Reaction Details Report a problem with these data
Target
Oxysterols receptor LXR-beta
Ligand
BDBM20133
Substrate
biotinylated SRC-1 peptide
Meas. Tech.
Fluorescence-Resonance Energy Transfer Assay
pH
7.2±n/a
Temperature
310.15±n/a K
EC50
76±n/a nM
Comments
Efficacy = 98 % in FRET LXRbeta assay. There was 42% induction of ABCA1 gene activity in human THP-1 cells @ 1uM.
Citation
 Molteni, V; Li, X; Nabakka, J; Liang, F; Wityak, J; Koder, A; Vargas, L; Romeo, R; Mitro, N; Mak, PA; Seidel, HM; Haslam, JA; Chow, D; Tuntland, T; Spalding, TA; Brock, A; Bradley, M; Castrillo, A; Tontonoz, P; Saez, E N-Acylthiadiazolines, a new class of liver X receptor agonists with selectivity for LXRbeta. J Med Chem 50:4255-9 (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:
BDBM20133
Synonyms:
2-(2,3-dimethoxyphenyl)-5-(4-fluorophenyl)-3-[(2,4,6-trifluorophenyl)carbonyl]-2,3-dihydro-1,3,4-thiadiazole | N-Acylthiadiazoline, 5
Type:
Small organic molecule
Emp. Form.:
C23H16F4N2O3S
Mol. Mass.:
476.443
SMILES:
COc1cccc(C2SC(=NN2C(=O)c2c(F)cc(F)cc2F)c2ccc(F)cc2)c1OC |c:9|
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
biotinylated SRC-1 peptide
Synonyms:
n/a
Type:
Peptide
Mol. Mass.:
2905.78
Organism:
n/a
Description:
n/a
Residue:
26
Sequence:
CPSSHSSLTERHKILHRLLQEGSPSC