Target
Peroxisome proliferator-activated receptor alpha
Ligand
BDBM28802
Substrate
BDBM10852
Meas. Tech.
Cell-Based Transcription Assay
EC50
123±10 nM
Comments
82 +/- 5 efficacy.
Citation
 Mukherjee, RLocke, KTMiao, BMeyers, DMonshizadegan, HZhang, RSearch, DGrimm, DFlynn, MO'Malley, KMZhang, LLi, JShi, YKennedy, LJBlanar, MCheng, PTTino, JSrivastava, RA Novel peroxisome proliferator-activated receptor alpha agonists lower low-density lipoprotein and triglycerides, raise high-density lipoprotein, and synergistically increase cholesterol excretion with a liver X receptor agonist. J Pharmacol Exp Ther 327:716-26 (2008) [PubMed]  Article 
Target
Name:
Peroxisome proliferator-activated receptor alpha
Synonyms:
Nr1c1 | Nuclear receptor subfamily 1 group C member 1 | PPAR-alpha | PPARA_RAT | Peroxisome Proliferator-Activated Receptor alpha | Ppar | Ppara
Type:
PROTEIN
Mol. Mass.:
52374.28
Organism:
Rattus norvegicus
Description:
ChEMBL_834194
Residue:
468
Sequence:
MVDTESPICPLSPLEADDLESPLSEEFLQEMGNIQEISQSLGEESSGSFSFADYQYLGSCPGSEGSVITDTLSPASSPSSVSCPAVPTSTDESPGNALNIECRICGDKASGYHYGVHACEGCKGFFRRTIRLKLAYDKCDRSCKIQKKNRNKCQYCRFHKCLSVGMSHNAIRFGRMPRSEKAKLKAEILTCEHDLKDSETADLKSLAKRIHEAYLKNFNMNKVKARVILAGKTSNNPPFVIHDMETLCMAEKTLVAKMVANGVENKEAEVRFFHCCQCMSVETVTELTEFAKAIPGFANLDLNDQVTLLKYGVYEAIFTMLSSLMNKDGMLIAYGNGFITREFLKNLRKPFCDIMEPKFDFAMKFNALELDDSDISLFVAAIICCGDRPGLLNIGYIEKLQEGIVHVLKLHLQSNHPDDTFLFPKLLQKMVDLRQLVTEHAQLVQVIKKTESDAALHPLLQEIYRDMY
  
Inhibitor
Name:
BDBM28802
Synonyms:
2-{[(5-{[2-(4-chlorophenyl)-5-methyl-1,3-oxazol-4-yl]methoxy}-2-fluorophenyl)methyl](methoxycarbonyl)amino}acetic acid | BMS-711939
Type:
Small organic molecule
Emp. Form.:
C22H20ClFN2O6
Mol. Mass.:
462.855
SMILES:
COC(=O)N(CC(O)=O)Cc1cc(OCc2nc(oc2C)-c2ccc(Cl)cc2)ccc1F
Structure:
Search PDB for entries with ligand similarity:
Substrate