Assay Detail
Functional
CHEMBL674127
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In vitro inhibition of DA 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 dopamine transporter (CHEMBL238) ↗| 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 | 6.93 | 7.55 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL322067 | — | — | 1 | 7.55 |
| CHEMBL326466 | — | — | 1 | 7.12 |
| CHEMBL111128 | — | — | 1 | 7.07 |
| CHEMBL331799 | — | — | 1 | 7.06 |
| CHEMBL109517 | — | — | 1 | 7.03 |
| CHEMBL109571 | — | — | 1 | 7.02 |
| CHEMBL113136 | — | — | 1 | 6.78 |
| CHEMBL323447 | — | — | 1 | 5.82 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL322067 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL326466 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL111128 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL331799 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL109517 | — | IC50 | = | 93.0 | nM | 7.03 |
| CHEMBL109571 | — | IC50 | = | 95.0 | nM | 7.02 |
| CHEMBL113136 | — | IC50 | = | 165.0 | nM | 6.78 |
| CHEMBL323447 | — | IC50 | = | 1514.0 | nM | 5.82 |