Assay Detail
Functional
CHEMBL4689302
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human TGR5 transfected in HEK293T cells assessed intracellular cAMP level by HTRF assay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293T |
| 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
Design, synthesis and evaluation of 1-benzyl-1H-imidazole-5-carboxamide derivatives as potent TGR5 agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 12 | 7.67 | 9.48 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4779837 | — | — | 1 | 9.48 |
| CHEMBL4743463 | — | — | 1 | 8.98 |
| CHEMBL4790044 | — | — | 1 | 8.96 |
| CHEMBL2181239 | — | — | 1 | 8.55 |
| CHEMBL4759282 | — | — | 1 | 8.36 |
| CHEMBL4759025 | — | — | 1 | 8.17 |
| CHEMBL4744582 | — | — | 1 | 8.02 |
| CHEMBL4796107 | — | — | 1 | 6.93 |
| CHEMBL4795121 | — | — | 1 | 6.47 |
| CHEMBL4789395 | — | — | 1 | 6.25 |
| CHEMBL567640 | — | — | 1 | 6.09 |
| CHEMBL4755237 | — | — | 1 | 5.76 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4779837 | — | EC50 | = | 0.33 | nM | 9.48 |
| CHEMBL4743463 | — | EC50 | = | 1.05 | nM | 8.98 |
| CHEMBL4790044 | — | EC50 | = | 1.09 | nM | 8.96 |
| CHEMBL2181239 | — | EC50 | = | 2.8 | nM | 8.55 |
| CHEMBL4759282 | — | EC50 | = | 4.39 | nM | 8.36 |
| CHEMBL4759025 | — | EC50 | = | 6.8 | nM | 8.17 |
| CHEMBL4744582 | — | EC50 | = | 9.5 | nM | 8.02 |
| CHEMBL4796107 | — | EC50 | = | 118.0 | nM | 6.93 |
| CHEMBL4795121 | — | EC50 | = | 338.0 | nM | 6.47 |
| CHEMBL4789395 | — | EC50 | = | 568.0 | nM | 6.25 |
| CHEMBL567640 | — | EC50 | = | 820.0 | nM | 6.09 |
| CHEMBL4755237 | — | EC50 | = | 1751.0 | nM | 5.76 |