Assay Detail
Binding
CHEMBL1008804
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Displacement of [3H]WIN-35428 from DAT in rat striatum membrane
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Striatum |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sodium-dependent dopamine transporter (CHEMBL338) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Dual DAT/sigma1 receptor ligands based on 3-(4-(3-(bis(4-fluorophenyl)amino)propyl)piperazin-1-yl)-1-phenylpropan-1-ol.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 20 | 7.87 | 8.76 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL495519 | — | — | 1 | 8.76 |
| CHEMBL281594 | VANOXERINE | 3.0 | 1 | 8.75 |
| CHEMBL489601 | — | — | 1 | 8.49 |
| CHEMBL314424 | — | — | 1 | 8.46 |
| CHEMBL498600 | — | — | 1 | 8.37 |
| CHEMBL495520 | — | — | 1 | 8.27 |
| CHEMBL497586 | — | — | 1 | 8.25 |
| CHEMBL496753 | — | — | 1 | 8.17 |
| CHEMBL507255 | — | — | 1 | 8.16 |
| CHEMBL502790 | — | — | 1 | 8.03 |
| CHEMBL505059 | — | — | 1 | 7.83 |
| CHEMBL490424 | — | — | 1 | 7.82 |
| CHEMBL495726 | — | — | 1 | 7.66 |
| CHEMBL487088 | — | — | 1 | 7.47 |
| CHEMBL443649 | — | — | 1 | 7.44 |
| CHEMBL444690 | — | — | 1 | 7.29 |
| CHEMBL275707 | RIMCAZOLE | 2.0 | 1 | 7.01 |
| CHEMBL521582 | — | — | 1 | 5.44 |
| CHEMBL60542 | (+)-PENTAZOCINE | — | 1 | - |
| CHEMBL560 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL495519 | — | Ki | = | 1.72 | nM | 8.76 |
| CHEMBL281594 | VANOXERINE | Ki | = | 1.77 | nM | 8.75 |
| CHEMBL489601 | — | Ki | = | 3.26 | nM | 8.49 |
| CHEMBL314424 | — | Ki | = | 3.45 | nM | 8.46 |
| CHEMBL498600 | — | Ki | = | 4.28 | nM | 8.37 |
| CHEMBL495520 | — | Ki | = | 5.36 | nM | 8.27 |
| CHEMBL497586 | — | Ki | = | 5.57 | nM | 8.25 |
| CHEMBL496753 | — | Ki | = | 6.71 | nM | 8.17 |
| CHEMBL507255 | — | Ki | = | 6.92 | nM | 8.16 |
| CHEMBL502790 | — | Ki | = | 9.36 | nM | 8.03 |
| CHEMBL505059 | — | Ki | = | 14.9 | nM | 7.83 |
| CHEMBL490424 | — | Ki | = | 15.1 | nM | 7.82 |
| CHEMBL495726 | — | Ki | = | 21.7 | nM | 7.66 |
| CHEMBL487088 | — | Ki | = | 33.5 | nM | 7.47 |
| CHEMBL443649 | — | Ki | = | 36.6 | nM | 7.44 |
| CHEMBL444690 | — | Ki | = | 51.3 | nM | 7.29 |
| CHEMBL275707 | RIMCAZOLE | Ki | = | 97.7 | nM | 7.01 |
| CHEMBL521582 | — | Ki | = | 3620.0 | nM | 5.44 |
| CHEMBL60542 | (+)-PENTAZOCINE | Ki | - | — | - | |
| CHEMBL560 | — | Ki | - | — | - |