Reaction Details Report a problem with these data
Target
Oxysterols receptor LXR-alpha
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
1400±n/a nM
Comments
FRET LXRalpha, efficacy = 62 %. 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-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:
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