Assay Detail
Functional
CHEMBL2339922
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human TGR5 expressed in deoxycycline-induced 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 | 7.83 | 8.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2331649 | — | — | 1 | 8.80 |
| CHEMBL2331653 | — | — | 1 | 8.70 |
| CHEMBL2331648 | — | — | 1 | 8.64 |
| CHEMBL2331646 | — | — | 1 | 8.60 |
| CHEMBL2331651 | — | — | 1 | 8.57 |
| CHEMBL2331655 | — | — | 1 | 8.55 |
| CHEMBL2331654 | — | — | 1 | 8.48 |
| CHEMBL2331650 | — | — | 1 | 8.33 |
| CHEMBL2331645 | — | — | 1 | 8.04 |
| CHEMBL576138 | — | — | 1 | 7.62 |
| CHEMBL2331652 | — | — | 1 | 7.37 |
| CHEMBL604131 | — | — | 1 | 7.33 |
| CHEMBL2331644 | — | — | 1 | 7.11 |
| CHEMBL2331647 | — | — | 1 | 6.86 |
| CHEMBL1258423 | — | — | 1 | 6.81 |
| CHEMBL567640 | — | — | 1 | 6.78 |
| CHEMBL2331643 | — | — | 1 | 6.59 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2331649 | — | EC50 | = | 1.6 | nM | 8.80 |
| CHEMBL2331653 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL2331648 | — | EC50 | = | 2.3 | nM | 8.64 |
| CHEMBL2331646 | — | EC50 | = | 2.5 | nM | 8.60 |
| CHEMBL2331651 | — | EC50 | = | 2.7 | nM | 8.57 |
| CHEMBL2331655 | — | EC50 | = | 2.8 | nM | 8.55 |
| CHEMBL2331654 | — | EC50 | = | 3.3 | nM | 8.48 |
| CHEMBL2331650 | — | EC50 | = | 4.7 | nM | 8.33 |
| CHEMBL2331645 | — | EC50 | = | 9.2 | nM | 8.04 |
| CHEMBL576138 | — | EC50 | = | 24.0 | nM | 7.62 |
| CHEMBL2331652 | — | EC50 | = | 43.0 | nM | 7.37 |
| CHEMBL604131 | — | EC50 | = | 47.0 | nM | 7.33 |
| CHEMBL2331644 | — | EC50 | = | 78.0 | nM | 7.11 |
| CHEMBL2331647 | — | EC50 | = | 137.0 | nM | 6.86 |
| CHEMBL1258423 | — | EC50 | = | 154.0 | nM | 6.81 |
| CHEMBL567640 | — | EC50 | = | 166.0 | nM | 6.78 |
| CHEMBL2331643 | — | EC50 | = | 257.0 | nM | 6.59 |