Assay Detail
Binding
CHEMBL1008806
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Displacement of [3H]nisoxetine from NET in rat frontal cortex membrane
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Frontal cortex |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
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 | 5.82 | 6.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL281594 | VANOXERINE | 3.0 | 1 | 6.30 |
| CHEMBL495519 | — | — | 1 | 6.12 |
| CHEMBL489601 | — | — | 1 | 6.09 |
| CHEMBL498600 | — | — | 1 | 6.00 |
| CHEMBL495726 | — | — | 1 | 5.98 |
| CHEMBL314424 | — | — | 1 | 5.90 |
| CHEMBL490424 | — | — | 1 | 5.87 |
| CHEMBL497586 | — | — | 1 | 5.82 |
| CHEMBL502790 | — | — | 1 | 5.82 |
| CHEMBL507255 | — | — | 1 | 5.78 |
| CHEMBL496753 | — | — | 1 | 5.71 |
| CHEMBL495520 | — | — | 1 | 5.68 |
| CHEMBL505059 | — | — | 1 | 5.56 |
| CHEMBL487088 | — | — | 1 | 5.46 |
| CHEMBL443649 | — | — | 1 | 5.27 |
| CHEMBL444690 | — | — | 1 | - |
| CHEMBL521582 | — | — | 1 | - |
| CHEMBL60542 | (+)-PENTAZOCINE | — | 1 | - |
| CHEMBL560 | — | — | 1 | - |
| CHEMBL275707 | RIMCAZOLE | 2.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL281594 | VANOXERINE | Ki | = | 497.0 | nM | 6.30 |
| CHEMBL495519 | — | Ki | = | 766.0 | nM | 6.12 |
| CHEMBL489601 | — | Ki | = | 810.0 | nM | 6.09 |
| CHEMBL498600 | — | Ki | = | 990.0 | nM | 6.00 |
| CHEMBL495726 | — | Ki | = | 1050.0 | nM | 5.98 |
| CHEMBL314424 | — | Ki | = | 1250.0 | nM | 5.90 |
| CHEMBL490424 | — | Ki | = | 1360.0 | nM | 5.87 |
| CHEMBL497586 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL502790 | — | Ki | = | 1520.0 | nM | 5.82 |
| CHEMBL507255 | — | Ki | = | 1680.0 | nM | 5.78 |
| CHEMBL496753 | — | Ki | = | 1950.0 | nM | 5.71 |
| CHEMBL495520 | — | Ki | = | 2110.0 | nM | 5.68 |
| CHEMBL505059 | — | Ki | = | 2740.0 | nM | 5.56 |
| CHEMBL487088 | — | Ki | = | 3460.0 | nM | 5.46 |
| CHEMBL443649 | — | Ki | = | 5350.0 | nM | 5.27 |
| CHEMBL444690 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL521582 | — | Ki | - | — | - | |
| CHEMBL60542 | (+)-PENTAZOCINE | Ki | - | — | - | |
| CHEMBL560 | — | Ki | - | — | - | |
| CHEMBL275707 | RIMCAZOLE | Ki | - | — | - |