Assay Detail
Binding
CHEMBL5349699
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Agonist activity at human GPR40/Galpha-16 expressed in HEK293 cells by Fluo4-AM dye based intracellular calcium flux assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 7 — Homologous 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 | 4 | 6.76 | 7.56 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5422928 | — | — | 1 | 7.56 |
| CHEMBL1829174 | FASIGLIFAM | 3.0 | 1 | 7.45 |
| CHEMBL2151289 | — | — | 1 | 7.03 |
| CHEMBL267476 | LINOLEIC ACID | 2.0 | 1 | 5.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5422928 | — | EC50 | = | 27.4 | nM | 7.56 |
| CHEMBL1829174 | FASIGLIFAM | EC50 | = | 35.8 | nM | 7.45 |
| CHEMBL2151289 | — | EC50 | = | 93.3 | nM | 7.03 |
| CHEMBL267476 | LINOLEIC ACID | EC50 | = | 10100.0 | nM | 5.00 |