Assay Detail
Functional
CHEMBL4808633
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Agonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assay
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Structure-Activity Relationship Study and Biological Evaluation of 2-(Disubstituted phenyl)-indole-5-propanoic Acid Derivatives as GPR40 Full Agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 24 | 8.50 | 10.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4859651 | — | — | 1 | 10.40 |
| CHEMBL4854804 | — | — | 1 | 9.60 |
| CHEMBL4848974 | — | — | 1 | 9.42 |
| CHEMBL4859407 | — | — | 1 | 9.39 |
| CHEMBL4847662 | — | — | 1 | 9.38 |
| CHEMBL4872298 | — | — | 1 | 9.14 |
| CHEMBL4857550 | — | — | 1 | 9.14 |
| CHEMBL4874972 | — | — | 1 | 8.70 |
| CHEMBL4869870 | — | — | 1 | 8.62 |
| CHEMBL4855306 | — | — | 1 | 8.32 |
| CHEMBL4297471 | MK-8666 | 1.0 | 1 | 8.25 |
| CHEMBL4868224 | — | — | 1 | 7.85 |
| CHEMBL4858086 | — | — | 1 | 7.79 |
| CHEMBL4866406 | — | — | 1 | 7.69 |
| CHEMBL207881 | GW9508 | — | 1 | 7.30 |
| CHEMBL2152070 | — | — | 1 | 6.80 |
| CHEMBL4846948 | — | — | 1 | 6.63 |
| CHEMBL4852865 | — | — | 1 | - |
| CHEMBL4866568 | — | — | 1 | - |
| CHEMBL4877893 | — | — | 1 | - |
| CHEMBL4868676 | — | — | 1 | - |
| CHEMBL4852222 | — | — | 1 | - |
| CHEMBL4865460 | — | — | 1 | - |
| CHEMBL4850966 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4859651 | — | EC50 | = | 0.04 | nM | 10.40 |
| CHEMBL4854804 | — | EC50 | = | 0.25 | nM | 9.60 |
| CHEMBL4848974 | — | EC50 | = | 0.38 | nM | 9.42 |
| CHEMBL4859407 | — | EC50 | = | 0.41 | nM | 9.39 |
| CHEMBL4847662 | — | EC50 | = | 0.417 | nM | 9.38 |
| CHEMBL4872298 | — | EC50 | = | 0.729 | nM | 9.14 |
| CHEMBL4857550 | — | EC50 | = | 0.73 | nM | 9.14 |
| CHEMBL4874972 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4869870 | — | EC50 | = | 2.41 | nM | 8.62 |
| CHEMBL4855306 | — | EC50 | = | 4.78 | nM | 8.32 |
| CHEMBL4297471 | MK-8666 | EC50 | = | 5.6 | nM | 8.25 |
| CHEMBL4868224 | — | EC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4858086 | — | EC50 | = | 16.26 | nM | 7.79 |
| CHEMBL4866406 | — | EC50 | = | 20.59 | nM | 7.69 |
| CHEMBL207881 | GW9508 | EC50 | = | 50.0 | nM | 7.30 |
| CHEMBL2152070 | — | EC50 | = | 160.0 | nM | 6.80 |
| CHEMBL4846948 | — | EC50 | = | 233.0 | nM | 6.63 |
| CHEMBL4852865 | — | EC50 | > | 25.0 | nM | - |
| CHEMBL4866568 | — | EC50 | > | 25.0 | nM | - |
| CHEMBL4877893 | — | EC50 | > | 25.0 | nM | - |
| CHEMBL4868676 | — | EC50 | > | 25.0 | nM | - |
| CHEMBL4852222 | — | EC50 | > | 25.0 | nM | - |
| CHEMBL4865460 | — | EC50 | > | 25.0 | nM | - |
| CHEMBL4850966 | — | EC50 | > | 25.0 | nM | - |