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Target
Oxysterols receptor LXR-alpha
Ligand
BDBM27273
Substrate
biotinylated SRC-1 peptide
Meas. Tech.
HTRF Cofactor Peptide Recruitment Assay
pH
7.5±n/a
Temperature
295.15±n/a K
EC50
220±n/a nM
Citation
 Kher, S; Lake, K; Sircar, I; Pannala, M; Bakir, F; Zapf, J; Xu, K; Zhang, SH; Liu, J; Morera, L; Sakurai, N; Jack, R; Cheng, JF 2-Aryl-N-acyl indole derivatives as liver X receptor (LXR) agonists. Bioorg Med Chem Lett 17:4442-6 (2007) [PubMed]  Article 
Target
Name:
Oxysterols receptor LXR-alpha
Synonyms:
LXRA | Liver X Receptor alpha (LXR-alpha) | Liver X receptor alpha | Liver X receptor alpha (LXRA) | Liver X receptor alpha (NR1H3) | Liver X, LXR alpha | NR1H3 | NR1H3_HUMAN | Nuclear orphan receptor LXR-alpha | Nuclear receptor subfamily 1 group H member 3
Type:
Enzyme Catalytic Domain
Mol. Mass.:
50403.85
Organism:
Homo sapiens (Human)
Description:
Q13133
Residue:
447
Sequence:
MSLWLGAPVPDIPPDSAVELWKPGAQDASSQAQGGSSCILREEARMPHSAGGTAGVGLEAAEPTALLTRAEPPSEPTEIRPQKRKKGPAPKMLGNELCSVCGDKASGFHYNVLSCEGCKGFFRRSVIKGAHYICHSGGHCPMDTYMRRKCQECRLRKCRQAGMREECVLSEEQIRLKKLKRQEEEQAHATSLPPRASSPPQILPQLSPEQLGMIEKLVAAQQQCNRRSFSDRLRVTPWPMAPDPHSREARQQRFAHFTELAIVSVQEIVDFAKQLPGFLQLSREDQIALLKTSAIEVMLLETSRRYNPGSESITFLKDFSYNREDFAKAGLQVEFINPIFEFSRAMNELQLNDAEFALLIAISIFSADRPNVQDQLQVERLQHTYVEALHAYVSIHHPHDRLMFPRMLMKLVSLRTLSSVHSEQVFALRLQDKKLPPLLSEIWDVHE
  
Inhibitor
Name:
BDBM27273
Synonyms:
3-[4-(1-benzoyl-1H-indol-2-yl)phenyl]propanenitrile | benzamide derivative, 8
Type:
Small organic molecule
Emp. Form.:
C24H18N2O
Mol. Mass.:
350.4125
SMILES:
O=C(c1ccccc1)n1c(cc2ccccc12)-c1ccc(CCC#N)cc1
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
biotinylated SRC-1 peptide
Synonyms:
n/a
Type:
Peptide
Mol. Mass.:
3157.52
Organism:
n/a
Description:
A biotinylated peptide comprises amino acids 675-699 of steroid receptor coactivator 1 (SRC1).
Residue:
28
Sequence:
CPSSHSSLTERHKILHRLLQEGSPSCNH