Assay Detail
Binding
CHEMBL4032662
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Agonist activity at human FXR expressed in HEK293T cells assessed as BSEP promoter driven cellular transcriptional activity after 24 hrs by luciferase reporter gene assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK-293T |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of Tropifexor (LJN452), a Highly Potent Non-bile Acid FXR Agonist for the Treatment of Cholestatic Liver Diseases and Nonalcoholic Steatohepatitis (NASH).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 15 | 7.88 | 9.59 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4062567 | — | — | 1 | 9.59 |
| CHEMBL4076774 | — | — | 1 | 9.38 |
| CHEMBL4061776 | — | — | 1 | 9.27 |
| CHEMBL4084716 | — | — | 1 | 9.16 |
| CHEMBL4083548 | — | — | 1 | 9.10 |
| CHEMBL4103787 | — | — | 1 | 9.09 |
| CHEMBL4062220 | — | — | 1 | 8.18 |
| CHEMBL4075736 | — | — | 1 | 8.02 |
| CHEMBL4062760 | — | — | 1 | 7.72 |
| CHEMBL566315 | OBETICHOLIC ACID | 4.0 | 1 | 7.38 |
| CHEMBL4076625 | — | — | 1 | 7.16 |
| CHEMBL4103649 | — | — | 1 | 7.06 |
| CHEMBL318457 | — | — | 1 | 7.02 |
| CHEMBL4067096 | — | — | 1 | 5.08 |
| CHEMBL4089107 | — | — | 1 | 5.04 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4062567 | — | EC50 | = | 0.26 | nM | 9.59 |
| CHEMBL4076774 | — | EC50 | = | 0.42 | nM | 9.38 |
| CHEMBL4061776 | — | EC50 | = | 0.54 | nM | 9.27 |
| CHEMBL4084716 | — | EC50 | = | 0.69 | nM | 9.16 |
| CHEMBL4083548 | — | EC50 | = | 0.8 | nM | 9.10 |
| CHEMBL4103787 | — | EC50 | = | 0.82 | nM | 9.09 |
| CHEMBL4062220 | — | EC50 | = | 6.6 | nM | 8.18 |
| CHEMBL4075736 | — | EC50 | = | 9.5 | nM | 8.02 |
| CHEMBL4062760 | — | EC50 | = | 19.0 | nM | 7.72 |
| CHEMBL566315 | OBETICHOLIC ACID | EC50 | = | 42.0 | nM | 7.38 |
| CHEMBL4076625 | — | EC50 | = | 70.0 | nM | 7.16 |
| CHEMBL4103649 | — | EC50 | = | 88.0 | nM | 7.06 |
| CHEMBL318457 | — | EC50 | = | 95.0 | nM | 7.02 |
| CHEMBL4067096 | — | EC50 | = | 8400.0 | nM | 5.08 |
| CHEMBL4089107 | — | EC50 | = | 9200.0 | nM | 5.04 |