Assay Detail
Binding
CHEMBL833483
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human Peroxisome proliferator activated receptor alpha
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Peroxisome proliferator-activated receptor alpha (CHEMBL239) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Design and synthesis of N-[(4-methoxyphenoxy)carbonyl]-N-[[4-[2-(5- methyl-2-phenyl-4-oxazolyl)ethoxy]phenyl]methyl]glycine [Muraglitazar/BMS-298585], a novel peroxisome proliferator-activated receptor alpha/gamma dual agonist with efficacious glucose and lipid-lowering activities.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 6.24 | 6.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL186179 | MURAGLITAZAR | 3.0 | 1 | 6.60 |
| CHEMBL248906 | — | — | 1 | 6.27 |
| CHEMBL371120 | — | — | 1 | 5.85 |
| CHEMBL121 | ROSIGLITAZONE | 4.0 | 1 | - |
| CHEMBL981 | FENOFIBRIC ACID | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL186179 | MURAGLITAZAR | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL248906 | — | IC50 | = | 538.0 | nM | 6.27 |
| CHEMBL371120 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL121 | ROSIGLITAZONE | IC50 | > | 100000.0 | nM | - |
| CHEMBL981 | FENOFIBRIC ACID | IC50 | > | 10000.0 | nM | - |