Assay Detail
Binding
CHEMBL4689738
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity against recombinant human FXR transfected in human HuH-7 cells co-transfected with FRE-luciferase assessed as reduction in CDCA-induced luciferase expression incubated for 24 hrs by luciferase reporter gene assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Huh-7 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of Orally Active and Nonsteroidal Farnesoid X Receptor (FXR) Antagonist with Propensity for Accumulation and Responsiveness in Ileum.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 9.93 | 10.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4453417 | — | — | 1 | 10.30 |
| CHEMBL4783205 | — | — | 1 | 10.30 |
| CHEMBL4749439 | — | — | 1 | 10.22 |
| CHEMBL4783777 | — | — | 1 | 10.05 |
| CHEMBL4785930 | — | — | 1 | 9.96 |
| CHEMBL4778665 | — | — | 1 | 8.74 |
| CHEMBL4552760 | — | — | 1 | - |
| CHEMBL4797745 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4453417 | — | IC50 | = | 0.05 | nM | 10.30 |
| CHEMBL4783205 | — | IC50 | = | 0.05 | nM | 10.30 |
| CHEMBL4749439 | — | IC50 | = | 0.06 | nM | 10.22 |
| CHEMBL4783777 | — | IC50 | = | 0.09 | nM | 10.05 |
| CHEMBL4785930 | — | IC50 | = | 0.11 | nM | 9.96 |
| CHEMBL4778665 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL4552760 | — | IC50 | < | 0.001 | nM | - |
| CHEMBL4797745 | — | IC50 | < | 0.001 | nM | - |