Reaction Details Report a problem with these data
Target
Peroxisome proliferator-activated receptor alpha
Ligand
BDBM28802
Substrate
BDBM10852
Meas. Tech.
Cell-Based Transcription Assay
EC50
145±55 nM
Comments
83 +/- 21 efficacy.
Citation
Mukherjee, R; Locke, KT; Miao, B; Meyers, D; Monshizadegan, H; Zhang, R; Search, D; Grimm, D; Flynn, M; O'Malley, KM; Zhang, L; Li, J; Shi, Y; Kennedy, LJ; Blanar, M; Cheng, PT; Tino, J; Srivastava, 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
More Info.:
Target
Name:
Peroxisome proliferator-activated receptor alpha
Synonyms:
Nr1c1 | Nuclear receptor subfamily 1 group C member 1 | PPAR-alpha | PPARA_MOUSE | Peroxisome Proliferator-Activated Receptor alpha | Ppar | Ppara
Type:
PROTEIN
Mol. Mass.:
52343.28
Organism:
Mus musculus
Description:
ChEMBL_572395
Residue:
468
Sequence:
MVDTESPICPLSPLEADDLESPLSEEFLQEMGNIQEISQSIGEESSGSFGFADYQYLGSCPGSEGSVITDTLSPASSPSSVSCPVIPASTDESPGSALNIECRICGDKASGYHYGVHACEGCKGFFRRTIRLKLVYDKCDRSCKIQKKNRNKCQYCRFHKCLSVGMSHNAIRFGRMPRSEKAKLKAEILTCEHDLKDSETADLKSLGKRIHEAYLKNFNMNKVKARVILAGKTSNNPPFVIHDMETLCMAEKTLVAKMVANGVEDKEAEVRFFHCCQCMSVETVTELTEFAKAIPGFANLDLNDQVTLLKYGVYEAIFTMLSSLMNKDGMLIAYGNGFITREFLKNLRKPFCDIMEPKFDFAMKFNALELDDSDISLFVAAIICCGDRPGLLNIGYIEKLQEGIVHVLKLHLQSNHPDDTFLFPKLLQKMVDLRQLVTEHAQLVQVIKKTESDAALHPLLQEIYRDMY
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
Substrate