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TargetEnzymes

Dual specificity protein kinase CLK2

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

Measurements
6
Compounds
1
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

CLK2_HUMANCLK2Homo sapiens

Dual specificity protein kinase CLK2

Dual specificity kinase acting on both serine/threonine and tyrosine-containing substrates. Phosphorylates serine- and arginine-rich (SR) proteins of the spliceosomal complex. May be a constituent of a network of regulatory mechanisms that enable SR proteins to control RNA splicing and can cause redistribution of SR proteins from speckles to a diffuse nucleoplasmic distribution. Acts as a suppressor of hepatic gluconeogenesis and glucose output by repressing PPARGC1A transcriptional activity on gluconeogenic genes via its phosphorylation. Phosphorylates PPP2R5B thereby stimulating the assembly of PP2A phosphatase with the PPP2R5B-AKT1 complex leading to dephosphorylation of AKT1. Phosphorylates: PTPN1, SRSF1 and SRSF3. Regulates the alternative splicing of tissue factor (F3) pre-mRNA in endothelial cells. Phosphorylates PAGE4 at several serine and threonine residues and this phosphorylation attenuates the ability of PAGE4 to potentiate the transcriptional activator activity of JUN28289210

Quoted from UniProt’s FUNCTION annotation for P49760 (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
RSRP10.8490.7910.0000.269
CLK30.8460.8360.0000.078
BCLAF10.8010.7810.0000.127
CLK10.7920.7790.0000.062
RBBP60.7880.7820.0000.000
SNIP10.7810.7810.0000.000
PAFAH1B30.7700.0000.0000.770
ACIN10.7480.7020.0000.090
SRSF120.7320.6300.0000.280
SRSF80.7290.7170.0000.082

Where it sits in the cell

  • Nucleoplasm
  • Nuclear bodiesadditional

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

UniProt, curated Nucleus · Nucleus speckle

Expression by cell type

Single cell type RNA, the 12 highest of those the Human Protein Atlas reports for this gene. Transcript, not protein, and a cell type rather than a tissue.

  • Proximal tubule cells25.4 nCPM
  • Choroid plexus epithelial cells22.4 nCPM
  • Podocytes19.1 nCPM
  • Bergmann glia18.8 nCPM
  • Loop of henle epithelial cells18.4 nCPM
  • Distal convoluted tubule cells18.3 nCPM
  • Astrocytes17.9 nCPM
  • Renal connecting tubule cells17.5 nCPM
  • Renal collecting duct intercalated cells17.3 nCPM
  • Renal collecting duct principal cells17.3 nCPM
  • Microglia16 nCPM
  • Oligodendrocytes14.2 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.

039 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 CLK2 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

  • pituitary gland30.3 nTPM
  • cerebellum27.9 nTPM
  • cerebral cortex14.4 nTPM
  • spinal cord12.3 nTPM
  • hippocampal formation11.7 nTPM
  • basal ganglia11.1 nTPM
  • midbrain10.7 nTPM
  • amygdala10.6 nTPM
  • hypothalamus10.1 nTPM
  • retina8.7 nTPM

Peripheral and autonomic · 16

  • spleen39.2 nTPM
  • thyroid gland32.5 nTPM
  • kidney28.7 nTPM
  • liver28.2 nTPM
  • urinary bladder27.2 nTPM
  • adrenal gland25.3 nTPM
  • pancreas23.8 nTPM
  • colon23.3 nTPM
  • small intestine23.1 nTPM
  • salivary gland22.3 nTPM
  • lung21.2 nTPM
  • stomach 120.6 nTPM
  • heart muscle17.9 nTPM
  • skeletal muscle15.5 nTPM
  • duodenum11.0 nTPM
  • smooth muscle10.2 nTPM

Transcript is not protein. These are RNA levels for CLK2, 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 3

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

TargetClassTypeValue (nM)pXOrganismAssay
Dual specificity protein kinase CLK2EnzymesIC501206.92Homo sapiensCHEMBL5235541
Dual specificity protein kinase CLK2EnzymesIC502806.55Mus musculusCHEMBL2182298
Dual specificity protein kinase CLK2EnzymesIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5251366

Other measurements 3

Everything else ChEMBL recorded for this compound — percentage inhibition, efficacy, half-life, cytotoxicity. Reported in the assay's own units, which is why no value is converted here.

TargetClassTypeValue (nM)pXOrganismAssay
Dual specificity protein kinase CLK2EnzymesActivity— no normalized value— value does not convert to pXHomo sapiensCHEMBL4151449
Dual specificity protein kinase CLK2EnzymesActivity— no normalized value— value does not convert to pXHomo sapiensCHEMBL4344393
Dual specificity protein kinase CLK2EnzymesActivity— no normalized value— value does not convert to pXHomo sapiensCHEMBL2186703