Assay Detail
Functional
CHEMBL2439686
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
31
Total Activities
31
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
Design, synthesis and biological evaluation of a novel class of potent TGR5 agonists based on a 4-phenyl pyridine scaffold.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 31 | 6.54 | 7.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2181247 | — | — | 1 | 7.72 |
| CHEMBL2435932 | — | — | 1 | 7.51 |
| CHEMBL2435933 | — | — | 1 | 7.50 |
| CHEMBL2435924 | — | — | 1 | 7.46 |
| CHEMBL2435926 | — | — | 1 | 7.29 |
| CHEMBL2435914 | — | — | 1 | 7.28 |
| CHEMBL2435928 | — | — | 1 | 7.21 |
| CHEMBL2435925 | — | — | 1 | 7.21 |
| CHEMBL2435927 | — | — | 1 | 7.20 |
| CHEMBL2435943 | — | — | 1 | 6.92 |
| CHEMBL2435921 | — | — | 1 | 6.69 |
| CHEMBL2435942 | — | — | 1 | 6.58 |
| CHEMBL2435945 | — | — | 1 | 6.51 |
| CHEMBL2435941 | — | — | 1 | 6.50 |
| CHEMBL2435937 | — | — | 1 | 6.46 |
| CHEMBL2435922 | — | — | 1 | 6.42 |
| CHEMBL2435915 | — | — | 1 | 6.39 |
| CHEMBL2435835 | — | — | 1 | 6.36 |
| CHEMBL2435919 | — | — | 1 | 6.34 |
| CHEMBL2435929 | — | — | 1 | 6.33 |
| CHEMBL2435940 | — | — | 1 | 6.33 |
| CHEMBL2435944 | — | — | 1 | 6.30 |
| CHEMBL2435918 | — | — | 1 | 6.24 |
| CHEMBL2435930 | — | — | 1 | 6.05 |
| CHEMBL2435934 | — | — | 1 | 6.04 |
| CHEMBL2435946 | — | — | 1 | 5.91 |
| CHEMBL567640 | — | — | 1 | 5.91 |
| CHEMBL2435935 | — | — | 1 | 5.90 |
| CHEMBL2435931 | — | — | 1 | 5.68 |
| CHEMBL2435939 | — | — | 1 | 5.39 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2181247 | — | EC50 | = | 19.0 | nM | 7.72 |
| CHEMBL2435932 | — | EC50 | = | 31.0 | nM | 7.51 |
| CHEMBL2435933 | — | EC50 | = | 32.0 | nM | 7.50 |
| CHEMBL2435924 | — | EC50 | = | 35.0 | nM | 7.46 |
| CHEMBL2435926 | — | EC50 | = | 51.0 | nM | 7.29 |
| CHEMBL2435914 | — | EC50 | = | 53.0 | nM | 7.28 |
| CHEMBL2435928 | — | EC50 | = | 62.0 | nM | 7.21 |
| CHEMBL2435925 | — | EC50 | = | 61.0 | nM | 7.21 |
| CHEMBL2435927 | — | EC50 | = | 63.0 | nM | 7.20 |
| CHEMBL2435943 | — | EC50 | = | 120.0 | nM | 6.92 |
| CHEMBL2435921 | — | EC50 | = | 204.0 | nM | 6.69 |
| CHEMBL2435942 | — | EC50 | = | 260.0 | nM | 6.58 |
| CHEMBL2435945 | — | EC50 | = | 310.0 | nM | 6.51 |
| CHEMBL2435941 | — | EC50 | = | 320.0 | nM | 6.50 |
| CHEMBL2435937 | — | EC50 | = | 350.0 | nM | 6.46 |
| CHEMBL2435922 | — | EC50 | = | 384.0 | nM | 6.42 |
| CHEMBL2435915 | — | EC50 | = | 406.0 | nM | 6.39 |
| CHEMBL2435835 | — | EC50 | = | 440.0 | nM | 6.36 |
| CHEMBL2435919 | — | EC50 | = | 458.0 | nM | 6.34 |
| CHEMBL2435929 | — | EC50 | = | 466.0 | nM | 6.33 |
| CHEMBL2435940 | — | EC50 | = | 470.0 | nM | 6.33 |
| CHEMBL2435944 | — | EC50 | = | 500.0 | nM | 6.30 |
| CHEMBL2435918 | — | EC50 | = | 580.0 | nM | 6.24 |
| CHEMBL2435930 | — | EC50 | = | 892.0 | nM | 6.05 |
| CHEMBL2435934 | — | EC50 | = | 910.0 | nM | 6.04 |
| CHEMBL2435946 | — | EC50 | = | 1230.0 | nM | 5.91 |
| CHEMBL567640 | — | EC50 | = | 1230.0 | nM | 5.91 |
| CHEMBL2435935 | — | EC50 | = | 1270.0 | nM | 5.90 |
| CHEMBL2435931 | — | EC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL2435939 | — | EC50 | = | 4080.0 | nM | 5.39 |
| CHEMBL2435938 | — | EC50 | = | 7430.0 | nM | 5.13 |