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Target
Peroxisome proliferator-activated receptor gamma
Ligand
BDBM28686
Substrate
[3H]rosiglitazone
Meas. Tech.
Radioligand Binding Assay (IC50) and Cell-Based Transcription Assay (EC50)
IC50
1585±n/a nM
Citation
 Shearer, BG; Patel, HS; Billin, AN; Way, JM; Winegar, DA; Lambert, MH; Xu, RX; Leesnitzer, LM; Merrihew, RV; Huet, S; Willson, TM Discovery of a novel class of PPARdelta partial agonists. Bioorg Med Chem Lett 18:5018-22 (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:
BDBM28686
Synonyms:
2-({3-[(5-chloro-1H-indole-1-)sulfonyl]benzene}amido)-5-methylbenzoic acid | Anthranilic acid deriv., 24
Type:
Small organic molecule
Emp. Form.:
C23H17ClN2O5S
Mol. Mass.:
468.909
SMILES:
Cc1ccc(NC(=O)c2cccc(c2)S(=O)(=O)n2ccc3cc(Cl)ccc23)c(c1)C(O)=O
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: