Assay Detail
Functional
CHEMBL5133049
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity against human GPBAR1 expressed in HEK293T cells assessed as transactivation of cAMP-responsive element incubated for 18 hrs by Dual-Luciferase reporter assay based luminometer analysis
16
Total Activities
16
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
Structural Basis for Developing Multitarget Compounds Acting on Cysteinyl Leukotriene Receptor 1 and G-Protein-Coupled Bile Acid Receptor 1.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 16 | 5.65 | 7.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5192002 | — | — | 1 | 7.00 |
| CHEMBL5173976 | — | — | 1 | 6.77 |
| CHEMBL18775 | — | — | 1 | 6.30 |
| CHEMBL5189181 | — | — | 1 | 6.00 |
| CHEMBL5172427 | — | — | 1 | 5.75 |
| CHEMBL8747 | REV-5901 | — | 1 | 5.60 |
| CHEMBL5169385 | — | — | 1 | 5.52 |
| CHEMBL5174405 | — | — | 1 | 5.13 |
| CHEMBL5202995 | — | — | 1 | 4.78 |
| CHEMBL5177797 | — | — | 1 | 4.70 |
| CHEMBL5185938 | — | — | 1 | 4.64 |
| CHEMBL5205902 | — | — | 1 | - |
| CHEMBL5181326 | — | — | 1 | - |
| CHEMBL5173307 | — | — | 1 | - |
| CHEMBL5193617 | — | — | 1 | - |
| CHEMBL5189686 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5192002 | — | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL5173976 | — | EC50 | = | 170.0 | nM | 6.77 |
| CHEMBL18775 | — | EC50 | = | 500.0 | nM | 6.30 |
| CHEMBL5189181 | — | EC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL5172427 | — | EC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL8747 | REV-5901 | EC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL5169385 | — | EC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL5174405 | — | EC50 | = | 7400.0 | nM | 5.13 |
| CHEMBL5202995 | — | EC50 | = | 16500.0 | nM | 4.78 |
| CHEMBL5177797 | — | EC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL5185938 | — | EC50 | = | 23000.0 | nM | 4.64 |
| CHEMBL5205902 | — | EC50 | - | — | - | |
| CHEMBL5181326 | — | EC50 | - | — | - | |
| CHEMBL5173307 | — | EC50 | - | — | - | |
| CHEMBL5193617 | — | EC50 | - | — | - | |
| CHEMBL5189686 | — | EC50 | - | — | - |