Assay Detail
Binding
CHEMBL918082
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Displacement of [3H]WIN-35428 from DAT in Sprague-Dawley rat striatum
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
Sodium-dependent dopamine transporter (CHEMBL338) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Novel azido and isothiocyanato analogues of [3-(4-phenylalkylpiperazin-1-yl)propyl]bis(4-fluorophenyl)amines as potential irreversible ligands for the dopamine transporter.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 7.22 | 8.25 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL221725 | — | — | 1 | 8.25 |
| CHEMBL330021 | — | — | 1 | 7.71 |
| CHEMBL281594 | VANOXERINE | 3.0 | 1 | 7.68 |
| CHEMBL87841 | — | — | 1 | 7.53 |
| CHEMBL375607 | — | — | 1 | 7.18 |
| CHEMBL222184 | — | — | 1 | 7.17 |
| CHEMBL221767 | — | — | 1 | 7.12 |
| CHEMBL223296 | — | — | 1 | 7.02 |
| CHEMBL374126 | — | — | 1 | 7.00 |
| CHEMBL221506 | — | — | 1 | 6.79 |
| CHEMBL223134 | — | — | 1 | 6.62 |
| CHEMBL221819 | — | — | 1 | 6.55 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL221725 | — | IC50 | = | 5.61 | nM | 8.25 |
| CHEMBL330021 | — | IC50 | = | 19.5 | nM | 7.71 |
| CHEMBL281594 | VANOXERINE | IC50 | = | 21.1 | nM | 7.68 |
| CHEMBL87841 | — | IC50 | = | 29.7 | nM | 7.53 |
| CHEMBL375607 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL222184 | — | IC50 | = | 68.3 | nM | 7.17 |
| CHEMBL221767 | — | IC50 | = | 75.4 | nM | 7.12 |
| CHEMBL223296 | — | IC50 | = | 95.5 | nM | 7.02 |
| CHEMBL374126 | — | IC50 | = | 99.8 | nM | 7.00 |
| CHEMBL221506 | — | IC50 | = | 163.0 | nM | 6.79 |
| CHEMBL223134 | — | IC50 | = | 242.0 | nM | 6.62 |
| CHEMBL221819 | — | IC50 | = | 282.0 | nM | 6.55 |