Assay Detail
Functional
CHEMBL1070842
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human FXR-LBD expressed in HEL293 cells by Gal4-luciferase assay
32
Total Activities
32
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
Improvement of physiochemical properties of the tetrahydroazepinoindole series of farnesoid X receptor (FXR) agonists: beneficial modulation of lipids in primates.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 32 | 6.41 | 7.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL454138 | TUROFEXORATE ISOPROPYL | 2.0 | 1 | 7.82 |
| CHEMBL603086 | — | — | 1 | 7.64 |
| CHEMBL603278 | — | — | 1 | 7.35 |
| CHEMBL589766 | — | — | 1 | 7.06 |
| CHEMBL601221 | — | — | 1 | 7.00 |
| CHEMBL601873 | — | — | 1 | 7.00 |
| CHEMBL592647 | — | — | 1 | 6.71 |
| CHEMBL602894 | — | — | 1 | 6.60 |
| CHEMBL603099 | — | — | 1 | 6.57 |
| CHEMBL602895 | — | — | 1 | 6.54 |
| CHEMBL602883 | — | — | 1 | 6.47 |
| CHEMBL611221 | — | — | 1 | 6.47 |
| CHEMBL602494 | — | — | 1 | 6.44 |
| CHEMBL601434 | — | — | 1 | 6.43 |
| CHEMBL602495 | — | — | 1 | 6.37 |
| CHEMBL604761 | — | — | 1 | 6.36 |
| CHEMBL603282 | — | — | 1 | 6.35 |
| CHEMBL601647 | — | — | 1 | 6.27 |
| CHEMBL602681 | — | — | 1 | 6.22 |
| CHEMBL601459 | — | — | 1 | 6.21 |
| CHEMBL600415 | — | — | 1 | 6.16 |
| CHEMBL602061 | — | — | 1 | 6.10 |
| CHEMBL605996 | — | — | 1 | 6.07 |
| CHEMBL602288 | — | — | 1 | 6.05 |
| CHEMBL602709 | — | — | 1 | 5.99 |
| CHEMBL603492 | — | — | 1 | 5.97 |
| CHEMBL604335 | — | — | 1 | 5.95 |
| CHEMBL602287 | — | — | 1 | 5.88 |
| CHEMBL602693 | — | — | 1 | 5.86 |
| CHEMBL604334 | — | — | 1 | 5.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL454138 | TUROFEXORATE ISOPROPYL | EC50 | = | 15.0 | nM | 7.82 |
| CHEMBL603086 | — | EC50 | = | 23.0 | nM | 7.64 |
| CHEMBL603278 | — | EC50 | = | 45.0 | nM | 7.35 |
| CHEMBL589766 | — | EC50 | = | 88.0 | nM | 7.06 |
| CHEMBL601221 | — | EC50 | = | 99.0 | nM | 7.00 |
| CHEMBL601873 | — | EC50 | = | 101.0 | nM | 7.00 |
| CHEMBL592647 | — | EC50 | = | 194.0 | nM | 6.71 |
| CHEMBL602894 | — | EC50 | = | 249.0 | nM | 6.60 |
| CHEMBL603099 | — | EC50 | = | 271.0 | nM | 6.57 |
| CHEMBL602895 | — | EC50 | = | 287.0 | nM | 6.54 |
| CHEMBL602883 | — | EC50 | = | 340.0 | nM | 6.47 |
| CHEMBL611221 | — | EC50 | = | 342.0 | nM | 6.47 |
| CHEMBL602494 | — | EC50 | = | 362.0 | nM | 6.44 |
| CHEMBL601434 | — | EC50 | = | 368.0 | nM | 6.43 |
| CHEMBL602495 | — | EC50 | = | 424.0 | nM | 6.37 |
| CHEMBL604761 | — | EC50 | = | 439.0 | nM | 6.36 |
| CHEMBL603282 | — | EC50 | = | 447.0 | nM | 6.35 |
| CHEMBL601647 | — | EC50 | = | 534.0 | nM | 6.27 |
| CHEMBL602681 | — | EC50 | = | 602.0 | nM | 6.22 |
| CHEMBL601459 | — | EC50 | = | 617.0 | nM | 6.21 |
| CHEMBL600415 | — | EC50 | = | 698.0 | nM | 6.16 |
| CHEMBL602061 | — | EC50 | = | 796.0 | nM | 6.10 |
| CHEMBL605996 | — | EC50 | = | 855.0 | nM | 6.07 |
| CHEMBL602288 | — | EC50 | = | 894.0 | nM | 6.05 |
| CHEMBL602709 | — | EC50 | = | 1023.0 | nM | 5.99 |
| CHEMBL603492 | — | EC50 | = | 1066.0 | nM | 5.97 |
| CHEMBL604335 | — | EC50 | = | 1121.0 | nM | 5.95 |
| CHEMBL602287 | — | EC50 | = | 1317.0 | nM | 5.88 |
| CHEMBL602693 | — | EC50 | = | 1386.0 | nM | 5.86 |
| CHEMBL604334 | — | EC50 | = | 1579.0 | nM | 5.80 |
| CHEMBL602059 | — | EC50 | = | 1603.0 | nM | 5.79 |
| CHEMBL601251 | — | EC50 | = | 2870.0 | nM | 5.54 |