| 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 | 80±45 nM |
|---|
| Comments | The relative efficacy (RE) compared to GW3965 is 1 in LXRalpha-SRC1 assay. The EC50=0.17 +/-0.01 uM for ABCA1 gene expression with RE=1. |
|---|
| Citation |  Jaye, MC; Krawiec, JA; Campobasso, N; Smallwood, A; Qiu, C; Lu, Q; Kerrigan, JJ; De Los Frailes Alvaro, M; Laffitte, B; Liu, WS; Marino, JP; Meyer, CR; Nichols, JA; Parks, DJ; Perez, P; Sarov-Blat, L; Seepersaud, SD; Steplewski, KM; Thompson, SK; Wang, P; Watson, MA; Webb, CL; Haigh, D; Caravella, JA; Macphee, CH; Willson, TM; Collins, JL Discovery of substituted maleimides as liver X receptor agonists and determination of a ligand-bound crystal structure. J Med Chem48:5419-22 (2005) [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
|
|
|
|---|
Search and Browse
