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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-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
CREDO 1H2K 1H2L 1H2M 1LM8 1LQB 2ILM 3HQR 3HQU 4AJY 4H6J
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