Assay Detail
Functional
CHEMBL2339911
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human TGR5 expressed in uninduced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassay
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| 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
Identification of Tetrahydropyrido[4,3-d]pyrimidine Amides as a New Class of Orally Bioavailable TGR5 Agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 17 | 6.33 | 7.37 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2331655 | — | — | 1 | 7.37 |
| CHEMBL2331649 | — | — | 1 | 7.32 |
| CHEMBL2331648 | — | — | 1 | 7.12 |
| CHEMBL2331653 | — | — | 1 | 7.08 |
| CHEMBL2331654 | — | — | 1 | 6.95 |
| CHEMBL2331651 | — | — | 1 | 6.84 |
| CHEMBL2331650 | — | — | 1 | 6.81 |
| CHEMBL2331646 | — | — | 1 | 6.80 |
| CHEMBL2331645 | — | — | 1 | 6.67 |
| CHEMBL576138 | — | — | 1 | 6.50 |
| CHEMBL604131 | — | — | 1 | 5.85 |
| CHEMBL2331647 | — | — | 1 | 5.61 |
| CHEMBL2331652 | — | — | 1 | 5.52 |
| CHEMBL1258423 | — | — | 1 | 5.49 |
| CHEMBL2331644 | — | — | 1 | 5.42 |
| CHEMBL567640 | — | — | 1 | 5.26 |
| CHEMBL2331643 | — | — | 1 | 5.08 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2331655 | — | EC50 | = | 43.0 | nM | 7.37 |
| CHEMBL2331649 | — | EC50 | = | 48.0 | nM | 7.32 |
| CHEMBL2331648 | — | EC50 | = | 75.0 | nM | 7.12 |
| CHEMBL2331653 | — | EC50 | = | 83.0 | nM | 7.08 |
| CHEMBL2331654 | — | EC50 | = | 112.0 | nM | 6.95 |
| CHEMBL2331651 | — | EC50 | = | 146.0 | nM | 6.84 |
| CHEMBL2331650 | — | EC50 | = | 154.0 | nM | 6.81 |
| CHEMBL2331646 | — | EC50 | = | 158.0 | nM | 6.80 |
| CHEMBL2331645 | — | EC50 | = | 215.0 | nM | 6.67 |
| CHEMBL576138 | — | EC50 | = | 316.0 | nM | 6.50 |
| CHEMBL604131 | — | EC50 | = | 1420.0 | nM | 5.85 |
| CHEMBL2331647 | — | EC50 | = | 2430.0 | nM | 5.61 |
| CHEMBL2331652 | — | EC50 | = | 2990.0 | nM | 5.52 |
| CHEMBL1258423 | — | EC50 | = | 3220.0 | nM | 5.49 |
| CHEMBL2331644 | — | EC50 | = | 3780.0 | nM | 5.42 |
| CHEMBL567640 | — | EC50 | = | 5540.0 | nM | 5.26 |
| CHEMBL2331643 | — | EC50 | = | 8320.0 | nM | 5.08 |