Assay Detail
Binding
CHEMBL670598
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Binding affinity at the dopamine transporter in rast striatum by [3H]WIN-35428 displacement.
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Striatum |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Sodium-dependent dopamine transporter (CHEMBL338) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
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 | 18 | 7.09 | 7.97 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL281594 | VANOXERINE | 3.0 | 1 | 7.97 |
| CHEMBL2114063 | — | — | 1 | 7.95 |
| CHEMBL39262 | — | — | 1 | 7.71 |
| CHEMBL2111541 | — | — | 1 | 7.50 |
| CHEMBL40607 | — | — | 1 | 7.49 |
| CHEMBL3216629 | — | — | 1 | 7.47 |
| CHEMBL2112227 | — | — | 1 | 7.32 |
| CHEMBL2112228 | — | — | 1 | 7.20 |
| CHEMBL2112226 | — | — | 1 | 7.18 |
| CHEMBL2112229 | — | — | 1 | 7.02 |
| CHEMBL2112224 | — | — | 1 | 6.96 |
| CHEMBL2448150 | — | — | 1 | 6.94 |
| CHEMBL3216400 | — | — | 1 | 6.76 |
| CHEMBL3215982 | — | — | 1 | 6.64 |
| CHEMBL370805 | COCAINE | 4.0 | 1 | 6.58 |
| CHEMBL2448152 | — | — | 1 | 6.57 |
| CHEMBL2448151 | — | — | 1 | 6.29 |
| CHEMBL2112225 | — | — | 1 | 6.08 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL281594 | VANOXERINE | IC50 | = | 10.6 | nM | 7.97 |
| CHEMBL2114063 | — | IC50 | = | 11.3 | nM | 7.95 |
| CHEMBL39262 | — | IC50 | = | 19.7 | nM | 7.71 |
| CHEMBL2111541 | — | IC50 | = | 31.5 | nM | 7.50 |
| CHEMBL40607 | — | IC50 | = | 32.5 | nM | 7.49 |
| CHEMBL3216629 | — | IC50 | = | 33.8 | nM | 7.47 |
| CHEMBL2112227 | — | IC50 | = | 47.5 | nM | 7.32 |
| CHEMBL2112228 | — | IC50 | = | 63.5 | nM | 7.20 |
| CHEMBL2112226 | — | IC50 | = | 65.9 | nM | 7.18 |
| CHEMBL2112229 | — | IC50 | = | 95.4 | nM | 7.02 |
| CHEMBL2112224 | — | IC50 | = | 109.0 | nM | 6.96 |
| CHEMBL2448150 | — | IC50 | = | 114.0 | nM | 6.94 |
| CHEMBL3216400 | — | IC50 | = | 173.0 | nM | 6.76 |
| CHEMBL3215982 | — | IC50 | = | 229.0 | nM | 6.64 |
| CHEMBL370805 | COCAINE | IC50 | = | 266.0 | nM | 6.58 |
| CHEMBL2448152 | — | IC50 | = | 267.0 | nM | 6.57 |
| CHEMBL2448151 | — | IC50 | = | 515.0 | nM | 6.29 |
| CHEMBL2112225 | — | IC50 | = | 834.0 | nM | 6.08 |