Assay Detail
Functional
CHEMBL4385324
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Agonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of a GPR40 Superagonist: The Impact of Aryl Propionic Acid α-Fluorination.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 10 | 8.67 | 9.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4541658 | — | — | 1 | 9.96 |
| CHEMBL4463571 | — | — | 1 | 9.70 |
| CHEMBL4457303 | — | — | 1 | 9.60 |
| CHEMBL4591657 | — | — | 1 | 9.03 |
| CHEMBL4534836 | — | — | 1 | 8.96 |
| CHEMBL4513748 | — | — | 1 | 8.66 |
| CHEMBL4464769 | — | — | 1 | 8.21 |
| CHEMBL4459220 | — | — | 1 | 7.80 |
| CHEMBL1829174 | FASIGLIFAM | 3.0 | 1 | 7.51 |
| CHEMBL4443853 | — | — | 1 | 7.27 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4541658 | — | EC50 | = | 0.11 | nM | 9.96 |
| CHEMBL4463571 | — | EC50 | = | 0.2 | nM | 9.70 |
| CHEMBL4457303 | — | EC50 | = | 0.25 | nM | 9.60 |
| CHEMBL4591657 | — | EC50 | = | 0.94 | nM | 9.03 |
| CHEMBL4534836 | — | EC50 | = | 1.1 | nM | 8.96 |
| CHEMBL4513748 | — | EC50 | = | 2.2 | nM | 8.66 |
| CHEMBL4464769 | — | EC50 | = | 6.1 | nM | 8.21 |
| CHEMBL4459220 | — | EC50 | = | 16.0 | nM | 7.80 |
| CHEMBL1829174 | FASIGLIFAM | EC50 | = | 31.0 | nM | 7.51 |
| CHEMBL4443853 | — | EC50 | = | 54.0 | nM | 7.27 |