Assay Detail
Binding
CHEMBL5137234
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-nisoxetine from NET in Sprague-Dawley rat brain prefrontal cortex incubated for 180 mins by radioligand binding assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Illuminating the norepinephrine transporter: fluorescent probes based on nisoxetine and talopram.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 6 | 7.91 | 8.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL295467 | NISOXETINE | 2.0 | 1 | 8.82 |
| CHEMBL299233 | TALOPRAM | 2.0 | 1 | 8.35 |
| CHEMBL5188712 | — | — | 1 | 7.37 |
| CHEMBL196760 | — | — | 1 | 7.10 |
| CHEMBL5170876 | — | — | 1 | - |
| CHEMBL5176356 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL295467 | NISOXETINE | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL299233 | TALOPRAM | Ki | = | 4.5 | nM | 8.35 |
| CHEMBL5188712 | — | Ki | = | 43.0 | nM | 7.37 |
| CHEMBL196760 | — | Ki | = | 79.0 | nM | 7.10 |
| CHEMBL5170876 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL5176356 | — | Ki | > | 10000.0 | nM | - |