Assay Detail
Functional
CHEMBL1116167
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Agonist activity at PPARgamma assessed as transcriptional activation
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Peroxisome proliferator-activated receptor gamma (CHEMBL235) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of a novel selective PPARgamma modulator from (-)-Cercosporamide derivatives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 23 | 5.95 | 7.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL121 | ROSIGLITAZONE | 4.0 | 1 | 7.96 |
| CHEMBL595 | PIOGLITAZONE | 4.0 | 1 | 7.06 |
| CHEMBL1092387 | — | — | 1 | 6.75 |
| CHEMBL1090521 | — | — | 1 | 6.66 |
| CHEMBL1092634 | — | — | 1 | 6.55 |
| CHEMBL1092559 | — | — | 1 | 6.25 |
| CHEMBL1091572 | — | — | 1 | 6.11 |
| CHEMBL1092855 | — | — | 1 | 5.92 |
| CHEMBL1090550 | — | — | 1 | 5.80 |
| CHEMBL1090549 | — | — | 1 | 5.77 |
| CHEMBL1089120 | — | — | 1 | 5.64 |
| CHEMBL1090870 | — | — | 1 | 5.62 |
| CHEMBL1092854 | — | — | 1 | 5.50 |
| CHEMBL1089859 | — | — | 1 | 5.42 |
| CHEMBL1089121 | — | — | 1 | 5.42 |
| CHEMBL1091530 | — | — | 1 | 5.36 |
| CHEMBL1092633 | — | — | 1 | 5.22 |
| CHEMBL1092900 | — | — | 1 | 5.17 |
| CHEMBL1092876 | — | — | 1 | 4.96 |
| CHEMBL1089802 | — | — | 1 | - |
| CHEMBL1092388 | — | — | 1 | - |
| CHEMBL1091573 | — | — | 1 | - |
| CHEMBL1089858 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL121 | ROSIGLITAZONE | EC50 | = | 11.0 | nM | 7.96 |
| CHEMBL595 | PIOGLITAZONE | EC50 | = | 88.0 | nM | 7.06 |
| CHEMBL1092387 | — | EC50 | = | 180.0 | nM | 6.75 |
| CHEMBL1090521 | — | EC50 | = | 220.0 | nM | 6.66 |
| CHEMBL1092634 | — | EC50 | = | 280.0 | nM | 6.55 |
| CHEMBL1092559 | — | EC50 | = | 560.0 | nM | 6.25 |
| CHEMBL1091572 | — | EC50 | = | 770.0 | nM | 6.11 |
| CHEMBL1092855 | — | EC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL1090550 | — | EC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL1090549 | — | EC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL1089120 | — | EC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL1090870 | — | EC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL1092854 | — | EC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL1089859 | — | EC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL1089121 | — | EC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL1091530 | — | EC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL1092633 | — | EC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL1092900 | — | EC50 | = | 6700.0 | nM | 5.17 |
| CHEMBL1092876 | — | EC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL1089802 | — | EC50 | - | — | - | |
| CHEMBL1092388 | — | EC50 | - | — | - | |
| CHEMBL1091573 | — | EC50 | - | — | - | |
| CHEMBL1089858 | — | EC50 | - | — | - |