Assay Detail
Binding
CHEMBL804696
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Ability to inhibit [3H]paroxetine binding to cloned human serotonin (5-HT) transporter
9
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Sodium-dependent serotonin transporter (CHEMBL228) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis and biological activity of some known and putative duloxetine metabolites.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 9 | 6.91 | 9.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1175 | DULOXETINE | 4.0 | 1 | 9.10 |
| CHEMBL326713 | — | — | 2 | 7.50 |
| CHEMBL119605 | — | — | 1 | 6.58 |
| CHEMBL2029052 | — | — | 1 | 5.84 |
| CHEMBL420142 | — | — | 1 | 5.51 |
| CHEMBL2029054 | — | — | 1 | - |
| CHEMBL2029055 | — | — | 1 | - |
| CHEMBL2029053 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1175 | DULOXETINE | Ki | = | 0.79 | nM | 9.10 |
| CHEMBL326713 | — | Ki | = | 31.7 | nM | 7.50 |
| CHEMBL326713 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL119605 | — | Ki | = | 266.0 | nM | 6.58 |
| CHEMBL2029052 | — | Ki | = | 1459.0 | nM | 5.84 |
| CHEMBL420142 | — | Ki | = | 3118.0 | nM | 5.51 |
| CHEMBL2029054 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL2029055 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL2029053 | — | Ki | > | 10000.0 | nM | - |