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Target Report Card

Target Name and Classification

Target ID CHEMBL4261
Target Type SINGLE PROTEIN
Preferred Name Hypoxia-inducible factor 1 alpha
Synonyms ARNT-interacting protein | BHLHE78 | Basic-helix-loop-helix-PAS protein MOP1 | Class E basic helix-loop-helix protein 78 | HIF-1-alpha | HIF1-alpha | HIF1A | Hypoxia-inducible factor 1-alpha | MOP1 | Member of PAS protein 1 | PAS domain-containing protein 8 | PASD8 | bHLHe78
Organism Homo sapiens
Species Group No
Protein Target Classification
  • transcription factor

Target Components

Component Description Relationship Accession
Hypoxia-inducible factor 1-alpha SINGLE PROTEIN Q16665

Target Relations

ChEMBL ID Pref Name Target Type
CHEMBL2221345 Hypoxia inducible factors; HIF-1-alpha, HIF-2-alpha PROTEIN FAMILY

Target Associated Bioactivities

Target Associated Assays

Target Ligand Efficiencies

Target Associated Compound Properties

Target Cross References - Gene

Array Express ENSG00000100644
Ensembl ENSG00000100644
GO Cellular Component GO:0005634 (nucleus)
GO:0005654 (nucleoplasm)
GO:0005667 (transcription factor complex)
GO:0005737 (cytoplasm)
GO:0005829 (cytosol)
GO:0016607 (nuclear speck)
GO:0031514 (motile cilium)
GO:0090575 (RNA polymerase II transcription factor complex)
GO:1904115 (axon cytoplasm)
GO Molecular Function GO:0000981 (RNA polymerase II transcription factor activity, sequence-specific DNA binding)
GO:0000989 (transcription factor activity, transcription factor binding)
GO:0001076 (transcription factor activity, RNA polymerase II transcription factor binding)
GO:0001077 (transcriptional activator activity, RNA polymerase II core promoter proximal region sequence-specific binding)
GO:0001228 (transcriptional activator activity, RNA polymerase II transcription regulatory region sequence-specific binding)
GO:0003677 (DNA binding)
GO:0003700 (transcription factor activity, sequence-specific DNA binding)
GO:0003705 (transcription factor activity, RNA polymerase II distal enhancer sequence-specific binding)
GO:0005515 (protein binding)
GO:0008134 (transcription factor binding)
GO:0019899 (enzyme binding)
GO:0019901 (protein kinase binding)
GO:0031625 (ubiquitin protein ligase binding)
GO:0032403 (protein complex binding)
GO:0035035 (histone acetyltransferase binding)
GO:0035257 (nuclear hormone receptor binding)
GO:0042826 (histone deacetylase binding)
GO:0043565 (sequence-specific DNA binding)
GO:0046982 (protein heterodimerization activity)
GO:0046983 (protein dimerization activity)
GO:0051879 (Hsp90 protein binding)
GO Biological Process GO:0000122 (negative regulation of transcription from RNA polymerase II promoter)
GO:0001525 (angiogenesis)
GO:0001568 (blood vessel development)
GO:0001666 (response to hypoxia)
GO:0001755 (neural crest cell migration)
GO:0001837 (epithelial to mesenchymal transition)
GO:0001892 (embryonic placenta development)
GO:0001922 (B-1 B cell homeostasis)
GO:0001938 (positive regulation of endothelial cell proliferation)
GO:0001944 (vasculature development)
GO:0001947 (heart looping)
GO:0002052 (positive regulation of neuroblast proliferation)
GO:0002248 (connective tissue replacement involved in inflammatory response wound healing)
GO:0003151 (outflow tract morphogenesis)
GO:0003208 (cardiac ventricle morphogenesis)
GO:0006089 (lactate metabolic process)
GO:0006110 (regulation of glycolytic process)
GO:0006351 (transcription, DNA-templated)
GO:0006355 (regulation of transcription, DNA-templated)
GO:0006366 (transcription from RNA polymerase II promoter)
GO:0006879 (cellular iron ion homeostasis)
GO:0006953 (acute-phase response)
GO:0007165 (signal transduction)
GO:0007595 (lactation)
GO:0008284 (positive regulation of cell proliferation)
GO:0008542 (visual learning)
GO:0009612 (response to mechanical stimulus)
GO:0009651 (response to salt stress)
GO:0009749 (response to glucose)
GO:0010165 (response to X-ray)
GO:0010468 (regulation of gene expression)
GO:0010508 (positive regulation of autophagy)
GO:0010573 (vascular endothelial growth factor production)
GO:0010575 (positive regulation of vascular endothelial growth factor production)
GO:0010628 (positive regulation of gene expression)
GO:0010634 (positive regulation of epithelial cell migration)
GO:0010870 (positive regulation of receptor biosynthetic process)
GO:0010996 (response to auditory stimulus)
GO:0014074 (response to purine-containing compound)
GO:0014823 (response to activity)
GO:0014850 (response to muscle activity)
GO:0016239 (positive regulation of macroautophagy)
GO:0019896 (axonal transport of mitochondrion)
GO:0021502 (neural fold elevation formation)
GO:0021987 (cerebral cortex development)
GO:0030154 (cell differentiation)
GO:0030279 (negative regulation of ossification)
GO:0030502 (negative regulation of bone mineralization)
GO:0030949 (positive regulation of vascular endothelial growth factor receptor signaling pathway)
GO:0032007 (negative regulation of TOR signaling)
GO:0032025 (response to cobalt ion)
GO:0032355 (response to estradiol)
GO:0032364 (oxygen homeostasis)
GO:0032722 (positive regulation of chemokine production)
GO:0032869 (cellular response to insulin stimulus)
GO:0032909 (regulation of transforming growth factor beta2 production)
GO:0032963 (collagen metabolic process)
GO:0035162 (embryonic hemopoiesis)
GO:0035690 (cellular response to drug)
GO:0035774 (positive regulation of insulin secretion involved in cellular response to glucose stimulus)
GO:0042127 (regulation of cell proliferation)
GO:0042493 (response to drug)
GO:0042541 (hemoglobin biosynthetic process)
GO:0042593 (glucose homeostasis)
GO:0042789 (mRNA transcription from RNA polymerase II promoter)
GO:0043065 (positive regulation of apoptotic process)
GO:0043066 (negative regulation of apoptotic process)
GO:0043279 (response to alkaloid)
GO:0043524 (negative regulation of neuron apoptotic process)
GO:0043619 (regulation of transcription from RNA polymerase II promoter in response to oxidative stress)
GO:0043627 (response to estrogen)
GO:0045648 (positive regulation of erythrocyte differentiation)
GO:0045766 (positive regulation of angiogenesis)
GO:0045793 (positive regulation of cell size)
GO:0045821 (positive regulation of glycolytic process)
GO:0045893 (positive regulation of transcription, DNA-templated)
GO:0045906 (negative regulation of vasoconstriction)
GO:0045926 (negative regulation of growth)
GO:0045944 (positive regulation of transcription from RNA polymerase II promoter)
GO:0046716 (muscle cell cellular homeostasis)
GO:0046886 (positive regulation of hormone biosynthetic process)
GO:0048514 (blood vessel morphogenesis)
GO:0048546 (digestive tract morphogenesis)
GO:0048593 (camera-type eye morphogenesis)
GO:0048661 (positive regulation of smooth muscle cell proliferation)
GO:0050790 (regulation of catalytic activity)
GO:0051000 (positive regulation of nitric-oxide synthase activity)
GO:0051216 (cartilage development)
GO:0051384 (response to glucocorticoid)
GO:0051541 (elastin metabolic process)
GO:0060135 (maternal process involved in female pregnancy)
GO:0060574 (intestinal epithelial cell maturation)
GO:0060992 (response to fungicide)
GO:0061030 (epithelial cell differentiation involved in mammary gland alveolus development)
GO:0061072 (iris morphogenesis)
GO:0061298 (retina vasculature development in camera-type eye)
GO:0061418 (regulation of transcription from RNA polymerase II promoter in response to hypoxia)
GO:0061419 (positive regulation of transcription from RNA polymerase II promoter in response to hypoxia)
GO:0070101 (positive regulation of chemokine-mediated signaling pathway)
GO:0070243 (regulation of thymocyte apoptotic process)
GO:0070244 (negative regulation of thymocyte apoptotic process)
GO:0070301 (cellular response to hydrogen peroxide)
GO:0071222 (cellular response to lipopolysaccharide)
GO:0071245 (cellular response to carbon monoxide)
GO:0071250 (cellular response to nitrite)
GO:0071257 (cellular response to electrical stimulus)
GO:0071260 (cellular response to mechanical stimulus)
GO:0071279 (cellular response to cobalt ion)
GO:0071333 (cellular response to glucose stimulus)
GO:0071347 (cellular response to interleukin-1)
GO:0071396 (cellular response to lipid)
GO:0071407 (cellular response to organic cyclic compound)
GO:0071456 (cellular response to hypoxia)
GO:0071482 (cellular response to light stimulus)
GO:0071542 (dopaminergic neuron differentiation)
GO:0072347 (response to anesthetic)
GO:0097237 (cellular response to toxic substance)
GO:0097411 (hypoxia-inducible factor-1alpha signaling pathway)
GO:1900037 (regulation of cellular response to hypoxia)
GO:1902895 (positive regulation of pri-miRNA transcription from RNA polymerase II promoter)
GO:1903377 (negative regulation of oxidative stress-induced neuron intrinsic apoptotic signaling pathway)
GO:1903599 (positive regulation of mitophagy)
GO:1903715 (regulation of aerobic respiration)
GO:1903928 (cellular response to cyanide)
GO:2000378 (negative regulation of reactive oxygen species metabolic process)
GO:2001054 (negative regulation of mesenchymal cell apoptotic process)
Wikipedia HIF1A

Target Cross References - Protein

canSAR Q16665
Human Protein Atlas ENSG00000100644
IntAct Q16665
Open Targets ENSG00000100644
PharmGKB PA29283
Reactome R-HSA-1234158 (Regulation of gene expression by Hypoxia-inducible Factor.)
R-HSA-1234162 (Oxygen-dependent asparagine hydroxylation of Hypoxia-inducible Factor Alpha.)
R-HSA-1234176 (Oxygen-dependent proline hydroxylation of Hypoxia-inducible Factor Alpha.)
R-HSA-1368108 (BMAL1:CLOCK,NPAS2 activates circadian gene expression.)
R-HSA-2122947 (NOTCH1 Intracellular Domain Regulates Transcription.)
R-HSA-400253 (Circadian Clock.)
R-HSA-5689880 (Ub-specific processing proteases.)
R-HSA-6785807 (Interleukin-4 and 13 signaling.)
R-HSA-8849473 (PTK6 Expression.)
R-HSA-8857538 (PTK6 promotes HIF1A stabilization.)
TIMBAL HIF-1a
UniProt C0LZJ3 Q16665 Q53XP6 Q96PT9 Q9UPB1

Target Cross References - Domain

InterPro IPR000014 (PAS.)
IPR001321 (HIF-1_alpha.)
IPR001610 (PAC.)
IPR011598 (bHLH_dom.)
IPR013655 (PAS_fold_3.)
IPR013767 (PAS_fold.)
IPR014887 (HIF-1_TAD_C.)
IPR021537 (HIF_alpha_subunit.)
Pfam PF00989 (PAS)
PF08447 (PAS_3)
PF08778 (HIF-1a_CTAD)
PF11413 (HIF-1)

Target Cross References - Structure

PDBe 1H2K 1H2L 1H2M 1LM8 1LQB 2ILM 3HQR 3HQU 4AJY 4H6J 5JWP 5L9B 5L9V 5LA9 5LAS
CREDO 1H2K 1H2L 1H2M 1LM8 1LQB 2ILM 3HQR 3HQU 4AJY 4H6J 5JWP 5L9B 5L9V 5LA9 5LAS
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