Reaction Details |
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Target | Peroxisome proliferator-activated receptor gamma |
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Ligand | BDBM28681 |
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Substrate/Competitor | biotinylated SRC1 peptide |
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Meas. Tech. | Co-activator Recruitment Assay (Kd) and Cell-Based Transcription Assay (EC50) |
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pH | 7.5±n/a |
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Temperature | 310.15±n/a K |
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Kd | 14.8±6.6 nM |
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EC50 | 3.8±1.5 nM |
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Comments | 100 +/- 10.5 % efficacy. |
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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 Chem282:17314-24 (2007) [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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BDBM28681 |
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biotinylated SRC1 peptide |
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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
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