interleukin 1 receptor associated kinase 3 | Interleukin-1 receptor-associated kinase (IRAK) family | IUPHAR Guide to IMMUNOPHARMACOLOGY

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interleukin 1 receptor associated kinase 3

  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

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 - 596 12q13.13 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
IL-1 receptor-associated kinase M | IRAK-M
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: 2.7.11.1

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 R-16 [PMID: 21967808] 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
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 Affinity Parameter
tamatinib Hs Inhibitor Inhibition 8.0 pKd
staurosporine Hs Inhibitor Inhibition 7.9 pKd
lestaurtinib Hs Inhibitor Inhibition 7.8 pKd
crizotinib Hs Inhibitor Inhibition 7.5 pKd
fedratinib Hs Inhibitor Inhibition 6.9 pKd
NVP-TAE684 Hs Inhibitor Inhibition 6.8 pKd
midostaurin Hs Inhibitor Inhibition 6.7 pKd
KW-2449 Hs Inhibitor Inhibition 6.6 pKd
foretinib Hs Inhibitor Inhibition 6.4 pKd
PHA-665752 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:   macrophage (CL:0000235)
monocyte (CL:0000576)
Immuno Process Associations
Immuno Process:  Inflammation
GO Annotations:  Associated to 3 GO processes
GO:0002755 MyD88-dependent toll-like receptor signaling pathway TAS
GO:0034122 negative regulation of toll-like receptor signaling pathway ISS
GO:0045824 negative regulation of innate immune response ISS
Immuno Process:  Immune regulation
GO Annotations:  Associated to 5 GO processes
GO:0002755 MyD88-dependent toll-like receptor signaling pathway TAS
GO:0010933 positive regulation of macrophage tolerance induction ISS
GO:0010936 negative regulation of macrophage cytokine production ISS
GO:0034122 negative regulation of toll-like receptor signaling pathway 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
Immuno Process:  Cellular signalling
GO Annotations:  Associated to 2 GO processes
GO:0002755 MyD88-dependent toll-like receptor signaling pathway TAS
GO:0034122 negative regulation of toll-like receptor signaling pathway ISS
Clinically-Relevant Mutations and Pathophysiology
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 22/05/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetoimmunopharmacology.org/GRAC/ObjectDisplayForward?objectId=2044.