Assay Detail
Binding
CHEMBL911775
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Displacement of [3H]nisoxetine from NET in Sprague-Dawley rat brain
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Structure-activity relationship studies on a novel series of (S)-2beta-substituted 3alpha-[bis(4-fluoro- or 4-chlorophenyl)methoxy]tropane analogues for in vivo investigation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 18 | 6.05 | 6.57 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL310650 | — | — | 1 | 6.57 |
| CHEMBL413927 | — | — | 1 | 6.57 |
| CHEMBL217160 | — | — | 1 | 6.36 |
| CHEMBL384482 | — | — | 1 | 6.34 |
| CHEMBL214234 | — | — | 1 | 6.33 |
| CHEMBL214923 | — | — | 1 | 6.25 |
| CHEMBL217456 | — | — | 1 | 6.24 |
| CHEMBL317362 | — | — | 1 | 6.20 |
| CHEMBL317757 | DIFLUOROBENZTROPINE | — | 1 | 6.07 |
| CHEMBL384104 | — | — | 1 | 6.03 |
| CHEMBL217295 | — | — | 1 | 6.01 |
| CHEMBL214574 | — | — | 1 | 5.67 |
| CHEMBL386064 | — | — | 1 | 5.67 |
| CHEMBL3084884 | — | — | 1 | 5.53 |
| CHEMBL370805 | COCAINE | 4.0 | 1 | 5.48 |
| CHEMBL217022 | — | — | 1 | 5.47 |
| CHEMBL217018 | — | — | 1 | - |
| CHEMBL216990 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL310650 | — | Ki | = | 269.0 | nM | 6.57 |
| CHEMBL413927 | — | Ki | = | 269.0 | nM | 6.57 |
| CHEMBL217160 | — | Ki | = | 440.0 | nM | 6.36 |
| CHEMBL384482 | — | Ki | = | 454.0 | nM | 6.34 |
| CHEMBL214234 | — | Ki | = | 473.0 | nM | 6.33 |
| CHEMBL214923 | — | Ki | = | 563.0 | nM | 6.25 |
| CHEMBL217456 | — | Ki | = | 580.0 | nM | 6.24 |
| CHEMBL317362 | — | Ki | = | 629.0 | nM | 6.20 |
| CHEMBL317757 | DIFLUOROBENZTROPINE | Ki | = | 844.0 | nM | 6.07 |
| CHEMBL384104 | — | Ki | = | 935.0 | nM | 6.03 |
| CHEMBL217295 | — | Ki | = | 983.0 | nM | 6.01 |
| CHEMBL214574 | — | Ki | = | 2130.0 | nM | 5.67 |
| CHEMBL386064 | — | Ki | = | 2150.0 | nM | 5.67 |
| CHEMBL3084884 | — | Ki | = | 2980.0 | nM | 5.53 |
| CHEMBL370805 | COCAINE | Ki | = | 3300.0 | nM | 5.48 |
| CHEMBL217022 | — | Ki | = | 3350.0 | nM | 5.47 |
| CHEMBL217018 | — | Ki | - | — | - | |
| CHEMBL216990 | — | Ki | - | — | - |