Assay Detail
Binding
CHEMBL3399719
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at GAL4-DNA binding domain fused human PPARalpha ligand binding domain expressed in human HepG2 cells assessed as receptor transactivation incubated for 20 hrs by luciferase reporter gene assay
19
Total Activities
19
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 alpha (CHEMBL239) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Design, synthesis and biological evaluation of a class of bioisosteric oximes of the novel dual peroxisome proliferator-activated receptor α/γ ligand LT175.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 19 | 5.58 | 6.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3397563 | — | — | 1 | 6.66 |
| CHEMBL191275 | — | — | 1 | 6.66 |
| CHEMBL3397561 | — | — | 1 | 5.92 |
| CHEMBL3397559 | — | — | 1 | 5.85 |
| CHEMBL295416 | PIRINIXIC ACID | 2.0 | 1 | 5.79 |
| CHEMBL3397562 | — | — | 1 | 5.68 |
| CHEMBL3397558 | — | — | 1 | 5.66 |
| CHEMBL3397556 | — | — | 1 | 5.42 |
| CHEMBL3397552 | — | — | 1 | 5.42 |
| CHEMBL3397553 | — | — | 1 | 5.41 |
| CHEMBL3397555 | — | — | 1 | 5.38 |
| CHEMBL3397560 | — | — | 1 | 5.28 |
| CHEMBL3397549 | — | — | 1 | 5.26 |
| CHEMBL3397557 | — | — | 1 | 5.17 |
| CHEMBL3397551 | — | — | 1 | 5.14 |
| CHEMBL3397550 | — | — | 1 | 5.11 |
| CHEMBL3397548 | — | — | 1 | 5.11 |
| CHEMBL3397554 | — | — | 1 | - |
| CHEMBL121 | ROSIGLITAZONE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3397563 | — | EC50 | = | 220.0 | nM | 6.66 |
| CHEMBL191275 | — | EC50 | = | 220.0 | nM | 6.66 |
| CHEMBL3397561 | — | EC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL3397559 | — | EC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL295416 | PIRINIXIC ACID | EC50 | = | 1620.0 | nM | 5.79 |
| CHEMBL3397562 | — | EC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL3397558 | — | EC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL3397556 | — | EC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL3397552 | — | EC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL3397553 | — | EC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL3397555 | — | EC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL3397560 | — | EC50 | = | 5200.0 | nM | 5.28 |
| CHEMBL3397549 | — | EC50 | = | 5500.0 | nM | 5.26 |
| CHEMBL3397557 | — | EC50 | = | 6800.0 | nM | 5.17 |
| CHEMBL3397551 | — | EC50 | = | 7300.0 | nM | 5.14 |
| CHEMBL3397550 | — | EC50 | = | 7800.0 | nM | 5.11 |
| CHEMBL3397548 | — | EC50 | = | 7750.0 | nM | 5.11 |
| CHEMBL3397554 | — | EC50 | - | — | - | |
| CHEMBL121 | ROSIGLITAZONE | EC50 | - | — | - |