Assay Detail
Binding
CHEMBL4399824
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of HA-tagged human NTCP expressed in human U2OS cells assessed as reduction in [14C]taurocholate uptake preincubated for 10 mins followed by [14C] taurocholate addition and further incubation for 10 mins by scintillation counting method
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | U2OS |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Hepatic sodium/bile acid cotransporter (CHEMBL5287) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Design, synthesis and biological evaluation of benzamide derivatives as novel NTCP inhibitors that induce apoptosis in HepG2 cells.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 5.17 | 5.29 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL121 | ROSIGLITAZONE | 4.0 | 1 | 5.29 |
| CHEMBL603 | ZAFIRLUKAST | 4.0 | 1 | 5.19 |
| CHEMBL41632 | TIRATRICOL | 3.0 | 1 | 5.16 |
| CHEMBL421 | SULFASALAZINE | 4.0 | 1 | 5.02 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL121 | ROSIGLITAZONE | IC50 | = | 5100.0 | nM | 5.29 |
| CHEMBL603 | ZAFIRLUKAST | IC50 | = | 6500.0 | nM | 5.19 |
| CHEMBL41632 | TIRATRICOL | IC50 | = | 6900.0 | nM | 5.16 |
| CHEMBL421 | SULFASALAZINE | IC50 | = | 9600.0 | nM | 5.02 |