Dual specificity tyrosine-phosphorylation-regulated kinase 1A
Named enzymes, including the metabolising cytochromes and the monoamine oxidases.
- Measurements
- 78
- Compounds
- 6
- Binding constants
- 3
- Median pX
- 7.87
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.
Dual specificity tyrosine-phosphorylation-regulated kinase 1A
Dual-specificity kinase which possesses both serine/threonine and tyrosine kinase activities20981014,21127067,23665168,30773093,8769099. Exhibits a substrate preference for proline at position P+1 and arginine at position P-323665168. Plays an important role in double-strand breaks (DSBs) repair following DNA damage31024071. Mechanistically, phosphorylates RNF169 and increases its ability to block accumulation of TP53BP1 at the DSB sites thereby promoting homologous recombination repair (HRR)30773093. Also acts as a positive regulator of transcription by acting as a CTD kinase that mediates phosphorylation of the CTD (C-terminal domain) of the large subunit of RNA polymerase II (RNAP II) POLR2A25620562,29849146. May play a role in a signaling pathway regulating nuclear functions of cell proliferation14500717. Modulates alternative splicing by phosphorylating the splice factor SRSF6 (By similarity). Has pro-survival function and negatively regulates the apoptotic process (By similarity). Promotes cell survival upon genotoxic stress through phosphorylation of SIRT1 (By similarity). This in turn inhibits p53/TP53 activity and apoptosis (By similarity). Phosphorylates SEPTIN4, SEPTIN5 and SF3B1 at 'Thr-434' (By similarity)
Quoted from UniProt’s FUNCTION annotation for Q13627 (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.
| Partner | Combined | Experiment | Database | Text mining |
|---|---|---|---|---|
| DCAF7 | 0.997 | 0.953 | 0.000 | 0.938 |
| RNF169 | 0.932 | 0.827 | 0.000 | 0.606 |
| RAD54L2 | 0.925 | 0.790 | 0.000 | 0.653 |
| LIN52 | 0.903 | 0.625 | 0.400 | 0.605 |
| FAM53C | 0.900 | 0.873 | 0.000 | 0.233 |
| FAM117B | 0.882 | 0.841 | 0.000 | 0.269 |
| RCAN1 | 0.881 | 0.097 | 0.000 | 0.874 |
| WDR26 | 0.842 | 0.292 | 0.000 | 0.000 |
| MED13L | 0.820 | 0.000 | 0.000 | 0.595 |
| NFATC1 | 0.819 | 0.000 | 0.000 | 0.817 |
Where it sits in the cell
- Nuclear speckles
- Nucleoplasmadditional
- Centrosomeadditional
- Cytosoladditional
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 1 highest of those the Human Protein Atlas reports for this gene. Transcript, not protein, and a cell type rather than a tissue.
- Neutrophils1,182.9 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
basal ganglia: drawn as the caudate nucleus, putamen and globus pallidus.
Measured but not drawn — this anatomogram has no outline for them: retina 25.7, pituitary gland 18.6, midbrain 13.4, spinal cord 12.6.
Body
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 DYRK1A 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
- retina25.7 nTPM
- cerebellum22.2 nTPM
- cerebral cortex21.0 nTPM
- pituitary gland18.6 nTPM
- basal ganglia16.9 nTPM
- hippocampal formation16.5 nTPM
- amygdala16.4 nTPM
- hypothalamus15.6 nTPM
- midbrain13.4 nTPM
- spinal cord12.6 nTPM
Peripheral and autonomic · 16
- skeletal muscle43.4 nTPM
- spleen28.6 nTPM
- heart muscle27.1 nTPM
- thyroid gland24.1 nTPM
- smooth muscle22.5 nTPM
- urinary bladder21.8 nTPM
- stomach 121.5 nTPM
- lung20.3 nTPM
- pancreas20.3 nTPM
- colon19.8 nTPM
- small intestine19.7 nTPM
- adrenal gland19.2 nTPM
- salivary gland19.1 nTPM
- kidney18.6 nTPM
- liver18.5 nTPM
- duodenum17.6 nTPM
Transcript is not protein. These are RNA levels for DYRK1A, 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.
III · Ranking
Compounds by strongest binding constant
One bar per compound: its strongest Ki or Kd at this target, expressed as pX. Compounds measured here only by a functional assay do not appear — they are in the table below.
IV · Evidence
Every measurement at this target
Each row links to the ChEMBL assay it came from.
Equilibrium binding constants 3
Ki and Kd — a concentration at equilibrium. Directly comparable across rows at the same target.
| Target | Class | Type | Value (nM) | pX | Organism | Assay |
|---|---|---|---|---|---|---|
| Dual specificity tyrosine-phosphorylation-regulated kinase 1A | Enzymes | Kd | 5.47 | 8.26 | Homo sapiens | CHEMBL5251383 |
| Dual specificity tyrosine-phosphorylation-regulated kinase 1A | Enzymes | Kd | 13.40 | 7.87 | Homo sapiens | CHEMBL5251692 |
| Dual specificity tyrosine-phosphorylation-regulated kinase 1A | Enzymes | Ki | 33.00 | 7.48 | Homo sapiens | CHEMBL2394349 |
Functional readouts 54
IC₅₀, EC₅₀, AC₅₀ and potency. Assay-dependent, and not interchangeable with a binding constant.
Other measurements 21
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.
| Target | Class | Type | Value (nM) | pX | Organism | Assay |
|---|---|---|---|---|---|---|
| Dual specificity tyrosine-phosphorylation-regulated kinase 1A | Enzymes | TIME | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5251386 |
| Dual specificity tyrosine-phosphorylation-regulated kinase 1A | Enzymes | Tm | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5251701 |
| Dual specificity tyrosine-phosphorylation-regulated kinase 1A | Enzymes | Activity | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL1062005 |
| Dual specificity tyrosine-phosphorylation-regulated kinase 1A | Enzymes | Activity | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL1062005 |
| Dual specificity tyrosine-phosphorylation-regulated kinase 1A | Enzymes | Activity | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL1062005 |
| Dual specificity tyrosine-phosphorylation-regulated kinase 1A | Enzymes | Activity | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL2186710 |
| Dual specificity tyrosine-phosphorylation-regulated kinase 1A | Enzymes | Inhibition | — no normalized value | — value does not convert to pX | Rattus norvegicus | CHEMBL2183878 |
| Dual specificity tyrosine-phosphorylation-regulated kinase 1A | Enzymes | Activity | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL4151461 |
| Dual specificity tyrosine-phosphorylation-regulated kinase 1A | Enzymes | Inhibition | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL4151432 |
| Dual specificity tyrosine-phosphorylation-regulated kinase 1A | Enzymes | Inhibition | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL4151433 |
| Dual specificity tyrosine-phosphorylation-regulated kinase 1A | Enzymes | FC | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL4151882 |
| Dual specificity tyrosine-phosphorylation-regulated kinase 1A | Enzymes | Activity | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL4263574 |
| Dual specificity tyrosine-phosphorylation-regulated kinase 1A | Enzymes | Inhibition | — no normalized value | — value does not convert to pX | Mus musculus | CHEMBL4344352 |
| Dual specificity tyrosine-phosphorylation-regulated kinase 1A | Enzymes | Activity | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL4344400 |
| Dual specificity tyrosine-phosphorylation-regulated kinase 1A | Enzymes | Inhibition | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5251703 |
| Dual specificity tyrosine-phosphorylation-regulated kinase 1A | Enzymes | Inhibition | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5251706 |
| Dual specificity tyrosine-phosphorylation-regulated kinase 1A | Enzymes | Inhibition | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5548730 |
| Dual specificity tyrosine-phosphorylation-regulated kinase 1A | Enzymes | Inhibition | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL4266652 |
| Dual specificity tyrosine-phosphorylation-regulated kinase 1A | Enzymes | Inhibition | — no normalized value | — value does not convert to pX | Rattus norvegicus | CHEMBL4824379 |
| Dual specificity tyrosine-phosphorylation-regulated kinase 1A | Enzymes | Inhibition | — no normalized value | — value does not convert to pX | Rattus norvegicus | CHEMBL4824380 |
| Dual specificity tyrosine-phosphorylation-regulated kinase 1A | Enzymes | Activity | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL1062005 |