Assay Detail
Binding
CHEMBL5522908
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at GST-tagged human FXR LBD expressed in HEK293T cotransfected with FXRE-luciferase reporter plasmid by luciferase reporter gene assay
35
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293T |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery and Optimization of Novel Nonbile Acid FXR Agonists as Preclinical Candidates for the Treatment of Inflammatory Bowel Disease.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 35 | 7.91 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5559957 | — | — | 1 | 10.00 |
| CHEMBL5559067 | — | — | 1 | 10.00 |
| CHEMBL5561496 | — | — | 1 | 8.89 |
| CHEMBL5555964 | — | — | 1 | 8.77 |
| CHEMBL5560140 | — | — | 1 | 8.43 |
| CHEMBL3746388 | TERN-101 | 2.0 | 1 | 8.39 |
| CHEMBL5556116 | — | — | 1 | 8.31 |
| CHEMBL5568192 | — | — | 1 | 8.26 |
| CHEMBL5558528 | — | — | 1 | 8.24 |
| CHEMBL5563110 | — | — | 1 | 8.17 |
| CHEMBL5564635 | — | — | 1 | 8.15 |
| CHEMBL5555480 | — | — | 1 | 8.11 |
| CHEMBL5556964 | — | — | 1 | 8.10 |
| CHEMBL5560772 | — | — | 1 | 8.06 |
| CHEMBL5555199 | — | — | 1 | 8.06 |
| CHEMBL5561445 | — | — | 1 | 8.04 |
| CHEMBL5549875 | — | — | 1 | 8.00 |
| CHEMBL5563946 | — | — | 1 | 7.99 |
| CHEMBL5567573 | — | — | 1 | 7.94 |
| CHEMBL5561278 | — | — | 1 | 7.92 |
| CHEMBL5564776 | — | — | 1 | 7.92 |
| CHEMBL5561797 | — | — | 1 | 7.87 |
| CHEMBL5564138 | — | — | 1 | 7.79 |
| CHEMBL5558779 | — | — | 1 | 7.59 |
| CHEMBL5561027 | — | — | 1 | 7.46 |
| CHEMBL5542969 | — | — | 1 | 7.43 |
| CHEMBL5561500 | — | — | 1 | 7.32 |
| CHEMBL5565429 | — | — | 1 | 7.32 |
| CHEMBL5560179 | — | — | 1 | 7.17 |
| CHEMBL5561681 | — | — | 1 | 7.06 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5559957 | — | EC50 | = | 0.1 | nM | 10.00 |
| CHEMBL5559067 | — | EC50 | = | 0.1 | nM | 10.00 |
| CHEMBL5561496 | — | EC50 | = | 1.3 | nM | 8.89 |
| CHEMBL5555964 | — | EC50 | = | 1.7 | nM | 8.77 |
| CHEMBL5560140 | — | EC50 | = | 3.7 | nM | 8.43 |
| CHEMBL3746388 | TERN-101 | EC50 | = | 4.1 | nM | 8.39 |
| CHEMBL5556116 | — | EC50 | = | 4.9 | nM | 8.31 |
| CHEMBL5568192 | — | EC50 | = | 5.5 | nM | 8.26 |
| CHEMBL5558528 | — | EC50 | = | 5.7 | nM | 8.24 |
| CHEMBL5563110 | — | EC50 | = | 6.8 | nM | 8.17 |
| CHEMBL5564635 | — | EC50 | = | 7.1 | nM | 8.15 |
| CHEMBL5555480 | — | EC50 | = | 7.7 | nM | 8.11 |
| CHEMBL5556964 | — | EC50 | = | 7.9 | nM | 8.10 |
| CHEMBL5560772 | — | EC50 | = | 8.7 | nM | 8.06 |
| CHEMBL5555199 | — | EC50 | = | 8.7 | nM | 8.06 |
| CHEMBL5561445 | — | EC50 | = | 9.1 | nM | 8.04 |
| CHEMBL5549875 | — | EC50 | = | 10.1 | nM | 8.00 |
| CHEMBL5563946 | — | EC50 | = | 10.2 | nM | 7.99 |
| CHEMBL5567573 | — | EC50 | = | 11.4 | nM | 7.94 |
| CHEMBL5561278 | — | EC50 | = | 12.1 | nM | 7.92 |
| CHEMBL5564776 | — | EC50 | = | 11.9 | nM | 7.92 |
| CHEMBL5561797 | — | EC50 | = | 13.5 | nM | 7.87 |
| CHEMBL5564138 | — | EC50 | = | 16.3 | nM | 7.79 |
| CHEMBL5558779 | — | EC50 | = | 25.7 | nM | 7.59 |
| CHEMBL5561027 | — | EC50 | = | 34.5 | nM | 7.46 |
| CHEMBL5542969 | — | EC50 | = | 36.8 | nM | 7.43 |
| CHEMBL5561500 | — | EC50 | = | 48.2 | nM | 7.32 |
| CHEMBL5565429 | — | EC50 | = | 47.5 | nM | 7.32 |
| CHEMBL5560179 | — | EC50 | = | 67.5 | nM | 7.17 |
| CHEMBL5561681 | — | EC50 | = | 86.7 | nM | 7.06 |
| CHEMBL5563833 | — | EC50 | = | 120.2 | nM | 6.92 |
| CHEMBL5568180 | — | EC50 | = | 123.9 | nM | 6.91 |
| CHEMBL5557829 | — | EC50 | = | 122.5 | nM | 6.91 |
| CHEMBL5557131 | — | EC50 | = | 130.9 | nM | 6.88 |
| CHEMBL5558721 | — | EC50 | = | 243.8 | nM | 6.61 |