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TargetPeroxisome proliferator-activated receptor gamma
LigandBDBM34017
Substrate/CompetitorBDBM33297
Meas. Tech.Scintillation Proximity Assay (IC50) and PPAR gamma Transactivation Assay (EC50)
pH7.4±n/a
Temperature296.15±n/a K
IC50 29±n/a nM
EC50 26±n/a nM
CommentsEfficacy=115% (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 Chem16:4883-907 (2008) [PubMed]  Article
More Info.:Get all data from this article,   Solution Info,  Assay Method
 
Peroxisome proliferator-activated receptor gamma
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:
MGETLGDSPIDPESDSFTDTLSANISQEMTMVDTEMPFWPTNFGISSVDLSVMEDHSHSF
DIKPFTTVDFSSISTPHYEDIPFTRTDPVVADYKYDLKLQEYQSAIKVEPASPPYYSEKT
QLYNKPHEEPSNSLMAIECRVCGDKASGFHYGVHACEGCKGFFRRTIRLKLIYDRCDLNC
RIHKKSRNKCQYCRFQKCLAVGMSHNAIRFGRMPQAEKEKLLAEISSDIDQLNPESADLR
ALAKHLYDSYIKSFPLTKAKARAILTGKTTDKSPFVIYDMNSLMMGEDKIKFKHITPLQE
QSKEVAIRIFQGCQFRSVEAVQEITEYAKSIPGFVNLDLNDQVTLLKYGVHEIIYTMLAS
LMNKDGVLISEGQGFMTREFLKSLRKPFGDFMEPKFEFAVKFNALELDDSDLAIFIAVII
LSGDRPGLLNVKPIEDIQDNLLQALELQLKLNHPESSQLFAKLLQKMTDLRQIVTEHVQL
LQVIKKTETDMSLHPLLQEIYKDLY
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BDBM34017
BDBM33297
NameBDBM34017
Synonyms:CHEMBL104850 | phenylpropanoic acid derivative, 7
TypeSmall organic molecule
Emp. Form.C25H24N2O4
Mol. Mass.416.4691
SMILESCc1oc(nc1CCOc1ccc(C[C@@H](C(O)=O)n2cccc2)cc1)-c1ccccc1 |r|
Structure
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