Assay Detail
Binding
CHEMBL806137
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Displacement of [3H]paroxetine from Serotonin transporter of rat frontal cortex membrane
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Frontal cortex |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Sodium-dependent serotonin transporter (CHEMBL313) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Synthesis of 3 beta-aryl-8-azabicyclo[3.2.1]octanes with high binding affinities and selectivities for the serotonin transporter site.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 14 | 8.11 | 9.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL85877 | — | — | 1 | 9.96 |
| CHEMBL36720 | — | — | 1 | 9.66 |
| CHEMBL85492 | — | — | 1 | 9.49 |
| CHEMBL418190 | — | — | 1 | 9.41 |
| CHEMBL82807 | — | — | 1 | 9.09 |
| CHEMBL314361 | — | — | 1 | 8.49 |
| CHEMBL85256 | — | — | 1 | 8.28 |
| CHEMBL87983 | — | — | 1 | 7.72 |
| CHEMBL278122 | — | — | 1 | 7.44 |
| CHEMBL84899 | — | — | 1 | 7.07 |
| CHEMBL87739 | — | — | 1 | 7.01 |
| CHEMBL23142 | — | — | 1 | 6.89 |
| CHEMBL87678 | — | — | 1 | 6.82 |
| CHEMBL314919 | — | — | 1 | 6.27 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL85877 | — | Ki | = | 0.11 | nM | 9.96 |
| CHEMBL36720 | — | Ki | = | 0.22 | nM | 9.66 |
| CHEMBL85492 | — | Ki | = | 0.32 | nM | 9.49 |
| CHEMBL418190 | — | Ki | = | 0.39 | nM | 9.41 |
| CHEMBL82807 | — | Ki | = | 0.82 | nM | 9.09 |
| CHEMBL314361 | — | Ki | = | 3.2 | nM | 8.49 |
| CHEMBL85256 | — | Ki | = | 5.3 | nM | 8.28 |
| CHEMBL87983 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL278122 | — | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL84899 | — | Ki | = | 85.0 | nM | 7.07 |
| CHEMBL87739 | — | Ki | = | 97.0 | nM | 7.01 |
| CHEMBL23142 | — | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL87678 | — | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL314919 | — | Ki | = | 540.0 | nM | 6.27 |