Assay Detail
Binding
CHEMBL805337
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity at serotonin transporter in rat brain by [3H]-citalopram displacement.
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Sodium-dependent serotonin transporter (CHEMBL313) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
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 | 17 | 5.81 | 6.54 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL370805 | COCAINE | 4.0 | 1 | 6.54 |
| CHEMBL2308105 | — | — | 1 | 6.42 |
| CHEMBL115370 | — | — | 1 | 6.30 |
| CHEMBL115311 | — | — | 1 | 6.26 |
| CHEMBL326604 | — | — | 1 | 6.25 |
| CHEMBL112528 | — | — | 1 | 6.24 |
| CHEMBL115253 | — | — | 1 | 6.22 |
| CHEMBL324518 | — | — | 1 | 5.96 |
| CHEMBL325826 | — | — | 1 | 5.89 |
| CHEMBL3085020 | — | — | 1 | 5.83 |
| CHEMBL3084884 | — | — | 1 | 5.79 |
| CHEMBL327055 | — | — | 1 | 5.68 |
| CHEMBL317757 | DIFLUOROBENZTROPINE | — | 1 | 5.49 |
| CHEMBL3085021 | — | — | 1 | 5.34 |
| CHEMBL111928 | — | — | 1 | 5.11 |
| CHEMBL326706 | — | — | 1 | 4.84 |
| CHEMBL115710 | — | — | 1 | 4.64 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL370805 | COCAINE | Ki | = | 286.0 | nM | 6.54 |
| CHEMBL2308105 | — | Ki | = | 376.0 | nM | 6.42 |
| CHEMBL115370 | — | Ki | = | 499.0 | nM | 6.30 |
| CHEMBL115311 | — | Ki | = | 555.0 | nM | 6.26 |
| CHEMBL326604 | — | Ki | = | 558.0 | nM | 6.25 |
| CHEMBL112528 | — | Ki | = | 572.0 | nM | 6.24 |
| CHEMBL115253 | — | Ki | = | 597.0 | nM | 6.22 |
| CHEMBL324518 | — | Ki | = | 1090.0 | nM | 5.96 |
| CHEMBL325826 | — | Ki | = | 1300.0 | nM | 5.89 |
| CHEMBL3085020 | — | Ki | = | 1490.0 | nM | 5.83 |
| CHEMBL3084884 | — | Ki | = | 1640.0 | nM | 5.79 |
| CHEMBL327055 | — | Ki | = | 2090.0 | nM | 5.68 |
| CHEMBL317757 | DIFLUOROBENZTROPINE | Ki | = | 3260.0 | nM | 5.49 |
| CHEMBL3085021 | — | Ki | = | 4600.0 | nM | 5.34 |
| CHEMBL111928 | — | Ki | = | 7730.0 | nM | 5.11 |
| CHEMBL326706 | — | Ki | = | 14300.0 | nM | 4.84 |
| CHEMBL115710 | — | Ki | = | 23000.0 | nM | 4.64 |