Assay Detail
Functional
CHEMBL854499
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity to FXR assessed as ligand-dependent SRC1 recruitment by FRET based co-activator assay
13
Total Activities
12
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Back door modulation of the farnesoid X receptor: design, synthesis, and biological evaluation of a series of side chain modified chenodeoxycholic acid derivatives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 12 | 5.84 | 7.01 |
| Efficacy | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL566315 | OBETICHOLIC ACID | 4.0 | 1 | 7.01 |
| CHEMBL3138428 | — | — | 1 | 6.39 |
| CHEMBL3138092 | — | — | 1 | 6.23 |
| CHEMBL3138089 | — | — | 1 | 6.22 |
| CHEMBL3138090 | — | — | 1 | 6.10 |
| CHEMBL3138339 | — | — | 1 | 5.94 |
| CHEMBL3138093 | — | — | 1 | 5.83 |
| CHEMBL3138341 | — | — | 1 | 5.60 |
| CHEMBL3138403 | — | — | 1 | 5.57 |
| CHEMBL3138091 | — | — | 1 | 5.15 |
| CHEMBL240597 | CHENODIOL | 4.0 | 2 | 5.06 |
| CHEMBL3138044 | — | — | 1 | 5.01 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL566315 | OBETICHOLIC ACID | EC50 | = | 98.0 | nM | 7.01 |
| CHEMBL3138428 | — | EC50 | = | 410.0 | nM | 6.39 |
| CHEMBL3138092 | — | EC50 | = | 590.0 | nM | 6.23 |
| CHEMBL3138089 | — | EC50 | = | 600.0 | nM | 6.22 |
| CHEMBL3138090 | — | EC50 | = | 790.0 | nM | 6.10 |
| CHEMBL3138339 | — | EC50 | = | 1140.0 | nM | 5.94 |
| CHEMBL3138093 | — | EC50 | = | 1480.0 | nM | 5.83 |
| CHEMBL3138341 | — | EC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL3138403 | — | EC50 | = | 2720.0 | nM | 5.57 |
| CHEMBL3138091 | — | EC50 | = | 7110.0 | nM | 5.15 |
| CHEMBL240597 | CHENODIOL | EC50 | = | 8660.0 | nM | 5.06 |
| CHEMBL3138044 | — | EC50 | = | 9680.0 | nM | 5.01 |
| CHEMBL240597 | CHENODIOL | Efficacy | = | 100.0 | % | - |