Assay Detail
Binding
CHEMBL2379283
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-citalopram from SERT in rat cerebral cortex after 1 hr by liquid scintillation counting analysis
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Cerebral cortex |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sodium-dependent serotonin transporter (CHEMBL313) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Synthesis and biological evaluation of novel pyrrolidine-2,5-dione derivatives as potential antidepressant agents. Part 1.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 26 | 7.07 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2377579 | — | — | 1 | 8.40 |
| CHEMBL2377582 | — | — | 1 | 8.28 |
| CHEMBL2377589 | — | — | 1 | 8.24 |
| CHEMBL2377574 | — | — | 1 | 7.95 |
| CHEMBL41 | FLUOXETINE | 4.0 | 1 | 7.90 |
| CHEMBL2377577 | — | — | 1 | 7.70 |
| CHEMBL2377584 | — | — | 1 | 7.47 |
| CHEMBL2377578 | — | — | 1 | 7.33 |
| CHEMBL2377580 | — | — | 1 | 7.29 |
| CHEMBL2377444 | — | — | 1 | 7.25 |
| CHEMBL2377587 | — | — | 1 | 7.17 |
| CHEMBL2377575 | — | — | 1 | 7.13 |
| CHEMBL2377585 | — | — | 1 | 7.01 |
| CHEMBL2377583 | — | — | 1 | 6.90 |
| CHEMBL2377581 | — | — | 1 | 6.74 |
| CHEMBL2377591 | — | — | 1 | 6.68 |
| CHEMBL2377576 | — | — | 1 | 6.68 |
| CHEMBL2377442 | — | — | 1 | 6.67 |
| CHEMBL2377443 | — | — | 1 | 6.66 |
| CHEMBL2377592 | — | — | 1 | 6.45 |
| CHEMBL2377445 | — | — | 1 | 6.42 |
| CHEMBL2377590 | — | — | 1 | 6.30 |
| CHEMBL2377586 | — | — | 1 | 6.17 |
| CHEMBL2377588 | — | — | 1 | 6.11 |
| CHEMBL2377446 | — | — | 1 | 5.73 |
| CHEMBL39 | SEROTONIN | 3.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2377579 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL2377582 | — | Ki | = | 5.2 | nM | 8.28 |
| CHEMBL2377589 | — | Ki | = | 5.7 | nM | 8.24 |
| CHEMBL2377574 | — | Ki | = | 11.3 | nM | 7.95 |
| CHEMBL41 | FLUOXETINE | Ki | = | 12.7 | nM | 7.90 |
| CHEMBL2377577 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL2377584 | — | Ki | = | 33.8 | nM | 7.47 |
| CHEMBL2377578 | — | Ki | = | 46.2 | nM | 7.33 |
| CHEMBL2377580 | — | Ki | = | 50.7 | nM | 7.29 |
| CHEMBL2377444 | — | Ki | = | 56.0 | nM | 7.25 |
| CHEMBL2377587 | — | Ki | = | 68.4 | nM | 7.17 |
| CHEMBL2377575 | — | Ki | = | 74.4 | nM | 7.13 |
| CHEMBL2377585 | — | Ki | = | 96.7 | nM | 7.01 |
| CHEMBL2377583 | — | Ki | = | 125.0 | nM | 6.90 |
| CHEMBL2377581 | — | Ki | = | 182.0 | nM | 6.74 |
| CHEMBL2377591 | — | Ki | = | 210.0 | nM | 6.68 |
| CHEMBL2377576 | — | Ki | = | 208.0 | nM | 6.68 |
| CHEMBL2377442 | — | Ki | = | 215.0 | nM | 6.67 |
| CHEMBL2377443 | — | Ki | = | 221.0 | nM | 6.66 |
| CHEMBL2377592 | — | Ki | = | 354.0 | nM | 6.45 |
| CHEMBL2377445 | — | Ki | = | 381.0 | nM | 6.42 |
| CHEMBL2377590 | — | Ki | = | 505.0 | nM | 6.30 |
| CHEMBL2377586 | — | Ki | = | 673.0 | nM | 6.17 |
| CHEMBL2377588 | — | Ki | = | 783.5 | nM | 6.11 |
| CHEMBL2377446 | — | Ki | = | 1850.0 | nM | 5.73 |
| CHEMBL39 | SEROTONIN | Ki | - | — | - |