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dual specificity tyrosine phosphorylation regulated kinase 3

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Target id: 2012

Nomenclature: dual specificity tyrosine phosphorylation regulated kinase 3

Abbreviated Name: DYRK3

Family: Dyrk2 subfamily

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 588 1q32.1 DYRK3 dual specificity tyrosine phosphorylation regulated kinase 3
Mouse - 586 1 E4 Dyrk3 dual-specificity tyrosine phosphorylation regulated kinase 3
Rat - 586 13q13 Dyrk3 dual specificity tyrosine phosphorylation regulated kinase 3
Previous and Unofficial Names Click here for help
REDK | regulatory erythroid kinase | dual-specificity tyrosine-(Y)-phosphorylation regulated kinase 3 | dual specificity tyrosine-(Y)-phosphorylation regulated kinase 3
Database Links Click here for help
Alphafold O43781 (Hs), Q922Y0 (Mm), Q4V8A3 (Rn)
BRENDA 2.7.12.1
ChEMBL Target CHEMBL4575 (Hs)
Ensembl Gene ENSG00000143479 (Hs), ENSMUSG00000016526 (Mm), ENSRNOG00000004870 (Rn)
Entrez Gene 8444 (Hs), 226419 (Mm), 304775 (Rn)
Human Protein Atlas ENSG00000143479 (Hs)
KEGG Enzyme 2.7.12.1
KEGG Gene hsa:8444 (Hs), mmu:226419 (Mm), rno:304775 (Rn)
OMIM 603497 (Hs)
Pharos O43781 (Hs)
RefSeq Nucleotide NM_003582 (Hs), NM_145508 (Mm), NM_001024767 (Rn)
RefSeq Protein NP_003573 (Hs), NP_663483 (Mm), NP_001019938 (Rn)
UniProtKB O43781 (Hs), Q922Y0 (Mm), Q4V8A3 (Rn)
Wikipedia DYRK3 (Hs)
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
compound 1a [PMID: 24900749] Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.2 pIC50 4
⤷ pIC50 7.2 (IC50 7x10-8 M) [4]
compound 20 [PMID: 30998356] Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.0 pIC50 5
⤷ pIC50 7.0 (IC50 1.04x10-7 M) [5]
Description: Measuring in vitro enzyme inhibitory activity.
compound 3b [PMID: 23454515] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.7 pIC50 2
⤷ pIC50 6.7 (IC50 1.8x10-7 M) [2]
kinase inhibitor 2 [PMID: 30199702] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.4 pIC50 3
⤷ pIC50 6.4 (IC50 3.8x10-7 M) [3]
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/DYRK3
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
K-252a Small molecule or natural product Hs Inhibitor Inhibition 10.4
SB 218078 Small molecule or natural product Hs Inhibitor Inhibition 16.6
JAK3 inhibitor VI Small molecule or natural product Hs Inhibitor Inhibition 30.4
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 31.3
PKR inhibitor Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 39.2
Cdc2-like kinase inhibitor Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 50.4
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 58.2
PI 3-Kg inhibitor Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 71.5
dorsomorphin Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 76.8
GSK-3 inhibitor XIII Small molecule or natural product Ligand has a PDB structure 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]

5. Riggs JR, Elsner J, Cashion D, Robinson D, Tehrani L, Nagy M, Fultz KE, Krishna Narla R, Peng X, Tran T et al.. (2019) Design and Optimization Leading to an Orally Active TTK Protein Kinase Inhibitor with Robust Single Agent Efficacy. J Med Chem, 62 (9): 4401-4410. [PMID:30998356]

How to cite this page

Dyrk2 subfamily: dual specificity tyrosine phosphorylation regulated kinase 3. Last modified on 02/05/2019. Accessed on 03/12/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=2012.