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
dusty protein kinase | receptor-interacting serine/threonine-protein kinase 5 | RIP5 | RIPK5
Database Links
BRENDA
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
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 24/10/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2008.