Assay Detail
Functional
CHEMBL1211233
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human full length FXR transfected in HEK293 cells coexpressing pTRexDest/pGL2promotor assessed as luciferase activity by direct reporter cellular assay
30
Total Activities
30
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
Synthesis and pharmacological validation of a novel series of non-steroidal FXR agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 30 | 7.05 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1209170 | — | — | 1 | 8.70 |
| CHEMBL1209173 | — | — | 1 | 8.22 |
| CHEMBL1209111 | — | — | 1 | 8.22 |
| CHEMBL1209112 | — | — | 1 | 7.96 |
| CHEMBL1209109 | — | — | 1 | 7.82 |
| CHEMBL1209110 | — | — | 1 | 7.80 |
| CHEMBL1209113 | — | — | 1 | 7.72 |
| CHEMBL1209171 | — | — | 1 | 7.70 |
| CHEMBL318457 | — | — | 1 | 7.52 |
| CHEMBL1209293 | — | — | 1 | 7.48 |
| CHEMBL1209294 | — | — | 1 | 7.42 |
| CHEMBL1209364 | — | — | 1 | 7.24 |
| CHEMBL1209228 | — | — | 1 | 7.21 |
| CHEMBL1209108 | — | — | 1 | 7.00 |
| CHEMBL1209175 | — | — | 1 | 6.95 |
| CHEMBL1209227 | — | — | 1 | 6.92 |
| CHEMBL1209169 | — | — | 1 | 6.81 |
| CHEMBL1209230 | — | — | 1 | 6.74 |
| CHEMBL1209229 | — | — | 1 | 6.70 |
| CHEMBL1208794 | — | — | 1 | 6.68 |
| CHEMBL1209172 | — | — | 1 | 6.67 |
| CHEMBL1209002 | — | — | 1 | 6.42 |
| CHEMBL1209058 | — | — | 1 | 6.27 |
| CHEMBL1209292 | — | — | 1 | 6.21 |
| CHEMBL1209365 | — | — | 1 | 6.21 |
| CHEMBL1209060 | — | — | 1 | 6.06 |
| CHEMBL1209174 | — | — | 1 | 6.03 |
| CHEMBL1209059 | — | — | 1 | 5.94 |
| CHEMBL1209003 | — | — | 1 | 5.92 |
| CHEMBL1209061 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1209170 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL1209173 | — | EC50 | = | 6.0 | nM | 8.22 |
| CHEMBL1209111 | — | EC50 | = | 6.0 | nM | 8.22 |
| CHEMBL1209112 | — | EC50 | = | 11.0 | nM | 7.96 |
| CHEMBL1209109 | — | EC50 | = | 15.0 | nM | 7.82 |
| CHEMBL1209110 | — | EC50 | = | 16.0 | nM | 7.80 |
| CHEMBL1209113 | — | EC50 | = | 19.0 | nM | 7.72 |
| CHEMBL1209171 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL318457 | — | EC50 | = | 30.0 | nM | 7.52 |
| CHEMBL1209293 | — | EC50 | = | 33.0 | nM | 7.48 |
| CHEMBL1209294 | — | EC50 | = | 38.0 | nM | 7.42 |
| CHEMBL1209364 | — | EC50 | = | 58.0 | nM | 7.24 |
| CHEMBL1209228 | — | EC50 | = | 61.0 | nM | 7.21 |
| CHEMBL1209108 | — | EC50 | = | 101.0 | nM | 7.00 |
| CHEMBL1209175 | — | EC50 | = | 113.0 | nM | 6.95 |
| CHEMBL1209227 | — | EC50 | = | 120.0 | nM | 6.92 |
| CHEMBL1209169 | — | EC50 | = | 155.0 | nM | 6.81 |
| CHEMBL1209230 | — | EC50 | = | 182.0 | nM | 6.74 |
| CHEMBL1209229 | — | EC50 | = | 202.0 | nM | 6.70 |
| CHEMBL1208794 | — | EC50 | = | 208.0 | nM | 6.68 |
| CHEMBL1209172 | — | EC50 | = | 216.0 | nM | 6.67 |
| CHEMBL1209002 | — | EC50 | = | 385.0 | nM | 6.42 |
| CHEMBL1209058 | — | EC50 | = | 537.0 | nM | 6.27 |
| CHEMBL1209292 | — | EC50 | = | 611.0 | nM | 6.21 |
| CHEMBL1209365 | — | EC50 | = | 611.0 | nM | 6.21 |
| CHEMBL1209060 | — | EC50 | = | 878.0 | nM | 6.06 |
| CHEMBL1209174 | — | EC50 | = | 925.0 | nM | 6.03 |
| CHEMBL1209059 | — | EC50 | = | 1140.0 | nM | 5.94 |
| CHEMBL1209003 | — | EC50 | = | 1190.0 | nM | 5.92 |
| CHEMBL1209061 | — | EC50 | - | — | - |