Assay Detail
Binding
CHEMBL990614
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Inhibition of [3H]5HT reuptake at SERT in rat cortical synaptosomes
16
Total Activities
15
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sodium-dependent serotonin transporter (CHEMBL313) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Novel 5-HT(1A/1B/1D) receptors antagonists with potent 5-HT reuptake inhibitory activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 11 | 7.23 | 8.40 |
| Activity | 5 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL490417 | — | — | 1 | 8.40 |
| CHEMBL483365 | — | — | 1 | 8.20 |
| CHEMBL183460 | — | — | 1 | 8.10 |
| CHEMBL485395 | — | — | 1 | 7.60 |
| CHEMBL484743 | — | — | 1 | 7.50 |
| CHEMBL484387 | — | — | 1 | 7.20 |
| CHEMBL485427 | — | — | 1 | 7.00 |
| CHEMBL484742 | — | — | 1 | 6.70 |
| CHEMBL484386 | — | — | 1 | 6.60 |
| CHEMBL484205 | — | — | 1 | 6.10 |
| CHEMBL485630 | — | — | 1 | 6.10 |
| CHEMBL484216 | — | — | 2 | - |
| CHEMBL519010 | — | — | 1 | - |
| CHEMBL519019 | — | — | 1 | - |
| CHEMBL519037 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL490417 | — | Ki | = | 3.981 | nM | 8.40 |
| CHEMBL483365 | — | Ki | = | 6.31 | nM | 8.20 |
| CHEMBL183460 | — | Ki | = | 7.943 | nM | 8.10 |
| CHEMBL485395 | — | Ki | = | 25.12 | nM | 7.60 |
| CHEMBL484743 | — | Ki | = | 31.62 | nM | 7.50 |
| CHEMBL484387 | — | Ki | = | 63.1 | nM | 7.20 |
| CHEMBL485427 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL484742 | — | Ki | = | 199.53 | nM | 6.70 |
| CHEMBL484386 | — | Ki | = | 251.19 | nM | 6.60 |
| CHEMBL484205 | — | Ki | = | 794.33 | nM | 6.10 |
| CHEMBL485630 | — | Ki | = | 794.33 | nM | 6.10 |
| CHEMBL484216 | — | Activity | - | — | - | |
| CHEMBL484216 | — | Activity | - | — | - | |
| CHEMBL519010 | — | Activity | - | — | - | |
| CHEMBL519019 | — | Activity | - | — | - | |
| CHEMBL519037 | — | Activity | - | — | - |