Assay Detail
Binding
CHEMBL3595873
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human NET expressed in CHOK1 cells incubated for 45 mins by [3H]-norepinephrine uptake assay
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| 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 biological evaluation of a novel series of peripheral-selective noradrenaline reuptake inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 8.21 | 9.48 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3593400 | — | — | 1 | 9.48 |
| CHEMBL3593399 | — | — | 1 | 9.11 |
| CHEMBL3593395 | — | — | 1 | 8.70 |
| CHEMBL3593274 | — | — | 1 | 8.68 |
| CHEMBL3593402 | — | — | 1 | 8.64 |
| CHEMBL3593404 | — | — | 1 | 8.48 |
| CHEMBL3593405 | — | — | 1 | 8.47 |
| CHEMBL3593392 | — | — | 1 | 8.25 |
| CHEMBL3593401 | — | — | 1 | 8.24 |
| CHEMBL3593396 | — | — | 1 | 8.24 |
| CHEMBL3593394 | — | — | 1 | 8.22 |
| CHEMBL3593393 | — | — | 1 | 8.07 |
| CHEMBL3593398 | — | — | 1 | 7.92 |
| CHEMBL3593403 | — | — | 1 | 7.89 |
| CHEMBL3593275 | — | — | 1 | 7.77 |
| CHEMBL3593397 | — | — | 1 | 7.28 |
| CHEMBL3593391 | — | — | 1 | 6.16 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3593400 | — | IC50 | = | 0.33 | nM | 9.48 |
| CHEMBL3593399 | — | IC50 | = | 0.77 | nM | 9.11 |
| CHEMBL3593395 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3593274 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL3593402 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL3593404 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL3593405 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL3593392 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL3593401 | — | IC50 | = | 5.8 | nM | 8.24 |
| CHEMBL3593396 | — | IC50 | = | 5.8 | nM | 8.24 |
| CHEMBL3593394 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3593393 | — | IC50 | = | 8.5 | nM | 8.07 |
| CHEMBL3593398 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3593403 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3593275 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3593397 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL3593391 | — | IC50 | = | 700.0 | nM | 6.16 |