Assay Detail
Functional
CHEMBL750497
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In vitro inhibition of [3H]NE re-uptake into synaptosome
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Tissue | Brain |
| Confidence | 8 — Homologous 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 |
|---|---|---|---|
| IC50 | 8 | 7.36 | 7.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL322067 | — | — | 1 | 7.66 |
| CHEMBL326466 | — | — | 1 | 7.60 |
| CHEMBL111128 | — | — | 1 | 7.55 |
| CHEMBL109517 | — | — | 1 | 7.47 |
| CHEMBL113136 | — | — | 1 | 7.36 |
| CHEMBL331799 | — | — | 1 | 7.35 |
| CHEMBL109571 | — | — | 1 | 7.35 |
| CHEMBL323447 | — | — | 1 | 6.53 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL322067 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL326466 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL111128 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL109517 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL113136 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL331799 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL109571 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL323447 | — | IC50 | = | 297.0 | nM | 6.53 |