endoplasmic reticulum to nucleus signaling 1 | IRE family | IUPHAR/BPS Guide to PHARMACOLOGY

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endoplasmic reticulum to nucleus signaling 1

Target not currently curated in GtoImmuPdb

Target id: 2020

Nomenclature: endoplasmic reticulum to nucleus signaling 1

Abbreviated Name: IRE1

Family: IRE family

Annotation status:  image of an orange circle Annotated and awaiting review. Please contact us if you can help with reviewing.  » Email us

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 1 977 17q23 ERN1 endoplasmic reticulum to nucleus signaling 1
Mouse 1 977 11 E1 Ern1 endoplasmic reticulum (ER) 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
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
RefSeq Nucleotide
RefSeq Protein
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  The crystal structure of human IRE1-alpha luminal domain
PDB Id:  2HZ6
Resolution:  3.1Å
Species:  Human
References:  5
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of the Human kinase and RNase domains in complex with ADP
PDB Id:  3P23
Ligand:  ADP   This ligand is endogenous
Resolution:  2.7Å
Species:  Human
References:  1
Enzyme Reaction
EC Number:
EC Number: 3.1.26.-

Download all structure-activity data for this target as a CSV file

Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
compound 34 [PMID: 24749861] Hs Inhibition 7.3 pIC50 3
pIC50 7.3 (IC50 4.7x10-8 M) [3]
Description: Inhibition of RNAse activity.
DiscoveRx KINOMEscan® screen
A screen of 72 inhibitors against 456 human kinases. Quantitative data were derived using DiscoveRx KINOMEscan® platform.
Reference: 2,4

Key to terms and symbols Click column headers to sort
Target used in screen: ERN1
Ligand Sp. Type Action Value Parameter
lestaurtinib Hs Inhibitor Inhibition 8.2 pKd
staurosporine Hs Inhibitor Inhibition 7.7 pKd
NVP-TAE684 Hs Inhibitor Inhibition 6.7 pKd
cediranib Hs Inhibitor Inhibition 6.3 pKd
sunitinib Hs Inhibitor Inhibition 6.2 pKd
BMS-345541 Hs Inhibitor Inhibition 6.0 pKd
fedratinib Hs Inhibitor Inhibition 5.9 pKd
tamatinib Hs Inhibitor Inhibition 5.8 pKd
SU-14813 Hs Inhibitor Inhibition 5.7 pKd
midostaurin Hs Inhibitor Inhibition 5.6 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »


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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. U.S.A., 103 (39): 14343-8. [PMID:16973740]

How to cite this page

IRE family: endoplasmic reticulum to nucleus signaling 1. Last modified on 09/02/2015. Accessed on 07/07/2020. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2020.