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Target
Peroxisome proliferator-activated receptor gamma
Ligand
BDBM28681
Substrate
biotinylated SRC1 peptide
Meas. Tech.
Co-activator Recruitment Assay (Kd) and Cell-Based Transcription Assay (EC50)
pH
7.5±n/a
Temperature
310.15±n/a K
Kd
14.8±6.6 nM
EC50
3.8±1.5 nM
Comments
100 +/- 10.5 % efficacy.
Citation
 Pochetti, G; Godio, C; Mitro, N; Caruso, D; Galmozzi, A; Scurati, S; Loiodice, F; Fracchiolla, G; Tortorella, P; Laghezza, A; Lavecchia, A; Novellino, E; Mazza, F; Crestani, 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:
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:
Substrate
Name:
Nuclear receptor coactivator 1 (aa 676-700)
Synonyms:
BHLHE74 | NCOA1 | NCOA1_HUMAN | SRC1 | Steroid receptor coactivator 1 (aa 676-700)
Type:
Peptide
Mol. Mass.:
2802.63
Organism:
Human sapiens (human)
Description:
Q15788 aa 676-700
Residue:
25
Sequence:
CPSSHSSLTERHKILHRLLQEGSPS