Reaction Details  Report a problem with these data
Target
Peroxisome proliferator-activated receptor gamma
Ligand
BDBM28762
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
684.8±106.8 nM
EC50
73.3±49.9 nM
Comments
116.1 +/- 9.0 % 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:
BDBM28762
Synonyms:
(2R)-2-(4-{2-[1,3-benzoxazol-2-yl(heptyl)amino]ethyl}phenoxy)-2-methylbutanoic acid | LT160 (ureidofibrate derivative), (R)-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:
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