Assay Detail
Binding
CHEMBL911774
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Displacement of [3H]citalopram from SERT 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 |
Target
Sodium-dependent serotonin transporter (CHEMBL313) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
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 | 5.87 | 6.54 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL370805 | COCAINE | 4.0 | 1 | 6.54 |
| CHEMBL386064 | — | — | 1 | 6.28 |
| CHEMBL413927 | — | — | 1 | 6.24 |
| CHEMBL310650 | — | — | 1 | 6.16 |
| CHEMBL217295 | — | — | 1 | 6.04 |
| CHEMBL384482 | — | — | 1 | 5.97 |
| CHEMBL217160 | — | — | 1 | 5.86 |
| CHEMBL217022 | — | — | 1 | 5.81 |
| CHEMBL3084884 | — | — | 1 | 5.79 |
| CHEMBL214234 | — | — | 1 | 5.75 |
| CHEMBL317362 | — | — | 1 | 5.73 |
| CHEMBL214923 | — | — | 1 | 5.67 |
| CHEMBL384104 | — | — | 1 | 5.64 |
| CHEMBL217456 | — | — | 1 | 5.60 |
| CHEMBL317757 | DIFLUOROBENZTROPINE | — | 1 | 5.49 |
| CHEMBL214574 | — | — | 1 | 5.42 |
| CHEMBL217018 | — | — | 1 | - |
| CHEMBL216990 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL370805 | COCAINE | Ki | = | 286.0 | nM | 6.54 |
| CHEMBL386064 | — | Ki | = | 528.0 | nM | 6.28 |
| CHEMBL413927 | — | Ki | = | 572.0 | nM | 6.24 |
| CHEMBL310650 | — | Ki | = | 690.0 | nM | 6.16 |
| CHEMBL217295 | — | Ki | = | 910.0 | nM | 6.04 |
| CHEMBL384482 | — | Ki | = | 1070.0 | nM | 5.97 |
| CHEMBL217160 | — | Ki | = | 1390.0 | nM | 5.86 |
| CHEMBL217022 | — | Ki | = | 1560.0 | nM | 5.81 |
| CHEMBL3084884 | — | Ki | = | 1640.0 | nM | 5.79 |
| CHEMBL214234 | — | Ki | = | 1790.0 | nM | 5.75 |
| CHEMBL317362 | — | Ki | = | 1850.0 | nM | 5.73 |
| CHEMBL214923 | — | Ki | = | 2150.0 | nM | 5.67 |
| CHEMBL384104 | — | Ki | = | 2280.0 | nM | 5.64 |
| CHEMBL217456 | — | Ki | = | 2500.0 | nM | 5.60 |
| CHEMBL317757 | DIFLUOROBENZTROPINE | Ki | = | 3260.0 | nM | 5.49 |
| CHEMBL214574 | — | Ki | = | 3780.0 | nM | 5.42 |
| CHEMBL217018 | — | Ki | - | — | - | |
| CHEMBL216990 | — | Ki | - | — | - |