Assay Detail
Functional
CHEMBL4772460
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 CRE-driven luciferase reporter gene activity incubated for 5.5 hrs and measured by Steady Glow reagent based luminescence assay
15
Total Activities
15
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 of G-protein-coupled bile acid receptor 1 (GPBAR1, TGR5) soft drugs with reduced gallbladder-filling effects.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 15 | 7.29 | 9.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4779084 | — | — | 1 | 9.05 |
| CHEMBL4776876 | — | — | 1 | 8.68 |
| CHEMBL4791709 | — | — | 1 | 8.55 |
| CHEMBL4794753 | — | — | 1 | 8.33 |
| CHEMBL4783037 | — | — | 1 | 8.15 |
| CHEMBL4798091 | — | — | 1 | 7.79 |
| CHEMBL4784355 | — | — | 1 | 7.63 |
| CHEMBL4793377 | — | — | 1 | 7.09 |
| CHEMBL4778884 | — | — | 1 | 7.08 |
| CHEMBL4794523 | — | — | 1 | 6.86 |
| CHEMBL4782069 | — | — | 1 | 6.84 |
| CHEMBL567640 | — | — | 1 | 6.00 |
| CHEMBL4783601 | — | — | 1 | 5.89 |
| CHEMBL3290724 | — | — | 1 | 5.78 |
| CHEMBL4792593 | — | — | 1 | 5.59 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4779084 | — | EC50 | = | 0.9 | nM | 9.05 |
| CHEMBL4776876 | — | EC50 | = | 2.1 | nM | 8.68 |
| CHEMBL4791709 | — | EC50 | = | 2.8 | nM | 8.55 |
| CHEMBL4794753 | — | EC50 | = | 4.7 | nM | 8.33 |
| CHEMBL4783037 | — | EC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4798091 | — | EC50 | = | 16.4 | nM | 7.79 |
| CHEMBL4784355 | — | EC50 | = | 23.3 | nM | 7.63 |
| CHEMBL4793377 | — | EC50 | = | 81.5 | nM | 7.09 |
| CHEMBL4778884 | — | EC50 | = | 83.7 | nM | 7.08 |
| CHEMBL4794523 | — | EC50 | = | 137.0 | nM | 6.86 |
| CHEMBL4782069 | — | EC50 | = | 145.0 | nM | 6.84 |
| CHEMBL567640 | — | EC50 | = | 1004.0 | nM | 6.00 |
| CHEMBL4783601 | — | EC50 | = | 1287.0 | nM | 5.89 |
| CHEMBL3290724 | — | EC50 | = | 1673.0 | nM | 5.78 |
| CHEMBL4792593 | — | EC50 | = | 2577.0 | nM | 5.59 |