Assay Detail
Functional
CHEMBL4154326
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium mobilization by Fluo-8 dye based fluorescence assay
39
Total Activities
39
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
Design, synthesis and structure-activity relationship studies of GPR40 agonists containing amide linker.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 39 | 6.86 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4167323 | — | — | 1 | 7.70 |
| CHEMBL4166892 | — | — | 1 | 7.41 |
| CHEMBL4174136 | — | — | 1 | 7.38 |
| CHEMBL4172828 | — | — | 1 | 7.33 |
| CHEMBL4166397 | — | — | 1 | 7.30 |
| CHEMBL4175272 | — | — | 1 | 7.27 |
| CHEMBL4165046 | — | — | 1 | 7.24 |
| CHEMBL4159848 | — | — | 1 | 7.14 |
| CHEMBL4175666 | — | — | 1 | 7.10 |
| CHEMBL4168467 | — | — | 1 | 7.03 |
| CHEMBL4163958 | — | — | 1 | 7.01 |
| CHEMBL4176612 | — | — | 1 | 6.97 |
| CHEMBL4172250 | — | — | 1 | 6.96 |
| CHEMBL4171827 | — | — | 1 | 6.95 |
| CHEMBL4162561 | — | — | 1 | 6.94 |
| CHEMBL4177506 | — | — | 1 | 6.88 |
| CHEMBL4167397 | — | — | 1 | 6.88 |
| CHEMBL3915620 | LY2881835 | 1.0 | 1 | 6.87 |
| CHEMBL4173953 | — | — | 1 | 6.86 |
| CHEMBL4163436 | — | — | 1 | 6.84 |
| CHEMBL4167766 | — | — | 1 | 6.81 |
| CHEMBL4173085 | — | — | 1 | 6.76 |
| CHEMBL4165184 | — | — | 1 | 6.75 |
| CHEMBL4160566 | — | — | 1 | 6.73 |
| CHEMBL4173246 | — | — | 1 | 6.69 |
| CHEMBL4170517 | — | — | 1 | 6.68 |
| CHEMBL4167970 | — | — | 1 | 6.64 |
| CHEMBL4175826 | — | — | 1 | 6.54 |
| CHEMBL4166005 | — | — | 1 | 6.51 |
| CHEMBL4162588 | — | — | 1 | 6.38 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4167323 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4166892 | — | EC50 | = | 39.0 | nM | 7.41 |
| CHEMBL4174136 | — | EC50 | = | 42.0 | nM | 7.38 |
| CHEMBL4172828 | — | EC50 | = | 47.0 | nM | 7.33 |
| CHEMBL4166397 | — | EC50 | = | 50.0 | nM | 7.30 |
| CHEMBL4175272 | — | EC50 | = | 54.0 | nM | 7.27 |
| CHEMBL4165046 | — | EC50 | = | 57.0 | nM | 7.24 |
| CHEMBL4159848 | — | EC50 | = | 72.0 | nM | 7.14 |
| CHEMBL4175666 | — | EC50 | = | 80.0 | nM | 7.10 |
| CHEMBL4168467 | — | EC50 | = | 94.0 | nM | 7.03 |
| CHEMBL4163958 | — | EC50 | = | 97.0 | nM | 7.01 |
| CHEMBL4176612 | — | EC50 | = | 106.0 | nM | 6.97 |
| CHEMBL4172250 | — | EC50 | = | 109.0 | nM | 6.96 |
| CHEMBL4171827 | — | EC50 | = | 113.0 | nM | 6.95 |
| CHEMBL4162561 | — | EC50 | = | 114.0 | nM | 6.94 |
| CHEMBL4177506 | — | EC50 | = | 133.0 | nM | 6.88 |
| CHEMBL4167397 | — | EC50 | = | 133.0 | nM | 6.88 |
| CHEMBL3915620 | LY2881835 | EC50 | = | 134.0 | nM | 6.87 |
| CHEMBL4173953 | — | EC50 | = | 138.0 | nM | 6.86 |
| CHEMBL4163436 | — | EC50 | = | 144.0 | nM | 6.84 |
| CHEMBL4167766 | — | EC50 | = | 155.0 | nM | 6.81 |
| CHEMBL4173085 | — | EC50 | = | 172.0 | nM | 6.76 |
| CHEMBL4165184 | — | EC50 | = | 179.0 | nM | 6.75 |
| CHEMBL4160566 | — | EC50 | = | 187.0 | nM | 6.73 |
| CHEMBL4173246 | — | EC50 | = | 203.0 | nM | 6.69 |
| CHEMBL4170517 | — | EC50 | = | 211.0 | nM | 6.68 |
| CHEMBL4167970 | — | EC50 | = | 231.0 | nM | 6.64 |
| CHEMBL4175826 | — | EC50 | = | 289.0 | nM | 6.54 |
| CHEMBL4166005 | — | EC50 | = | 308.0 | nM | 6.51 |
| CHEMBL4162588 | — | EC50 | = | 417.0 | nM | 6.38 |
| CHEMBL4174315 | — | EC50 | = | 531.0 | nM | 6.28 |
| CHEMBL4161630 | — | EC50 | = | 610.0 | nM | 6.21 |
| CHEMBL4172853 | — | EC50 | = | 820.0 | nM | 6.09 |
| CHEMBL4169459 | — | EC50 | = | 1136.0 | nM | 5.95 |
| CHEMBL4162180 | — | EC50 | > | 5000.0 | nM | - |
| CHEMBL4177310 | — | EC50 | > | 5000.0 | nM | - |
| CHEMBL4169432 | — | EC50 | > | 1667.0 | nM | - |
| CHEMBL4161498 | — | EC50 | > | 1667.0 | nM | - |
| CHEMBL4164920 | — | EC50 | > | 5000.0 | nM | - |