Assay Detail
Binding
CHEMBL2390171
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at FXR (unknown origin) expressed in human HepG2 cells co-expressing RXR assessed as inhibition of CDCA-induced transactivation after 18 hrs by luciferase reporter gene assay
3
Total Activities
2
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HepG2 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Binding mechanism of the farnesoid X receptor marine antagonist suvanine reveals a strategy to forestall drug modulation on nuclear receptors. Design, synthesis, and biological evaluation of novel ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 2 | 4.61 | 4.62 |
| Inhibition | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1818099 | SUVANINE'S SODIUM SALT | — | 2 | 4.62 |
| CHEMBL2386485 | — | — | 1 | 4.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1818099 | SUVANINE'S SODIUM SALT | EC50 | = | 24000.0 | nM | 4.62 |
| CHEMBL2386485 | — | EC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL1818099 | SUVANINE'S SODIUM SALT | Inhibition | - | % | - |