Target
Peroxisome proliferator-activated receptor gamma
Ligand
BDBM34033
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
11000±n/a nM
EC50
3600±n/a nM
Comments
Efficacy=57% (The maximum efficacy of darglitazone was defined as 100%)
Citation
 Casimiro-Garcia, ABigge, CFDavis, JAPadalino, TPulaski, JOhren, JFMcConnell, PKane, CDRoyer, LJStevens, KAAuerbach, BJCollard, WTMcGregor, CFakhoury, SASchaum, RPZhou, H Effects of modifications of the linker in a series of phenylpropanoic acid derivatives: Synthesis, evaluation as PPARalpha/gamma dual agonists, and X-ray crystallographic studies. Bioorg Med Chem 16:4883-907 (2008) [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:
BDBM34033
Synonyms:
phenylpropanoic acid derivative, 60
Type:
Small organic molecule
Emp. Form.:
C23H26N2O2
Mol. Mass.:
362.4647
SMILES:
CN(CCCc1ccc(C[C@@H](C(O)=O)n2cccc2)cc1)c1ccccc1 |r|
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: