Assay Detail
Functional
CHEMBL5349697
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human GPR40 expressed in HEK293 cells by Fluo4-AM dye based intracellular calcium flux assay
34
Total Activities
34
Compounds Tested
2
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 orally effective and safe GPR40 agonists by incorporating a chiral, rigid and polar sulfoxide into β-position to the carboxylic acid.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 24 | 6.18 | 7.53 |
| Activity | 10 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1829174 | FASIGLIFAM | 3.0 | 1 | 7.53 |
| CHEMBL5422928 | — | — | 1 | 7.34 |
| CHEMBL5410722 | — | — | 1 | 7.32 |
| CHEMBL5430309 | — | — | 1 | 7.20 |
| CHEMBL5406754 | — | — | 1 | 7.18 |
| CHEMBL5397459 | — | — | 1 | 7.12 |
| CHEMBL5414403 | — | — | 1 | 7.04 |
| CHEMBL4209845 | — | — | 1 | 6.60 |
| CHEMBL5432772 | — | — | 1 | 6.34 |
| CHEMBL5429960 | — | — | 1 | 6.20 |
| CHEMBL5435507 | — | — | 1 | 6.14 |
| CHEMBL5412865 | — | — | 1 | 6.12 |
| CHEMBL5423697 | — | — | 1 | 6.00 |
| CHEMBL5419668 | — | — | 1 | 5.87 |
| CHEMBL5415281 | — | — | 1 | 5.70 |
| CHEMBL5409372 | — | — | 1 | 5.70 |
| CHEMBL5438434 | — | — | 1 | 5.54 |
| CHEMBL5422997 | — | — | 1 | 5.51 |
| CHEMBL5417303 | — | — | 1 | 5.45 |
| CHEMBL5395377 | — | — | 1 | 5.40 |
| CHEMBL5436210 | — | — | 1 | 5.31 |
| CHEMBL5422345 | — | — | 1 | 5.27 |
| CHEMBL267476 | LINOLEIC ACID | 2.0 | 1 | 5.22 |
| CHEMBL5435670 | — | — | 1 | 5.19 |
| CHEMBL5439302 | — | — | 1 | - |
| CHEMBL5415122 | — | — | 1 | - |
| CHEMBL5410054 | — | — | 1 | - |
| CHEMBL5412225 | — | — | 1 | - |
| CHEMBL5435028 | — | — | 1 | - |
| CHEMBL5423930 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1829174 | FASIGLIFAM | EC50 | = | 29.5 | nM | 7.53 |
| CHEMBL5422928 | — | EC50 | = | 45.34 | nM | 7.34 |
| CHEMBL5410722 | — | EC50 | = | 47.65 | nM | 7.32 |
| CHEMBL5430309 | — | EC50 | = | 62.79 | nM | 7.20 |
| CHEMBL5406754 | — | EC50 | = | 66.72 | nM | 7.18 |
| CHEMBL5397459 | — | EC50 | = | 75.85 | nM | 7.12 |
| CHEMBL5414403 | — | EC50 | = | 90.15 | nM | 7.04 |
| CHEMBL4209845 | — | EC50 | = | 251.6 | nM | 6.60 |
| CHEMBL5432772 | — | EC50 | = | 453.8 | nM | 6.34 |
| CHEMBL5429960 | — | EC50 | = | 627.0 | nM | 6.20 |
| CHEMBL5435507 | — | EC50 | = | 716.0 | nM | 6.14 |
| CHEMBL5412865 | — | EC50 | = | 755.8 | nM | 6.12 |
| CHEMBL5423697 | — | EC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL5419668 | — | EC50 | = | 1364.0 | nM | 5.87 |
| CHEMBL5409372 | — | EC50 | = | 2004.0 | nM | 5.70 |
| CHEMBL5415281 | — | EC50 | = | 2004.0 | nM | 5.70 |
| CHEMBL5438434 | — | EC50 | = | 2898.0 | nM | 5.54 |
| CHEMBL5422997 | — | EC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL5417303 | — | EC50 | = | 3521.0 | nM | 5.45 |
| CHEMBL5395377 | — | EC50 | = | 3967.0 | nM | 5.40 |
| CHEMBL5436210 | — | EC50 | = | 4885.0 | nM | 5.31 |
| CHEMBL5422345 | — | EC50 | = | 5382.0 | nM | 5.27 |
| CHEMBL267476 | LINOLEIC ACID | EC50 | = | 6043.0 | nM | 5.22 |
| CHEMBL5435670 | — | EC50 | = | 6518.0 | nM | 5.19 |
| CHEMBL5439302 | — | Activity | - | — | - | |
| CHEMBL5415122 | — | Activity | - | — | - | |
| CHEMBL5410054 | — | Activity | - | — | - | |
| CHEMBL5412225 | — | Activity | - | — | - | |
| CHEMBL5435028 | — | Activity | - | — | - | |
| CHEMBL5423930 | — | Activity | - | — | - | |
| CHEMBL5409132 | — | Activity | - | — | - | |
| CHEMBL5405481 | — | Activity | - | — | - | |
| CHEMBL5408131 | — | Activity | - | — | - | |
| CHEMBL5418658 | — | Activity | - | — | - |