Assay Detail
Binding
CHEMBL1217136
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]nisoxetine from human NET
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sodium-dependent noradrenaline transporter (CHEMBL222) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis, fluorine-18 radiolabeling, and biological evaluation of N-((E)-4-fluorobut-2-en-1-yl)-2beta-carbomethoxy-3beta-(4'-halophenyl)nortropanes: candidate radioligands for in vivo imaging of the brain dopamine transporter with positron emission tomography.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 9 | 7.00 | 9.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1696 | DESIPRAMINE HYDROCHLORIDE | 4.0 | 1 | 9.10 |
| CHEMBL1214007 | — | — | 1 | 7.06 |
| CHEMBL1214006 | — | — | 1 | 6.85 |
| CHEMBL1214059 | — | — | 1 | 6.84 |
| CHEMBL1214060 | — | — | 1 | 6.58 |
| CHEMBL1214005 | — | — | 1 | 5.58 |
| CHEMBL2079586 | — | — | 1 | - |
| CHEMBL529437 | COCAINE HYDROCHLORIDE | 4.0 | 1 | - |
| CHEMBL1200322 | ESCITALOPRAM OXALATE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1696 | DESIPRAMINE HYDROCHLORIDE | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL1214007 | — | Ki | = | 87.0 | nM | 7.06 |
| CHEMBL1214006 | — | Ki | = | 142.0 | nM | 6.85 |
| CHEMBL1214059 | — | Ki | = | 145.0 | nM | 6.84 |
| CHEMBL1214060 | — | Ki | = | 265.0 | nM | 6.58 |
| CHEMBL1214005 | — | Ki | = | 2607.0 | nM | 5.58 |
| CHEMBL2079586 | — | Ki | - | — | - | |
| CHEMBL529437 | COCAINE HYDROCHLORIDE | Ki | - | — | - | |
| CHEMBL1200322 | ESCITALOPRAM OXALATE | Ki | - | — | - |