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

Top ▲

interleukin 1 receptor associated kinase 3

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

   GtoImmuPdb view: ON :     interleukin 1 receptor associated kinase 3 has curated data in GtoImmuPdb

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
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 Units 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 Units
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 »
Clinically-Relevant Mutations and Pathophysiology
Disease:  Asthma-related traits, susceptibility to, 5
OMIM: 611064

References

Show »

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 16/01/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://guidetoimmunopharmacology.org/GRAC/ObjectDisplayForward?objectId=2044.