Assay Detail
Binding
CHEMBL2379023
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at GAL4-fused PPARgamma (unknown origin) expressed in human HepG2 cells by transactivation assay
25
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HepG2 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Peroxisome proliferator-activated receptor gamma (CHEMBL235) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Molecular determinants for nuclear receptors selectivity: chemometric analysis, dockings and site-directed mutagenesis of dual peroxisome proliferator-activated receptors α/γ agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 25 | 6.02 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL121 | ROSIGLITAZONE | 4.0 | 1 | 8.00 |
| CHEMBL472245 | — | — | 2 | 7.57 |
| CHEMBL472246 | — | — | 1 | 7.31 |
| CHEMBL472451 | — | — | 1 | 7.19 |
| CHEMBL2375948 | — | — | 1 | 6.50 |
| CHEMBL489075 | — | — | 1 | 6.40 |
| CHEMBL471011 | — | — | 1 | 6.38 |
| CHEMBL191275 | — | — | 1 | 6.25 |
| CHEMBL489074 | — | — | 2 | 6.24 |
| CHEMBL192518 | — | — | 1 | 6.05 |
| CHEMBL2375947 | — | — | 1 | 6.04 |
| CHEMBL2375950 | — | — | 1 | 5.90 |
| CHEMBL426632 | — | — | 1 | 5.82 |
| CHEMBL2375951 | — | — | 1 | 5.80 |
| CHEMBL2375949 | — | — | 1 | 5.78 |
| CHEMBL364748 | — | — | 1 | 5.57 |
| CHEMBL191060 | — | — | 1 | 5.44 |
| CHEMBL2375946 | — | — | 1 | 5.15 |
| CHEMBL366157 | — | — | 1 | 5.14 |
| CHEMBL2375952 | — | — | 1 | 5.05 |
| CHEMBL190368 | — | — | 1 | 4.91 |
| CHEMBL371320 | — | — | 1 | 4.70 |
| CHEMBL370054 | — | — | 1 | 4.59 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL121 | ROSIGLITAZONE | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL472245 | — | EC50 | = | 26.92 | nM | 7.57 |
| CHEMBL472246 | — | EC50 | = | 48.98 | nM | 7.31 |
| CHEMBL472451 | — | EC50 | = | 64.57 | nM | 7.19 |
| CHEMBL2375948 | — | EC50 | = | 316.23 | nM | 6.50 |
| CHEMBL472245 | — | EC50 | = | 320.0 | nM | 6.50 |
| CHEMBL489075 | — | EC50 | = | 398.11 | nM | 6.40 |
| CHEMBL471011 | — | EC50 | = | 416.87 | nM | 6.38 |
| CHEMBL191275 | — | EC50 | = | 562.34 | nM | 6.25 |
| CHEMBL489074 | — | EC50 | = | 575.44 | nM | 6.24 |
| CHEMBL489074 | — | EC50 | = | 600.0 | nM | 6.22 |
| CHEMBL192518 | — | EC50 | = | 891.25 | nM | 6.05 |
| CHEMBL2375947 | — | EC50 | = | 912.01 | nM | 6.04 |
| CHEMBL2375950 | — | EC50 | = | 1258.93 | nM | 5.90 |
| CHEMBL426632 | — | EC50 | = | 1513.56 | nM | 5.82 |
| CHEMBL2375951 | — | EC50 | = | 1584.89 | nM | 5.80 |
| CHEMBL2375949 | — | EC50 | = | 1659.59 | nM | 5.78 |
| CHEMBL364748 | — | EC50 | = | 2691.53 | nM | 5.57 |
| CHEMBL191060 | — | EC50 | = | 3630.78 | nM | 5.44 |
| CHEMBL2375946 | — | EC50 | = | 7079.46 | nM | 5.15 |
| CHEMBL366157 | — | EC50 | = | 7244.36 | nM | 5.14 |
| CHEMBL2375952 | — | EC50 | = | 8912.51 | nM | 5.05 |
| CHEMBL190368 | — | EC50 | = | 12302.69 | nM | 4.91 |
| CHEMBL371320 | — | EC50 | = | 19952.62 | nM | 4.70 |
| CHEMBL370054 | — | EC50 | = | 25703.96 | nM | 4.59 |