — | IC50 | < | 3.0 | nM | - |