Design of a partial PPARdelta agonist.

Article Details


Pettersson I, Ebdrup S, Havranek M, Pihera P, Korinek M, Mogensen JP, Jeppesen CB, Johansson E, Sauerberg P

Design of a partial PPARdelta agonist.

Bioorg Med Chem Lett. 2007 Aug 15;17(16):4625-9. Epub 2007 May 27.

PubMed ID
17560785 [ View in PubMed

Structure based ligand design was used in order to design a partial agonist for the PPARdelta receptor. The maximum activation in the transactivation assay was reduced from 87% to 39%. The crystal structure of the ligand binding domain of the PPARdelta receptor in complex with compound 2 was determined in order to understand the structural changes which gave rise to the decrease in maximum activation.

DrugBank Data that Cites this Article

NameUniProt ID
Peroxisome proliferator-activated receptor deltaQ03181Details
Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
CardarinePeroxisome proliferator-activated receptor alphaEC 50 (nM)3900N/AN/ADetails
CardarinePeroxisome proliferator-activated receptor deltaEC 50 (nM)8N/AN/ADetails
RosiglitazonePeroxisome proliferator-activated receptor alphaEC 50 (nM)>10000N/AN/ADetails
RosiglitazonePeroxisome proliferator-activated receptor gammaEC 50 (nM)300N/AN/ADetails