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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 | ||||||
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 |
IL-1 receptor-associated kinase M | IRAK-M |
Database Links | |
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 | ||||
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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 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Inhibitor Comments | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
IRAK3 activity is inhibited by 97% in the presence of 1μM compound R-16 [PMID 21967808] [3]. |
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: 1,4 |
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Target used in screen: IRAK3 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Immunopharmacology Comments |
IRAK3 expression is restricted to monocytes and macrophages. |
Cell Type Associations | ||||
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Immuno Process Associations | ||
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Clinically-Relevant Mutations and Pathophysiology | ||||||||
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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]
Interleukin-1 receptor-associated kinase (IRAK) family: interleukin 1 receptor associated kinase 3. Last modified on 02/11/2021. Accessed on 06/12/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetoimmunopharmacology.org/GRAC/ObjectDisplayForward?objectId=2044.