Assay Detail
Binding
CHEMBL4380185
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of wild type human NET expressed in HEK293 cells assessed as inhibition of [3H]-MPP+ reuptake preincubated for 5 mins followed by [3H]MPP+ addition and measured after 3 mins by liquid scintillation counting analysis
69
Total Activities
67
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 noradrenaline transporter (CHEMBL222) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Structure-Activity Relationships of Novel Thiazole-Based Modafinil Analogues Acting at Monoamine Transporters.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 69 | 4.26 | 4.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4438894 | — | — | 1 | 4.64 |
| CHEMBL4464187 | — | — | 1 | 4.44 |
| CHEMBL4459947 | — | — | 1 | 4.41 |
| CHEMBL4568351 | — | — | 1 | 4.34 |
| CHEMBL4473574 | — | — | 1 | 4.28 |
| CHEMBL4543324 | — | — | 1 | 4.17 |
| CHEMBL4456526 | — | — | 1 | 4.17 |
| CHEMBL4469951 | — | — | 1 | 4.14 |
| CHEMBL4465494 | — | — | 1 | 4.13 |
| CHEMBL4473522 | — | — | 1 | 4.07 |
| CHEMBL4455184 | — | — | 1 | 4.05 |
| CHEMBL4536039 | — | — | 1 | - |
| CHEMBL4437734 | — | — | 1 | - |
| CHEMBL4453638 | — | — | 1 | - |
| CHEMBL4439598 | — | — | 1 | - |
| CHEMBL4541596 | — | — | 1 | - |
| CHEMBL4579575 | — | — | 1 | - |
| CHEMBL4593487 | — | — | 1 | - |
| CHEMBL4466697 | — | — | 1 | - |
| CHEMBL4437004 | — | — | 1 | - |
| CHEMBL4562715 | — | — | 1 | - |
| CHEMBL4443822 | — | — | 1 | - |
| CHEMBL4539793 | — | — | 1 | - |
| CHEMBL4583781 | — | — | 1 | - |
| CHEMBL4441345 | — | — | 1 | - |
| CHEMBL4569016 | — | — | 1 | - |
| CHEMBL4459806 | — | — | 1 | - |
| CHEMBL4475690 | — | — | 1 | - |
| CHEMBL4436791 | — | — | 1 | - |
| CHEMBL4454714 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4438894 | — | IC50 | = | 22700.0 | nM | 4.64 |
| CHEMBL4464187 | — | IC50 | = | 36500.0 | nM | 4.44 |
| CHEMBL4459947 | — | IC50 | = | 38600.0 | nM | 4.41 |
| CHEMBL4568351 | — | IC50 | = | 45490.0 | nM | 4.34 |
| CHEMBL4473574 | — | IC50 | = | 52560.0 | nM | 4.28 |
| CHEMBL4543324 | — | IC50 | = | 67800.0 | nM | 4.17 |
| CHEMBL4456526 | — | IC50 | = | 68200.0 | nM | 4.17 |
| CHEMBL4469951 | — | IC50 | = | 72000.0 | nM | 4.14 |
| CHEMBL4465494 | — | IC50 | = | 73250.0 | nM | 4.13 |
| CHEMBL4473522 | — | IC50 | = | 85000.0 | nM | 4.07 |
| CHEMBL4455184 | — | IC50 | = | 89800.0 | nM | 4.05 |
| CHEMBL4517473 | — | IC50 | = | 108200.0 | nM | - |
| CHEMBL4587340 | — | IC50 | - | — | - | |
| CHEMBL4593487 | — | IC50 | = | 109100.0 | nM | - |
| CHEMBL4588349 | — | IC50 | - | — | - | |
| CHEMBL4536039 | — | IC50 | - | — | - | |
| CHEMBL4437734 | — | IC50 | - | — | - | |
| CHEMBL4453638 | — | IC50 | - | — | - | |
| CHEMBL4439598 | — | IC50 | = | 687200.0 | nM | - |
| CHEMBL4541596 | — | IC50 | = | 107300.0 | nM | - |
| CHEMBL4579575 | — | IC50 | - | — | - | |
| CHEMBL4445285 | — | IC50 | = | 195800.0 | nM | - |
| CHEMBL4439670 | — | IC50 | - | — | - | |
| CHEMBL4461901 | — | IC50 | - | — | - | |
| CHEMBL4444833 | — | IC50 | - | — | - | |
| CHEMBL4444833 | — | IC50 | - | — | - | |
| CHEMBL4542509 | — | IC50 | - | — | - | |
| CHEMBL4542611 | — | IC50 | - | — | - | |
| CHEMBL4464920 | — | IC50 | - | — | - | |
| CHEMBL4449011 | — | IC50 | - | — | - | |
| CHEMBL4443822 | — | IC50 | - | — | - | |
| CHEMBL4436791 | — | IC50 | - | — | - | |
| CHEMBL4466697 | — | IC50 | - | — | - | |
| CHEMBL4454714 | — | IC50 | - | — | - | |
| CHEMBL4475690 | — | IC50 | = | 129800.0 | nM | - |
| CHEMBL4441345 | — | IC50 | - | — | - | |
| CHEMBL4459806 | — | IC50 | - | — | - | |
| CHEMBL4569016 | — | IC50 | = | 110500.0 | nM | - |
| CHEMBL4583781 | — | IC50 | = | 107100.0 | nM | - |
| CHEMBL4539793 | — | IC50 | - | — | - | |
| CHEMBL4458656 | — | IC50 | - | — | - | |
| CHEMBL4562715 | — | IC50 | - | — | - | |
| CHEMBL4437004 | — | IC50 | - | — | - | |
| CHEMBL4437729 | — | IC50 | - | — | - | |
| CHEMBL1201192 | ARMODAFINIL | IC50 | = | 170000.0 | nM | - |
| CHEMBL4455022 | — | IC50 | - | — | - | |
| CHEMBL4470394 | — | IC50 | = | 120800.0 | nM | - |
| CHEMBL4444833 | — | IC50 | = | 215500.0 | nM | - |
| CHEMBL4560378 | — | IC50 | = | 138800.0 | nM | - |
| CHEMBL4446076 | — | IC50 | - | — | - |