Assay Detail
Functional
CHEMBL2051554
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human GPR40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of phenylpropanoic acid derivatives containing polar functionalities as potent and orally bioavailable G protein-coupled receptor 40 agonists for the treatment of type 2 diabetes.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 21 | 7.66 | 8.35 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2048618 | — | — | 1 | 8.35 |
| CHEMBL2048614 | — | — | 1 | 7.92 |
| CHEMBL2048617 | — | — | 1 | 7.89 |
| CHEMBL2048616 | — | — | 1 | 7.85 |
| CHEMBL2048615 | — | — | 1 | 7.82 |
| CHEMBL2048624 | — | — | 1 | 7.82 |
| CHEMBL2048613 | — | — | 1 | 7.70 |
| CHEMBL1688486 | — | — | 1 | 7.66 |
| CHEMBL2048626 | — | — | 1 | 7.64 |
| CHEMBL2048619 | — | — | 1 | 7.64 |
| CHEMBL2048623 | — | — | 1 | 7.60 |
| CHEMBL2048622 | — | — | 1 | 7.60 |
| CHEMBL2048628 | — | — | 1 | 7.58 |
| CHEMBL2048627 | — | — | 1 | 7.54 |
| CHEMBL1688473 | — | — | 1 | 7.52 |
| CHEMBL2048620 | — | — | 1 | 7.51 |
| CHEMBL2048621 | — | — | 1 | 7.50 |
| CHEMBL2048610 | — | — | 1 | 7.40 |
| CHEMBL2048625 | — | — | 1 | 7.00 |
| CHEMBL2048612 | — | — | 1 | - |
| CHEMBL2048611 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2048618 | — | EC50 | = | 4.5 | nM | 8.35 |
| CHEMBL2048614 | — | EC50 | = | 12.0 | nM | 7.92 |
| CHEMBL2048617 | — | EC50 | = | 13.0 | nM | 7.89 |
| CHEMBL2048616 | — | EC50 | = | 14.0 | nM | 7.85 |
| CHEMBL2048615 | — | EC50 | = | 15.0 | nM | 7.82 |
| CHEMBL2048624 | — | EC50 | = | 15.0 | nM | 7.82 |
| CHEMBL2048613 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL1688486 | — | EC50 | = | 22.0 | nM | 7.66 |
| CHEMBL2048626 | — | EC50 | = | 23.0 | nM | 7.64 |
| CHEMBL2048619 | — | EC50 | = | 23.0 | nM | 7.64 |
| CHEMBL2048623 | — | EC50 | = | 25.0 | nM | 7.60 |
| CHEMBL2048622 | — | EC50 | = | 25.0 | nM | 7.60 |
| CHEMBL2048628 | — | EC50 | = | 26.0 | nM | 7.58 |
| CHEMBL2048627 | — | EC50 | = | 29.0 | nM | 7.54 |
| CHEMBL1688473 | — | EC50 | = | 30.0 | nM | 7.52 |
| CHEMBL2048620 | — | EC50 | = | 31.0 | nM | 7.51 |
| CHEMBL2048621 | — | EC50 | = | 32.0 | nM | 7.50 |
| CHEMBL2048610 | — | EC50 | = | 40.0 | nM | 7.40 |
| CHEMBL2048625 | — | EC50 | = | 99.0 | nM | 7.00 |
| CHEMBL2048612 | — | EC50 | - | — | - | |
| CHEMBL2048611 | — | EC50 | - | — | - |