Assay Detail
Binding
CHEMBL749359
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Displacement of [3H]nisoxetine from norepinephrine transporter (NET) of rat brain
14
Total Activities
14
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 relationships at monoamine transporters for a series of N-substituted 3alpha-(bis[4-fluorophenyl]methoxy)tropanes: comparative molecular field analysis, synthesis, and pharmacological evaluation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 14 | 5.63 | 6.21 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL317757 | DIFLUOROBENZTROPINE | — | 1 | 6.21 |
| CHEMBL115253 | — | — | 1 | 6.20 |
| CHEMBL112528 | — | — | 1 | 6.19 |
| CHEMBL324518 | — | — | 1 | 5.95 |
| CHEMBL3085021 | — | — | 1 | 5.85 |
| CHEMBL3085020 | — | — | 1 | 5.85 |
| CHEMBL2308105 | — | — | 1 | 5.66 |
| CHEMBL3084884 | — | — | 1 | 5.53 |
| CHEMBL325826 | — | — | 1 | 5.51 |
| CHEMBL370805 | COCAINE | 4.0 | 1 | 5.48 |
| CHEMBL327055 | — | — | 1 | 5.46 |
| CHEMBL326706 | — | — | 1 | 5.44 |
| CHEMBL111928 | — | — | 1 | 4.92 |
| CHEMBL115710 | — | — | 1 | 4.55 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL317757 | DIFLUOROBENZTROPINE | Ki | = | 610.0 | nM | 6.21 |
| CHEMBL115253 | — | Ki | = | 637.0 | nM | 6.20 |
| CHEMBL112528 | — | Ki | = | 652.0 | nM | 6.19 |
| CHEMBL324518 | — | Ki | = | 1130.0 | nM | 5.95 |
| CHEMBL3085021 | — | Ki | = | 1420.0 | nM | 5.85 |
| CHEMBL3085020 | — | Ki | = | 1420.0 | nM | 5.85 |
| CHEMBL2308105 | — | Ki | = | 2210.0 | nM | 5.66 |
| CHEMBL3084884 | — | Ki | = | 2980.0 | nM | 5.53 |
| CHEMBL325826 | — | Ki | = | 3060.0 | nM | 5.51 |
| CHEMBL370805 | COCAINE | Ki | = | 3300.0 | nM | 5.48 |
| CHEMBL327055 | — | Ki | = | 3450.0 | nM | 5.46 |
| CHEMBL326706 | — | Ki | = | 3650.0 | nM | 5.44 |
| CHEMBL111928 | — | Ki | = | 12100.0 | nM | 4.92 |
| CHEMBL115710 | — | Ki | = | 28100.0 | nM | 4.55 |