Assay Detail
Functional
CHEMBL949258
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human FXR expressed in COS1 cells by luciferase assay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | COS-1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Novel potent and selective bile acid derivatives as TGR5 agonists: biological screening, structure-activity relationships, and molecular modeling studies.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 12 | 4.91 | 5.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL270287 | — | — | 1 | 5.22 |
| CHEMBL261826 | — | — | 1 | 4.97 |
| CHEMBL240597 | CHENODIOL | 4.0 | 1 | 4.89 |
| CHEMBL270105 | — | — | 1 | 4.79 |
| CHEMBL1478 | LITHOCHOLIC ACID | — | 1 | 4.70 |
| CHEMBL3138525 | — | — | 1 | - |
| CHEMBL1253814 | — | — | 1 | - |
| CHEMBL406923 | — | — | 1 | - |
| CHEMBL405879 | — | — | 1 | - |
| CHEMBL270494 | — | — | 1 | - |
| CHEMBL273087 | 3 ALPHA-HYDROXY-7 ALPHA-FLUORO-5 BETA-CHOLAN-24-OIC A | — | 1 | - |
| CHEMBL1551 | URSODIOL | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL270287 | — | EC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL261826 | — | EC50 | = | 10600.0 | nM | 4.97 |
| CHEMBL240597 | CHENODIOL | EC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL270105 | — | EC50 | = | 16200.0 | nM | 4.79 |
| CHEMBL1478 | LITHOCHOLIC ACID | EC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL3138525 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL1253814 | — | EC50 | > | 31600.0 | nM | - |
| CHEMBL406923 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL405879 | — | EC50 | > | 31600.0 | nM | - |
| CHEMBL270494 | — | EC50 | > | 50000.0 | nM | - |
| CHEMBL273087 | 3 ALPHA-HYDROXY-7 ALPHA-FLUORO-5 BETA-CHOLAN-24-OIC A | EC50 | > | 100000.0 | nM | - |
| CHEMBL1551 | URSODIOL | EC50 | > | 50000.0 | nM | - |