Assay Detail
Functional
CHEMBL782600
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of DAT uptake was determined by measuring the [3H]DA accumulation in rat striatal synaptosomes
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Subcellular | Synaptosomes |
| Confidence | 1 — Organism |
| Curated By | Intermediate |
Publication
Interaction of cis-(6-benzhydrylpiperidin-3-yl)benzylamine analogues with monoamine transporters: structure-activity relationship study of structurally constrained 3,6-disubstituted piperidine analogues of (2,2-diphenylethyl)-[1-(4-fluorobenzyl)piperidin-4-ylmethyl]amine.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 7.37 | 8.18 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL281594 | VANOXERINE | 3.0 | 1 | 8.18 |
| CHEMBL2114063 | — | — | 1 | 8.04 |
| CHEMBL2111541 | — | — | 1 | 7.52 |
| CHEMBL2112227 | — | — | 1 | 7.39 |
| CHEMBL40607 | — | — | 1 | 7.34 |
| CHEMBL39262 | — | — | 1 | 7.30 |
| CHEMBL2112229 | — | — | 1 | 7.29 |
| CHEMBL3216629 | — | — | 1 | 7.27 |
| CHEMBL2112228 | — | — | 1 | 7.11 |
| CHEMBL3215982 | — | — | 1 | 6.85 |
| CHEMBL2112224 | — | — | 1 | 6.82 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL281594 | VANOXERINE | IC50 | = | 6.63 | nM | 8.18 |
| CHEMBL2114063 | — | IC50 | = | 9.1 | nM | 8.04 |
| CHEMBL2111541 | — | IC50 | = | 30.2 | nM | 7.52 |
| CHEMBL2112227 | — | IC50 | = | 40.5 | nM | 7.39 |
| CHEMBL40607 | — | IC50 | = | 45.7 | nM | 7.34 |
| CHEMBL39262 | — | IC50 | = | 49.6 | nM | 7.30 |
| CHEMBL2112229 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL3216629 | — | IC50 | = | 53.8 | nM | 7.27 |
| CHEMBL2112228 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL3215982 | — | IC50 | = | 142.0 | nM | 6.85 |
| CHEMBL2112224 | — | IC50 | = | 152.0 | nM | 6.82 |