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Target not currently curated in GtoImmuPdb
Target id: 2020
Nomenclature: endoplasmic reticulum to nucleus signaling 1
Abbreviated Name: IRE1
Family: IRE family
Gene and Protein Information ![]() |
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Species | TM | AA | Chromosomal Location | Gene Symbol | Gene Name | Reference |
Human | 1 | 977 | 17q23.3 | ERN1 | endoplasmic reticulum to nucleus signaling 1 | |
Mouse | 1 | 977 | 11 E1 | Ern1 | endoplasmic reticulum to nucleus signalling 1 | |
Rat | - | 965 | 10 q32.1 | Ern1 | endoplasmic reticulum to nucleus signaling 1 |
Previous and Unofficial Names ![]() |
inositol-requiring enzyme 1 |
Database Links ![]() |
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Alphafold | O75460 (Hs), Q9EQY0 (Mm) |
BRENDA | 2.7.11.1, 3.1.26.- |
ChEMBL Target | CHEMBL1163101 (Hs), CHEMBL4523450 (Mm) |
Ensembl Gene | ENSG00000178607 (Hs), ENSMUSG00000020715 (Mm), ENSRNOG00000012864 (Rn) |
Entrez Gene | 2081 (Hs), 78943 (Mm), 498013 (Rn) |
Human Protein Atlas | ENSG00000178607 (Hs) |
KEGG Enzyme | 2.7.11.1, 3.1.26.- |
KEGG Gene | hsa:2081 (Hs), mmu:78943 (Mm), rno:498013 (Rn) |
OMIM | 604033 (Hs) |
Pharos | O75460 (Hs) |
RefSeq Nucleotide | NM_001433 (Hs), NM_023913 (Mm), NM_001191926 (Rn) |
RefSeq Protein | NP_001424 (Hs), NP_076402 (Mm), NP_001178855 (Rn) |
UniProtKB | O75460 (Hs), Q9EQY0 (Mm) |
Wikipedia | ERN1 (Hs) |
Selected 3D Structures ![]() |
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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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DiscoveRx KINOMEscan® screen ![]() |
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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: 2,4 |
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Target used in screen: ERN1 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Displaying the top 10 most potent ligands View all ligands in screen » |
1. Ali MM, Bagratuni T, Davenport EL, Nowak PR, Silva-Santisteban MC, Hardcastle A, McAndrews C, Rowlands MG, Morgan GJ, Aherne W et al.. (2011) Structure of the Ire1 autophosphorylation complex and implications for the unfolded protein response. EMBO J, 30 (5): 894-905. [PMID:21317875]
2. 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]
3. Ranatunga S, Tang CH, Kang CW, Kriss CL, Kloppenburg BJ, Hu CC, Del Valle JR. (2014) Synthesis of novel tricyclic chromenone-based inhibitors of IRE-1 RNase activity. J Med Chem, 57 (10): 4289-301. [PMID:24749861]
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]
5. Zhou J, Liu CY, Back SH, Clark RL, Peisach D, Xu Z, Kaufman RJ. (2006) The crystal structure of human IRE1 luminal domain reveals a conserved dimerization interface required for activation of the unfolded protein response. Proc Natl Acad Sci USA, 103 (39): 14343-8. [PMID:16973740]
IRE family: endoplasmic reticulum to nucleus signaling 1. Last modified on 09/02/2015. Accessed on 18/02/2025. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2020.