Assay Detail
Binding
CHEMBL807674
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Inhibition of [3H]paroxetine (0.2 nM) binding to 5-HT transporter
13
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Sodium-dependent serotonin transporter (CHEMBL313) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Synthesis and ligand binding of tropane ring analogues of paroxetine.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 7.14 | 9.55 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL490 | PAROXETINE | 4.0 | 1 | 9.55 |
| CHEMBL88301 | — | — | 2 | 8.25 |
| CHEMBL87616 | — | — | 2 | 7.72 |
| CHEMBL606825 | — | — | 1 | 7.28 |
| CHEMBL312977 | — | — | 1 | 7.25 |
| CHEMBL314878 | — | — | 1 | 7.05 |
| CHEMBL606828 | — | — | 1 | 7.05 |
| CHEMBL606927 | — | — | 1 | 6.75 |
| CHEMBL606877 | — | — | 1 | 6.53 |
| CHEMBL606881 | — | — | 1 | 6.38 |
| CHEMBL606826 | — | — | 1 | 6.35 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL490 | PAROXETINE | IC50 | = | 0.28 | nM | 9.55 |
| CHEMBL88301 | — | IC50 | = | 5.62 | nM | 8.25 |
| CHEMBL87616 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL606825 | — | IC50 | = | 52.9 | nM | 7.28 |
| CHEMBL312977 | — | IC50 | = | 55.8 | nM | 7.25 |
| CHEMBL314878 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL606828 | — | IC50 | = | 88.1 | nM | 7.05 |
| CHEMBL606927 | — | IC50 | = | 178.0 | nM | 6.75 |
| CHEMBL606877 | — | IC50 | = | 294.0 | nM | 6.53 |
| CHEMBL606881 | — | IC50 | = | 422.0 | nM | 6.38 |
| CHEMBL88301 | — | IC50 | = | 424.0 | nM | 6.37 |
| CHEMBL606826 | — | IC50 | = | 447.0 | nM | 6.35 |
| CHEMBL87616 | — | IC50 | = | 480.0 | nM | 6.32 |