Assay Detail
Binding
CHEMBL804806
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of Serotonin transporter in cerebral cortical synaptic membrane of rats using [3H]paroxetine
11
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Sodium-dependent serotonin transporter (CHEMBL313) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Synthesis and biological activity of conformationally restricted analogues of milnacipran: (1S, 2R)-1-phenyl-2-[(R)-1-amino-2-propynyl]-N,N- diethylcyclopropanecarboxamide is a novel class of NMDA receptor channel blocker.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 11 | 6.04 | 8.07 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL99946 | LEVOMILNACIPRAN | 4.0 | 1 | 8.07 |
| CHEMBL330958 | — | — | 2 | 7.85 |
| CHEMBL326735 | — | — | 2 | 6.72 |
| CHEMBL119554 | — | — | 2 | 4.62 |
| CHEMBL117681 | — | — | 1 | 4.60 |
| CHEMBL118690 | — | — | 1 | - |
| CHEMBL119462 | — | — | 1 | - |
| CHEMBL431687 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL99946 | LEVOMILNACIPRAN | Ki | = | 8.5 | nM | 8.07 |
| CHEMBL330958 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL326735 | — | Ki | = | 190.0 | nM | 6.72 |
| CHEMBL330958 | — | Ki | = | 2400.0 | nM | 5.62 |
| CHEMBL326735 | — | Ki | = | 15000.0 | nM | 4.82 |
| CHEMBL119554 | — | Ki | = | 24000.0 | nM | 4.62 |
| CHEMBL117681 | — | Ki | = | 25000.0 | nM | 4.60 |
| CHEMBL119554 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL118690 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL119462 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL431687 | — | Ki | > | 100000.0 | nM | - |