Reaction Details |
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Target | Peroxisome proliferator-activated receptor gamma |
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Ligand | BDBM28759 |
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Substrate/Competitor | BDBM10852 |
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Meas. Tech. | Cell-Based Transcription Assay |
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EC50 | 480±80 nM |
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Comments | 35 +/- 6.5 % of maximal activation compared to rosiglitazone normalized to 100%. |
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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 Chem51:7768-76 (2008) [PubMed] Article |
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More Info.: | Get all data from this article, Solution Info, Assay Method |
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Peroxisome proliferator-activated receptor gamma |
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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: | MGETLGDSPIDPESDSFTDTLSANISQEMTMVDTEMPFWPTNFGISSVDLSVMEDHSHSF
DIKPFTTVDFSSISTPHYEDIPFTRTDPVVADYKYDLKLQEYQSAIKVEPASPPYYSEKT
QLYNKPHEEPSNSLMAIECRVCGDKASGFHYGVHACEGCKGFFRRTIRLKLIYDRCDLNC
RIHKKSRNKCQYCRFQKCLAVGMSHNAIRFGRMPQAEKEKLLAEISSDIDQLNPESADLR
ALAKHLYDSYIKSFPLTKAKARAILTGKTTDKSPFVIYDMNSLMMGEDKIKFKHITPLQE
QSKEVAIRIFQGCQFRSVEAVQEITEYAKSIPGFVNLDLNDQVTLLKYGVHEIIYTMLAS
LMNKDGVLISEGQGFMTREFLKSLRKPFGDFMEPKFEFAVKFNALELDDSDLAIFIAVII
LSGDRPGLLNVKPIEDIQDNLLQALELQLKLNHPESSQLFAKLLQKMTDLRQIVTEHVQL
LQVIKKTETDMSLHPLLQEIYKDLY
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BDBM28759 |
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BDBM10852 |
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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 |
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