eukaryotic translation initiation factor 2 alpha kinase 1 | Other PEK family kinases | IUPHAR/BPS Guide to PHARMACOLOGY

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eukaryotic translation initiation factor 2 alpha kinase 1

Target not currently curated in GtoImmuPdb

Target id: 2015

Nomenclature: eukaryotic translation initiation factor 2 alpha kinase 1

Abbreviated Name: HRI

Family: Other PEK family kinases

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 630 7p22 EIF2AK1 eukaryotic translation initiation factor 2 alpha kinase 1
Mouse - 619 5 G2 Eif2ak1 eukaryotic translation initiation factor 2 alpha kinase 1
Rat - 620 12 p11 Eif2ak1 eukaryotic translation initiation factor 2 alpha kinase 1
Previous and Unofficial Names
HCR | heme-controlled repressor | heme regulated initiation factor 2 alpha kinase | HRI
Database Links
BRENDA
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
Pharos
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 Value Parameter Reference
compound 27 [PMID: 19854648] Hs Inhibition 8.2 pIC50 3
pIC50 8.2 (IC50 6.31x10-9 M) [3]
RIPK1 inhibitor 22b Hs Inhibition 7.6 pIC50 2
pIC50 7.6 (IC50 2.6x10-8 M) [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: 1,4

Key to terms and symbols Click column headers to sort
Target used in screen: EIF2AK1
Ligand Sp. Type Action Value Parameter
bosutinib Hs Inhibitor Inhibition 6.2 pKd
alvocidib Hs Inhibitor Inhibition 6.1 pKd
foretinib Hs Inhibitor Inhibition 6.0 pKd
fedratinib Hs Inhibitor Inhibition 6.0 pKd
barasertib-hQPA Hs Inhibitor Inhibition 5.8 pKd
SB203580 Hs Inhibitor Inhibition <5.5 pKd
ruboxistaurin Hs Inhibitor Inhibition <5.5 pKd
erlotinib Hs Inhibitor Inhibition <5.5 pKd
GSK690693 Hs Inhibitor Inhibition <5.5 pKd
masitinib Hs Inhibitor Inhibition <5.5 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »
Immuno Process Associations
Immuno Process:  Inflammation
GO Annotations:  Associated to 2 GO processes, IEA only
click arrow to show/hide IEA associations
GO:0002526 acute inflammatory response IEA
GO:0006909 phagocytosis IEA
Immuno Process:  Immune system development
GO Annotations:  Associated to 1 GO processes, IEA only
click arrow to show/hide IEA associations
GO:0030225 macrophage differentiation IEA

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 26/09/2020. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2015.