Assay Detail
Binding
CHEMBL754232
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Ability to displace [3H]-nisoxatine radioligand for the Norepinephrine transporter in rat brain
9
Total Activities
5
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
Enantioselective synthesis of S-(+)-2beta-carboalkoxy-3alpha-[bis(4-fluorophenyl)methoxy]tropanes as novel probes for the dopamine transporter.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 9 | 6.02 | 6.57 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL21859 | — | — | 2 | 6.57 |
| CHEMBL317757 | DIFLUOROBENZTROPINE | — | 1 | 6.21 |
| CHEMBL281388 | — | — | 2 | 6.20 |
| CHEMBL428704 | — | — | 2 | 6.19 |
| CHEMBL283154 | — | — | 2 | 5.65 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL21859 | — | Ki | = | 269.0 | nM | 6.57 |
| CHEMBL21859 | — | Ki | = | 474.0 | nM | 6.32 |
| CHEMBL317757 | DIFLUOROBENZTROPINE | Ki | = | 610.0 | nM | 6.21 |
| CHEMBL281388 | — | Ki | = | 629.0 | nM | 6.20 |
| CHEMBL428704 | — | Ki | = | 642.0 | nM | 6.19 |
| CHEMBL281388 | — | Ki | = | 1020.0 | nM | 5.99 |
| CHEMBL428704 | — | Ki | = | 1990.0 | nM | 5.70 |
| CHEMBL283154 | — | Ki | = | 2230.0 | nM | 5.65 |
| CHEMBL283154 | — | Ki | = | 4110.0 | nM | 5.39 |