Assay Detail
Binding
CHEMBL803033
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibitory activity against Serotonin transporter was determined for [3H]5-HT (serotonin) uptake by striated synaptosomes
16
Total Activities
16
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
Synthesis and biological properties of new 2beta-alkyl- and 2beta-aryl-3-(substituted phenyl)tropane derivatives: stereochemical effect of C-3 on affinity and selectivity for neuronal dopamine and serotonin transporters.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 6.98 | 7.95 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL607061 | — | — | 1 | 7.95 |
| CHEMBL607063 | — | — | 1 | 7.78 |
| CHEMBL607112 | — | — | 1 | 7.62 |
| CHEMBL312037 | — | — | 1 | 7.59 |
| CHEMBL148419 | — | — | 1 | 7.26 |
| CHEMBL145888 | — | — | 1 | 7.25 |
| CHEMBL607114 | — | — | 1 | 7.09 |
| CHEMBL607113 | — | — | 1 | 7.02 |
| CHEMBL147787 | — | — | 1 | 6.96 |
| CHEMBL146195 | — | — | 1 | 6.87 |
| CHEMBL370805 | COCAINE | 4.0 | 1 | 6.78 |
| CHEMBL607111 | — | — | 1 | 6.69 |
| CHEMBL421777 | — | — | 1 | 6.50 |
| CHEMBL345026 | — | — | 1 | 6.37 |
| CHEMBL439629 | — | — | 1 | 6.08 |
| CHEMBL607062 | — | — | 1 | 5.92 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL607061 | — | IC50 | = | 11.3 | nM | 7.95 |
| CHEMBL607063 | — | IC50 | = | 16.5 | nM | 7.78 |
| CHEMBL607112 | — | IC50 | = | 23.7 | nM | 7.62 |
| CHEMBL312037 | — | IC50 | = | 25.5 | nM | 7.59 |
| CHEMBL148419 | — | IC50 | = | 54.8 | nM | 7.26 |
| CHEMBL145888 | — | IC50 | = | 55.8 | nM | 7.25 |
| CHEMBL607114 | — | IC50 | = | 80.8 | nM | 7.09 |
| CHEMBL607113 | — | IC50 | = | 95.4 | nM | 7.02 |
| CHEMBL147787 | — | IC50 | = | 109.0 | nM | 6.96 |
| CHEMBL146195 | — | IC50 | = | 134.0 | nM | 6.87 |
| CHEMBL370805 | COCAINE | IC50 | = | 168.0 | nM | 6.78 |
| CHEMBL607111 | — | IC50 | = | 204.0 | nM | 6.69 |
| CHEMBL421777 | — | IC50 | = | 314.0 | nM | 6.50 |
| CHEMBL345026 | — | IC50 | = | 427.0 | nM | 6.37 |
| CHEMBL439629 | — | IC50 | = | 823.0 | nM | 6.08 |
| CHEMBL607062 | — | IC50 | = | 1200.0 | nM | 5.92 |