Assay Detail
Binding
CHEMBL4344578
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Binding affinity to His-tagged PPARalpha LBD (unknown origin) expressed in Escherichia coli Rosetta (DE3) at 25 degree C by isothermal titration calorimetry
4
Total Activities
4
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
Evolution of a 4-Benzyloxy-benzylamino Chemotype to Provide Efficacious, Potent, and Isoform Selective PPARα Agonists as Leads for Retinal Disorders.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 4 | 5.92 | 6.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4463341 | — | — | 1 | 6.85 |
| CHEMBL219586 | GW590735 | 2.0 | 1 | 6.77 |
| CHEMBL4564731 | — | — | 1 | 5.27 |
| CHEMBL4237449 | — | — | 1 | 4.77 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4463341 | — | Kd | = | 140.0 | nM | 6.85 |
| CHEMBL219586 | GW590735 | Kd | = | 170.0 | nM | 6.77 |
| CHEMBL4564731 | — | Kd | = | 5320.0 | nM | 5.27 |
| CHEMBL4237449 | — | Kd | = | 16900.0 | nM | 4.77 |