Reaction Details
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Peroxisome proliferator-activated receptor gamma
Ligand
BDBM28759
Substrate
BDBM10852
Meas. Tech.
Cell-Based Transcription Assay
EC50
480±80 nM
Comments
35 +/- 6.5 % of maximal activation compared to rosiglitazone normalized to 100%.
Citation
Montanari, R; Saccoccia, F; Scotti, E; Crestani, M; Godio, C; Gilardi, F; Loiodice, F; Fracchiolla, G; Laghezza, A; Tortorella, P; Lavecchia, A; Novellino, E; Mazza, F; Aschi, M; Pochetti, G Crystal structure of the peroxisome proliferator-activated receptor gamma (PPARgamma) ligand binding domain complexed with a novel partial agonist: a new region of the hydrophobic pocket could be exploited for drug design. J Med Chem 51:7768-76 (2008) [PubMed] Article More Info.:
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:
BDBM28759
Synonyms:
(2S)-3-phenyl-2-(4-phenylphenoxy)propanoic acid | CHEMBL191275 | LT175 (S-1)
Type:
Small organic molecule
Emp. Form.:
C21H18O3
Mol. Mass.:
318.3658
SMILES:
OC(=O)[C@H](Cc1ccccc1)Oc1ccc(cc1)-c1ccccc1 |r|
Structure:
Substrate