Assay Detail
Functional
CHEMBL3367085
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human TGR5 expressed in HEK293 cells assessed as cAMP level after 48 hrs by fluorescent assay
14
Total Activities
14
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 |
Target
G-protein coupled bile acid receptor 1 (CHEMBL5409) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of novel pyrimidine and malonamide derivatives as TGR5 agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 14 | 7.63 | 8.46 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3321845 | — | — | 1 | 8.46 |
| CHEMBL3321846 | — | — | 1 | 8.41 |
| CHEMBL3321850 | — | — | 1 | 8.29 |
| CHEMBL3321841 | — | — | 1 | 8.21 |
| CHEMBL3321843 | — | — | 1 | 7.92 |
| CHEMBL3321758 | — | — | 1 | 7.70 |
| CHEMBL3321844 | — | — | 1 | 7.39 |
| CHEMBL2181251 | — | — | 1 | 7.32 |
| CHEMBL3356914 | — | — | 1 | 6.91 |
| CHEMBL3321849 | — | — | 1 | 6.75 |
| CHEMBL567640 | — | — | 1 | 6.53 |
| CHEMBL3321847 | — | — | 1 | - |
| CHEMBL3321848 | — | — | 1 | - |
| CHEMBL3321842 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3321845 | — | EC50 | = | 3.5 | nM | 8.46 |
| CHEMBL3321846 | — | EC50 | = | 3.9 | nM | 8.41 |
| CHEMBL3321850 | — | EC50 | = | 5.1 | nM | 8.29 |
| CHEMBL3321841 | — | EC50 | = | 6.1 | nM | 8.21 |
| CHEMBL3321843 | — | EC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3321758 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL3321844 | — | EC50 | = | 41.0 | nM | 7.39 |
| CHEMBL2181251 | — | EC50 | = | 48.0 | nM | 7.32 |
| CHEMBL3356914 | — | EC50 | = | 122.0 | nM | 6.91 |
| CHEMBL3321849 | — | EC50 | = | 178.0 | nM | 6.75 |
| CHEMBL567640 | — | EC50 | = | 293.0 | nM | 6.53 |
| CHEMBL3321847 | — | EC50 | > | 1000.0 | nM | - |
| CHEMBL3321848 | — | EC50 | > | 1000.0 | nM | - |
| CHEMBL3321842 | — | EC50 | > | 1000.0 | nM | - |