Assay Detail
Binding
CHEMBL3102346
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Displacement of [3H]5-HT from rat cerebral cortex SERT after 10 mins
18
Total Activities
18
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
Flexible and biomimetic analogs of triple uptake inhibitor 4-((((3S,6S)-6-benzhydryltetrahydro-2H-pyran-3-yl)amino)methyl)phenol: Synthesis, biological characterization, and development of a pharmacophore model.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 18 | 6.76 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3099494 | — | — | 1 | 8.52 |
| CHEMBL41 | FLUOXETINE | 4.0 | 1 | 7.91 |
| CHEMBL213627 | — | — | 1 | 7.79 |
| CHEMBL209808 | — | — | 1 | 7.60 |
| CHEMBL211077 | — | — | 1 | 7.54 |
| CHEMBL3099493 | — | — | 1 | 7.23 |
| CHEMBL3099495 | — | — | 1 | 7.16 |
| CHEMBL3099487 | — | — | 1 | 6.82 |
| CHEMBL3099501 | — | — | 1 | 6.46 |
| CHEMBL3099488 | — | — | 1 | 6.45 |
| CHEMBL3099491 | — | — | 1 | 6.39 |
| CHEMBL3099502 | — | — | 1 | 6.33 |
| CHEMBL14370 | REBOXETINE | 4.0 | 1 | 6.30 |
| CHEMBL3099492 | — | — | 1 | 6.07 |
| CHEMBL3099486 | — | — | 1 | 5.94 |
| CHEMBL3099489 | — | — | 1 | 5.87 |
| CHEMBL3099490 | — | — | 1 | 5.69 |
| CHEMBL3099485 | — | — | 1 | 5.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3099494 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL41 | FLUOXETINE | Ki | = | 12.2 | nM | 7.91 |
| CHEMBL213627 | — | Ki | = | 16.1 | nM | 7.79 |
| CHEMBL209808 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL211077 | — | Ki | = | 29.1 | nM | 7.54 |
| CHEMBL3099493 | — | Ki | = | 58.4 | nM | 7.23 |
| CHEMBL3099495 | — | Ki | = | 69.1 | nM | 7.16 |
| CHEMBL3099487 | — | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL3099501 | — | Ki | = | 346.0 | nM | 6.46 |
| CHEMBL3099488 | — | Ki | = | 358.0 | nM | 6.45 |
| CHEMBL3099491 | — | Ki | = | 408.0 | nM | 6.39 |
| CHEMBL3099502 | — | Ki | = | 473.0 | nM | 6.33 |
| CHEMBL14370 | REBOXETINE | Ki | = | 503.0 | nM | 6.30 |
| CHEMBL3099492 | — | Ki | = | 844.0 | nM | 6.07 |
| CHEMBL3099486 | — | Ki | = | 1147.0 | nM | 5.94 |
| CHEMBL3099489 | — | Ki | = | 1353.0 | nM | 5.87 |
| CHEMBL3099490 | — | Ki | = | 2046.0 | nM | 5.69 |
| CHEMBL3099485 | — | Ki | = | 2496.0 | nM | 5.60 |