Assay Detail
Binding
CHEMBL4143972
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Agonist activity at human FXR assessed as recruitment of SRC1 peptide by TR-FRET assay
5
Total Activities
3
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis and Biological Evaluation of a Series of Bile Acid Derivatives as FXR Agonists for Treatment of NASH.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 3 | 5.62 | 5.91 |
| Efficacy | 2 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4167134 | — | — | 2 | 5.91 |
| CHEMBL270311 | — | — | 2 | 5.89 |
| CHEMBL240597 | CHENODIOL | 4.0 | 1 | 5.06 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4167134 | — | EC50 | = | 1220.0 | nM | 5.91 |
| CHEMBL270311 | — | EC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL240597 | CHENODIOL | EC50 | = | 8660.0 | nM | 5.06 |
| CHEMBL270311 | — | Efficacy | = | 87.0 | % | - |
| CHEMBL4167134 | — | Efficacy | = | 111.0 | % | - |