Reaction Details |
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Target | Peroxisome proliferator-activated receptor gamma |
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Ligand | BDBM34017 |
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Substrate/Competitor | BDBM33297 |
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Meas. Tech. | Scintillation Proximity Assay (IC50) and PPAR gamma Transactivation Assay (EC50) |
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pH | 7.4±n/a |
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Temperature | 296.15±n/a K |
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IC50 | 29±n/a nM |
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EC50 | 26±n/a nM |
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Comments | Efficacy=115% (The maximum efficacy of darglitazone was defined as 100%) |
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Citation | Casimiro-Garcia, A; Bigge, CF; Davis, JA; Padalino, T; Pulaski, J; Ohren, JF; McConnell, P; Kane, CD; Royer, LJ; Stevens, KA; Auerbach, BJ; Collard, WT; McGregor, C; Fakhoury, SA; Schaum, RP; Zhou, H Effects of modifications of the linker in a series of phenylpropanoic acid derivatives: Synthesis, evaluation as PPARalpha/gamma dual agonists, and X-ray crystallographic studies. Bioorg Med Chem16:4883-907 (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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BDBM34017 |
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BDBM33297 |
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Name | BDBM34017 |
Synonyms: | CHEMBL104850 | phenylpropanoic acid derivative, 7 |
Type | Small organic molecule |
Emp. Form. | C25H24N2O4 |
Mol. Mass. | 416.4691 |
SMILES | Cc1oc(nc1CCOc1ccc(C[C@@H](C(O)=O)n2cccc2)cc1)-c1ccccc1 |r| |
Structure |
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