Assay Detail
Binding
CHEMBL1821157
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Modulation of human PPARgamma-LBD expressed in african green monkey COS7 cells co-transfected with Gal4 assessed as activation of transactivation activity by luciferase assay
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | COS-7 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Peroxisome proliferator-activated receptor gamma (CHEMBL235) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
SAR studies of acidic dual γ-secretase/PPARγ modulators.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 17 | 5.57 | 7.37 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL121 | ROSIGLITAZONE | 4.0 | 1 | 7.37 |
| CHEMBL595 | PIOGLITAZONE | 4.0 | 1 | 6.52 |
| CHEMBL1819481 | — | — | 1 | 5.96 |
| CHEMBL1819483 | — | — | 1 | 5.82 |
| CHEMBL1819397 | — | — | 1 | 5.75 |
| CHEMBL1819394 | — | — | 1 | 5.66 |
| CHEMBL1819482 | — | — | 1 | 5.60 |
| CHEMBL1819392 | — | — | 1 | 5.47 |
| CHEMBL1819393 | — | — | 1 | 5.43 |
| CHEMBL1819390 | — | — | 1 | 5.33 |
| CHEMBL1817687 | — | — | 1 | 5.32 |
| CHEMBL1171834 | — | — | 1 | 5.18 |
| CHEMBL1819478 | — | — | 1 | 5.14 |
| CHEMBL1819391 | — | — | 1 | 5.11 |
| CHEMBL461883 | — | — | 1 | 5.08 |
| CHEMBL1819396 | — | — | 1 | 4.97 |
| CHEMBL1170264 | — | — | 1 | 4.96 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL121 | ROSIGLITAZONE | EC50 | = | 43.0 | nM | 7.37 |
| CHEMBL595 | PIOGLITAZONE | EC50 | = | 300.0 | nM | 6.52 |
| CHEMBL1819481 | — | EC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL1819483 | — | EC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL1819397 | — | EC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL1819394 | — | EC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL1819482 | — | EC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL1819392 | — | EC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL1819393 | — | EC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL1819390 | — | EC50 | = | 4700.0 | nM | 5.33 |
| CHEMBL1817687 | — | EC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL1171834 | — | EC50 | = | 6600.0 | nM | 5.18 |
| CHEMBL1819478 | — | EC50 | = | 7200.0 | nM | 5.14 |
| CHEMBL1819391 | — | EC50 | = | 7800.0 | nM | 5.11 |
| CHEMBL461883 | — | EC50 | = | 8300.0 | nM | 5.08 |
| CHEMBL1819396 | — | EC50 | = | 10800.0 | nM | 4.97 |
| CHEMBL1170264 | — | EC50 | = | 11000.0 | nM | 4.96 |