Assay Detail
Functional
CHEMBL2166571
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Agonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilization
8
Total Activities
7
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
Free fatty acid receptor 1 (FFA1/GPR40) agonists: mesylpropoxy appendage lowers lipophilicity and improves ADME properties.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 8 | 7.74 | 8.04 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2164242 | — | — | 1 | 8.04 |
| CHEMBL2164239 | — | — | 1 | 8.03 |
| CHEMBL2164241 | — | — | 1 | 7.75 |
| CHEMBL1773261 | — | — | 1 | 7.73 |
| CHEMBL2163923 | — | — | 2 | 7.66 |
| CHEMBL2164240 | — | — | 1 | 7.63 |
| CHEMBL1688473 | — | — | 1 | 7.46 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2164242 | — | EC50 | = | 9.12 | nM | 8.04 |
| CHEMBL2164239 | — | EC50 | = | 9.333 | nM | 8.03 |
| CHEMBL2164241 | — | EC50 | = | 17.78 | nM | 7.75 |
| CHEMBL1773261 | — | EC50 | = | 18.62 | nM | 7.73 |
| CHEMBL2163923 | — | EC50 | = | 21.88 | nM | 7.66 |
| CHEMBL2164240 | — | EC50 | = | 23.44 | nM | 7.63 |
| CHEMBL2163923 | — | EC50 | = | 26.0 | nM | 7.58 |
| CHEMBL1688473 | — | EC50 | = | 34.67 | nM | 7.46 |