Target
Peroxisome proliferator-activated receptor gamma
Ligand
BDBM28763
Substrate
[3H]rosiglitazone
Meas. Tech.
Competition Binding Assay (Ki)
pH
7.5±n/a
Temperature
295.15±n/a K
Ki
971±399 nM
Citation
 Pochetti, GGodio, CMitro, NCaruso, DGalmozzi, AScurati, SLoiodice, FFracchiolla, GTortorella, PLaghezza, ALavecchia, ANovellino, EMazza, FCrestani, M Insights into the mechanism of partial agonism: crystal structures of the peroxisome proliferator-activated receptor gamma ligand-binding domain in the complex with two enantiomeric ligands. J Biol Chem 282:17314-24 (2007) [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:
BDBM28763
Synonyms:
(2S)-2-(4-{2-[1,3-benzoxazol-2-yl(heptyl)amino]ethyl}phenoxy)-2-methylbutanoic acid | LT127 (ureidofibrate derivative), (S)-1
Type:
Small organic molecule
Emp. Form.:
C27H36N2O4
Mol. Mass.:
452.5857
SMILES:
CCCCCCCN(CCc1ccc(O[C@@](C)(CC)C(O)=O)cc1)c1nc2ccccc2o1 |r|
Structure:
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Substrate
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: