Assay Detail
Functional
CHEMBL986147
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human PPARgamma expressed in african green monkey CV-1 co-transfected with GAL4 by by dual-glo luciferase reporter gene assay
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Peroxisome proliferator-activated receptor gamma (CHEMBL235) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Design, synthesis, and evaluation of novel aryl-tetrahydropyridine PPARalpha/gamma dual agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 34 | 5.79 | 7.48 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL121 | ROSIGLITAZONE | 4.0 | 1 | 7.48 |
| CHEMBL186179 | MURAGLITAZAR | 3.0 | 1 | 6.82 |
| CHEMBL489171 | — | — | 1 | 6.76 |
| CHEMBL489364 | — | — | 1 | 6.40 |
| CHEMBL489591 | — | — | 1 | 6.30 |
| CHEMBL513886 | — | — | 1 | 6.19 |
| CHEMBL522754 | — | — | 1 | 6.18 |
| CHEMBL490402 | — | — | 1 | 6.17 |
| CHEMBL490395 | — | — | 1 | 6.16 |
| CHEMBL282686 | TESAGLITAZAR | 3.0 | 1 | 6.15 |
| CHEMBL489172 | — | — | 1 | 6.15 |
| CHEMBL523944 | — | — | 1 | 6.14 |
| CHEMBL489178 | — | — | 1 | 6.06 |
| CHEMBL489377 | — | — | 1 | 5.85 |
| CHEMBL490401 | — | — | 1 | 5.84 |
| CHEMBL475916 | — | — | 1 | 5.78 |
| CHEMBL516274 | — | — | 1 | 5.72 |
| CHEMBL475915 | — | — | 1 | 5.69 |
| CHEMBL478675 | — | — | 1 | 5.67 |
| CHEMBL477801 | — | — | 1 | 5.65 |
| CHEMBL492031 | — | — | 1 | 5.64 |
| CHEMBL491623 | — | — | 1 | 5.63 |
| CHEMBL489563 | — | — | 1 | 5.62 |
| CHEMBL491423 | — | — | 1 | 5.48 |
| CHEMBL489363 | — | — | 1 | 5.43 |
| CHEMBL491606 | — | — | 1 | 5.41 |
| CHEMBL523649 | — | — | 1 | 5.34 |
| CHEMBL491597 | — | — | 1 | 5.31 |
| CHEMBL491596 | — | — | 1 | 5.28 |
| CHEMBL514871 | — | — | 1 | 5.23 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL121 | ROSIGLITAZONE | EC50 | = | 33.0 | nM | 7.48 |
| CHEMBL186179 | MURAGLITAZAR | EC50 | = | 153.0 | nM | 6.82 |
| CHEMBL489171 | — | EC50 | = | 174.0 | nM | 6.76 |
| CHEMBL489364 | — | EC50 | = | 396.0 | nM | 6.40 |
| CHEMBL489591 | — | EC50 | = | 504.0 | nM | 6.30 |
| CHEMBL513886 | — | EC50 | = | 639.0 | nM | 6.19 |
| CHEMBL522754 | — | EC50 | = | 661.0 | nM | 6.18 |
| CHEMBL490402 | — | EC50 | = | 670.0 | nM | 6.17 |
| CHEMBL490395 | — | EC50 | = | 689.0 | nM | 6.16 |
| CHEMBL282686 | TESAGLITAZAR | EC50 | = | 704.0 | nM | 6.15 |
| CHEMBL489172 | — | EC50 | = | 706.0 | nM | 6.15 |
| CHEMBL523944 | — | EC50 | = | 728.0 | nM | 6.14 |
| CHEMBL489178 | — | EC50 | = | 862.0 | nM | 6.06 |
| CHEMBL489377 | — | EC50 | = | 1420.0 | nM | 5.85 |
| CHEMBL490401 | — | EC50 | = | 1440.0 | nM | 5.84 |
| CHEMBL475916 | — | EC50 | = | 1670.0 | nM | 5.78 |
| CHEMBL516274 | — | EC50 | = | 1890.0 | nM | 5.72 |
| CHEMBL475915 | — | EC50 | = | 2060.0 | nM | 5.69 |
| CHEMBL478675 | — | EC50 | = | 2150.0 | nM | 5.67 |
| CHEMBL477801 | — | EC50 | = | 2230.0 | nM | 5.65 |
| CHEMBL492031 | — | EC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL491623 | — | EC50 | = | 2320.0 | nM | 5.63 |
| CHEMBL489563 | — | EC50 | = | 2380.0 | nM | 5.62 |
| CHEMBL491423 | — | EC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL489363 | — | EC50 | = | 3720.0 | nM | 5.43 |
| CHEMBL491606 | — | EC50 | = | 3930.0 | nM | 5.41 |
| CHEMBL523649 | — | EC50 | = | 4600.0 | nM | 5.34 |
| CHEMBL491597 | — | EC50 | = | 4880.0 | nM | 5.31 |
| CHEMBL491596 | — | EC50 | = | 5290.0 | nM | 5.28 |
| CHEMBL514871 | — | EC50 | = | 5830.0 | nM | 5.23 |
| CHEMBL514544 | — | EC50 | = | 7560.0 | nM | 5.12 |
| CHEMBL491622 | — | EC50 | = | 12600.0 | nM | 4.90 |
| CHEMBL489769 | — | EC50 | = | 18760.0 | nM | 4.73 |
| CHEMBL489768 | — | EC50 | = | 22830.0 | nM | 4.64 |