Assay Detail
Functional
CHEMBL986146
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human PPARalpha expressed in african green monkey CV-1 by 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 alpha (CHEMBL239) ↗| 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 | 5.50 | 7.19 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL522754 | — | — | 1 | 7.19 |
| CHEMBL489769 | — | — | 1 | 6.48 |
| CHEMBL514544 | — | — | 1 | 6.27 |
| CHEMBL489178 | — | — | 1 | 6.21 |
| CHEMBL489768 | — | — | 1 | 6.06 |
| CHEMBL490401 | — | — | 1 | 5.95 |
| CHEMBL489172 | — | — | 1 | 5.95 |
| CHEMBL490402 | — | — | 1 | 5.94 |
| CHEMBL523944 | — | — | 1 | 5.77 |
| CHEMBL513886 | — | — | 1 | 5.76 |
| CHEMBL489171 | — | — | 1 | 5.68 |
| CHEMBL489363 | — | — | 1 | 5.65 |
| CHEMBL489377 | — | — | 1 | 5.52 |
| CHEMBL282686 | TESAGLITAZAR | 3.0 | 1 | 5.51 |
| CHEMBL477801 | — | — | 1 | 5.51 |
| CHEMBL475916 | — | — | 1 | 5.49 |
| CHEMBL516274 | — | — | 1 | 5.47 |
| CHEMBL121 | ROSIGLITAZONE | 4.0 | 1 | 5.46 |
| CHEMBL491622 | — | — | 1 | 5.43 |
| CHEMBL491596 | — | — | 1 | 5.41 |
| CHEMBL186179 | MURAGLITAZAR | 3.0 | 1 | 5.39 |
| CHEMBL478675 | — | — | 1 | 5.22 |
| CHEMBL475915 | — | — | 1 | 5.15 |
| CHEMBL490395 | — | — | 1 | 5.12 |
| CHEMBL523649 | — | — | 1 | 5.12 |
| CHEMBL514871 | — | — | 1 | 5.11 |
| CHEMBL491423 | — | — | 1 | 5.07 |
| CHEMBL491623 | — | — | 1 | 5.01 |
| CHEMBL489591 | — | — | 1 | 5.01 |
| CHEMBL492031 | — | — | 1 | 4.99 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL522754 | — | EC50 | = | 64.0 | nM | 7.19 |
| CHEMBL489769 | — | EC50 | = | 331.0 | nM | 6.48 |
| CHEMBL514544 | — | EC50 | = | 542.0 | nM | 6.27 |
| CHEMBL489178 | — | EC50 | = | 615.0 | nM | 6.21 |
| CHEMBL489768 | — | EC50 | = | 868.0 | nM | 6.06 |
| CHEMBL490401 | — | EC50 | = | 1120.0 | nM | 5.95 |
| CHEMBL489172 | — | EC50 | = | 1120.0 | nM | 5.95 |
| CHEMBL490402 | — | EC50 | = | 1150.0 | nM | 5.94 |
| CHEMBL523944 | — | EC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL513886 | — | EC50 | = | 1730.0 | nM | 5.76 |
| CHEMBL489171 | — | EC50 | = | 2080.0 | nM | 5.68 |
| CHEMBL489363 | — | EC50 | = | 2230.0 | nM | 5.65 |
| CHEMBL489377 | — | EC50 | = | 2990.0 | nM | 5.52 |
| CHEMBL282686 | TESAGLITAZAR | EC50 | = | 3120.0 | nM | 5.51 |
| CHEMBL477801 | — | EC50 | = | 3120.0 | nM | 5.51 |
| CHEMBL475916 | — | EC50 | = | 3240.0 | nM | 5.49 |
| CHEMBL516274 | — | EC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL121 | ROSIGLITAZONE | EC50 | = | 3460.0 | nM | 5.46 |
| CHEMBL491622 | — | EC50 | = | 3670.0 | nM | 5.43 |
| CHEMBL491596 | — | EC50 | = | 3860.0 | nM | 5.41 |
| CHEMBL186179 | MURAGLITAZAR | EC50 | = | 4110.0 | nM | 5.39 |
| CHEMBL478675 | — | EC50 | = | 5980.0 | nM | 5.22 |
| CHEMBL475915 | — | EC50 | = | 7070.0 | nM | 5.15 |
| CHEMBL490395 | — | EC50 | = | 7580.0 | nM | 5.12 |
| CHEMBL523649 | — | EC50 | = | 7670.0 | nM | 5.12 |
| CHEMBL514871 | — | EC50 | = | 7720.0 | nM | 5.11 |
| CHEMBL491423 | — | EC50 | = | 8580.0 | nM | 5.07 |
| CHEMBL491623 | — | EC50 | = | 9800.0 | nM | 5.01 |
| CHEMBL489591 | — | EC50 | = | 9790.0 | nM | 5.01 |
| CHEMBL492031 | — | EC50 | = | 10200.0 | nM | 4.99 |
| CHEMBL489364 | — | EC50 | = | 11300.0 | nM | 4.95 |
| CHEMBL489563 | — | EC50 | = | 17300.0 | nM | 4.76 |
| CHEMBL491606 | — | EC50 | = | 18100.0 | nM | 4.74 |
| CHEMBL491597 | — | EC50 | = | 25480.0 | nM | 4.59 |