| Reaction Details |
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| Report a problem with these data |
| Target | Liver Receptor Homolog 1 |
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| Ligand | GSK 8470 |
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| Substrate/Competitor | Biotinylated TIF2 Peptide |
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| Meas. Tech. | FRET Assay for LRH-1 |
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| pH | 7.5±n/a |
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| Temperature | 295.15±n/a K |
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| EC50 | 430±70 nM |
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| Citation |  Whitby, RJ; Dixon, S; Maloney, PR; Delerive, P; Goodwin, BJ; Parks, DJ; Willson, TM Identification of small molecule agonists of the orphan nuclear receptors liver receptor homolog-1 and steroidogenic factor-1.J Med Chem.49:6652-5(2006)[PubMed] |
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| More Info. |
Get all data from this article
, Solution Info
, Assay Method
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| Liver Receptor Homolog 1 |
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| Name | Liver Receptor Homolog 1 |
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| Synonyms | B1-binding factor | hB1F | CYP7A promoter-binding factor | LRH-1| Nuclear receptor subfamily 5 group A member 2 | Alpha-1-fetoprotein transcription factor | Hepatocytic transcription factor |
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| Type | Nuclear Hormone Receptor |
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| Mol. Mass. | 61331 |
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| Organism | Homo sapiens (human) |
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| Description | n/a |
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| Residue | 541 |
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| Sequence | MSSNSDTGDLQESLKHGLTPIGAGLPDRHGSPIPARGRLVMLPKVETEALGLARSHGEQG
QMPENMQVSQFKMVNYSYDEDLEELCPVCGDKVSGYHYGLLTCESCKGFFKRTVQNNKRY
TCIENQNCQIDKTQRKRCPYCRFQKCLSVGMKLEAVRADRMRGGRNKFGPMYKRDRALKQ
QKKALIRANGLKLEAMSQVIQAMPSDLTISSAIQNIHSASKGLPLNHAALPPTDYDRSPF
VTSPISMTMPPHGSLQGYQTYGHFPSRAIKSEYPDPYTSSPESIMGYSYMDSYQTSSPAS
IPHLILELLKCEPDEPQVQAKIMAYLQQEQANRSKHEKLSTFGLMCKMADQTLFSIVEWA
RSSIFFRELKVDDQMKLLQNCWSELLILDHIYRQVVHGKEGSIFLVTGQQVDYSIIASQA
GATLNNLMSHAQELVAKLRSLQFDQREFVCLKFLVLFSLDVKNLENFQLVEGVQEQVNAA
LLDYTMCNYPQQTEKFGQLLLRLPEIRAISMQAEEYLYYKHLNGDVPYNNLLIEMLHAKR
A
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| GSK 8470 |
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| Name | GSK 8470 |
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| Synonyms: | (3aS,6aR)-5-[(4E)-oct-4-en-4-yl]-N,4-diphenyl-1,2,3,3a,6,6a-hexahydropentalen-3a-amine | bicyclo[3.3.0]-oct-2-ene, 5a |
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| Type | Small organic molecule |
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| Emp. Form. | C28H35N |
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| Mol. Mass. | 385.5842 |
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| SMILES | [H][C@]12CCC[C@@]1(Nc1ccccc1)C(=C(C2)\C(CCC)=C\CCC)c1ccccc1 |r,c:15| |
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| Structure | |
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| Biotinylated TIF2 Peptide |
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| Name | Biotinylated TIF2 Peptide |
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| Synonyms | n/a |
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| Type | Peptide |
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| Mol. Mass. | n/a |
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| Organism | n/a |
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| Description | A peptide derived from TIF2 amino acids 732-756. |
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| Residue | 25 |
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| Sequence | Biotin-QEPVSPKKKENALLRYLLDKDDTKD-CONH2
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