Assay Detail
Binding
CHEMBL4018946
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of Fluormone-Pan-PPAR Green from human GST-tagged PPARdelta LBD by TR-FRET assay
12
Total Activities
12
Compounds Tested
2
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 delta (CHEMBL3979) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Polypharmacology of N6-(3-Iodobenzyl)adenosine-5'-N-methyluronamide (IB-MECA) and Related A3 Adenosine Receptor Ligands: Peroxisome Proliferator Activated Receptor (PPAR) γ Partial Agonist and PPARδ Antagonist Activity Suggests Their Antidiabetic Potential.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 11 | 9.25 | 10.99 |
| Inhibition | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL387921 | — | — | 1 | 10.99 |
| CHEMBL38943 | GW501516 | 2.0 | 1 | 10.32 |
| CHEMBL200732 | — | — | 1 | 9.80 |
| CHEMBL431733 | NAMODENOSON | 3.0 | 1 | 9.37 |
| CHEMBL227279 | — | — | 1 | 9.21 |
| CHEMBL603424 | — | — | 1 | 8.62 |
| CHEMBL522152 | — | — | 1 | 8.60 |
| CHEMBL594625 | — | — | 1 | 8.58 |
| CHEMBL596014 | — | — | 1 | 8.53 |
| CHEMBL596042 | — | — | 1 | 8.50 |
| CHEMBL413686 | — | — | 1 | - |
| CHEMBL119709 | IB-MECA | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL387921 | — | Ki | = | 0.0102 | nM | 10.99 |
| CHEMBL38943 | GW501516 | Ki | = | 0.048 | nM | 10.32 |
| CHEMBL200732 | — | Ki | = | 0.16 | nM | 9.80 |
| CHEMBL431733 | NAMODENOSON | Ki | = | 0.43 | nM | 9.37 |
| CHEMBL227279 | — | Ki | = | 0.62 | nM | 9.21 |
| CHEMBL603424 | — | Ki | = | 2.37 | nM | 8.62 |
| CHEMBL522152 | — | Ki | = | 2.54 | nM | 8.60 |
| CHEMBL594625 | — | Ki | = | 2.61 | nM | 8.58 |
| CHEMBL596014 | — | Ki | = | 2.98 | nM | 8.53 |
| CHEMBL596042 | — | Ki | = | 3.15 | nM | 8.50 |
| CHEMBL413686 | — | Ki | = | 0.00483 | nM | - |
| CHEMBL119709 | IB-MECA | Inhibition | - | % | - |