Assay Detail
Functional
CHEMBL831084
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Concentration required to inhibit [3H]DA (dopamine) uptake into rat striatal synaptosomes
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Subcellular | Synaptosomes |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Sodium-dependent dopamine transporter (CHEMBL338) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Further structurally constrained analogues of cis-(6-benzhydrylpiperidin-3-yl)benzylamine with elucidation of bioactive conformation: discovery of 1,4-diazabicyclo[3.3.1]nonane derivatives and evaluation of their biological properties for the monoamine transporters.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 7.20 | 8.18 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL543876 | — | — | 1 | 8.18 |
| CHEMBL189082 | — | — | 1 | 8.04 |
| CHEMBL408192 | — | — | 1 | 7.74 |
| CHEMBL188363 | — | — | 1 | 7.39 |
| CHEMBL39262 | — | — | 1 | 7.30 |
| CHEMBL40607 | — | — | 1 | 7.27 |
| CHEMBL189084 | — | — | 1 | 7.25 |
| CHEMBL280518 | — | — | 1 | 7.24 |
| CHEMBL189805 | — | — | 1 | 6.86 |
| CHEMBL2096807 | — | — | 1 | 6.57 |
| CHEMBL364561 | — | — | 1 | 6.45 |
| CHEMBL189713 | — | — | 1 | 6.09 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL543876 | — | IC50 | = | 6.63 | nM | 8.18 |
| CHEMBL189082 | — | IC50 | = | 9.1 | nM | 8.04 |
| CHEMBL408192 | — | IC50 | = | 18.4 | nM | 7.74 |
| CHEMBL188363 | — | IC50 | = | 40.5 | nM | 7.39 |
| CHEMBL39262 | — | IC50 | = | 49.6 | nM | 7.30 |
| CHEMBL40607 | — | IC50 | = | 53.8 | nM | 7.27 |
| CHEMBL189084 | — | IC50 | = | 56.9 | nM | 7.25 |
| CHEMBL280518 | — | IC50 | = | 57.2 | nM | 7.24 |
| CHEMBL189805 | — | IC50 | = | 138.0 | nM | 6.86 |
| CHEMBL2096807 | — | IC50 | = | 269.0 | nM | 6.57 |
| CHEMBL364561 | — | IC50 | = | 357.0 | nM | 6.45 |
| CHEMBL189713 | — | IC50 | = | 809.0 | nM | 6.09 |