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ChEMBL Statistics
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Target Report Card

Target Name and Classification

Target ID CHEMBL239
Target Type SINGLE PROTEIN
Preferred Name Peroxisome proliferator-activated receptor alpha
Synonyms NR1C1 | Nuclear receptor subfamily 1 group C member 1 | PPAR | PPAR-alpha | PPARA | Peroxisome proliferator-activated receptor 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 c > nuclear hormone receptor subfamily 1 group c member 1

Target Components

Component Description Relationship Accession
Peroxisome proliferator-activated receptor alpha SINGLE PROTEIN Q07869

Target Relations

ChEMBL ID Pref Name Target Type
CHEMBL3559683 Peroxisome proliferator-activated receptor PROTEIN FAMILY
CHEMBL2111325 PPAR alpha/gamma SELECTIVITY GROUP

Approved Drugs and Clinical Candidates

ChEMBL ID Name Mechanism of Action Max Phase References
CHEMBL457 GEMFIBROZIL Peroxisome proliferator-activated receptor alpha agonist 4 DailyMed
CHEMBL565 CLOFIBRATE Peroxisome proliferator-activated receptor alpha agonist 4 ISBN
CHEMBL672 FENOFIBRATE Peroxisome proliferator-activated receptor alpha agonist 4 DailyMed
CHEMBL981 FENOFIBRIC ACID Peroxisome proliferator-activated receptor alpha agonist 4 DailyMed
CHEMBL1201745 CHOLINE FENOFIBRATE Peroxisome proliferator-activated receptor alpha agonist 4 DailyMed
CHEMBL282686 TESAGLITAZAR Peroxisome proliferator-activated receptor alpha agonist 3 PubMed PubMed
CHEMBL186179 MURAGLITAZAR Peroxisome proliferator-activated receptor alpha agonist 3 PubMed
CHEMBL519504 ALEGLITAZAR Peroxisome proliferator-activated receptor alpha agonist 3 PubMed
CHEMBL592054 IMIGLITAZAR Peroxisome proliferator-activated receptor alpha agonist 3 PubMed PubMed
CHEMBL3545412 K-877 Peroxisome proliferator-activated receptor alpha agonist 3 Other Other
CHEMBL424133 LY-518674 Peroxisome proliferator-activated receptor alpha agonist 2 PubMed
CHEMBL181954 NAVEGLITAZAR Peroxisome proliferator-activated receptor alpha agonist 2 KEGG PubMed PubMed
CHEMBL219586 GW590735 Peroxisome proliferator-activated receptor alpha agonist 2 PubMed
CHEMBL3545018 GFT505 Peroxisome proliferator-activated receptor alpha agonist 2 Other PubMed PubMed
CHEMBL3545093 ZYH7 Peroxisome proliferator-activated receptor alpha agonist 2 Other
CHEMBL3545276 CP-778875 Peroxisome proliferator-activated receptor alpha agonist 2 PubMed PubMed PubMed
CHEMBL3545334 AVE8134 Peroxisome proliferator-activated receptor alpha agonist 2 PubMed
CHEMBL3545394 DRF-10945 Peroxisome proliferator-activated receptor alpha agonist 2 Other
More...

Target Associated Bioactivities

Target Associated Assays

Target Ligand Efficiencies

Target Associated Compound Properties

Target Cross References - Gene

Array Express ENSG00000186951
Ensembl ENSG00000186951
GO Cellular Component GO:0005634 (nucleus)
GO:0005654 (nucleoplasm)
GO Molecular Function GO:0000978 (RNA polymerase II core promoter proximal region sequence-specific DNA binding)
GO:0001077 (transcriptional activator activity, RNA polymerase II core promoter proximal region sequence-specific binding)
GO:0001078 (transcriptional repressor activity, RNA polymerase II core promoter proximal region sequence-specific binding)
GO:0001103 (RNA polymerase II repressing transcription factor binding)
GO:0001190 (transcriptional activator activity, RNA polymerase II transcription factor binding)
GO:0003677 (DNA binding)
GO:0003700 (sequence-specific DNA binding transcription factor activity)
GO:0003700 (transcription factor activity, sequence-specific DNA binding)
GO:0003706 (ligand-regulated transcription factor activity)
GO:0003707 (steroid hormone receptor activity)
GO:0004879 (RNA polymerase II transcription factor activity, ligand-activated sequence-specific DNA binding)
GO:0008144 (drug binding)
GO:0008270 (zinc ion binding)
GO:0008289 (lipid binding)
GO:0016563 (transcription activator activity)
GO:0031624 (ubiquitin conjugating enzyme binding)
GO:0043565 (sequence-specific DNA binding)
GO Biological Process GO:0000122 (negative regulation of transcription from RNA polymerase II promoter)
GO:0001666 (response to hypoxia)
GO:0006367 (transcription initiation from RNA polymerase II promoter)
GO:0006629 (lipid metabolic process)
GO:0006631 (fatty acid metabolic process)
GO:0007507 (heart development)
GO:0007623 (circadian rhythm)
GO:0008544 (epidermis development)
GO:0010467 (gene expression)
GO:0010745 (negative regulation of macrophage derived foam cell differentiation)
GO:0010871 (negative regulation of receptor biosynthetic process)
GO:0010887 (negative regulation of cholesterol storage)
GO:0010891 (negative regulation of sequestering of triglyceride)
GO:0015908 (fatty acid transport)
GO:0030522 (intracellular receptor signaling pathway)
GO:0032000 (positive regulation of fatty acid beta-oxidation)
GO:0032091 (negative regulation of protein binding)
GO:0032099 (negative regulation of appetite)
GO:0032868 (response to insulin)
GO:0032922 (circadian regulation of gene expression)
GO:0034339 (regulation of transcription from RNA polymerase II promoter by nuclear hormone receptor)
GO:0035095 (behavioral response to nicotine)
GO:0042060 (wound healing)
GO:0042157 (lipoprotein metabolic process)
GO:0042752 (regulation of circadian rhythm)
GO:0044255 (cellular lipid metabolic process)
GO:0044281 (small molecule metabolic process)
GO:0045722 (positive regulation of gluconeogenesis)
GO:0045776 (negative regulation of blood pressure)
GO:0045820 (negative regulation of glycolytic process)
GO:0045893 (positive regulation of transcription, DNA-templated)
GO:0045944 (positive regulation of transcription from RNA polymerase II promoter)
GO:0046321 (positive regulation of fatty acid oxidation)
GO:0070166 (enamel mineralization)
GO:0072363 (regulation of glycolysis by positive regulation of transcription from an RNA polymerase II promoter)
GO:0072363 (regulation of glycolytic process by positive regulation of transcription from RNA polymerase II promoter)
GO:0072366 (regulation of cellular ketone metabolic process by positive regulation of transcription from RNA polymerase II promoter)
GO:0072366 (regulation of cellular ketone metabolic process by positive regulation of transcription from an RNA polymerase II promoter)
GO:0072369 (regulation of lipid transport by positive regulation of transcription from RNA polymerase II promoter)
GO:0072369 (regulation of lipid transport by positive regulation of transcription from an RNA polymerase II promoter)
GO:1901215 (negative regulation of neuron death)
GO:2000678 (negative regulation of transcription regulatory region DNA binding)
Wikipedia Peroxisome_proliferator-activated_receptor_alpha

Target Cross References - Protein

canSAR Q07869
Human Protein Atlas ENSG00000186951
IntAct Q07869
PharmGKB PA280
UniProt Q07869 Q16241 Q6I9S0 Q92486 Q92689 Q9Y3N1

Target Cross References - Domain

InterPro IPR000536 (Nucl_hrmn_rcpt_lig-bd.)
IPR000536 (Nucl_hrmn_rcpt_lig-bd_core.)
IPR001628 (Znf_hrmn_rcpt.)
IPR001723 (Nuclear_hrmn_rcpt.)
IPR001723 (Str_hrmn_rcpt.)
IPR003074 (1Cnucl_rcpt.)
IPR003076 (1Cnucl_rcpt_A.)
IPR008946 (Nucl_hormone_rcpt_ligand-bd.)
IPR013088 (Znf_NHR/GATA.)
Pfam PF00104 (Hormone_recep)
PF00105 (zf-C4)

Target Cross References - Structure

PDBe 1I7G 1K7L 1KKQ 2NPA 2P54 2REW 2ZNN 3ET1 3FEI 3G8I 3KDT 3KDU 3SP6 3VI8 4BCR 4CI4
CREDO 1I7G 1K7L 1KKQ 2NPA 2P54 2REW 2ZNN 3ET1 3FEI 3G8I 3KDT 3KDU 3SP6 3VI8 4BCR 4CI4
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