Assay Detail
Functional
CHEMBL5372118
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Positive allosteric modulator activity at human TGR5 expressed in HEK293T cells assessed as increase in cAMP accumulation incubated for 1 hr at 37 degC and further incubated for 1 hr at room temperature by glosensor cAMP accumulation assay
23
Total Activities
23
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
Discovery and biological evaluation of cholic acid derivatives as potent TGR5 positive allosteric modulators.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 23 | 4.71 | 5.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5439396 | — | — | 1 | 5.28 |
| CHEMBL5416364 | — | — | 1 | 5.26 |
| CHEMBL5440059 | — | — | 1 | 5.20 |
| CHEMBL5406515 | — | — | 1 | 5.10 |
| CHEMBL5422935 | — | — | 1 | 5.05 |
| CHEMBL5415850 | — | — | 1 | 5.02 |
| CHEMBL5435987 | — | — | 1 | 5.01 |
| CHEMBL5429083 | — | — | 1 | 4.92 |
| CHEMBL5430487 | — | — | 1 | 4.85 |
| CHEMBL5419988 | — | — | 1 | 4.73 |
| CHEMBL5423954 | — | — | 1 | 4.70 |
| CHEMBL5440151 | — | — | 1 | 4.66 |
| CHEMBL5414606 | — | — | 1 | 4.64 |
| CHEMBL5435030 | — | — | 1 | 4.59 |
| CHEMBL5427709 | — | — | 1 | 4.50 |
| CHEMBL5431401 | — | — | 1 | 4.42 |
| CHEMBL205596 | CHOLIC ACID | 4.0 | 1 | 4.41 |
| CHEMBL5395512 | — | — | 1 | 4.31 |
| CHEMBL5422399 | — | — | 1 | 4.21 |
| CHEMBL5401550 | — | — | 1 | 4.12 |
| CHEMBL5440153 | — | — | 1 | 4.03 |
| CHEMBL5395727 | — | — | 1 | - |
| CHEMBL5398083 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5439396 | — | EC50 | = | 5300.0 | nM | 5.28 |
| CHEMBL5416364 | — | EC50 | = | 5500.0 | nM | 5.26 |
| CHEMBL5440059 | — | EC50 | = | 6300.0 | nM | 5.20 |
| CHEMBL5406515 | — | EC50 | = | 8000.0 | nM | 5.10 |
| CHEMBL5422935 | — | EC50 | = | 8900.0 | nM | 5.05 |
| CHEMBL5415850 | — | EC50 | = | 9500.0 | nM | 5.02 |
| CHEMBL5435987 | — | EC50 | = | 9800.0 | nM | 5.01 |
| CHEMBL5429083 | — | EC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL5430487 | — | EC50 | = | 14100.0 | nM | 4.85 |
| CHEMBL5419988 | — | EC50 | = | 18500.0 | nM | 4.73 |
| CHEMBL5423954 | — | EC50 | = | 19800.0 | nM | 4.70 |
| CHEMBL5440151 | — | EC50 | = | 21800.0 | nM | 4.66 |
| CHEMBL5414606 | — | EC50 | = | 23000.0 | nM | 4.64 |
| CHEMBL5435030 | — | EC50 | = | 25800.0 | nM | 4.59 |
| CHEMBL5427709 | — | EC50 | = | 31600.0 | nM | 4.50 |
| CHEMBL5431401 | — | EC50 | = | 38000.0 | nM | 4.42 |
| CHEMBL205596 | CHOLIC ACID | EC50 | = | 38700.0 | nM | 4.41 |
| CHEMBL5395512 | — | EC50 | = | 48500.0 | nM | 4.31 |
| CHEMBL5422399 | — | EC50 | = | 62000.0 | nM | 4.21 |
| CHEMBL5401550 | — | EC50 | = | 76500.0 | nM | 4.12 |
| CHEMBL5440153 | — | EC50 | = | 92500.0 | nM | 4.03 |
| CHEMBL5395727 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL5398083 | — | EC50 | > | 100000.0 | nM | - |