Assay Detail
Binding
CHEMBL873467
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Binding affinity against Serotonin transporter in rat cerebral cortex using [3H]paroxetine binding assay.
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Cerebral cortex |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Sodium-dependent serotonin transporter (CHEMBL313) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Dual NK(1) antagonists--serotonin reuptake inhibitors as potential antidepressants. Part 2: SAR and activity of benzyloxyphenethyl piperazine derivatives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 7.29 | 9.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL111303 | — | — | 1 | 9.10 |
| CHEMBL107941 | — | — | 1 | 8.60 |
| CHEMBL41 | FLUOXETINE | 4.0 | 1 | 8.20 |
| CHEMBL432627 | — | — | 1 | 8.20 |
| CHEMBL111244 | — | — | 1 | 8.10 |
| CHEMBL108667 | — | — | 1 | 8.00 |
| CHEMBL107831 | — | — | 1 | 7.90 |
| CHEMBL320535 | — | — | 1 | 7.80 |
| CHEMBL111176 | — | — | 1 | 7.60 |
| CHEMBL107829 | — | — | 1 | 7.50 |
| CHEMBL320544 | — | — | 1 | 7.00 |
| CHEMBL109514 | — | — | 1 | 6.80 |
| CHEMBL109183 | — | — | 1 | 6.70 |
| CHEMBL108200 | — | — | 1 | 6.70 |
| CHEMBL108889 | — | — | 1 | 6.70 |
| CHEMBL321892 | — | — | 1 | 6.70 |
| CHEMBL108422 | — | — | 1 | 6.60 |
| CHEMBL419742 | — | — | 1 | 6.60 |
| CHEMBL109937 | — | — | 1 | 6.60 |
| CHEMBL107875 | — | — | 1 | 6.50 |
| CHEMBL110086 | — | — | 1 | 6.50 |
| CHEMBL111304 | — | — | 1 | 6.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL111303 | — | IC50 | = | 0.7943 | nM | 9.10 |
| CHEMBL107941 | — | IC50 | = | 2.512 | nM | 8.60 |
| CHEMBL41 | FLUOXETINE | IC50 | = | 6.31 | nM | 8.20 |
| CHEMBL432627 | — | IC50 | = | 6.31 | nM | 8.20 |
| CHEMBL111244 | — | IC50 | = | 7.943 | nM | 8.10 |
| CHEMBL108667 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL107831 | — | IC50 | = | 12.59 | nM | 7.90 |
| CHEMBL320535 | — | IC50 | = | 15.85 | nM | 7.80 |
| CHEMBL111176 | — | IC50 | = | 25.12 | nM | 7.60 |
| CHEMBL107829 | — | IC50 | = | 31.62 | nM | 7.50 |
| CHEMBL320544 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL109514 | — | IC50 | = | 158.49 | nM | 6.80 |
| CHEMBL109183 | — | IC50 | = | 199.53 | nM | 6.70 |
| CHEMBL108200 | — | IC50 | = | 199.53 | nM | 6.70 |
| CHEMBL108889 | — | IC50 | = | 199.53 | nM | 6.70 |
| CHEMBL321892 | — | IC50 | = | 199.53 | nM | 6.70 |
| CHEMBL108422 | — | IC50 | = | 251.19 | nM | 6.60 |
| CHEMBL419742 | — | IC50 | = | 251.19 | nM | 6.60 |
| CHEMBL109937 | — | IC50 | = | 251.19 | nM | 6.60 |
| CHEMBL107875 | — | IC50 | = | 316.23 | nM | 6.50 |
| CHEMBL110086 | — | IC50 | = | 316.23 | nM | 6.50 |
| CHEMBL111304 | — | IC50 | = | 1000.0 | nM | 6.00 |