Assay Detail
Binding
CHEMBL5265685
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at Gal4-fused human PPAR-gamma ligand binding domain expressed in CHO-K1 cells assessed as receptor transactivation incubated for 24 to 48 hrs by luciferase reporter gene assay
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Peroxisome proliferator-activated receptor gamma (CHEMBL235) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery and structure-activity relationship study of 2-piperazinyl-benzothiazole derivatives as potent and selective PPARδ agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 23 | 6.09 | 7.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5288454 | — | — | 1 | 7.80 |
| CHEMBL5277165 | — | — | 1 | 6.57 |
| CHEMBL5283926 | — | — | 1 | 6.43 |
| CHEMBL5272996 | — | — | 1 | 6.37 |
| CHEMBL5281528 | — | — | 1 | 6.36 |
| CHEMBL5285352 | — | — | 1 | 6.32 |
| CHEMBL5180073 | — | — | 1 | 6.27 |
| CHEMBL5267473 | — | — | 1 | 6.15 |
| CHEMBL5278892 | — | — | 1 | 6.10 |
| CHEMBL5290870 | — | — | 1 | 6.05 |
| CHEMBL5271479 | — | — | 1 | 5.96 |
| CHEMBL5271300 | — | — | 1 | 5.96 |
| CHEMBL5289017 | — | — | 1 | 5.92 |
| CHEMBL5279586 | — | — | 1 | 5.92 |
| CHEMBL5278648 | — | — | 1 | 5.85 |
| CHEMBL5268646 | — | — | 1 | 5.85 |
| CHEMBL5279568 | — | — | 1 | 5.82 |
| CHEMBL5268424 | — | — | 1 | 5.72 |
| CHEMBL5272924 | — | — | 1 | 5.68 |
| CHEMBL5273427 | — | — | 1 | 5.51 |
| CHEMBL38943 | GW501516 | 2.0 | 1 | 5.36 |
| CHEMBL5290260 | — | — | 1 | - |
| CHEMBL5289740 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5288454 | — | EC50 | = | 16.0 | nM | 7.80 |
| CHEMBL5277165 | — | EC50 | = | 270.0 | nM | 6.57 |
| CHEMBL5283926 | — | EC50 | = | 370.0 | nM | 6.43 |
| CHEMBL5272996 | — | EC50 | = | 430.0 | nM | 6.37 |
| CHEMBL5281528 | — | EC50 | = | 440.0 | nM | 6.36 |
| CHEMBL5285352 | — | EC50 | = | 480.0 | nM | 6.32 |
| CHEMBL5180073 | — | EC50 | = | 542.0 | nM | 6.27 |
| CHEMBL5267473 | — | EC50 | = | 710.0 | nM | 6.15 |
| CHEMBL5278892 | — | EC50 | = | 800.0 | nM | 6.10 |
| CHEMBL5290870 | — | EC50 | = | 890.0 | nM | 6.05 |
| CHEMBL5271479 | — | EC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL5271300 | — | EC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL5289017 | — | EC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL5279586 | — | EC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL5278648 | — | EC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL5268646 | — | EC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL5279568 | — | EC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL5268424 | — | EC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL5272924 | — | EC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL5273427 | — | EC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL38943 | GW501516 | EC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL5290260 | — | EC50 | - | — | - | |
| CHEMBL5289740 | — | EC50 | - | — | - |