Assay Detail
Binding
CHEMBL5734028
Review assay metadata, readout intent, target linkage, and publication context from the same page.
TGR5/CRE Luciferase Assay: In the following tables TGR5 activation by compounds and subsequent increase in intracellular cAMP were evaluated using a luciferase reporter gene assay. Human embryonic kidney (HEK) 293 cells were transiently co-transfected with pCMV tag4b-TGR5 h (to follow hTGR5 activation) or pCMV AC6-TGR5m (to follow mTGR5 activation) expression plasmids and the pCRE TA-Luciferase reporter plasmid using the JET PEI reagent (Polyplus transfection). Transfected cells were seeded in 96-well plates and incubated overnight with the test compounds at increasing concentrations tested in duplicate. Lithocolic acid (LCA) at 10 μM was used as a positive reference compound. The cAMP-dependent luciferase expression was followed using the BrightGlo reagent according to the manufacturer (Promega) instructions. Luminescence was read with a Mithras plate reader (Berthold). Data were expressed as percentage of the 10 μM LCA value and EC50 values were calculated using XL fit 5 software or GraphPad Prism 5. Concentration-response curves were fitted by a nonlinear regression analysis to a 4 parameter logistic equation.
72
Total Activities
23
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| 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
Imidazol- or 1,2,4-triazol-derivatives and their use
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 24 | 6.56 | 7.82 |
| kon | 24 | - | - |
| k_off | 24 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4094487 | — | — | 3 | 7.82 |
| CHEMBL4090147 | — | — | 3 | 7.46 |
| CHEMBL4084668 | — | — | 3 | 7.41 |
| CHEMBL4116055 | — | — | 3 | 7.40 |
| CHEMBL4068227 | — | — | 3 | 7.33 |
| CHEMBL4104359 | — | — | 6 | 7.15 |
| CHEMBL4075688 | — | — | 3 | 6.89 |
| CHEMBL4085664 | — | — | 3 | 6.81 |
| CHEMBL5816372 | — | — | 3 | 6.80 |
| CHEMBL4116110 | — | — | 3 | 6.75 |
| CHEMBL4117224 | — | — | 3 | 6.62 |
| CHEMBL4104779 | — | — | 3 | 6.60 |
| CHEMBL4081298 | — | — | 3 | 6.52 |
| CHEMBL6013098 | — | — | 3 | 6.48 |
| CHEMBL5828397 | — | — | 3 | 6.24 |
| CHEMBL4088938 | — | — | 3 | 6.12 |
| CHEMBL4073081 | — | — | 3 | 6.06 |
| CHEMBL4060122 | — | — | 3 | 6.05 |
| CHEMBL4063932 | — | — | 3 | 6.00 |
| CHEMBL4091702 | — | — | 3 | 5.96 |
| CHEMBL5877867 | — | — | 3 | 5.92 |
| CHEMBL4102610 | — | — | 3 | 5.37 |
| CHEMBL4085777 | — | — | 3 | 5.11 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4094487 | — | EC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4090147 | — | EC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4084668 | — | EC50 | = | 39.0 | nM | 7.41 |
| CHEMBL4116055 | — | EC50 | = | 40.0 | nM | 7.40 |
| CHEMBL4068227 | — | EC50 | = | 47.0 | nM | 7.33 |
| CHEMBL4104359 | — | EC50 | = | 71.0 | nM | 7.15 |
| CHEMBL4075688 | — | EC50 | = | 128.0 | nM | 6.89 |
| CHEMBL4085664 | — | EC50 | = | 156.0 | nM | 6.81 |
| CHEMBL5816372 | — | EC50 | = | 160.0 | nM | 6.80 |
| CHEMBL4116110 | — | EC50 | = | 177.0 | nM | 6.75 |
| CHEMBL4117224 | — | EC50 | = | 240.0 | nM | 6.62 |
| CHEMBL4104779 | — | EC50 | = | 250.0 | nM | 6.60 |
| CHEMBL4104359 | — | EC50 | = | 260.0 | nM | 6.58 |
| CHEMBL4081298 | — | EC50 | = | 299.0 | nM | 6.52 |
| CHEMBL6013098 | — | EC50 | = | 330.0 | nM | 6.48 |
| CHEMBL5828397 | — | EC50 | = | 580.0 | nM | 6.24 |
| CHEMBL4088938 | — | EC50 | = | 750.0 | nM | 6.12 |
| CHEMBL4073081 | — | EC50 | = | 880.0 | nM | 6.06 |
| CHEMBL4060122 | — | EC50 | = | 900.0 | nM | 6.05 |
| CHEMBL4063932 | — | EC50 | = | 990.0 | nM | 6.00 |
| CHEMBL4091702 | — | EC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL5877867 | — | EC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL4102610 | — | EC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL4085777 | — | EC50 | = | 7700.0 | nM | 5.11 |
| CHEMBL4116055 | — | k_off | = | - | s-1 | - |
| CHEMBL5828397 | — | kon | = | - | — | - |
| CHEMBL5828397 | — | k_off | = | - | s-1 | - |
| CHEMBL5877867 | — | kon | = | - | — | - |
| CHEMBL6013098 | — | kon | = | - | — | - |
| CHEMBL6013098 | — | k_off | = | - | s-1 | - |
| CHEMBL4104359 | — | kon | = | - | — | - |
| CHEMBL4085664 | — | kon | = | - | — | - |
| CHEMBL4085664 | — | k_off | = | - | s-1 | - |
| CHEMBL4081298 | — | kon | = | - | — | - |
| CHEMBL4081298 | — | k_off | = | - | s-1 | - |
| CHEMBL4075688 | — | kon | = | - | — | - |
| CHEMBL4075688 | — | k_off | = | - | s-1 | - |
| CHEMBL4090147 | — | k_off | = | - | s-1 | - |
| CHEMBL5877867 | — | k_off | = | - | s-1 | - |
| CHEMBL4090147 | — | kon | = | - | — | - |
| CHEMBL4117224 | — | kon | = | - | — | - |
| CHEMBL4094487 | — | kon | = | - | — | - |
| CHEMBL4117224 | — | k_off | = | - | s-1 | - |
| CHEMBL4068227 | — | k_off | = | - | s-1 | - |
| CHEMBL4068227 | — | kon | = | - | — | - |
| CHEMBL4116055 | — | kon | = | - | — | - |
| CHEMBL4094487 | — | k_off | = | - | s-1 | - |
| CHEMBL4088938 | — | k_off | = | - | s-1 | - |
| CHEMBL4088938 | — | kon | = | - | — | - |
| CHEMBL4091702 | — | k_off | = | - | s-1 | - |