dual serine/threonine and tyrosine protein kinase | Other-unique family | IUPHAR/BPS Guide to PHARMACOLOGY

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dual serine/threonine and tyrosine protein kinase

Target not currently curated in GtoImmuPdb

Target id: 2008

Nomenclature: dual serine/threonine and tyrosine protein kinase

Abbreviated Name: SgK496

Family: Other-unique 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 - 929 1q32 DSTYK dual serine/threonine and tyrosine protein kinase
Mouse - 927 1 E4 Dstyk dual serine/threonine and tyrosine protein kinase
Rat - 927 13 q13 Dstyk dual serine/threonine and tyrosine protein kinase
Previous and Unofficial Names
RIP5 | RIPK5 | receptor-interacting serine/threonine-protein kinase 5 | dusty protein kinase
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: 2.7.12.1
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: 2-3

Key to terms and symbols Click column headers to sort
Target used in screen: RIPK5
Ligand Sp. Type Action Value Parameter
lestaurtinib Hs Inhibitor Inhibition 8.3 pKd
staurosporine Hs Inhibitor Inhibition 8.0 pKd
NVP-TAE684 Hs Inhibitor Inhibition 7.2 pKd
AST-487 Hs Inhibitor Inhibition 6.4 pKd
bosutinib Hs Inhibitor Inhibition 6.4 pKd
crizotinib Hs Inhibitor Inhibition 6.3 pKd
foretinib Hs Inhibitor Inhibition 6.3 pKd
PP-242 Hs Inhibitor Inhibition 6.3 pKd
KW-2449 Hs Inhibitor Inhibition 6.2 pKd
JNJ-28312141 Hs Inhibitor Inhibition 6.1 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/RIPK5
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
K-252a Hs Inhibitor Inhibition 1.4
Gö 6976 Hs Inhibitor Inhibition 9.9
Cdk1/2 inhibitor III Hs Inhibitor Inhibition 17.8
staurosporine Hs Inhibitor Inhibition 18.7
SB 218078 Hs Inhibitor Inhibition 45.5
JAK inhibitor I Hs Inhibitor Inhibition 62.0
Cdk4 inhibitor Hs Inhibitor Inhibition 65.6
alsterpaullone 2-cyanoethyl Hs Inhibitor Inhibition 67.1
Cdk4 inhibitor III Hs Inhibitor Inhibition 76.1
fascaplysin Hs Inhibitor Inhibition 77.3
Displaying the top 10 most potent ligands  View all ligands in screen »
Clinically-Relevant Mutations and Pathophysiology
Disease:  Congenital anomalies of kidney and urinary tract, susceptibility to; CAKUT
OMIM: 610805

References

Show »

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. 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-unique family: dual serine/threonine and tyrosine protein kinase. Last modified on 06/05/2015. Accessed on 27/05/2020. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2008.