Assay Detail
Binding
CHEMBL1060391
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]paroxetine from 5HT transporter in rat cortical membrane
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
Sodium-dependent serotonin transporter (CHEMBL313) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Synthesis, potency, and in vivo evaluation of 2-piperazin-1-ylquinoline analogues as dual serotonin reuptake inhibitors and serotonin 5-HT1A receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 16 | 8.03 | 9.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL556474 | — | — | 1 | 9.60 |
| CHEMBL559579 | — | — | 1 | 9.06 |
| CHEMBL564148 | — | — | 1 | 8.96 |
| CHEMBL562248 | — | — | 1 | 8.63 |
| CHEMBL41 | FLUOXETINE | 4.0 | 1 | 8.57 |
| CHEMBL551909 | — | — | 1 | 8.41 |
| CHEMBL551304 | — | — | 1 | 8.13 |
| CHEMBL565234 | — | — | 1 | 7.99 |
| CHEMBL550700 | — | — | 1 | 7.90 |
| CHEMBL551964 | — | — | 1 | 7.86 |
| CHEMBL559778 | — | — | 1 | 7.77 |
| CHEMBL551107 | — | — | 1 | 7.48 |
| CHEMBL550169 | — | — | 1 | 7.18 |
| CHEMBL550576 | — | — | 1 | 7.12 |
| CHEMBL560170 | — | — | 1 | 7.05 |
| CHEMBL551105 | — | — | 1 | 6.83 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL556474 | — | Ki | = | 0.25 | nM | 9.60 |
| CHEMBL559579 | — | Ki | = | 0.88 | nM | 9.06 |
| CHEMBL564148 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL562248 | — | Ki | = | 2.34 | nM | 8.63 |
| CHEMBL41 | FLUOXETINE | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL551909 | — | Ki | = | 3.9 | nM | 8.41 |
| CHEMBL551304 | — | Ki | = | 7.4 | nM | 8.13 |
| CHEMBL565234 | — | Ki | = | 10.3 | nM | 7.99 |
| CHEMBL550700 | — | Ki | = | 12.7 | nM | 7.90 |
| CHEMBL551964 | — | Ki | = | 13.8 | nM | 7.86 |
| CHEMBL559778 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL551107 | — | Ki | = | 32.8 | nM | 7.48 |
| CHEMBL550169 | — | Ki | = | 66.0 | nM | 7.18 |
| CHEMBL550576 | — | Ki | = | 75.0 | nM | 7.12 |
| CHEMBL560170 | — | Ki | = | 89.6 | nM | 7.05 |
| CHEMBL551105 | — | Ki | = | 148.5 | nM | 6.83 |