Assay Detail
Binding
CHEMBL935696
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Binding affinity at human PPARalpha by fluorescence polarization
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| 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 structure-activity relationships of piperidine and dehydropiperidine carboxylic acids as novel, potent dual PPARalpha/gamma agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 6.16 | 7.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL255309 | — | — | 1 | 7.47 |
| CHEMBL403432 | — | — | 1 | 7.31 |
| CHEMBL256142 | — | — | 1 | 7.06 |
| CHEMBL257345 | — | — | 1 | 6.96 |
| CHEMBL256358 | — | — | 1 | 6.89 |
| CHEMBL401534 | — | — | 1 | 6.88 |
| CHEMBL186179 | MURAGLITAZAR | 3.0 | 1 | 6.72 |
| CHEMBL255872 | — | — | 1 | 6.54 |
| CHEMBL257164 | — | — | 1 | 6.35 |
| CHEMBL257165 | — | — | 1 | 5.90 |
| CHEMBL256569 | — | — | 1 | 5.88 |
| CHEMBL255271 | — | — | 1 | 5.86 |
| CHEMBL257180 | — | — | 1 | 5.52 |
| CHEMBL255097 | — | — | 1 | 5.51 |
| CHEMBL256134 | — | — | 1 | 5.35 |
| CHEMBL402956 | — | — | 1 | 5.33 |
| CHEMBL258212 | — | — | 1 | 5.22 |
| CHEMBL255251 | — | — | 1 | 5.13 |
| CHEMBL445942 | — | — | 1 | 5.11 |
| CHEMBL256505 | — | — | 1 | - |
| CHEMBL258428 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL255309 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL403432 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL256142 | — | IC50 | = | 88.0 | nM | 7.06 |
| CHEMBL257345 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL256358 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL401534 | — | IC50 | = | 133.0 | nM | 6.88 |
| CHEMBL186179 | MURAGLITAZAR | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL255872 | — | IC50 | = | 287.0 | nM | 6.54 |
| CHEMBL257164 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL257165 | — | IC50 | = | 1250.0 | nM | 5.90 |
| CHEMBL256569 | — | IC50 | = | 1320.0 | nM | 5.88 |
| CHEMBL255271 | — | IC50 | = | 1384.0 | nM | 5.86 |
| CHEMBL257180 | — | IC50 | = | 3036.0 | nM | 5.52 |
| CHEMBL255097 | — | IC50 | = | 3089.0 | nM | 5.51 |
| CHEMBL256134 | — | IC50 | = | 4510.0 | nM | 5.35 |
| CHEMBL402956 | — | IC50 | = | 4730.0 | nM | 5.33 |
| CHEMBL258212 | — | IC50 | = | 6030.0 | nM | 5.22 |
| CHEMBL255251 | — | IC50 | = | 7400.0 | nM | 5.13 |
| CHEMBL445942 | — | IC50 | = | 7692.0 | nM | 5.11 |
| CHEMBL256505 | — | IC50 | > | 27500.0 | nM | - |
| CHEMBL258428 | — | IC50 | > | 27300.0 | nM | - |