Assay Detail
Binding
CHEMBL922844
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Inhibition of [3H]dopamine uptake in DAT in rat striatum
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Striatum |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sodium-dependent dopamine transporter (CHEMBL338) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
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 | 15 | 7.27 | 8.06 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL260682 | — | — | 1 | 8.06 |
| CHEMBL261737 | — | — | 1 | 8.04 |
| CHEMBL281594 | VANOXERINE | 3.0 | 1 | 7.97 |
| CHEMBL258725 | — | — | 1 | 7.97 |
| CHEMBL410244 | — | — | 1 | 7.78 |
| CHEMBL408192 | — | — | 1 | 7.74 |
| CHEMBL258511 | — | — | 1 | 7.60 |
| CHEMBL263636 | — | — | 1 | 7.38 |
| CHEMBL408950 | — | — | 1 | 7.18 |
| CHEMBL260151 | — | — | 1 | 7.08 |
| CHEMBL265454 | — | — | 1 | 6.80 |
| CHEMBL409881 | — | — | 1 | 6.69 |
| CHEMBL261736 | — | — | 1 | 6.63 |
| CHEMBL412263 | — | — | 1 | 6.58 |
| CHEMBL258724 | — | — | 1 | 5.51 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL260682 | — | Ki | = | 8.63 | nM | 8.06 |
| CHEMBL261737 | — | Ki | = | 9.1 | nM | 8.04 |
| CHEMBL281594 | VANOXERINE | Ki | = | 10.6 | nM | 7.97 |
| CHEMBL258725 | — | Ki | = | 10.6 | nM | 7.97 |
| CHEMBL410244 | — | Ki | = | 16.8 | nM | 7.78 |
| CHEMBL408192 | — | Ki | = | 18.4 | nM | 7.74 |
| CHEMBL258511 | — | Ki | = | 25.3 | nM | 7.60 |
| CHEMBL263636 | — | Ki | = | 41.8 | nM | 7.38 |
| CHEMBL408950 | — | Ki | = | 66.5 | nM | 7.18 |
| CHEMBL260151 | — | Ki | = | 82.9 | nM | 7.08 |
| CHEMBL265454 | — | Ki | = | 160.0 | nM | 6.80 |
| CHEMBL409881 | — | Ki | = | 204.0 | nM | 6.69 |
| CHEMBL261736 | — | Ki | = | 236.0 | nM | 6.63 |
| CHEMBL412263 | — | Ki | = | 266.0 | nM | 6.58 |
| CHEMBL258724 | — | Ki | = | 3117.0 | nM | 5.51 |