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eukaryotic translation initiation factor 2 alpha kinase 1

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Target id: 2015

Nomenclature: eukaryotic translation initiation factor 2 alpha kinase 1

Abbreviated Name: HRI

Family: Other PEK family kinases

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 630 7p22.1 EIF2AK1 eukaryotic translation initiation factor 2 alpha kinase 1
Mouse - 619 5 G2 Eif2ak1 eukaryotic translation initiation factor 2 alpha kinase 1
Rat - 620 12p11 Eif2ak1 eukaryotic translation initiation factor 2 alpha kinase 1
Previous and Unofficial Names Click here for help
HCR | heme-controlled repressor | heme regulated initiation factor 2 alpha kinase | HRI
Database Links Click here for help
Alphafold Q9BQI3 (Hs), Q9Z2R9 (Mm), Q63185 (Rn)
BRENDA 2.7.11.1
ChEMBL Target CHEMBL6029 (Hs), CHEMBL1938213 (Mm)
Ensembl Gene ENSG00000086232 (Hs), ENSMUSG00000029613 (Mm), ENSRNOG00000001050 (Rn)
Entrez Gene 27102 (Hs), 15467 (Mm), 27137 (Rn)
Human Protein Atlas ENSG00000086232 (Hs)
KEGG Enzyme 2.7.11.1
KEGG Gene hsa:27102 (Hs), mmu:15467 (Mm), rno:27137 (Rn)
OMIM 613635 (Hs)
Pharos Q9BQI3 (Hs)
RefSeq Nucleotide NM_014413 (Hs), NM_013557 (Mm), NM_013223 (Rn)
RefSeq Protein NP_055228 (Hs), NP_038585 (Mm), NP_037355 (Rn)
UniProtKB Q9BQI3 (Hs), Q9Z2R9 (Mm), Q63185 (Rn)
Wikipedia EIF2AK1 (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
compound 27 [PMID: 19854648] Small molecule or natural product Primary target of this compound Hs Inhibition 8.2 pIC50 3
⤷ pIC50 8.2 (IC50 6.31x10-9 M) [3]
RIPK1 inhibitor 22b Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.6 pIC50 2
⤷ pIC50 7.6 (IC50 2.6x10-8 M) [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: 1,4
Key to terms and symbols Click column headers to sort
Target used in screen: EIF2AK1
Ligand Sp. Type Action Value Parameter
bosutinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.2 pKd
alvocidib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.1 pKd
foretinib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.0 pKd
fedratinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 6.0 pKd
barasertib-hQPA Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 5.8 pKd
SB203580 Small molecule or natural product Immunopharmacology Ligand Hs Inhibitor Inhibition <5.5 pKd
ruboxistaurin Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition <5.5 pKd
erlotinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition <5.5 pKd
linifanib Small molecule or natural product Hs Inhibitor Inhibition <5.5 pKd
GSK690693 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition <5.5 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »
Immuno Process Associations
Immuno Process:  Inflammation
Immuno Process:  Immune system development

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. Li Y, Xiong Y, Zhang G, Zhang L, Yang W, Yang J, Huang L, Qiao Z, Miao Z, Lin G et al.. (2018) Identification of 5-(2,3-Dihydro-1 H-indol-5-yl)-7 H-pyrrolo[2,3- d]pyrimidin-4-amine Derivatives as a New Class of Receptor-Interacting Protein Kinase 1 (RIPK1) Inhibitors, Which Showed Potent Activity in a Tumor Metastasis Model. J Med Chem, 61 (24): 11398-11414. [PMID:30480444]

3. Rosen MD, Woods CR, Goldberg SD, Hack MD, Bounds AD, Yang Y, Wagaman PC, Phuong VK, Ameriks AP, Barrett TD et al.. (2009) Discovery of the first known small-molecule inhibitors of heme-regulated eukaryotic initiation factor 2alpha (HRI) kinase. Bioorg Med Chem Lett, 19 (23): 6548-51. [PMID:19854648]

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

Other PEK family kinases: eukaryotic translation initiation factor 2 alpha kinase 1. Last modified on 11/12/2018. Accessed on 12/10/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=2015.