Assay Detail
Binding
CHEMBL3767599
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human SERT expressed in HEK293 cells preincubated for 30 mins followed by fluorescent substrate addition measured after 30 mins by plate reader analysis
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sodium-dependent serotonin transporter (CHEMBL228) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of Vibegron: A Potent and Selective β3 Adrenergic Receptor Agonist for the Treatment of Overactive Bladder.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 5.87 | 6.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3764774 | — | — | 1 | 6.70 |
| CHEMBL3128178 | — | — | 1 | 6.38 |
| CHEMBL3764950 | — | — | 1 | 6.16 |
| CHEMBL3763998 | — | — | 1 | 6.10 |
| CHEMBL3128188 | — | — | 1 | 6.05 |
| CHEMBL3764592 | — | — | 1 | 5.96 |
| CHEMBL1684585 | — | — | 1 | 5.85 |
| CHEMBL3763594 | — | — | 1 | 5.60 |
| CHEMBL3764088 | — | — | 1 | 5.36 |
| CHEMBL111201 | — | — | 1 | 5.30 |
| CHEMBL3763934 | — | — | 1 | 5.15 |
| CHEMBL3765335 | — | — | 1 | - |
| CHEMBL2107826 | VIBEGRON | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3764774 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL3128178 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL3764950 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL3763998 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL3128188 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL3764592 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL1684585 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL3763594 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL3764088 | — | IC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL111201 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL3763934 | — | IC50 | = | 7100.0 | nM | 5.15 |
| CHEMBL3765335 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2107826 | VIBEGRON | IC50 | > | 10000.0 | nM | - |