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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

Contents:

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 Q9Y616 (Hs), Q8K4B2 (Mm)
BRENDA 2.7.11.1
ChEMBL Target CHEMBL5081 (Hs)
Ensembl Gene ENSG00000090376 (Hs), ENSMUSG00000020227 (Mm), ENSRNOG00000004226 (Rn)
Entrez Gene 11213 (Hs), 73914 (Mm), 314870 (Rn)
Human Protein Atlas ENSG00000090376 (Hs)
KEGG Enzyme 2.7.11.1
KEGG Gene hsa:11213 (Hs), mmu:73914 (Mm), rno:314870 (Rn)
OMIM 604459 (Hs)
Pharos Q9Y616 (Hs)
RefSeq Nucleotide NM_007199 (Hs), NM_028679 (Mm), NM_001108101 (Rn)
RefSeq Protein NP_009130 (Hs), NP_082955 (Mm), NP_001101571 (Rn)
UniProtKB Q9Y616 (Hs), Q8K4B2 (Mm)
Wikipedia IRAK3 (Hs)
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
IRAK3 PROTAC 23 Small molecule or natural product Hs Binding 8.3 pIC50 2
⤷ pIC50 8.3 (IC50 5x10-9 M) [2]
Description: LanthaScreen Eu IRAK3 binding displacement assay
compound R-16 [PMID: 21967808] Small molecule or natural product Click here for species-specific activity table Hs Inhibition - - 3
⤷ [3]
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] [3].
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: 1,4
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 Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 7.8 pKd
crizotinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand 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:   macrophage (CL:0000235)
monocyte (CL:0000576)
Immuno Process Associations
Immuno Process:  Inflammation
Immuno Process:  Immune regulation
Immuno Process:  Immune system development
Immuno Process:  Cytokine production & signalling
Immuno Process:  Cellular signalling
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. Degorce SL, Tavana O, Banks E, Crafter C, Gingipalli L, Kouvchinov D, Mao Y, Pachl F, Solanki A, Valge-Archer V et al.. (2020) Discovery of Proteolysis-Targeting Chimera Molecules that Selectively Degrade the IRAK3 Pseudokinase. J Med Chem, 63 (18): 10460-10473. [PMID:32803978]

3. 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]

4. 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 02/11/2021. Accessed on 20/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetoimmunopharmacology.org/GRAC/ObjectDisplayForward?objectId=2044.