Reaction Details |
| Report a problem with these data |
Target | Oxysterols receptor LXR-alpha |
---|
Ligand | BDBM19992 |
---|
Substrate/Competitor | biotinylated SRC-1 peptide |
---|
Meas. Tech. | Cell-Free Ligand Sensing Assay (LiSA)-LXRalpha-SRC1 Assay |
---|
pH | 7.5±n/a |
---|
Temperature | 295.15±n/a K |
---|
EC50 | 125±20 nM |
---|
Comments | The relative efficacy (RE) compared to 24(S),25-epoxycholesterol is 1.0 in LXRalpha-SRC1 assay. The EC50=190 +/- 30 nM for LXRalpha-GAL4 gene expression with RE=1.7. |
---|
Citation | Collins, JL; Fivush, AM; Watson, MA; Galardi, CM; Lewis, MC; Moore, LB; Parks, DJ; Wilson, JG; Tippin, TK; Binz, JG; Plunket, KD; Morgan, DG; Beaudet, EJ; Whitney, KD; Kliewer, SA; Willson, TM Identification of a nonsteroidal liver X receptor agonist through parallel array synthesis of tertiary amines. J Med Chem45:1963-6 (2002) [PubMed] Article |
---|
More Info.: | Get all data from this article, Solution Info, Assay Method |
---|
|
Oxysterols receptor LXR-alpha |
---|
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: | MSLWLGAPVPDIPPDSAVELWKPGAQDASSQAQGGSSCILREEARMPHSAGGTAGVGLEA
AEPTALLTRAEPPSEPTEIRPQKRKKGPAPKMLGNELCSVCGDKASGFHYNVLSCEGCKG
FFRRSVIKGAHYICHSGGHCPMDTYMRRKCQECRLRKCRQAGMREECVLSEEQIRLKKLK
RQEEEQAHATSLPPRASSPPQILPQLSPEQLGMIEKLVAAQQQCNRRSFSDRLRVTPWPM
APDPHSREARQQRFAHFTELAIVSVQEIVDFAKQLPGFLQLSREDQIALLKTSAIEVMLL
ETSRRYNPGSESITFLKDFSYNREDFAKAGLQVEFINPIFEFSRAMNELQLNDAEFALLI
AISIFSADRPNVQDQLQVERLQHTYVEALHAYVSIHHPHDRLMFPRMLMKLVSLRTLSSV
HSEQVFALRLQDKKLPPLLSEIWDVHE
|
|
|
BDBM19992 |
---|
biotinylated SRC-1 peptide |
---|
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: | CPSSHSSLTERHKILHRLLQEGSPS-CONH2
|
|
|