Assay Detail
Binding
CHEMBL1020452
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]nisoxetine from human NET receptor expressed in HEK293 cells
6
Total Activities
6
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
Synthesis, radiosynthesis, and biological evaluation of carbon-11 and fluorine-18 labeled reboxetine analogues: potential positron emission tomography radioligands for in vivo imaging of the norepinephrine transporter.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 6 | 8.91 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL179249 | — | — | 1 | 9.52 |
| CHEMBL223166 | — | — | 1 | 9.02 |
| CHEMBL467432 | — | — | 1 | 8.99 |
| CHEMBL180101 | ESREBOXETINE | 3.0 | 1 | 8.98 |
| CHEMBL466187 | — | — | 1 | 8.50 |
| CHEMBL505592 | — | — | 1 | 8.43 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL179249 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL223166 | — | Ki | = | 0.95 | nM | 9.02 |
| CHEMBL467432 | — | Ki | = | 1.02 | nM | 8.99 |
| CHEMBL180101 | ESREBOXETINE | Ki | = | 1.04 | nM | 8.98 |
| CHEMBL466187 | — | Ki | = | 3.14 | nM | 8.50 |
| CHEMBL505592 | — | Ki | = | 3.68 | nM | 8.43 |