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dual serine/threonine and tyrosine protein kinase

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Target id: 2008

Nomenclature: dual serine/threonine and tyrosine protein kinase

Abbreviated Name: SgK496

Family: Other-unique family

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 929 1q32.1 DSTYK dual serine/threonine and tyrosine protein kinase
Mouse - 927 1 E4 Dstyk dual serine/threonine and tyrosine protein kinase
Rat - 927 13q13 Dstyk dual serine/threonine and tyrosine protein kinase
Previous and Unofficial Names Click here for help
dusty protein kinase | receptor-interacting serine/threonine-protein kinase 5 | RIP5 | RIPK5
Database Links Click here for help
Alphafold Q6XUX3 (Hs), Q6XUX1 (Mm), Q6XUX2 (Rn)
BRENDA 2.7.12.1
ChEMBL Target CHEMBL1908386 (Hs)
Ensembl Gene ENSG00000133059 (Hs), ENSMUSG00000042046 (Mm), ENSRNOG00000021298 (Rn)
Entrez Gene 25778 (Hs), 213452 (Mm), 304791 (Rn)
Human Protein Atlas ENSG00000133059 (Hs)
KEGG Enzyme 2.7.12.1
KEGG Gene hsa:25778 (Hs), mmu:213452 (Mm), rno:304791 (Rn)
OMIM 612666 (Hs)
Pharos Q6XUX3 (Hs)
RefSeq Nucleotide NM_015375 (Hs), NM_172516 (Mm), NM_199463 (Rn)
RefSeq Protein NP_056190 (Hs), NP_766104 (Mm), NP_955750 (Rn)
UniProtKB Q6XUX3 (Hs), Q6XUX1 (Mm), Q6XUX2 (Rn)
Wikipedia DSTYK (Hs)
Enzyme Reaction Click here for help
EC Number: 2.7.12.1
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: 2-3
Key to terms and symbols Click column headers to sort
Target used in screen: RIPK5
Ligand Sp. Type Action Value Parameter
lestaurtinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 8.3 pKd
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.0 pKd
NVP-TAE684 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.2 pKd
AST-487 Small molecule or natural product Hs Inhibitor Inhibition 6.4 pKd
bosutinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.4 pKd
crizotinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.3 pKd
PP-242 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.3 pKd
foretinib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.3 pKd
KW-2449 Small molecule or natural product Hs Inhibitor Inhibition 6.2 pKd
JNJ-28312141 Small molecule or natural product 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 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/RIPK5
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
K-252a Small molecule or natural product Hs Inhibitor Inhibition 1.4
Gö 6976 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 9.9
Cdk1/2 inhibitor III Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 17.8
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 18.7
SB 218078 Small molecule or natural product Hs Inhibitor Inhibition 45.5
JAK inhibitor I Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 62.0
Cdk4 inhibitor Small molecule or natural product Hs Inhibitor Inhibition 65.6
alsterpaullone 2-cyanoethyl Small molecule or natural product Hs Inhibitor Inhibition 67.1
Cdk4 inhibitor III Small molecule or natural product Hs Inhibitor Inhibition 76.1
fascaplysin Small molecule or natural product Hs Inhibitor Inhibition 77.3
Displaying the top 10 most potent ligands  View all ligands in screen »
Clinically-Relevant Mutations and Pathophysiology Click here for help
Disease:  Congenital anomalies of kidney and urinary tract, susceptibility to; CAKUT
OMIM: 610805

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. 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 13/09/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=2008.