Reaction Details |
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Target | Oxysterols receptor LXR-beta |
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Ligand | BDBM28154 |
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Substrate/Competitor | BDBM19993 |
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Meas. Tech. | Radioligand Binding Assay and Luciferase Transcriptional Reporter Gene Assay |
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IC50 | 13±n/a nM |
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EC50 | 120±n/a nM |
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Citation | Ratni, H; Blum-Kaelin, D; Dehmlow, H; Hartman, P; Jablonski, P; Masciadri, R; Maugeais, C; Patiny-Adam, A; Panday, N; Wright, M Discovery of tetrahydro-cyclopenta[b]indole as selective LXRs modulator. Bioorg Med Chem Lett19:1654-7 (2009) [PubMed] Article |
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More Info.: | Get all data from this article, Solution Info, Assay Method |
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Oxysterols receptor LXR-beta |
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Name: | Oxysterols receptor LXR-beta |
Synonyms: | LXRB | Liver X receptor beta (NR1H2) | Liver X, LXR beta | NER | NR1H2 | NR1H2_HUMAN | Nuclear receptor NER | UNR | Ubiquitously-expressed nuclear receptor |
Type: | Enzyme Catalytic Domain |
Mol. Mass.: | 50978.79 |
Organism: | Homo sapiens (Human) |
Description: | P55055 |
Residue: | 460 |
Sequence: | MSSPTTSSLDTPLPGNGPPQPGAPSSSPTVKEEGPEPWPGGPDPDVPGTDEASSACSTDW
VIPDPEEEPERKRKKGPAPKMLGHELCRVCGDKASGFHYNVLSCEGCKGFFRRSVVRGGA
RRYACRGGGTCQMDAFMRRKCQQCRLRKCKEAGMREQCVLSEEQIRKKKIRKQQQESQSQ
SQSPVGPQGSSSSASGPGASPGGSEAGSQGSGEGEGVQLTAAQELMIQQLVAAQLQCNKR
SFSDQPKVTPWPLGADPQSRDARQQRFAHFTELAIISVQEIVDFAKQVPGFLQLGREDQI
ALLKASTIEIMLLETARRYNHETECITFLKDFTYSKDDFHRAGLQVEFINPIFEFSRAMR
RLGLDDAEYALLIAINIFSADRPNVQEPGRVEALQQPYVEALLSYTRIKRPQDQLRFPRM
LMKLVSLRTLSSVHSEQVFALRLQDKKLPPLLSEIWDVHE
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BDBM28154 |
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BDBM19993 |
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Name | BDBM28154 |
Synonyms: | 5-[(S)-(benzenesulfonyl)[(2R)-7-chloro-1H,2H,3H,4H-cyclopenta[b]indol-2-yl]fluoromethyl]-N,N-dimethyl-1,2,4-oxadiazol-3-amine | tetrahydro-cyclopenta[b]indole, (+/-)28c |
Type | Small organic molecule |
Emp. Form. | C22H20ClFN4O3S |
Mol. Mass. | 474.936 |
SMILES | [H][C@@]1(Cc2[nH]c3ccc(Cl)cc3c2C1)[C@@](F)(c1nc(no1)N(C)C)S(=O)(=O)c1ccccc1 |r| |
Structure |
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