Assay Detail
Binding
CHEMBL883548
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Displacement of [3H]-Nisoxetine from norepinephrine transporter
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Sodium-dependent noradrenaline transporter (CHEMBL222) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Bicyclo[2.2.1]heptanes as novel triple re-uptake inhibitors for the treatment of depression.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 12 | 6.88 | 7.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL419385 | — | — | 1 | 7.30 |
| CHEMBL113136 | — | — | 1 | 7.29 |
| CHEMBL323678 | — | — | 1 | 7.17 |
| CHEMBL111128 | — | — | 1 | 7.00 |
| CHEMBL109571 | — | — | 1 | 6.96 |
| CHEMBL322348 | — | — | 1 | 6.92 |
| CHEMBL109517 | — | — | 1 | 6.83 |
| CHEMBL326466 | — | — | 1 | 6.82 |
| CHEMBL323447 | — | — | 1 | 6.74 |
| CHEMBL331799 | — | — | 1 | 6.58 |
| CHEMBL432022 | — | — | 1 | 6.50 |
| CHEMBL324269 | — | — | 1 | 6.42 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL419385 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL113136 | — | Ki | = | 51.0 | nM | 7.29 |
| CHEMBL323678 | — | Ki | = | 68.0 | nM | 7.17 |
| CHEMBL111128 | — | Ki | = | 99.0 | nM | 7.00 |
| CHEMBL109571 | — | Ki | = | 111.0 | nM | 6.96 |
| CHEMBL322348 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL109517 | — | Ki | = | 149.0 | nM | 6.83 |
| CHEMBL326466 | — | Ki | = | 152.0 | nM | 6.82 |
| CHEMBL323447 | — | Ki | = | 183.0 | nM | 6.74 |
| CHEMBL331799 | — | Ki | = | 266.0 | nM | 6.58 |
| CHEMBL432022 | — | Ki | = | 316.0 | nM | 6.50 |
| CHEMBL324269 | — | Ki | = | 385.0 | nM | 6.42 |