Assay Detail
Binding
CHEMBL806804
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of [3H]-paroxetine binding on serotonin transporter of rat cerebral cortical synaptic membrane
13
Total Activities
9
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 analogs of milnacipran: (1S,2R)-1-phenyl-2-[(S)-1-aminopropyl]-N,N-diethylcyclopropanecarboxami de, an efficient noncompetitive N-methyl-D-aspartic acid receptor antagonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 13 | 6.43 | 8.07 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL99946 | LEVOMILNACIPRAN | 4.0 | 1 | 8.07 |
| CHEMBL330958 | — | — | 2 | 7.85 |
| CHEMBL434836 | — | — | 1 | 7.64 |
| CHEMBL145773 | — | — | 2 | 6.77 |
| CHEMBL119554 | — | — | 2 | 4.62 |
| CHEMBL343694 | — | — | 1 | 4.43 |
| CHEMBL145378 | — | — | 1 | - |
| CHEMBL356782 | — | — | 2 | - |
| CHEMBL145226 | — | — | 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 |
| CHEMBL434836 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL145773 | — | Ki | = | 170.0 | nM | 6.77 |
| CHEMBL330958 | — | Ki | = | 2400.0 | nM | 5.62 |
| CHEMBL119554 | — | Ki | = | 24000.0 | nM | 4.62 |
| CHEMBL343694 | — | Ki | = | 37000.0 | nM | 4.43 |
| CHEMBL119554 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL145378 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL145773 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL356782 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL145226 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL356782 | — | Ki | > | 100000.0 | nM | - |