Assay Detail
Binding
CHEMBL1768535
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human GST-fused FXR LBD assessed as coactivator interaction with receptor ligand binding domain by Alphascreen assay
4
Total Activities
4
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
Extending SAR of bile acids as FXR ligands: discovery of 23-N-(carbocinnamyloxy)-3α,7α-dihydroxy-6α-ethyl-24-nor-5β-cholan-23-amine.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 4 | 6.06 | 6.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1765565 | — | — | 1 | 6.82 |
| CHEMBL566315 | OBETICHOLIC ACID | 4.0 | 1 | 6.70 |
| CHEMBL3138092 | — | — | 1 | 6.05 |
| CHEMBL240597 | CHENODIOL | 4.0 | 1 | 4.68 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1765565 | — | EC50 | = | 150.0 | nM | 6.82 |
| CHEMBL566315 | OBETICHOLIC ACID | EC50 | = | 200.0 | nM | 6.70 |
| CHEMBL3138092 | — | EC50 | = | 900.0 | nM | 6.05 |
| CHEMBL240597 | CHENODIOL | EC50 | = | 21000.0 | nM | 4.68 |