Assay Detail
Binding
CHEMBL805325
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Binding affinity for Serotonin transporter was determined by [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 |
|---|---|---|---|
| Ki | 16 | 7.02 | 7.99 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL607061 | — | — | 1 | 7.99 |
| CHEMBL607063 | — | — | 1 | 7.82 |
| CHEMBL607112 | — | — | 1 | 7.66 |
| CHEMBL312037 | — | — | 1 | 7.63 |
| CHEMBL148419 | — | — | 1 | 7.30 |
| CHEMBL145888 | — | — | 1 | 7.29 |
| CHEMBL607114 | — | — | 1 | 7.13 |
| CHEMBL607113 | — | — | 1 | 7.06 |
| CHEMBL147787 | — | — | 1 | 7.00 |
| CHEMBL146195 | — | — | 1 | 6.91 |
| CHEMBL370805 | COCAINE | 4.0 | 1 | 6.81 |
| CHEMBL607111 | — | — | 1 | 6.73 |
| CHEMBL421777 | — | — | 1 | 6.54 |
| CHEMBL345026 | — | — | 1 | 6.41 |
| CHEMBL439629 | — | — | 1 | 6.12 |
| CHEMBL607062 | — | — | 1 | 5.96 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL607061 | — | Ki | = | 10.3 | nM | 7.99 |
| CHEMBL607063 | — | Ki | = | 15.1 | nM | 7.82 |
| CHEMBL607112 | — | Ki | = | 21.7 | nM | 7.66 |
| CHEMBL312037 | — | Ki | = | 23.2 | nM | 7.63 |
| CHEMBL148419 | — | Ki | = | 50.1 | nM | 7.30 |
| CHEMBL145888 | — | Ki | = | 51.0 | nM | 7.29 |
| CHEMBL607114 | — | Ki | = | 73.8 | nM | 7.13 |
| CHEMBL607113 | — | Ki | = | 86.8 | nM | 7.06 |
| CHEMBL147787 | — | Ki | = | 99.6 | nM | 7.00 |
| CHEMBL146195 | — | Ki | = | 122.0 | nM | 6.91 |
| CHEMBL370805 | COCAINE | Ki | = | 155.0 | nM | 6.81 |
| CHEMBL607111 | — | Ki | = | 186.0 | nM | 6.73 |
| CHEMBL421777 | — | Ki | = | 287.0 | nM | 6.54 |
| CHEMBL345026 | — | Ki | = | 389.0 | nM | 6.41 |
| CHEMBL439629 | — | Ki | = | 753.0 | nM | 6.12 |
| CHEMBL607062 | — | Ki | = | 1100.0 | nM | 5.96 |