Target
Peroxisome proliferator-activated receptor alpha
Ligand
BDBM28681
Substrate
BDBM33283
Meas. Tech.
Scintillation Proximity Assay (IC50) and PPAR alpha Transactivation Assay (EC50)
pH
7.2±n/a
Temperature
288.15±n/a K
EC50
>12000±n/a nM
Comments
21% inhibition @ 10 uM.Efficacy=23% (The maximum efficacy of GW9578 was defined as 100%).
Citation
 Casimiro-Garcia, ABigge, CFDavis, JAPadalino, TPulaski, JOhren, JFMcConnell, PKane, CDRoyer, LJStevens, KAAuerbach, BCollard, WMcGregor, CSong, K Synthesis and evaluation of novel alpha-heteroaryl-phenylpropanoic acid derivatives as PPARalpha/gamma dual agonists. Bioorg Med Chem 17:7113-25 (2009) [PubMed]  Article 
Target
Name:
Peroxisome proliferator-activated receptor alpha
Synonyms:
NR1C1 | Nuclear receptor subfamily 1 group C member 1 | PPAR | PPAR alpha/gamma | PPAR-alpha | PPARA | PPARA_HUMAN | Peroxisome Proliferator-Activated Receptor alpha | Peroxisome proliferator-activated receptor | Peroxisome proliferator-activated receptor alpha (PPAR alpha)
Type:
Enzyme
Mol. Mass.:
52222.08
Organism:
Homo sapiens (Human)
Description:
Q07869
Residue:
468
Sequence:
MVDTESPLCPLSPLEAGDLESPLSEEFLQEMGNIQEISQSIGEDSSGSFGFTEYQYLGSCPGSDGSVITDTLSPASSPSSVTYPVVPGSVDESPSGALNIECRICGDKASGYHYGVHACEGCKGFFRRTIRLKLVYDKCDRSCKIQKKNRNKCQYCRFHKCLSVGMSHNAIRFGRMPRSEKAKLKAEILTCEHDIEDSETADLKSLAKRIYEAYLKNFNMNKVKARVILSGKASNNPPFVIHDMETLCMAEKTLVAKLVANGIQNKEAEVRIFHCCQCTSVETVTELTEFAKAIPGFANLDLNDQVTLLKYGVYEAIFAMLSSVMNKDGMLVAYGNGFITREFLKSLRKPFCDIMEPKFDFAMKFNALELDDSDISLFVAAIICCGDRPGLLNVGHIEKMQEGIVHVLRLHLQSNHPDDIFLFPKLLQKMADLRQLVTEHAQLVQIIKKTESDAALHPLLQEIYRDMY
  
Inhibitor
Name:
BDBM28681
Synonyms:
5-[(4-{2-[methyl(pyridin-2-yl)amino]ethoxy}phenyl)methyl]-1,3-thiazolidine-2,4-dione | Avandia | BRL 49653 | Brl-49653 | CHEMBL121 | ROSIGLITAZONE MALEATE | [3H]rosiglitazone | cid_5281055 | rosiglitazone
Type:
radiolabeled ligand
Emp. Form.:
C18H19N3O3S
Mol. Mass.:
357.427
SMILES:
CN(CCOc1ccc(Cc2sc(=O)[nH]c2O)cc1)c1ccccn1
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
BDBM33283
Synonyms:
(3-{4-[(3-phenyl-7-propyl-1,2-benzisoxazol-6-yl)oxy]butoxy}phenyl)acetic acid | CHEMBL435523 | [3H]nTZD3
Type:
radiolabeled ligand
Emp. Form.:
C28H29NO5
Mol. Mass.:
459.5336
SMILES:
CCCc1c(OCCCCOc2cccc(CC(O)=O)c2)ccc2c(noc12)-c1ccccc1
Structure:
Search PDB for entries with ligand similarity: