oxidative stress responsive kinase 1 | FRAY subfamily | IUPHAR/BPS Guide to PHARMACOLOGY

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oxidative stress responsive kinase 1

Target not currently curated in GtoImmuPdb

Target id: 2132

Nomenclature: oxidative stress responsive kinase 1

Abbreviated Name: OSR1

Family: FRAY subfamily

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 - 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
oxidative stress responsive 1
Database Links
BRENDA
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Selected 3D Structures
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
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 74 [PMID: 24793884] 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
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 Hs Inhibitor Inhibition 7.3 pKd
staurosporine Hs Inhibitor Inhibition 6.4 pKd
sunitinib Hs Inhibitor Inhibition 6.3 pKd
SU-14813 Hs Inhibitor Inhibition 5.8 pKd
KW-2449 Hs Inhibitor Inhibition 5.8 pKd
TG-100-115 Hs Inhibitor Inhibition 5.6 pKd
ruxolitinib Hs Inhibitor Inhibition 5.6 pKd
SB203580 Hs Inhibitor Inhibition <5.5 pKd
ruboxistaurin Hs Inhibitor Inhibition <5.5 pKd
erlotinib 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
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 Hs Inhibitor Inhibition 14.2
Cdk1/2 inhibitor III Hs Inhibitor Inhibition 67.6
AG 112 Hs Inhibitor Inhibition 72.2
aurora kinase inhibitor III Hs Inhibitor Inhibition 78.9
PKR inhibitor Hs Inhibitor Inhibition 79.8
SU11652 Hs Inhibitor Inhibition 80.1
PDK1/Akt/Flt dual pathway inhibitor Hs Inhibitor Inhibition 83.0
p38 MAP kinase inhibitor Hs Inhibitor Inhibition 83.3
TGF-beta RI kinase inhibitor Hs Inhibitor Inhibition 85.3
Flt-3 inhibitor III Hs Inhibitor Inhibition 85.3
Displaying the top 10 most potent ligands  View all ligands in screen »

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 13/11/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2132.