Reaction Details Report a problem with these data
Target
Oxysterols receptor LXR-beta
Ligand
BDBM27282
Substrate
biotinylated SRC-1 peptide
Meas. Tech.
HTRF Cofactor Peptide Recruitment Assay
pH
7.5±n/a
Temperature
295.15±n/a K
EC50
18000±n/a nM
Citation
 Bakir, F; Kher, S; Pannala, M; Wilson, N; Nguyen, T; Sircar, I; Takedomi, K; Fukushima, C; Zapf, J; Xu, K; Zhang, SH; Liu, J; Morera, L; Schneider, L; Sakurai, N; Jack, R; Cheng, JF Discovery and structure-activity relationship studies of indole derivatives as liver X receptor (LXR) agonists. Bioorg Med Chem Lett 17:3473-9 (2007) [PubMed]  Article 
Target
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:
MSSPTTSSLDTPLPGNGPPQPGAPSSSPTVKEEGPEPWPGGPDPDVPGTDEASSACSTDWVIPDPEEEPERKRKKGPAPKMLGHELCRVCGDKASGFHYNVLSCEGCKGFFRRSVVRGGARRYACRGGGTCQMDAFMRRKCQQCRLRKCKEAGMREQCVLSEEQIRKKKIRKQQQESQSQSQSPVGPQGSSSSASGPGASPGGSEAGSQGSGEGEGVQLTAAQELMIQQLVAAQLQCNKRSFSDQPKVTPWPLGADPQSRDARQQRFAHFTELAIISVQEIVDFAKQVPGFLQLGREDQIALLKASTIEIMLLETARRYNHETECITFLKDFTYSKDDFHRAGLQVEFINPIFEFSRAMRRLGLDDAEYALLIAINIFSADRPNVQEPGRVEALQQPYVEALLSYTRIKRPQDQLRFPRMLMKLVSLRTLSSVHSEQVFALRLQDKKLPPLLSEIWDVHE
  
Inhibitor
Name:
BDBM27282
Synonyms:
indole derivative, 1h | tert-butyl 2-(2-benzenesulfonamido-2,3-dihydro-1H-inden-5-yl)-5-methyl-1H-indole-1-carboxylate
Type:
Small organic molecule
Emp. Form.:
C29H30N2O4S
Mol. Mass.:
502.624
SMILES:
Cc1ccc2n(C(=O)OC(C)(C)C)c(cc2c1)-c1ccc2CC(Cc2c1)NS(=O)(=O)c1ccccc1
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