Assay Detail
Functional
CHEMBL1781232
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human PPARdelta-LBD expressed in CV1 cells co-transfected with Gal4 after 40 hrs by luciferase based transactivation assay
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CV-1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Peroxisome proliferator-activated receptor delta (CHEMBL3979) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Biological evaluation of novel benzisoxazole derivatives as PPARδ agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 20 | 6.31 | 8.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL38943 | GW501516 | 2.0 | 1 | 8.77 |
| CHEMBL1778840 | — | — | 1 | 7.96 |
| CHEMBL1778839 | — | — | 1 | 7.68 |
| CHEMBL1644614 | — | — | 1 | 7.60 |
| CHEMBL1778837 | — | — | 1 | 7.00 |
| CHEMBL1778836 | — | — | 1 | 6.16 |
| CHEMBL1777824 | — | — | 1 | 6.05 |
| CHEMBL1778835 | — | — | 1 | 5.92 |
| CHEMBL1778831 | — | — | 1 | 5.89 |
| CHEMBL1778833 | — | — | 1 | 5.70 |
| CHEMBL219586 | GW590735 | 2.0 | 1 | 5.58 |
| CHEMBL1778830 | — | — | 1 | 5.27 |
| CHEMBL1778733 | — | — | 1 | 5.17 |
| CHEMBL1778829 | — | — | 1 | 5.01 |
| CHEMBL1778732 | — | — | 1 | 4.83 |
| CHEMBL1778834 | — | — | 1 | - |
| CHEMBL1778832 | — | — | 1 | - |
| CHEMBL1778838 | — | — | 1 | - |
| CHEMBL121 | ROSIGLITAZONE | 4.0 | 1 | - |
| CHEMBL24458 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL38943 | GW501516 | EC50 | = | 1.7 | nM | 8.77 |
| CHEMBL1778840 | — | EC50 | = | 11.0 | nM | 7.96 |
| CHEMBL1778839 | — | EC50 | = | 21.0 | nM | 7.68 |
| CHEMBL1644614 | — | EC50 | = | 25.0 | nM | 7.60 |
| CHEMBL1778837 | — | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL1778836 | — | EC50 | = | 700.0 | nM | 6.16 |
| CHEMBL1777824 | — | EC50 | = | 900.0 | nM | 6.05 |
| CHEMBL1778835 | — | EC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL1778831 | — | EC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL1778833 | — | EC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL219586 | GW590735 | EC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL1778830 | — | EC50 | = | 5400.0 | nM | 5.27 |
| CHEMBL1778733 | — | EC50 | = | 6700.0 | nM | 5.17 |
| CHEMBL1778829 | — | EC50 | = | 9800.0 | nM | 5.01 |
| CHEMBL1778732 | — | EC50 | = | 14900.0 | nM | 4.83 |
| CHEMBL1778834 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL1778832 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL1778838 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL121 | ROSIGLITAZONE | EC50 | > | 10000.0 | nM | - |
| CHEMBL24458 | — | EC50 | > | 10000.0 | nM | - |