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Target Report Card

Target Name and Classification

Target ID CHEMBL2808
Preferred Name LXR-alpha
Synonyms LXRA | Liver X receptor alpha | NR1H3 | Nuclear receptor subfamily 1 group H member 3 | Oxysterols receptor LXR-alpha
Organism Homo sapiens
Species Group No
Protein Target Classification
  • transcription factor > nuclear receptor > nuclear hormone receptor subfamily 1 > nuclear hormone receptor subfamily 1 group h > nuclear hormone receptor subfamily 1 group h member 3

Target Components

Component Description Relationship Accession
Oxysterols receptor LXR-alpha SINGLE PROTEIN Q13133

Target Relations

ChEMBL ID Pref Name Target Type
CHEMBL3430879 Retinoic acid receptor RXR-alpha/oxysterols receptor LXR-alpha PROTEIN COMPLEX
CHEMBL3706564 Liver X receptor PROTEIN FAMILY
CHEMBL3706565 Liver X receptor (LXR alpha AND LXR beta) SELECTIVITY GROUP

Approved Drugs and Clinical Candidates

ChEMBL ID Name Mechanism of Action Max Phase References
CHEMBL272621 HYODEOXYCHOLIC_ACID LXR-alpha agonist 1 PubMed PubMed
CHEMBL456237 LXR-623 LXR-alpha agonist 1 PubMed PubMed
CHEMBL3545047 BMS-852927 LXR-alpha modulator 1 PubMed
CHEMBL3545238 CS-8080 LXR-alpha agonist 1 PubMed

Target Associated Bioactivities

Target Associated Assays

Target Ligand Efficiencies

Target Associated Compound Properties

Target Cross References - Gene

Array Express ENSG00000025434
Ensembl ENSG00000025434
GO Cellular Component GO:0000790 (nuclear chromatin)
GO:0005634 (nucleus)
GO:0005654 (nucleoplasm)
GO:0043235 (receptor complex)
GO:0090575 (RNA polymerase II transcription factor complex)
GO Molecular Function GO:0000981 (RNA polymerase II transcription factor activity, sequence-specific DNA binding)
GO:0003677 (DNA binding)
GO:0003700 (transcription factor activity, sequence-specific DNA binding)
GO:0003707 (steroid hormone receptor activity)
GO:0003713 (transcription coactivator activity)
GO:0004879 (RNA polymerase II transcription factor activity, ligand-activated sequence-specific DNA binding)
GO:0005515 (protein binding)
GO:0008270 (zinc ion binding)
GO:0015485 (cholesterol binding)
GO:0032810 (sterol response element binding)
GO:0043565 (sequence-specific DNA binding)
GO:0044212 (transcription regulatory region DNA binding)
GO:0046872 (metal ion binding)
GO Biological Process GO:0000122 (negative regulation of transcription from RNA polymerase II promoter)
GO:0006351 (transcription, DNA-templated)
GO:0006355 (regulation of transcription, DNA-templated)
GO:0006367 (transcription initiation from RNA polymerase II promoter)
GO:0010745 (negative regulation of macrophage derived foam cell differentiation)
GO:0010867 (positive regulation of triglyceride biosynthetic process)
GO:0010870 (positive regulation of receptor biosynthetic process)
GO:0010875 (positive regulation of cholesterol efflux)
GO:0010887 (negative regulation of cholesterol storage)
GO:0030522 (intracellular receptor signaling pathway)
GO:0032270 (positive regulation of cellular protein metabolic process)
GO:0032369 (negative regulation of lipid transport)
GO:0032376 (positive regulation of cholesterol transport)
GO:0032570 (response to progesterone)
GO:0034145 (positive regulation of toll-like receptor 4 signaling pathway)
GO:0042632 (cholesterol homeostasis)
GO:0042752 (regulation of circadian rhythm)
GO:0043031 (negative regulation of macrophage activation)
GO:0043277 (apoptotic cell clearance)
GO:0043401 (steroid hormone mediated signaling pathway)
GO:0045723 (positive regulation of fatty acid biosynthetic process)
GO:0045893 (positive regulation of transcription, DNA-templated)
GO:0045944 (positive regulation of transcription from RNA polymerase II promoter)
GO:0048550 (negative regulation of pinocytosis)
GO:0050728 (negative regulation of inflammatory response)
GO:0051006 (positive regulation of lipoprotein lipase activity)
GO:0055088 (lipid homeostasis)
GO:0055092 (sterol homeostasis)
GO:0060336 (negative regulation of interferon-gamma-mediated signaling pathway)
GO:0070328 (triglyceride homeostasis)
GO:0071222 (cellular response to lipopolysaccharide)
GO:0090188 (negative regulation of pancreatic juice secretion)
GO:0090341 (negative regulation of secretion of lysosomal enzymes)
Wikipedia Liver_X_receptor_alpha

Target Cross References - Protein

canSAR Q13133
Human Protein Atlas ENSG00000025434
IntAct Q13133
Guide to Pharmacology 602
Open Targets ENSG00000025434
PharmGKB PA31751
Pharos Q13133 (Tchem)
Reactome R-HSA-383280 (Nuclear Receptor transcription pathway.)
R-HSA-8866427 (VLDLR internalisation and degradation.)
UniProt A8K3J9 D3DQR1 Q13133 Q8IW13 Q96H87

Target Cross References - Domain

InterPro IPR000536 (Nucl_hrmn_rcpt_lig-bd.)
IPR001628 (Znf_hrmn_rcpt.)
IPR001723 (Nuclear_hrmn_rcpt.)
IPR013088 (Znf_NHR/GATA.)
IPR023257 (Liver_X_rcpt.)
IPR035500 (NHR_like_dom_sf.)
Pfam PF00104 (Hormone_recep)
PF00105 (zf-C4)

Target Cross References - Structure