Assay Detail
Functional
CHEMBL892388
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonistic activity at FXR in HEK293 cells by GAL4 transactivation activity
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Design, synthesis, and evaluation of non-steroidal farnesoid X receptor (FXR) antagonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 11 | 5.58 | 7.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL318457 | — | — | 1 | 7.16 |
| CHEMBL427601 | — | — | 1 | 6.08 |
| CHEMBL234749 | — | — | 1 | 5.89 |
| CHEMBL233696 | — | — | 1 | 5.89 |
| CHEMBL233484 | — | — | 1 | 5.68 |
| CHEMBL395918 | — | — | 1 | 5.60 |
| CHEMBL389998 | — | — | 1 | 5.52 |
| CHEMBL429794 | — | — | 1 | 5.51 |
| CHEMBL234113 | — | — | 1 | 5.05 |
| CHEMBL240597 | CHENODIOL | 4.0 | 1 | 4.57 |
| CHEMBL263872 | — | — | 1 | 4.46 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL318457 | — | EC50 | = | 70.0 | nM | 7.16 |
| CHEMBL427601 | — | EC50 | = | 840.0 | nM | 6.08 |
| CHEMBL234749 | — | EC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL233696 | — | EC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL233484 | — | EC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL395918 | — | EC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL389998 | — | EC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL429794 | — | EC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL234113 | — | EC50 | = | 9000.0 | nM | 5.05 |
| CHEMBL240597 | CHENODIOL | EC50 | = | 27000.0 | nM | 4.57 |
| CHEMBL263872 | — | EC50 | = | 35100.0 | nM | 4.46 |