Assay Detail
Functional
CHEMBL2034293
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human recombinant FXR expressed in HEK293 cells coexpressing CMX-GAL4N by luciferase reporter gene assay
12
Total Activities
12
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 | Autocuration |
Publication
E297G mutated bile salt export pump (BSEP) function enhancers derived from GW4064: structural development study and separation from farnesoid X receptor-agonistic activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 12 | 5.65 | 7.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL318457 | — | — | 1 | 7.16 |
| CHEMBL2032446 | — | — | 1 | 6.39 |
| CHEMBL427601 | — | — | 1 | 6.08 |
| CHEMBL2017541 | — | — | 1 | 5.96 |
| CHEMBL395918 | — | — | 1 | 5.60 |
| CHEMBL2017548 | — | — | 1 | 5.58 |
| CHEMBL2017542 | — | — | 1 | 5.52 |
| CHEMBL389998 | — | — | 1 | 5.52 |
| CHEMBL429794 | — | — | 1 | 5.51 |
| CHEMBL240597 | CHENODIOL | 4.0 | 1 | 4.57 |
| CHEMBL406393 | DEOXYCHOLIC ACID | 4.0 | 1 | 4.30 |
| CHEMBL2032445 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL318457 | — | EC50 | = | 70.0 | nM | 7.16 |
| CHEMBL2032446 | — | EC50 | = | 410.0 | nM | 6.39 |
| CHEMBL427601 | — | EC50 | = | 840.0 | nM | 6.08 |
| CHEMBL2017541 | — | EC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL395918 | — | EC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL2017548 | — | EC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL2017542 | — | EC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL389998 | — | EC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL429794 | — | EC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL240597 | CHENODIOL | EC50 | = | 27000.0 | nM | 4.57 |
| CHEMBL406393 | DEOXYCHOLIC ACID | EC50 | = | 50000.0 | nM | 4.30 |
| CHEMBL2032445 | — | EC50 | > | 10000.0 | nM | - |