Assay Detail
Binding
CHEMBL5734029
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 | Mus musculus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
G-protein coupled bile acid receptor 1 (CHEMBL1255150) ↗| Type | SINGLE PROTEIN |
| Organism | Mus musculus |
Publication
Imidazol- or 1,2,4-triazol-derivatives and their use
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 24 | 7.67 | 9.30 |
| kon | 24 | - | - |
| k_off | 24 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4116055 | — | — | 3 | 9.30 |
| CHEMBL4084668 | — | — | 3 | 9.00 |
| CHEMBL4094487 | — | — | 3 | 9.00 |
| CHEMBL4090147 | — | — | 3 | 8.70 |
| CHEMBL4104359 | — | — | 6 | 8.40 |
| CHEMBL4068227 | — | — | 3 | 8.32 |
| CHEMBL4104779 | — | — | 3 | 8.30 |
| CHEMBL4116110 | — | — | 3 | 8.15 |
| CHEMBL4117224 | — | — | 3 | 8.00 |
| CHEMBL4075688 | — | — | 3 | 7.92 |
| CHEMBL5816372 | — | — | 3 | 7.75 |
| CHEMBL6013098 | — | — | 3 | 7.58 |
| CHEMBL5828397 | — | — | 3 | 7.54 |
| CHEMBL4081298 | — | — | 3 | 7.36 |
| CHEMBL4073081 | — | — | 3 | 7.36 |
| CHEMBL5877867 | — | — | 3 | 7.17 |
| CHEMBL4085664 | — | — | 3 | 7.17 |
| CHEMBL4063932 | — | — | 3 | 7.05 |
| CHEMBL4091702 | — | — | 3 | 6.85 |
| CHEMBL4102610 | — | — | 3 | 6.75 |
| CHEMBL4060122 | — | — | 3 | 6.43 |
| CHEMBL4088938 | — | — | 3 | 6.29 |
| CHEMBL4085777 | — | — | 3 | 6.03 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4116055 | — | EC50 | = | 0.5 | nM | 9.30 |
| CHEMBL4094487 | — | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4084668 | — | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4090147 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4104359 | — | EC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4068227 | — | EC50 | = | 4.8 | nM | 8.32 |
| CHEMBL4104779 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4116110 | — | EC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4117224 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4075688 | — | EC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4104359 | — | EC50 | = | 17.0 | nM | 7.77 |
| CHEMBL5816372 | — | EC50 | = | 18.0 | nM | 7.75 |
| CHEMBL6013098 | — | EC50 | = | 26.0 | nM | 7.58 |
| CHEMBL5828397 | — | EC50 | = | 29.0 | nM | 7.54 |
| CHEMBL4073081 | — | EC50 | = | 44.0 | nM | 7.36 |
| CHEMBL4081298 | — | EC50 | = | 44.0 | nM | 7.36 |
| CHEMBL4085664 | — | EC50 | = | 68.0 | nM | 7.17 |
| CHEMBL5877867 | — | EC50 | = | 68.0 | nM | 7.17 |
| CHEMBL4063932 | — | EC50 | = | 90.0 | nM | 7.05 |
| CHEMBL4091702 | — | EC50 | = | 140.0 | nM | 6.85 |
| CHEMBL4102610 | — | EC50 | = | 180.0 | nM | 6.75 |
| CHEMBL4060122 | — | EC50 | = | 370.0 | nM | 6.43 |
| CHEMBL4088938 | — | EC50 | = | 510.0 | nM | 6.29 |
| CHEMBL4085777 | — | EC50 | = | 940.0 | nM | 6.03 |
| CHEMBL5877867 | — | k_off | = | - | s-1 | - |
| CHEMBL4090147 | — | k_off | = | - | s-1 | - |
| CHEMBL5877867 | — | kon | = | - | — | - |
| CHEMBL5828397 | — | kon | = | - | — | - |
| CHEMBL5828397 | — | k_off | = | - | s-1 | - |
| 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 | — | kon | = | - | — | - |
| CHEMBL4117224 | — | kon | = | - | — | - |
| CHEMBL4094487 | — | k_off | = | - | s-1 | - |
| CHEMBL4094487 | — | kon | = | - | — | - |
| CHEMBL6013098 | — | kon | = | - | — | - |
| CHEMBL4116055 | — | kon | = | - | — | - |
| CHEMBL4068227 | — | k_off | = | - | s-1 | - |
| CHEMBL4068227 | — | kon | = | - | — | - |
| CHEMBL4116055 | — | k_off | = | - | s-1 | - |
| CHEMBL4088938 | — | k_off | = | - | s-1 | - |
| CHEMBL4088938 | — | kon | = | - | — | - |
| CHEMBL4091702 | — | k_off | = | - | s-1 | - |
| CHEMBL4117224 | — | k_off | = | - | s-1 | - |