Assay Detail
Functional
CHEMBL872975
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of neuronal uptake of 5 - Hydroxytryptamine in rat brain homogenate
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Tissue | Brain |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Sodium-dependent serotonin transporter (CHEMBL313) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Novel tacrine analogues for potential use against Alzheimer's disease: potent and selective acetylcholinesterase inhibitors and 5-HT uptake inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 5.56 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL118139 | — | — | 1 | 7.70 |
| CHEMBL41 | FLUOXETINE | 4.0 | 1 | 6.89 |
| CHEMBL431844 | — | — | 1 | 6.70 |
| CHEMBL119634 | — | — | 1 | 6.16 |
| CHEMBL118968 | — | — | 1 | 5.96 |
| CHEMBL60167 | — | — | 1 | 5.66 |
| CHEMBL330883 | — | — | 1 | 5.44 |
| CHEMBL115697 | — | — | 1 | 5.38 |
| CHEMBL115580 | — | — | 1 | 5.36 |
| CHEMBL89012 | — | — | 1 | 5.34 |
| CHEMBL332454 | — | — | 1 | 5.33 |
| CHEMBL119390 | — | — | 1 | 5.29 |
| CHEMBL118033 | — | — | 1 | 5.24 |
| CHEMBL325203 | — | — | 1 | 5.16 |
| CHEMBL119528 | — | — | 1 | 5.15 |
| CHEMBL95 | TACRINE | 4.0 | 1 | 5.12 |
| CHEMBL331637 | — | — | 1 | 4.89 |
| CHEMBL119389 | — | — | 1 | 4.89 |
| CHEMBL333011 | — | — | 1 | 4.84 |
| CHEMBL118752 | — | — | 1 | 4.68 |
| CHEMBL117826 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL118139 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL41 | FLUOXETINE | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL431844 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL119634 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL118968 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL60167 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL330883 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL115697 | — | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL115580 | — | IC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL89012 | — | IC50 | = | 4600.0 | nM | 5.34 |
| CHEMBL332454 | — | IC50 | = | 4700.0 | nM | 5.33 |
| CHEMBL119390 | — | IC50 | = | 5100.0 | nM | 5.29 |
| CHEMBL118033 | — | IC50 | = | 5800.0 | nM | 5.24 |
| CHEMBL325203 | — | IC50 | = | 6900.0 | nM | 5.16 |
| CHEMBL119528 | — | IC50 | = | 7100.0 | nM | 5.15 |
| CHEMBL95 | TACRINE | IC50 | = | 7600.0 | nM | 5.12 |
| CHEMBL331637 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL119389 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL333011 | — | IC50 | = | 14300.0 | nM | 4.84 |
| CHEMBL118752 | — | IC50 | = | 21000.0 | nM | 4.68 |
| CHEMBL117826 | — | IC50 | > | 95000.0 | nM | - |