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PsychedeliaDokholyan Laboratory
TargetUnclassified

Hypoxia-inducible factor 1-alpha

Matched no rule. Shown as-is rather than assigned a class by guesswork. Values below are reported as measured; because this is not a molecular target, they are not treated as affinities anywhere on this site.

Measurements
4
Compounds
2
Binding constants
0
Median pX
—

I · Identity

What this target is

Its function as UniProt states it, where in a cell the protein is found, and which cell types and tissues transcribe its gene.

Protein

HIF1A_HUMANHIF1AHomo sapiens

Hypoxia-inducible factor 1-alpha

Functions as a master transcriptional regulator of the adaptive response to hypoxia11292861,11566883,15465032,16973622,17610843,18658046,20624928,22009797,30125331,9887100. Under hypoxic conditions, activates the transcription of over 40 genes, including erythropoietin, glucose transporters, glycolytic enzymes, vascular endothelial growth factor, HILPDA, and other genes whose protein products increase oxygen delivery or facilitate metabolic adaptation to hypoxia11292861,11566883,15465032,16973622,17610843,20624928,22009797,30125331,9887100. Plays an essential role in embryonic vascularization, tumor angiogenesis and pathophysiology of ischemic disease22009797. Heterodimerizes with ARNT; heterodimer binds to core DNA sequence 5'-TACGTG-3' within the hypoxia response element (HRE) of target gene promoters (By similarity). Activation requires recruitment of transcriptional coactivators such as CREBBP and EP30016543236,9887100. Activity is enhanced by interaction with NCOA1 and/or NCOA210594042. Interaction with redox regulatory protein APEX1 seems to activate CTAD and potentiates activation by NCOA1 and CREBBP10202154,10594042. Involved in the axonal distribution and transport of mitochondria in neurons during hypoxia19528298
(Microbial infection) Upon infection by human coronavirus SARS-CoV-2, is required for induction of glycolysis in monocytes and the consequent pro-inflammatory state32697943. In monocytes, induces expression of ACE2 and cytokines such as IL1B, TNF, IL6, and interferons32697943. Promotes human coronavirus SARS-CoV-2 replication and monocyte inflammatory response32697943

Quoted from UniProt’s FUNCTION annotation for Q16665 (reviewed). The superscript numbers are UniProt’s own PubMed citations, kept in the sentence and in order, each linking to the paper it names.

What it acts with

STRING’s highest-confidence human functional partners. The combined score mixes several kinds of evidence, so each channel is shown separately — a partner supported by experiment is a different claim from one supported only by text mining, and for a receptor this is where its coupling appears as evidence rather than as assertion.

PartnerCombinedExperimentDatabaseText mining
EGLN30.9990.9420.9000.950
ARNT0.9990.9990.9000.990
CUL20.9990.7880.9000.958
CREBBP0.9990.9910.9000.990
HIF1AN0.9990.9910.7500.931
ARNT20.9990.6940.9000.984
EGLN20.9990.8920.9000.937
TP530.9990.8470.0000.994
EP3000.9990.9990.9000.996
ELOB0.9990.9660.9000.972

Where it sits in the cell

  • Nucleoplasm
  • Nuclear bodies

Human Protein Atlas, by antibody immunofluorescence in cell lines — a different assay from the expression figures below, which are RNA.

UniProt, curated Cytoplasm · Nucleus · Nucleus speckle

Expression by cell type

Single cell type RNA, the 4 highest of those the Human Protein Atlas reports for this gene. Transcript, not protein, and a cell type rather than a tissue.

  • Neutrophils1,937.7 nCPM
  • monocytes643.4 nCPM
  • Neutrophil progenitors642.2 nCPM
  • Renal collecting duct principal cells611.8 nCPM

Expression by tissue

The tissues this gene is enriched in, by consensus RNA. A tissue absent from this list is one the Atlas does not call specific for this gene, which is not the same as absent from it.

  • bone marrow423.5 nTPM

II · Anatomy

Where the gene is transcribed

The same two atlases the compound plates use, asked about this gene alone. Brain on the left, peripheral and autonomic tissues on the right.

Brain

cerebral cortex — 49.3 nTPM, from HIF1Acerebellum — 29.6 nTPM, from HIF1Ahippocampal formation — 20.4 nTPM, from HIF1Aamygdala — 24.8 nTPM, from HIF1Ahypothalamus — 25.5 nTPM, from HIF1Athalamus — no resolved target expressed herebasal ganglia — 27.6 nTPM, from HIF1Amedulla oblongata — no resolved target expressed here

basal ganglia: drawn as the caudate nucleus, putamen and globus pallidus.

Measured but not drawn — this anatomogram has no outline for them: retina 32.9, midbrain 30.5, pituitary gland 28.8, spinal cord 28.3.

Body

heart — 34.2 nTPM, from HIF1Asmooth muscle — 55.1 nTPM, from HIF1Alung — 71.4 nTPM, from HIF1Aliver — 48.3 nTPM, from HIF1Akidney — 74.1 nTPM, from HIF1Astomach — 35.5 nTPM, from HIF1Aduodenum — 31.7 nTPM, from HIF1Asmall intestine — 35.1 nTPM, from HIF1Acolon — 40.1 nTPM, from HIF1Aadrenal gland — 126.2 nTPM, from HIF1Athyroid gland — 46.4 nTPM, from HIF1Apancreas — 33.9 nTPM, from HIF1Aurinary bladder — 158.4 nTPM, from HIF1Askeletal muscle — 11.5 nTPM, from HIF1Aspleen — 68.2 nTPM, from HIF1Asalivary gland — 42.8 nTPM, from HIF1A
0158 nTPM

Square-root ramp · shared scale across both plates

Shading is transcript level — not affinity, and not affinity combined with expression. Outlined but unshaded organs hold none of HIF1A transcript above the atlas’s detection threshold. Anatomy from EMBL-EBI Anatomogram (Apache License 2.0); regions identified by Uberon (uberon.org), CC BY 3.0.

Brain · 10

  • cerebral cortex49.3 nTPM
  • retina32.9 nTPM
  • midbrain30.5 nTPM
  • cerebellum29.6 nTPM
  • pituitary gland28.8 nTPM
  • spinal cord28.3 nTPM
  • basal ganglia27.6 nTPM
  • hypothalamus25.5 nTPM
  • amygdala24.8 nTPM
  • hippocampal formation20.4 nTPM

Peripheral and autonomic · 16

  • urinary bladder158.4 nTPM
  • adrenal gland126.2 nTPM
  • kidney74.1 nTPM
  • lung71.4 nTPM
  • spleen68.2 nTPM
  • smooth muscle55.1 nTPM
  • liver48.3 nTPM
  • thyroid gland46.4 nTPM
  • salivary gland42.8 nTPM
  • colon40.1 nTPM
  • stomach 135.5 nTPM
  • small intestine35.1 nTPM
  • heart muscle34.2 nTPM
  • pancreas33.9 nTPM
  • duodenum31.7 nTPM
  • skeletal muscle11.5 nTPM

Transcript is not protein. These are RNA levels for HIF1A, shaded on √nTPM so that a three-order range stays legible — on a linear ramp every region but the strongest would read as blank, which looks like absence rather than less. A region carrying no shading is one the atlas reports no consensus value for, not one where the gene is silent. And a gene being transcribed somewhere is not evidence that any compound reaches it. Human Protein Atlas, RNA expression, nTPM (normalized transcripts per million), consensus tissue dataset.

IV · Evidence

Every measurement at this target

Each row links to the ChEMBL assay it came from.

Functional readouts 4

IC₅₀, EC₅₀, AC₅₀ and potency. Assay-dependent, and not interchangeable with a binding constant.

TargetClassTypeValue (nM)pXOrganismAssay
Hypoxia-inducible factor 1-alphaUnclassifiedPotency— no normalized value— value does not convert to pXHomo sapiensCHEMBL1614456
Hypoxia-inducible factor 1-alphaUnclassifiedPotency— no normalized value— value does not convert to pXHomo sapiensCHEMBL1614456
Hypoxia-inducible factor 1-alphaUnclassifiedPotency— no normalized value— value does not convert to pXHomo sapiensCHEMBL1613803
Hypoxia-inducible factor 1-alphaUnclassifiedPotency— no normalized value— value does not convert to pXHomo sapiensCHEMBL1613803
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