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dual specificity tyrosine phosphorylation regulated kinase 4

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Target not currently curated in GtoImmuPdb

Target id: 2013

Nomenclature: dual specificity tyrosine phosphorylation regulated kinase 4

Abbreviated Name: DYRK4

Family: Dyrk1 subfamily

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 520 12p13.32 DYRK4 dual specificity tyrosine phosphorylation regulated kinase 4
Mouse - 632 6 F3 Dyrk4 dual-specificity tyrosine-(Y)-phosphorylation regulated kinase 4
Rat - - 4 q42 Dyrk4 dual specificity tyrosine phosphorylation regulated kinase 4
Previous and Unofficial Names Click here for help
RAD51 associated protein 1 | Rad51ap1 | dual specificity tyrosine-(Y)-phosphorylation regulated kinase 4
Database Links Click here for help
Alphafold
BRENDA
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
Pharos
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Enzyme Reaction Click here for help
EC Number: 2.7.12.1

Download all structure-activity data for this target as a CSV file go icon to follow link

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
leucettine L41 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.3 pIC50 2
pIC50 6.3 (IC50 5.2x10-7 M) [2]
EMD Millipore KinaseProfilerTM screen/Reaction Biology Kinase HotspotSM screen Click here for help
A screen profiling 158 kinase inhibitors (Calbiochem Protein Kinase Inhibitor Library I and II, catalogue numbers 539744 and 539745) for their inhibitory activity at 1µM and 10µM against 234 human recombinant kinases using the EMD Millipore KinaseProfilerTM service.

A screen profiling the inhibitory activity of 178 commercially available kinase inhibitors at 0.5µM against a panel of 300 recombinant protein kinases using the Reaction Biology Corporation Kinase HotspotSM platform.

http://www.millipore.com/techpublications/tech1/pf3036
http://www.reactionbiology.com/webapps/main/pages/kinase.aspx


Reference: ...1

Key to terms and symbols Click column headers to sort
Target used in screen: nd/DYRK4
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
JNK inhibitor V Small molecule or natural product Hs Inhibitor Inhibition 65.0
Syk inhibitor Small molecule or natural product Immunopharmacology Ligand Hs Inhibitor Inhibition 73.7
PDGF receptor tyrosine kinase inhibitor III Small molecule or natural product Hs Inhibitor Inhibition 79.8
p38 MAP kinase inhibitor Small molecule or natural product Hs Inhibitor Inhibition 81.5
Cdc2-like kinase inhibitor Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 82.3
Tpl2 kinase inhibitor Small molecule or natural product Hs Inhibitor Inhibition 84.4
Syk inhibitor III Small molecule or natural product Hs Inhibitor Inhibition 84.9
D4476 Small molecule or natural product Immunopharmacology Ligand Hs Inhibitor Inhibition 85.6
Cdk4 inhibitor Small molecule or natural product Hs Inhibitor Inhibition 86.0
PDGF receptor tyrosine kinase inhibitor II Small molecule or natural product Hs Inhibitor Inhibition 86.0
Displaying the top 10 most potent ligands  View all ligands in screen »

References

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1. Anastassiadis T, Deacon SW, Devarajan K, Ma H, Peterson JR. (2011) Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity. Nat Biotechnol, 29 (11): 1039-45. [PMID:22037377]

2. Tahtouh T, Elkins JM, Filippakopoulos P, Soundararajan M, Burgy G, Durieu E, Cochet C, Schmid RS, Lo DC, Delhommel F et al.. (2012) Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B. J Med Chem, 55 (21): 9312-30. [PMID:22998443]

How to cite this page

Dyrk1 subfamily: dual specificity tyrosine phosphorylation regulated kinase 4. Last modified on 30/03/2016. Accessed on 20/09/2021. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2013.