Assay Detail
Binding
CHEMBL3366032
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Activation of human PPARgamma ligand binding domain expressed in COS7 cells by luciferase reporter gene assay
19
Total Activities
19
Compounds Tested
2
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
Identification of pirinixic acid derivatives bearing a 2-aminothiazole moiety combines dual PPARα/γ activation and dual 5-LO/mPGES-1 inhibition.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 13 | 5.41 | 5.89 |
| IC50 | 6 | 5.27 | 5.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3094412 | — | — | 1 | 5.89 |
| CHEMBL456792 | — | — | 1 | 5.82 |
| CHEMBL3094425 | — | — | 1 | 5.64 |
| CHEMBL3094415 | — | — | 1 | 5.54 |
| CHEMBL3094417 | — | — | 1 | 5.47 |
| CHEMBL459721 | — | — | 1 | 5.46 |
| CHEMBL518038 | — | — | 1 | 5.44 |
| CHEMBL3094416 | — | — | 1 | 5.44 |
| CHEMBL518507 | — | — | 1 | 5.43 |
| CHEMBL3094410 | — | — | 1 | 5.43 |
| CHEMBL3094426 | — | — | 1 | 5.42 |
| CHEMBL3094433 | — | — | 1 | 5.41 |
| CHEMBL3094418 | — | — | 1 | 5.39 |
| CHEMBL3091498 | — | — | 1 | 5.24 |
| CHEMBL455936 | — | — | 1 | 5.21 |
| CHEMBL3094431 | — | — | 1 | 5.19 |
| CHEMBL3091499 | — | — | 1 | 5.14 |
| CHEMBL3094432 | — | — | 1 | 5.12 |
| CHEMBL295416 | PIRINIXIC ACID | 2.0 | 1 | 4.27 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3094412 | — | EC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL456792 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL3094425 | — | EC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL3094415 | — | EC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL3094417 | — | EC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL459721 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL518038 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL3094416 | — | EC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL518507 | — | IC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL3094410 | — | EC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL3094426 | — | EC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL3094433 | — | EC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL3094418 | — | EC50 | = | 4100.0 | nM | 5.39 |
| CHEMBL3091498 | — | EC50 | = | 5700.0 | nM | 5.24 |
| CHEMBL455936 | — | IC50 | = | 6200.0 | nM | 5.21 |
| CHEMBL3094431 | — | EC50 | = | 6400.0 | nM | 5.19 |
| CHEMBL3091499 | — | EC50 | = | 7200.0 | nM | 5.14 |
| CHEMBL3094432 | — | EC50 | = | 7600.0 | nM | 5.12 |
| CHEMBL295416 | PIRINIXIC ACID | IC50 | = | 53700.0 | nM | 4.27 |