Assay Detail
Binding
CHEMBL3749489
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at recombinant His-tagged human FXR ligand binding domain assessed as SRC-1 coactivator recruitment after 4 hrs by luminescence analysis
2
Total Activities
2
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
Discovery of 6-(4-{[5-Cyclopropyl-3-(2,6-dichlorophenyl)isoxazol-4-yl]methoxy}piperidin-1-yl)-1-methyl-1H-indole-3-carboxylic Acid: A Novel FXR Agonist for the Treatment of Dyslipidemia.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 2 | 6.79 | 6.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3746388 | TERN-101 | 2.0 | 1 | 6.92 |
| CHEMBL318457 | — | — | 1 | 6.66 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3746388 | TERN-101 | EC50 | = | 121.0 | nM | 6.92 |
| CHEMBL318457 | — | EC50 | = | 220.0 | nM | 6.66 |