Reaction Details Report a problem with these data
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, A; Bigge, CF; Davis, JA; Padalino, T; Pulaski, J; Ohren, JF; McConnell, P; Kane, CD; Royer, LJ; Stevens, KA; Auerbach, BJ; Collard, WT; McGregor, C; Fakhoury, SA; Schaum, RP; Zhou, 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
More Info.:
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|