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Target
Peroxisome proliferator-activated receptor gamma
Ligand
BDBM28802
Substrate
rosiglitazone
Meas. Tech.
PPAR gamma Fluorescence Polarization Assay (IC50) and Cell-Based Transcription Assay (EC50)
pH
8±n/a
Temperature
295.15±n/a K
IC50
>15000±n/a nM
EC50
4511±1314 nM
Comments
67 +/- 13 efficacy.
Citation
 Mukherjee, R; Locke, KT; Miao, B; Meyers, D; Monshizadegan, H; Zhang, R; Search, D; Grimm, D; Flynn, M; O'Malley, KM; Zhang, L; Li, J; Shi, Y; Kennedy, LJ; Blanar, M; Cheng, PT; Tino, J; Srivastava, RA Novel peroxisome proliferator-activated receptor alpha agonists lower low-density lipoprotein and triglycerides, raise high-density lipoprotein, and synergistically increase cholesterol excretion with a liver X receptor agonist. J Pharmacol Exp Ther 327:716-26 (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:
BDBM28802
Synonyms:
2-{[(5-{[2-(4-chlorophenyl)-5-methyl-1,3-oxazol-4-yl]methoxy}-2-fluorophenyl)methyl](methoxycarbonyl)amino}acetic acid | BMS-711939
Type:
Small organic molecule
Emp. Form.:
C22H20ClFN2O6
Mol. Mass.:
462.855
SMILES:
COC(=O)N(CC(O)=O)Cc1cc(OCc2nc(oc2C)-c2ccc(Cl)cc2)ccc1F
Structure:
Search PDB for entries with ligand similarity:
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: