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PsychedeliaDokholyan Laboratory
TargetEnzymes

cGMP-specific 3',5'-cyclic phosphodiesterase

Named enzymes, including the metabolising cytochromes and the monoamine oxidases.

Measurements
14
Compounds
7
Binding constants
7
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

PDE5A_HUMANPDE5AHomo sapiens

cGMP-specific 3',5'-cyclic phosphodiesterase

Plays a role in signal transduction by regulating the intracellular concentration of cyclic nucleotides. This phosphodiesterase catalyzes the specific hydrolysis of cGMP to 5'-GMP15489334,9714779. Specifically regulates nitric-oxide-generated cGMP15489334

Quoted from UniProt’s FUNCTION annotation for O76074 (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
PDE2A0.9500.9010.4000.228
ALDH7A10.9460.0000.0000.946
PDE6G0.9320.9130.0000.244
APRT0.9160.0000.9000.197
GMPR0.9100.1070.9000.072
GUK10.9060.0460.9000.074
ITPA0.9040.0000.9000.080
HPRT10.9030.0000.9000.079
GMPS0.9030.0000.9000.073
GUCY1B10.8880.1260.6940.561

Where it sits in the cell

  • Cytosol
  • Basal bodyadditional

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

Expression by cell type

Single cell type RNA, the 8 highest of those the Human Protein Atlas reports for this gene. Transcript, not protein, and a cell type rather than a tissue.

  • Cardiomyocytes588.8 nCPM
  • Platelets551.1 nCPM
  • Epicardial cells498 nCPM
  • Adipocytes362 nCPM
  • Fibro-adipogenic progenitors334.3 nCPM
  • Vascular smooth muscle cells333.2 nCPM
  • Peritubular myoid cells329.7 nCPM
  • Myonuclei310.9 nCPM

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 — 3.8 nTPM, from PDE5Acerebellum — 1.9 nTPM, from PDE5Ahippocampal formation — 1.8 nTPM, from PDE5Aamygdala — 1.8 nTPM, from PDE5Ahypothalamus — 2.6 nTPM, from PDE5Athalamus — no resolved target expressed herebasal ganglia — 2.0 nTPM, from PDE5Amedulla 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 9.8, pituitary gland 3.3, midbrain 2.1, spinal cord 1.4.

Body

heart — 12.1 nTPM, from PDE5Asmooth muscle — 10.6 nTPM, from PDE5Alung — 21.0 nTPM, from PDE5Aliver — 1.5 nTPM, from PDE5Akidney — 5.6 nTPM, from PDE5Astomach — 9.0 nTPM, from PDE5Aduodenum — 14.7 nTPM, from PDE5Asmall intestine — 17.9 nTPM, from PDE5Acolon — 34.6 nTPM, from PDE5Aadrenal gland — 10.8 nTPM, from PDE5Athyroid gland — 15.9 nTPM, from PDE5Apancreas — 11.9 nTPM, from PDE5Aurinary bladder — 13.7 nTPM, from PDE5Askeletal muscle — 6.7 nTPM, from PDE5Aspleen — 5.6 nTPM, from PDE5Asalivary gland — 9.3 nTPM, from PDE5A
035 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 PDE5A 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

  • retina9.8 nTPM
  • cerebral cortex3.8 nTPM
  • pituitary gland3.3 nTPM
  • hypothalamus2.6 nTPM
  • midbrain2.1 nTPM
  • basal ganglia2.0 nTPM
  • cerebellum1.9 nTPM
  • hippocampal formation1.8 nTPM
  • amygdala1.8 nTPM
  • spinal cord1.4 nTPM

Peripheral and autonomic · 16

  • colon34.6 nTPM
  • lung21.0 nTPM
  • small intestine17.9 nTPM
  • thyroid gland15.9 nTPM
  • duodenum14.7 nTPM
  • urinary bladder13.7 nTPM
  • heart muscle12.1 nTPM
  • pancreas11.9 nTPM
  • adrenal gland10.8 nTPM
  • smooth muscle10.6 nTPM
  • salivary gland9.3 nTPM
  • stomach 19.0 nTPM
  • skeletal muscle6.7 nTPM
  • kidney5.6 nTPM
  • spleen5.6 nTPM
  • liver1.5 nTPM

Transcript is not protein. These are RNA levels for PDE5A, 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.

Equilibrium binding constants 7

Ki and Kd — a concentration at equilibrium. Directly comparable across rows at the same target.

TargetClassTypeValue (nM)pXOrganismAssay
cGMP-specific 3',5'-cyclic phosphodiesteraseEnzymesKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909186
cGMP-specific 3',5'-cyclic phosphodiesteraseEnzymesKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909186
cGMP-specific 3',5'-cyclic phosphodiesteraseEnzymesKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909186
cGMP-specific 3',5'-cyclic phosphodiesteraseEnzymesKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909186
cGMP-specific 3',5'-cyclic phosphodiesteraseEnzymesKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909186
cGMP-specific 3',5'-cyclic phosphodiesteraseEnzymesKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909186
cGMP-specific 3',5'-cyclic phosphodiesteraseEnzymesKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909186

Functional readouts 7

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

TargetClassTypeValue (nM)pXOrganismAssay
cGMP-specific 3',5'-cyclic phosphodiesteraseEnzymesIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909186
cGMP-specific 3',5'-cyclic phosphodiesteraseEnzymesIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909186
cGMP-specific 3',5'-cyclic phosphodiesteraseEnzymesIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909186
cGMP-specific 3',5'-cyclic phosphodiesteraseEnzymesIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909186
cGMP-specific 3',5'-cyclic phosphodiesteraseEnzymesIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909186
cGMP-specific 3',5'-cyclic phosphodiesteraseEnzymesIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909186
cGMP-specific 3',5'-cyclic phosphodiesteraseEnzymesIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909186
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