Assay Detail
Binding
CHEMBL4233797
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human NET expressed in HEK293 cells assessed as reduction in [3H]-NE uptake by micro beta scintillation counting analysis
29
Total Activities
29
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
Design, synthesis and docking study of 4-arylpiperazine carboxamides as monoamine neurotransmitters reuptake inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 29 | 5.62 | 6.58 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4245867 | — | — | 1 | 6.58 |
| CHEMBL4243862 | — | — | 1 | 5.87 |
| CHEMBL1201066 | VENLAFAXINE HYDROCHLORIDE | 4.0 | 1 | 5.59 |
| CHEMBL4251399 | — | — | 1 | 5.59 |
| CHEMBL4239115 | — | — | 1 | 5.57 |
| CHEMBL4248022 | — | — | 1 | 5.50 |
| CHEMBL894 | BUPROPION | 4.0 | 1 | 5.49 |
| CHEMBL4237635 | — | — | 1 | 5.44 |
| CHEMBL4248596 | — | — | 1 | 5.30 |
| CHEMBL4250965 | — | — | 1 | 5.22 |
| CHEMBL4237546 | — | — | 1 | - |
| CHEMBL4247560 | — | — | 1 | - |
| CHEMBL4248092 | — | — | 1 | - |
| CHEMBL4240083 | — | — | 1 | - |
| CHEMBL4244291 | — | — | 1 | - |
| CHEMBL4247932 | — | — | 1 | - |
| CHEMBL4243712 | — | — | 1 | - |
| CHEMBL4246682 | — | — | 1 | - |
| CHEMBL4242062 | — | — | 1 | - |
| CHEMBL4250502 | — | — | 1 | - |
| CHEMBL4243340 | — | — | 1 | - |
| CHEMBL4237912 | — | — | 1 | - |
| CHEMBL4238362 | — | — | 1 | - |
| CHEMBL4247254 | — | — | 1 | - |
| CHEMBL4249668 | — | — | 1 | - |
| CHEMBL4240379 | — | — | 1 | - |
| CHEMBL4241632 | — | — | 1 | - |
| CHEMBL4237739 | — | — | 1 | - |
| CHEMBL4245408 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4245867 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL4243862 | — | IC50 | = | 1340.0 | nM | 5.87 |
| CHEMBL1201066 | VENLAFAXINE HYDROCHLORIDE | IC50 | = | 2550.0 | nM | 5.59 |
| CHEMBL4251399 | — | IC50 | = | 2550.0 | nM | 5.59 |
| CHEMBL4239115 | — | IC50 | = | 2690.0 | nM | 5.57 |
| CHEMBL4248022 | — | IC50 | = | 3150.0 | nM | 5.50 |
| CHEMBL894 | BUPROPION | IC50 | = | 3240.0 | nM | 5.49 |
| CHEMBL4237635 | — | IC50 | = | 3660.0 | nM | 5.44 |
| CHEMBL4248596 | — | IC50 | = | 4960.0 | nM | 5.30 |
| CHEMBL4250965 | — | IC50 | = | 6070.0 | nM | 5.22 |
| CHEMBL4237546 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4247560 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4248092 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4240083 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4244291 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4247932 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4243712 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4246682 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4242062 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4250502 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4243340 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4237912 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4238362 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4247254 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4249668 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4240379 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4241632 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4237739 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4245408 | — | IC50 | > | 10000.0 | nM | - |