Assay Detail
Binding
CHEMBL922846
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Inhibition of [3H]NE uptake in NET in rat cerebral cortex
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Cerebral cortex |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Further structural optimization of cis-(6-benzhydryl-piperidin-3-yl)-benzylamine and 1,4-diazabicyclo[3.3.1]nonane derivatives by introducing an exocyclic hydroxyl group: interaction with dopamine, serotonin, and norepinephrine transporters.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 13 | 6.51 | 8.44 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL258724 | — | — | 1 | 8.44 |
| CHEMBL281594 | VANOXERINE | 3.0 | 1 | 6.99 |
| CHEMBL258725 | — | — | 1 | 6.77 |
| CHEMBL258511 | — | — | 1 | 6.64 |
| CHEMBL410244 | — | — | 1 | 6.59 |
| CHEMBL408950 | — | — | 1 | 6.50 |
| CHEMBL263636 | — | — | 1 | 6.41 |
| CHEMBL260682 | — | — | 1 | 6.38 |
| CHEMBL265454 | — | — | 1 | 6.14 |
| CHEMBL260151 | — | — | 1 | 6.14 |
| CHEMBL409881 | — | — | 1 | 6.02 |
| CHEMBL261736 | — | — | 1 | 5.84 |
| CHEMBL412263 | — | — | 1 | 5.76 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL258724 | — | Ki | = | 3.6 | nM | 8.44 |
| CHEMBL281594 | VANOXERINE | Ki | = | 102.0 | nM | 6.99 |
| CHEMBL258725 | — | Ki | = | 170.0 | nM | 6.77 |
| CHEMBL258511 | — | Ki | = | 231.0 | nM | 6.64 |
| CHEMBL410244 | — | Ki | = | 259.0 | nM | 6.59 |
| CHEMBL408950 | — | Ki | = | 319.0 | nM | 6.50 |
| CHEMBL263636 | — | Ki | = | 388.0 | nM | 6.41 |
| CHEMBL260682 | — | Ki | = | 418.0 | nM | 6.38 |
| CHEMBL265454 | — | Ki | = | 728.0 | nM | 6.14 |
| CHEMBL260151 | — | Ki | = | 730.0 | nM | 6.14 |
| CHEMBL409881 | — | Ki | = | 954.0 | nM | 6.02 |
| CHEMBL261736 | — | Ki | = | 1435.0 | nM | 5.84 |
| CHEMBL412263 | — | Ki | = | 1730.0 | nM | 5.76 |