Assay Detail
Binding
CHEMBL1960410
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at GAL4-tagged human PPARgamma ligand binding domain expressed in HepG2 cells assessed as transactivation after 20 hrs by beta-galactosidase reporter gene assay
21
Total Activities
21
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
Synthesis, biological evaluation and molecular investigation of fluorinated peroxisome proliferator-activated receptors α/γ dual agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 21 | 5.20 | 6.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1956364 | — | — | 1 | 6.30 |
| CHEMBL595 | PIOGLITAZONE | 4.0 | 1 | 6.24 |
| CHEMBL192518 | — | — | 1 | 6.05 |
| CHEMBL1956363 | — | — | 1 | 6.05 |
| CHEMBL1956368 | — | — | 1 | 5.62 |
| CHEMBL1956362 | — | — | 1 | 5.60 |
| CHEMBL1956349 | — | — | 1 | 5.46 |
| CHEMBL1956367 | — | — | 1 | 5.31 |
| CHEMBL1956350 | — | — | 1 | 5.28 |
| CHEMBL1956366 | — | — | 1 | 5.24 |
| CHEMBL364748 | — | — | 1 | 5.02 |
| CHEMBL451321 | METAGLIDASEN | — | 1 | 5.00 |
| CHEMBL1956369 | — | — | 1 | 4.94 |
| CHEMBL1956365 | — | — | 1 | 4.85 |
| CHEMBL1956360 | — | — | 1 | 4.80 |
| CHEMBL1956371 | — | — | 1 | 4.79 |
| CHEMBL1956359 | — | — | 1 | 4.72 |
| CHEMBL1956361 | — | — | 1 | 4.52 |
| CHEMBL1956370 | — | — | 1 | 4.50 |
| CHEMBL1956357 | — | — | 1 | 4.45 |
| CHEMBL1956358 | — | — | 1 | 4.39 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1956364 | — | EC50 | = | 500.0 | nM | 6.30 |
| CHEMBL595 | PIOGLITAZONE | EC50 | = | 570.0 | nM | 6.24 |
| CHEMBL192518 | — | EC50 | = | 900.0 | nM | 6.05 |
| CHEMBL1956363 | — | EC50 | = | 900.0 | nM | 6.05 |
| CHEMBL1956368 | — | EC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL1956362 | — | EC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL1956349 | — | EC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL1956367 | — | EC50 | = | 4900.0 | nM | 5.31 |
| CHEMBL1956350 | — | EC50 | = | 5200.0 | nM | 5.28 |
| CHEMBL1956366 | — | EC50 | = | 5800.0 | nM | 5.24 |
| CHEMBL364748 | — | EC50 | = | 9600.0 | nM | 5.02 |
| CHEMBL451321 | METAGLIDASEN | EC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL1956369 | — | EC50 | = | 11600.0 | nM | 4.94 |
| CHEMBL1956365 | — | EC50 | = | 14100.0 | nM | 4.85 |
| CHEMBL1956360 | — | EC50 | = | 15900.0 | nM | 4.80 |
| CHEMBL1956371 | — | EC50 | = | 16400.0 | nM | 4.79 |
| CHEMBL1956359 | — | EC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL1956361 | — | EC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL1956370 | — | EC50 | = | 32000.0 | nM | 4.50 |
| CHEMBL1956357 | — | EC50 | = | 35200.0 | nM | 4.45 |
| CHEMBL1956358 | — | EC50 | = | 41000.0 | nM | 4.39 |