Assay Detail
Binding
CHEMBL4433552
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Transactivation of human FXR (unknown origin) expressed in HepG2 cells co-expressing pSG5RXR/pGL4.70 after 24 hrs post transfection by luciferase reporter gene assay
24
Total Activities
24
Compounds Tested
1
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
Novel Isoxazole Derivatives with Potent FXR Agonistic Activity Prevent Acetaminophen-Induced Liver Injury.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 24 | 5.81 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL318457 | — | — | 1 | 7.70 |
| CHEMBL4591419 | — | — | 1 | 6.52 |
| CHEMBL4588863 | — | — | 1 | 6.34 |
| CHEMBL566315 | OBETICHOLIC ACID | 4.0 | 1 | 6.30 |
| CHEMBL4455475 | — | — | 1 | 6.17 |
| CHEMBL4455911 | — | — | 1 | 6.14 |
| CHEMBL4553281 | — | — | 1 | 6.13 |
| CHEMBL4448603 | — | — | 1 | 6.09 |
| CHEMBL4585144 | — | — | 1 | 6.08 |
| CHEMBL4461163 | — | — | 1 | 6.03 |
| CHEMBL4456883 | — | — | 1 | 5.96 |
| CHEMBL4532035 | — | — | 1 | 5.94 |
| CHEMBL4445722 | — | — | 1 | 5.85 |
| CHEMBL4451432 | — | — | 1 | 5.80 |
| CHEMBL4591348 | — | — | 1 | 5.69 |
| CHEMBL4562865 | — | — | 1 | 5.55 |
| CHEMBL4436469 | — | — | 1 | 5.53 |
| CHEMBL4535914 | — | — | 1 | 5.45 |
| CHEMBL4450943 | — | — | 1 | 5.36 |
| CHEMBL4578551 | — | — | 1 | 5.27 |
| CHEMBL4592387 | — | — | 1 | 5.18 |
| CHEMBL4471591 | — | — | 1 | 4.99 |
| CHEMBL4465344 | — | — | 1 | 4.71 |
| CHEMBL240597 | CHENODIOL | 4.0 | 1 | 4.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL318457 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4591419 | — | EC50 | = | 300.0 | nM | 6.52 |
| CHEMBL4588863 | — | EC50 | = | 460.0 | nM | 6.34 |
| CHEMBL566315 | OBETICHOLIC ACID | EC50 | = | 500.0 | nM | 6.30 |
| CHEMBL4455475 | — | EC50 | = | 670.0 | nM | 6.17 |
| CHEMBL4455911 | — | EC50 | = | 730.0 | nM | 6.14 |
| CHEMBL4553281 | — | EC50 | = | 740.0 | nM | 6.13 |
| CHEMBL4448603 | — | EC50 | = | 810.0 | nM | 6.09 |
| CHEMBL4585144 | — | EC50 | = | 830.0 | nM | 6.08 |
| CHEMBL4461163 | — | EC50 | = | 940.0 | nM | 6.03 |
| CHEMBL4456883 | — | EC50 | = | 1090.0 | nM | 5.96 |
| CHEMBL4532035 | — | EC50 | = | 1150.0 | nM | 5.94 |
| CHEMBL4445722 | — | EC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL4451432 | — | EC50 | = | 1590.0 | nM | 5.80 |
| CHEMBL4591348 | — | EC50 | = | 2060.0 | nM | 5.69 |
| CHEMBL4562865 | — | EC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL4436469 | — | EC50 | = | 2930.0 | nM | 5.53 |
| CHEMBL4535914 | — | EC50 | = | 3590.0 | nM | 5.45 |
| CHEMBL4450943 | — | EC50 | = | 4370.0 | nM | 5.36 |
| CHEMBL4578551 | — | EC50 | = | 5400.0 | nM | 5.27 |
| CHEMBL4592387 | — | EC50 | = | 6670.0 | nM | 5.18 |
| CHEMBL4471591 | — | EC50 | = | 10170.0 | nM | 4.99 |
| CHEMBL4465344 | — | EC50 | = | 19740.0 | nM | 4.71 |
| CHEMBL240597 | CHENODIOL | EC50 | = | 20000.0 | nM | 4.70 |