Novel selective small molecule agonists for peroxisome proliferator-activated receptor delta (PPARdelta)--synthesis and biological activity.
Article Details
- CitationCopy to clipboard
Sznaidman ML, Haffner CD, Maloney PR, Fivush A, Chao E, Goreham D, Sierra ML, LeGrumelec C, Xu HE, Montana VG, Lambert MH, Willson TM, Oliver WR Jr, Sternbach DD
Novel selective small molecule agonists for peroxisome proliferator-activated receptor delta (PPARdelta)--synthesis and biological activity.
Bioorg Med Chem Lett. 2003 May 5;13(9):1517-21.
- PubMed ID
- 12699745 [ View in PubMed]
- Abstract
We report the synthesis and biological activity of a new series of small molecule agonists of the human Peroxisome Proliferator-Activated Receptor delta (PPARdelta). Several hits were identified from our original libraries containing lipophilic carboxylic acids. Optimization of these hits by structure-guided design led to 7k (GW501516) and 7l (GW0742), which shows an EC(50) of 1.1 nM against PPARdelta with 1000-fold selectivity over the other human subtypes.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Cardarine Peroxisome proliferator-activated receptor alpha EC 50 (nM) 1100 N/A N/A Details Cardarine Peroxisome proliferator-activated receptor delta EC 50 (nM) 1 N/A N/A Details Cardarine Peroxisome proliferator-activated receptor delta IC 50 (nM) 1 N/A N/A Details