Assay Detail
Binding
CHEMBL675898
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Inhibition of binding of [3H]WIN-35 428 to (DAT) dopamine transporter in rat striatum
9
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Striatum |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Sodium-dependent dopamine transporter (CHEMBL338) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Design, synthesis, and activity of novel cis- and trans-3,6-disubstituted pyran biomimetics of 3,6-disubstituted piperidine as potential ligands for the dopamine transporter.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 7.20 | 7.97 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL281594 | VANOXERINE | 3.0 | 1 | 7.97 |
| CHEMBL39262 | — | — | 1 | 7.71 |
| CHEMBL40607 | — | — | 1 | 7.49 |
| CHEMBL288128 | — | — | 1 | 7.42 |
| CHEMBL39259 | — | — | 1 | 7.28 |
| CHEMBL289028 | — | — | 1 | 7.08 |
| CHEMBL41558 | — | — | 2 | 6.79 |
| CHEMBL370805 | COCAINE | 4.0 | 1 | 6.58 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL281594 | VANOXERINE | IC50 | = | 10.6 | nM | 7.97 |
| CHEMBL39262 | — | IC50 | = | 19.7 | nM | 7.71 |
| CHEMBL40607 | — | IC50 | = | 32.5 | nM | 7.49 |
| CHEMBL288128 | — | IC50 | = | 38.3 | nM | 7.42 |
| CHEMBL39259 | — | IC50 | = | 52.6 | nM | 7.28 |
| CHEMBL289028 | — | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL41558 | — | IC50 | = | 163.0 | nM | 6.79 |
| CHEMBL370805 | COCAINE | IC50 | = | 266.0 | nM | 6.58 |
| CHEMBL41558 | — | IC50 | = | 313.0 | nM | 6.50 |