Assay Detail
Binding
CHEMBL4374526
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Noncompetitive antagonist activity at GST-tagged human FXR-LBD domain assessed as EC50 for OCA-induced biotinylated SRC-1 recruitment at 50 uM after 30 mins in presence of FXR agonist, OCA by Alpha Screen assay (Rvb = 0.2 uM)
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Dissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 1 | 6.51 | 6.51 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL402063 | E-GUGGULSTERONE | — | 1 | 6.51 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL402063 | E-GUGGULSTERONE | EC50 | = | 310.0 | nM | 6.51 |