Reaction Details |
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Target | Peroxisome proliferator-activated receptor gamma |
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Ligand | BDBM28679 |
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Substrate/Competitor | [3H]rosiglitazone |
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Meas. Tech. | Radioligand Binding Assay (IC50) and Cell-Based Transcription Assay (EC50) |
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IC50 | 5012±n/a nM |
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Citation | Shearer, BG; Patel, HS; Billin, AN; Way, JM; Winegar, DA; Lambert, MH; Xu, RX; Leesnitzer, LM; Merrihew, RV; Huet, S; Willson, TM Discovery of a novel class of PPARdelta partial agonists. Bioorg Med Chem Lett18:5018-22 (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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BDBM28679 |
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[3H]rosiglitazone |
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Name | BDBM28679 |
Synonyms: | 5-chloro-2-({3-[(7-chloro-8-methyl-1,2,3,4-tetrahydroisoquinoline-2-)sulfonyl]benzene}amido)benzoic acid | Anthranilic acid deriv., 18 |
Type | Small organic molecule |
Emp. Form. | C24H20Cl2N2O5S |
Mol. Mass. | 519.397 |
SMILES | Cc1c(Cl)ccc2CCN(Cc12)S(=O)(=O)c1cccc(c1)C(=O)Nc1ccc(Cl)cc1C(O)=O |
Structure |
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