Assay Detail
Binding
CHEMBL1647802
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at Gal4-fused human PPARdelta DNA binding domain expressed in HEK293 cells by luciferase reporter gene assay
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Peroxisome proliferator-activated receptor delta (CHEMBL3979) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of isoindoline and tetrahydroisoquinoline derivatives as potent, selective PPARδ agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 14 | 7.19 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1643201 | — | — | 1 | 9.30 |
| CHEMBL38943 | GW501516 | 2.0 | 1 | 8.70 |
| CHEMBL1081917 | — | — | 1 | 8.52 |
| CHEMBL1643200 | — | — | 1 | 8.30 |
| CHEMBL1643199 | — | — | 1 | 8.00 |
| CHEMBL1643194 | — | — | 1 | 7.60 |
| CHEMBL1643195 | — | — | 1 | 6.50 |
| CHEMBL1643202 | — | — | 1 | 6.30 |
| CHEMBL1643193 | — | — | 1 | 6.00 |
| CHEMBL1643192 | — | — | 1 | 5.80 |
| CHEMBL1643203 | — | — | 1 | 5.70 |
| CHEMBL1643196 | — | — | 1 | 5.60 |
| CHEMBL1643197 | — | — | 1 | - |
| CHEMBL1643198 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1643201 | — | EC50 | = | 0.5 | nM | 9.30 |
| CHEMBL38943 | GW501516 | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL1081917 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL1643200 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL1643199 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL1643194 | — | EC50 | = | 25.0 | nM | 7.60 |
| CHEMBL1643195 | — | EC50 | = | 320.0 | nM | 6.50 |
| CHEMBL1643202 | — | EC50 | = | 500.0 | nM | 6.30 |
| CHEMBL1643193 | — | EC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL1643192 | — | EC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL1643203 | — | EC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL1643196 | — | EC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL1643197 | — | EC50 | > | 60000.0 | nM | - |
| CHEMBL1643198 | — | EC50 | > | 20000.0 | nM | - |