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interleukin 1 receptor associated kinase 3

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Immunopharmacology Ligand  Target has curated data in GtoImmuPdb

Target id: 2044

Nomenclature: interleukin 1 receptor associated kinase 3

Abbreviated Name: IRAK3

Family: Interleukin-1 receptor-associated kinase (IRAK) family

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 596 12q14.3 IRAK3 interleukin 1 receptor associated kinase 3
Mouse - 609 10 D2 Irak3 interleukin-1 receptor-associated kinase 3
Rat - 610 7 q22 Irak3 interleukin-1 receptor-associated kinase 3
Previous and Unofficial Names Click here for help
IL-1 receptor-associated kinase M | IRAK-M
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: 2.7.11.1

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 R-16 [PMID: 21967808] Small molecule or natural product Click here for species-specific activity table Hs Inhibition - - 2
[2]
Description: Measured as % inhibition using 1μM compound.
Inhibitor Comments
IRAK3 activity is inhibited by 97% in the presence of 1μM compound R-16 [PMID 21967808] [2].
DiscoveRx KINOMEscan® screen Click here for help
A screen of 72 inhibitors against 456 human kinases. Quantitative data were derived using DiscoveRx KINOMEscan® platform.
http://www.discoverx.com/services/drug-discovery-development-services/kinase-profiling/kinomescan
Reference: 1,3

Key to terms and symbols Click column headers to sort
Target used in screen: IRAK3
Ligand Sp. Type Action Value Parameter
tamatinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 8.0 pKd
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.9 pKd
lestaurtinib Small molecule or natural product Immunopharmacology Ligand Hs Inhibitor Inhibition 7.8 pKd
crizotinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 7.5 pKd
fedratinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 6.9 pKd
NVP-TAE684 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.8 pKd
midostaurin Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.7 pKd
KW-2449 Small molecule or natural product Hs Inhibitor Inhibition 6.6 pKd
foretinib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.4 pKd
PHA-665752 Small molecule or natural product Hs Inhibitor Inhibition 6.2 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »
Immunopharmacology Comments
IRAK3 expression is restricted to monocytes and macrophages.
Cell Type Associations
Immuno Cell Type:  Macrophages & monocytes
Cell Ontology Term:   monocyte (CL:0000576)
macrophage (CL:0000235)
Immuno Process Associations
Immuno Process:  Inflammation
GO Annotations:  Associated to 1 GO processes
GO:0045824 negative regulation of innate immune response ISS
Immuno Process:  Immune regulation
GO Annotations:  Associated to 3 GO processes
GO:0010933 positive regulation of macrophage tolerance induction ISS
GO:0010936 negative regulation of macrophage cytokine production ISS
GO:0045824 negative regulation of innate immune response ISS
Immuno Process:  Immune system development
GO Annotations:  Associated to 1 GO processes
GO:0010933 positive regulation of macrophage tolerance induction ISS
Immuno Process:  Cytokine production & signalling
GO Annotations:  Associated to 8 GO processes
GO:0001960 negative regulation of cytokine-mediated signaling pathway IC
GO:0010936 negative regulation of macrophage cytokine production ISS
GO:0019221 cytokine-mediated signaling pathway ISS
GO:0032695 negative regulation of interleukin-12 production IMP
GO:0032715 negative regulation of interleukin-6 production IMP
GO:0032720 negative regulation of tumor necrosis factor production IMP
GO:0070498 interleukin-1-mediated signaling pathway IMP
GO:0070555 response to interleukin-1 IMP
Clinically-Relevant Mutations and Pathophysiology Click here for help
Disease:  Asthma-related traits, susceptibility to, 5
OMIM: 611064

References

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1. Davis MI, Hunt JP, Herrgard S, Ciceri P, Wodicka LM, Pallares G, Hocker M, Treiber DK, Zarrinkar PP. (2011) Comprehensive analysis of kinase inhibitor selectivity. Nat Biotechnol, 29 (11): 1046-51. [PMID:22037378]

2. Milkiewicz KL, Aimone LD, Albom MS, Angeles TS, Chang H, Grobelny JV, Husten J, Losardo C, Miknyoczki S, Murthy S et al.. (2011) Improvement in oral bioavailability of 2,4-diaminopyrimidine c-Met inhibitors by incorporation of a 3-amidobenzazepin-2-one group. Bioorg Med Chem, 19 (21): 6274-84. [PMID:21967808]

3. Wodicka LM, Ciceri P, Davis MI, Hunt JP, Floyd M, Salerno S, Hua XH, Ford JM, Armstrong RC, Zarrinkar PP et al.. (2010) Activation state-dependent binding of small molecule kinase inhibitors: structural insights from biochemistry. Chem Biol, 17 (11): 1241-9. [PMID:21095574]

How to cite this page

Interleukin-1 receptor-associated kinase (IRAK) family: interleukin 1 receptor associated kinase 3. Last modified on 14/03/2017. Accessed on 02/12/2021. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetoimmunopharmacology.org/GRAC/ObjectDisplayForward?objectId=2044.