dual specificity tyrosine phosphorylation regulated kinase 3 | Dyrk2 subfamily | IUPHAR/BPS Guide to PHARMACOLOGY

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dual specificity tyrosine phosphorylation regulated kinase 3

Target not currently curated in GtoImmuPdb

Target id: 2012

Nomenclature: dual specificity tyrosine phosphorylation regulated kinase 3

Abbreviated Name: DYRK3

Family: Dyrk2 subfamily

Annotation status:  image of an orange circle Annotated and awaiting review. Please contact us if you can help with reviewing.  » Email us

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 588 1q32 DYRK3 dual specificity tyrosine phosphorylation regulated kinase 3
Mouse - 586 1 E4 Dyrk3 dual-specificity tyrosine-(Y)-phosphorylation regulated kinase 3
Rat - 586 13 q13 Dyrk3 dual specificity tyrosine phosphorylation regulated kinase 3
Previous and Unofficial Names
REDK | regulatory erythroid kinase | dual-specificity tyrosine-(Y)-phosphorylation regulated kinase 3 | dual specificity tyrosine-(Y)-phosphorylation regulated kinase 3
Database Links
BRENDA
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Enzyme Reaction
EC Number: 2.7.12.1

Download all structure-activity data for this target as a CSV file

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Parameter Reference
compound 1a [PMID: 24900749] Hs Inhibition 7.2 pIC50 4
pIC50 7.2 (IC50 7x10-8 M) [4]
compound 3b [PMID: 23454515] Hs Inhibition 6.7 pIC50 2
pIC50 6.7 (IC50 1.8x10-7 M) [2]
kinase inhibitor 2 [PMID: 30199702] Hs Inhibition 6.4 pIC50 3
pIC50 6.4 (IC50 3.8x10-7 M) [3]
EMD Millipore KinaseProfilerTM screen/Reaction Biology Kinase HotspotSM screen
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/DYRK3
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
K-252a Hs Inhibitor Inhibition 10.4
SB 218078 Hs Inhibitor Inhibition 16.6
JAK3 inhibitor VI Hs Inhibitor Inhibition 30.4
staurosporine Hs Inhibitor Inhibition 31.3
PKR inhibitor Hs Inhibitor Inhibition 39.2
Cdc2-like kinase inhibitor Hs Inhibitor Inhibition 50.4
sunitinib Hs Inhibitor Inhibition 58.2
PI 3-Kg inhibitor Hs Inhibitor Inhibition 71.5
dorsomorphin Hs Inhibitor Inhibition 76.8
GSK-3 inhibitor XIII Hs Inhibitor Inhibition 79.6
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. Burgy G, Tahtouh T, Durieu E, Foll-Josselin B, Limanton E, Meijer L, Carreaux F, Bazureau JP. (2013) Chemical synthesis and biological validation of immobilized protein kinase inhibitory Leucettines. Eur J Med Chem, 62: 728-37. [PMID:23454515]

3. Compain G, Oumata N, Clarhaut J, Péraudeau E, Renoux B, Galons H, Papot S. (2018) A β-glucuronidase-responsive albumin-binding prodrug for potential selective kinase inhibitor-based cancer chemotherapy. Eur J Med Chem, 158: 1-6. [PMID:30199702]

4. Dowling JE, Alimzhanov M, Bao L, Block MH, Chuaqui C, Cooke EL, Denz CR, Hird A, Huang S, Larsen NA et al.. (2013) Structure and Property Based Design of Pyrazolo[1,5-a]pyrimidine Inhibitors of CK2 Kinase with Activity in Vivo. ACS Med Chem Lett, 4 (8): 800-5. [PMID:24900749]

How to cite this page

Dyrk2 subfamily: dual specificity tyrosine phosphorylation regulated kinase 3. Last modified on 11/09/2018. Accessed on 24/04/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2012.