Assay Detail
Functional
CHEMBL4010812
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay
24
Total Activities
24
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 |
Publication
Discovery of Potent and Orally Bioavailable GPR40 Full Agonists Bearing Thiophen-2-ylpropanoic Acid Scaffold.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 24 | 6.27 | 8.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1688486 | — | — | 1 | 8.10 |
| CHEMBL1829174 | FASIGLIFAM | 3.0 | 1 | 7.57 |
| CHEMBL3288346 | — | — | 1 | 7.50 |
| CHEMBL4091723 | — | — | 1 | 7.30 |
| CHEMBL4101950 | — | — | 1 | 7.24 |
| CHEMBL4066238 | — | — | 1 | 7.09 |
| CHEMBL4087365 | — | — | 1 | 7.09 |
| CHEMBL4091211 | — | — | 1 | 6.96 |
| CHEMBL4083960 | — | — | 1 | 6.68 |
| CHEMBL4094216 | — | — | 1 | 6.68 |
| CHEMBL4080911 | — | — | 1 | 6.62 |
| CHEMBL4088797 | — | — | 1 | 6.39 |
| CHEMBL4071066 | — | — | 1 | 6.35 |
| CHEMBL4065959 | — | — | 1 | 6.24 |
| CHEMBL4083913 | — | — | 1 | 6.19 |
| CHEMBL4102878 | — | — | 1 | 5.70 |
| CHEMBL4063167 | — | — | 1 | 5.63 |
| CHEMBL4092577 | — | — | 1 | 5.62 |
| CHEMBL4064922 | — | — | 1 | 5.57 |
| CHEMBL4073587 | — | — | 1 | 5.41 |
| CHEMBL4065921 | — | — | 1 | 4.83 |
| CHEMBL4093521 | — | — | 1 | 4.83 |
| CHEMBL4074547 | — | — | 1 | 4.49 |
| CHEMBL4063956 | — | — | 1 | 4.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1688486 | — | EC50 | = | 8.0 | nM | 8.10 |
| CHEMBL1829174 | FASIGLIFAM | EC50 | = | 27.0 | nM | 7.57 |
| CHEMBL3288346 | — | EC50 | = | 32.0 | nM | 7.50 |
| CHEMBL4091723 | — | EC50 | = | 50.0 | nM | 7.30 |
| CHEMBL4101950 | — | EC50 | = | 57.0 | nM | 7.24 |
| CHEMBL4066238 | — | EC50 | = | 81.0 | nM | 7.09 |
| CHEMBL4087365 | — | EC50 | = | 82.0 | nM | 7.09 |
| CHEMBL4091211 | — | EC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4083960 | — | EC50 | = | 210.0 | nM | 6.68 |
| CHEMBL4094216 | — | EC50 | = | 210.0 | nM | 6.68 |
| CHEMBL4080911 | — | EC50 | = | 240.0 | nM | 6.62 |
| CHEMBL4088797 | — | EC50 | = | 410.0 | nM | 6.39 |
| CHEMBL4071066 | — | EC50 | = | 450.0 | nM | 6.35 |
| CHEMBL4065959 | — | EC50 | = | 580.0 | nM | 6.24 |
| CHEMBL4083913 | — | EC50 | = | 640.0 | nM | 6.19 |
| CHEMBL4102878 | — | EC50 | = | 2010.0 | nM | 5.70 |
| CHEMBL4063167 | — | EC50 | = | 2320.0 | nM | 5.63 |
| CHEMBL4092577 | — | EC50 | = | 2420.0 | nM | 5.62 |
| CHEMBL4064922 | — | EC50 | = | 2710.0 | nM | 5.57 |
| CHEMBL4073587 | — | EC50 | = | 3920.0 | nM | 5.41 |
| CHEMBL4065921 | — | EC50 | = | 14800.0 | nM | 4.83 |
| CHEMBL4093521 | — | EC50 | = | 14700.0 | nM | 4.83 |
| CHEMBL4074547 | — | EC50 | = | 32200.0 | nM | 4.49 |
| CHEMBL4063956 | — | EC50 | = | 40100.0 | nM | 4.40 |