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oxidative stress responsive kinase 1

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Target id: 2132

Nomenclature: oxidative stress responsive kinase 1

Abbreviated Name: OSR1

Family: FRAY subfamily

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 527 3p22.2 OXSR1 oxidative stress responsive kinase 1
Mouse - 527 9 F3 Oxsr1 oxidative-stress responsive 1
Rat - 527 8 q32 Oxsr1 oxidative stress responsive kinase 1
Previous and Unofficial Names Click here for help
oxidative stress responsive 1
Database Links Click here for help
Alphafold O95747 (Hs), Q6P9R2 (Mm)
BRENDA 2.7.11.1
ChEMBL Target CHEMBL1163104 (Hs)
Ensembl Gene ENSG00000172939 (Hs), ENSMUSG00000036737 (Mm), ENSRNOG00000013136 (Rn)
Entrez Gene 9943 (Hs), 108737 (Mm), 316064 (Rn)
Human Protein Atlas ENSG00000172939 (Hs)
KEGG Enzyme 2.7.11.1
KEGG Gene hsa:9943 (Hs), mmu:108737 (Mm), rno:316064 (Rn)
OMIM 604046 (Hs)
Pharos O95747 (Hs)
RefSeq Nucleotide NM_005109 (Hs), NM_133985 (Mm), NM_001108194 (Rn)
RefSeq Protein NP_005100 (Hs), NP_598746 (Mm), NP_001101664 (Rn)
UniProtKB O95747 (Hs), Q6P9R2 (Mm)
Wikipedia OXSR1 (Hs)
Selected 3D Structures Click here for help
Image of receptor 3D structure from RCSB PDB
Description:  STRUCTURAL INSIGHTS INTO THE RECOGNITION OF SUBSTRATES AND ACTIVATORS BY THE OSR1 KINASE
PDB Id:  2V3S
Resolution:  1.7Å
Species:  Human
References:  4
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 74 [PMID: 24793884] Small molecule or natural product Click here for species-specific activity table Hs Inhibition - - 3
⤷ [3]
Description: Measured as % inhibition using 1μM compound.
Inhibitor Comments
OXSR1 activity is inhibited by approximately 86% (average of n=2) in the presence of 1μM compound 74 [PMID 24793884] [3] (note that OXSR1 is referred to as OSR1 in the article's Supplementary data table)..
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: 2,5
Key to terms and symbols Click column headers to sort
Target used in screen: OSR1
Ligand Sp. Type Action Value Parameter
NVP-TAE684 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.3 pKd
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.4 pKd
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 6.3 pKd
SU-14813 Small molecule or natural product Hs Inhibitor Inhibition 5.8 pKd
KW-2449 Small molecule or natural product Hs Inhibitor Inhibition 5.8 pKd
TG-100-115 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 5.6 pKd
ruxolitinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 5.6 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
Displaying the top 10 most potent ligands  View all ligands in screen »
EMD Millipore KinaseProfilerTM screen/Reaction Biology Kinase HotspotSM screen Click here for help
A screen profiling 158 kinase inhibitors (Calbiochem Protein Kinase Inhibitor Library I and II, catalogue numbers 539744 and 539745) for their inhibitory activity at 1µM and 10µM against 234 human recombinant kinases using the EMD Millipore KinaseProfilerTM service.

A screen profiling the inhibitory activity of 178 commercially available kinase inhibitors at 0.5µM against a panel of 300 recombinant protein kinases using the Reaction Biology Corporation Kinase HotspotSM platform.

http://www.millipore.com/techpublications/tech1/pf3036
http://www.reactionbiology.com/webapps/main/pages/kinase.aspx

Reference: ...1
Key to terms and symbols Click column headers to sort
Target used in screen: nd/OSR1(OXSR1)
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 14.2
Cdk1/2 inhibitor III Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 67.6
AG 112 Small molecule or natural product Hs Inhibitor Inhibition 72.2
aurora kinase inhibitor III Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 78.9
PKR inhibitor Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 79.8
SU11652 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 80.1
PDK1/Akt/Flt dual pathway inhibitor Small molecule or natural product Hs Inhibitor Inhibition 83.0
p38 MAP kinase inhibitor Small molecule or natural product Hs Inhibitor Inhibition 83.3
Flt-3 inhibitor III Small molecule or natural product Hs Inhibitor Inhibition 85.3
TGF-beta RI kinase inhibitor Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 85.3
Displaying the top 10 most potent ligands  View all ligands in screen »
Immuno Process Associations
Immuno Process:  Chemotaxis & migration
Immuno Process:  Cytokine production & signalling
Immuno Process:  Immune regulation
Immuno Process:  Inflammation

References

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1. Anastassiadis T, Deacon SW, Devarajan K, Ma H, Peterson JR. (2011) Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity. Nat Biotechnol, 29 (11): 1039-45. [PMID:22037377]

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. Reichelt A, Bailis JM, Bartberger MD, Yao G, Shu H, Kaller MR, Allen JG, Weidner MF, Keegan KS, Dao JH. (2014) Synthesis and structure-activity relationship of trisubstituted thiazoles as Cdc7 kinase inhibitors. Eur J Med Chem, 80: 364-82. [PMID:24793884]

4. Villa F, Goebel J, Rafiqi FH, Deak M, Thastrup J, Alessi DR, van Aalten DM. (2007) Structural insights into the recognition of substrates and activators by the OSR1 kinase. EMBO Rep, 8 (9): 839-45. [PMID:17721439]

5. 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

FRAY subfamily: oxidative stress responsive kinase 1. Last modified on 27/03/2019. Accessed on 25/04/2025. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=2132.