Target
Peroxisome proliferator-activated receptor gamma
Ligand
BDBM28681
Substrate
BDBM33297
Meas. Tech.
Scintillation Proximity Assay (IC50) and PPAR gamma Transactivation Assay (EC50)
pH
7.4±n/a
Temperature
296.15±n/a K
IC50
274±n/a nM
EC50
223±n/a nM
Comments
Efficacy=84% (The maximum efficacy of darglitazone 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 gamma
Synonyms:
NR1C3 | Nuclear receptor subfamily 1 group C member 3 | PPAR-gamma | PPARG | PPARG_HUMAN | Peroxisome proliferator-activated receptor | Peroxisome proliferator-activated receptor gamma (PPAR gamma) | Peroxisome proliferator-activated receptor gamma (PPARG) | Peroxisome proliferator-activated receptor gamma (PPARĪ³) | Peroxisome proliferator-activated receptor gamma/Nuclear receptor corepressor 2 | peroxisome proliferator-activated receptor gamma isoform 2
Type:
Nuclear Receptor
Mol. Mass.:
57613.46
Organism:
Homo sapiens (Human)
Description:
P37231
Residue:
505
Sequence:
MGETLGDSPIDPESDSFTDTLSANISQEMTMVDTEMPFWPTNFGISSVDLSVMEDHSHSFDIKPFTTVDFSSISTPHYEDIPFTRTDPVVADYKYDLKLQEYQSAIKVEPASPPYYSEKTQLYNKPHEEPSNSLMAIECRVCGDKASGFHYGVHACEGCKGFFRRTIRLKLIYDRCDLNCRIHKKSRNKCQYCRFQKCLAVGMSHNAIRFGRMPQAEKEKLLAEISSDIDQLNPESADLRALAKHLYDSYIKSFPLTKAKARAILTGKTTDKSPFVIYDMNSLMMGEDKIKFKHITPLQEQSKEVAIRIFQGCQFRSVEAVQEITEYAKSIPGFVNLDLNDQVTLLKYGVHEIIYTMLASLMNKDGVLISEGQGFMTREFLKSLRKPFGDFMEPKFEFAVKFNALELDDSDLAIFIAVIILSGDRPGLLNVKPIEDIQDNLLQALELQLKLNHPESSQLFAKLLQKMTDLRQIVTEHVQLLQVIKKTETDMSLHPLLQEIYKDLY
  
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:
BDBM33297
Synonyms:
[3H]Darglitazone
Type:
radiolabeled ligand
Emp. Form.:
C23H20N2O4S
Mol. Mass.:
420.481
SMILES:
Cc1oc(nc1CCC(=O)c1ccc(CC2SC(=O)NC2=O)cc1)-c1ccccc1
Structure:
Search PDB for entries with ligand similarity: