Assay Detail
ADMET
CHEMBL4702906
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human TGR5 expressed in HEK293 cells measured after 30 mins by cAMP substrate based assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
G-protein coupled bile acid receptor 1 (CHEMBL5409) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery and Optimization of Non-bile Acid FXR Agonists as Preclinical Candidates for the Treatment of Nonalcoholic Steatohepatitis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 5 | 6.82 | 7.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL566315 | OBETICHOLIC ACID | 4.0 | 1 | 7.62 |
| CHEMBL567640 | — | — | 1 | 7.02 |
| CHEMBL3746388 | TERN-101 | 2.0 | 1 | 5.83 |
| CHEMBL4751890 | — | — | 1 | - |
| CHEMBL4747855 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL566315 | OBETICHOLIC ACID | EC50 | = | 23.7 | nM | 7.62 |
| CHEMBL567640 | — | EC50 | = | 95.8 | nM | 7.02 |
| CHEMBL3746388 | TERN-101 | EC50 | = | 1497.0 | nM | 5.83 |
| CHEMBL4751890 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL4747855 | — | EC50 | > | 100000.0 | nM | - |