Assay Detail
Functional
CHEMBL5336737
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP level incubated for 60 mins by HTR-FRET assay
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | NCI-H716 |
| 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
Chemical exploration of TGR5 functional hot-spots: Synthesis and structure-activity relationships of C7- and C23-Substituted cholic acid derivatives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 25 | 5.03 | 6.07 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL567640 | — | — | 1 | 6.07 |
| CHEMBL5431182 | — | — | 1 | 5.70 |
| CHEMBL5396857 | — | — | 1 | 5.40 |
| CHEMBL5416586 | — | — | 1 | 5.40 |
| CHEMBL5431752 | — | — | 1 | 5.35 |
| CHEMBL5438844 | — | — | 1 | 5.30 |
| CHEMBL5436516 | — | — | 1 | 5.25 |
| CHEMBL5409189 | — | — | 1 | 5.17 |
| CHEMBL5440980 | — | — | 1 | 5.08 |
| CHEMBL5425544 | — | — | 1 | 5.05 |
| CHEMBL5435161 | — | — | 1 | 4.80 |
| CHEMBL5412957 | — | — | 1 | 4.76 |
| CHEMBL5424633 | — | — | 1 | 4.72 |
| CHEMBL5430282 | — | — | 1 | 4.70 |
| CHEMBL205596 | CHOLIC ACID | 4.0 | 1 | 4.38 |
| CHEMBL5426065 | — | — | 1 | 4.35 |
| CHEMBL5424602 | — | — | 1 | 4.05 |
| CHEMBL5407394 | — | — | 1 | - |
| CHEMBL5418782 | — | — | 1 | - |
| CHEMBL5433595 | — | — | 1 | - |
| CHEMBL5411038 | — | — | 1 | - |
| CHEMBL5422960 | — | — | 1 | - |
| CHEMBL5408411 | — | — | 1 | - |
| CHEMBL5420121 | — | — | 1 | - |
| CHEMBL5437734 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL567640 | — | EC50 | = | 850.0 | nM | 6.07 |
| CHEMBL5431182 | — | EC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL5396857 | — | EC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL5416586 | — | EC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL5431752 | — | EC50 | = | 4500.0 | nM | 5.35 |
| CHEMBL5438844 | — | EC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL5436516 | — | EC50 | = | 5600.0 | nM | 5.25 |
| CHEMBL5409189 | — | EC50 | = | 6800.0 | nM | 5.17 |
| CHEMBL5440980 | — | EC50 | = | 8400.0 | nM | 5.08 |
| CHEMBL5425544 | — | EC50 | = | 9000.0 | nM | 5.05 |
| CHEMBL5435161 | — | EC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL5412957 | — | EC50 | = | 17500.0 | nM | 4.76 |
| CHEMBL5424633 | — | EC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL5430282 | — | EC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL205596 | CHOLIC ACID | EC50 | = | 41500.0 | nM | 4.38 |
| CHEMBL5426065 | — | EC50 | = | 44700.0 | nM | 4.35 |
| CHEMBL5424602 | — | EC50 | = | 90000.0 | nM | 4.05 |
| CHEMBL5407394 | — | EC50 | > | 50000.0 | nM | - |
| CHEMBL5418782 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL5433595 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL5411038 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL5422960 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL5408411 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL5420121 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL5437734 | — | EC50 | > | 100000.0 | nM | - |