Assay Detail
Functional
CHEMBL4151259
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
29
Total Activities
20
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
Structure-Activity Relationship of Novel and Selective Biaryl-Chroman GPR40 AgoPAMs.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 29 | 6.17 | 7.46 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4165147 | — | — | 1 | 7.46 |
| CHEMBL4160527 | — | — | 2 | 7.44 |
| CHEMBL4163182 | — | — | 2 | 7.18 |
| CHEMBL4159416 | — | — | 2 | 6.90 |
| CHEMBL4162778 | — | — | 2 | 6.61 |
| CHEMBL4168422 | — | — | 2 | 6.61 |
| CHEMBL4166625 | — | — | 2 | 6.42 |
| CHEMBL4165008 | — | — | 2 | 6.42 |
| CHEMBL4159022 | — | — | 2 | 6.33 |
| CHEMBL4163916 | — | — | 1 | 6.04 |
| CHEMBL4170346 | — | — | 1 | 5.92 |
| CHEMBL3883407 | — | — | 1 | 5.91 |
| CHEMBL4171104 | — | — | 2 | 5.61 |
| CHEMBL4166943 | — | — | 1 | 5.59 |
| CHEMBL4164618 | — | — | 1 | 5.39 |
| CHEMBL4168048 | — | — | 1 | 5.34 |
| CHEMBL4171391 | — | — | 1 | 5.29 |
| CHEMBL4160127 | — | — | 1 | 5.26 |
| CHEMBL4163496 | — | — | 1 | 5.19 |
| CHEMBL4174833 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4165147 | — | EC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4160527 | — | EC50 | = | 36.0 | nM | 7.44 |
| CHEMBL4163182 | — | EC50 | = | 66.0 | nM | 7.18 |
| CHEMBL4163182 | — | EC50 | = | 105.0 | nM | 6.98 |
| CHEMBL4159416 | — | EC50 | = | 127.0 | nM | 6.90 |
| CHEMBL4159416 | — | EC50 | = | 146.0 | nM | 6.84 |
| CHEMBL4168422 | — | EC50 | = | 243.0 | nM | 6.61 |
| CHEMBL4162778 | — | EC50 | = | 247.0 | nM | 6.61 |
| CHEMBL4160527 | — | EC50 | = | 328.0 | nM | 6.48 |
| CHEMBL4166625 | — | EC50 | = | 382.0 | nM | 6.42 |
| CHEMBL4165008 | — | EC50 | = | 382.0 | nM | 6.42 |
| CHEMBL4159022 | — | EC50 | = | 462.0 | nM | 6.33 |
| CHEMBL4166625 | — | EC50 | = | 521.0 | nM | 6.28 |
| CHEMBL4165008 | — | EC50 | = | 757.0 | nM | 6.12 |
| CHEMBL4159022 | — | EC50 | = | 838.0 | nM | 6.08 |
| CHEMBL4163916 | — | EC50 | = | 920.0 | nM | 6.04 |
| CHEMBL4168422 | — | EC50 | = | 1031.0 | nM | 5.99 |
| CHEMBL4170346 | — | EC50 | = | 1206.0 | nM | 5.92 |
| CHEMBL3883407 | — | EC50 | = | 1227.0 | nM | 5.91 |
| CHEMBL4162778 | — | EC50 | = | 1379.0 | nM | 5.86 |
| CHEMBL4171104 | — | EC50 | = | 2468.0 | nM | 5.61 |
| CHEMBL4166943 | — | EC50 | = | 2561.0 | nM | 5.59 |
| CHEMBL4164618 | — | EC50 | = | 4033.0 | nM | 5.39 |
| CHEMBL4168048 | — | EC50 | = | 4580.0 | nM | 5.34 |
| CHEMBL4171391 | — | EC50 | = | 5174.0 | nM | 5.29 |
| CHEMBL4171104 | — | EC50 | = | 5332.0 | nM | 5.27 |
| CHEMBL4160127 | — | EC50 | = | 5442.0 | nM | 5.26 |
| CHEMBL4163496 | — | EC50 | = | 6431.0 | nM | 5.19 |
| CHEMBL4174833 | — | EC50 | > | 10000.0 | nM | - |