Assay Detail
Binding
CHEMBL1043355
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of norepinephrine reuptake at NET
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Sodium-dependent noradrenaline transporter (CHEMBL222) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Dual acting norepinephrine reuptake inhibitors and 5-HT(2A) receptor antagonists: Identification, synthesis and activity of novel 4-aminoethyl-3-(phenylsulfonyl)-1H-indoles.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 5 | 8.59 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL180101 | ESREBOXETINE | 3.0 | 1 | 9.52 |
| CHEMBL72 | DESIPRAMINE | 4.0 | 1 | 9.22 |
| CHEMBL295467 | NISOXETINE | 2.0 | 1 | 8.22 |
| CHEMBL609883 | — | — | 1 | 8.05 |
| CHEMBL21731 | MAPROTILINE | 4.0 | 1 | 7.92 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL180101 | ESREBOXETINE | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL72 | DESIPRAMINE | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL295467 | NISOXETINE | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL609883 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL21731 | MAPROTILINE | Ki | = | 12.0 | nM | 7.92 |