megakaryocyte-associated tyrosine kinase | Csk family | IUPHAR/BPS Guide to PHARMACOLOGY

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megakaryocyte-associated tyrosine kinase

Target not currently curated in GtoImmuPdb

Target id: 2101

Nomenclature: megakaryocyte-associated tyrosine kinase

Abbreviated Name: CTK

Family: Csk 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 - 508 19p13.3 MATK megakaryocyte-associated tyrosine kinase
Mouse - 505 10 C1 Matk megakaryocyte-associated tyrosine kinase
Rat - 467 7 q11 Matk megakaryocyte-associated tyrosine kinase
Previous and Unofficial Names
CHK | HHYLTK | hydroxyaryl-protein kinase | HYLTK | Lsk | protein kinase BATK | protein kinase HYL | tyrosine kinase MATK
Database Links
BRENDA
CATH/Gene3D
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:  Crystal structure of a SH2 domain of a megakaryocyte-associated tyrosine kinase (MATK) from Homo sapiens at 1.50 A resolution
PDB Id:  3US4
Resolution:  1.5Å
Species:  Human
References: 
Enzyme Reaction
EC Number: 2.7.10.2
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: CTK
Ligand Sp. Type Action Affinity Parameter
staurosporine Hs Inhibitor Inhibition 6.6 pKd
lestaurtinib Hs Inhibitor Inhibition 6.0 pKd
AST-487 Hs Inhibitor Inhibition 5.9 pKd
fedratinib Hs Inhibitor Inhibition 5.8 pKd
NVP-TAE684 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
GSK690693 Hs Inhibitor Inhibition <5.5 pKd
masitinib 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/CTK(MATK)
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
tofacitinib Hs Inhibitor Inhibition 66.9
Chk2 inhibitor II Hs Inhibitor Inhibition 68.5
dovitinib Hs Inhibitor Inhibition 74.9
staurosporine Hs Inhibitor Inhibition 75.0
lapatinib Hs Inhibitor Inhibition 75.9
erlotinib Hs Inhibitor Inhibition 77.2
seliciclib Hs Inhibitor Inhibition 77.6
VX-702 Hs Inhibitor Inhibition 77.6
vatalanib Hs Inhibitor Inhibition 78.1
tozasertib Hs Inhibitor Inhibition 78.6
Displaying the top 10 most potent ligands  View all ligands in screen »

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

Csk family: megakaryocyte-associated tyrosine kinase. Last modified on 26/03/2013. Accessed on 20/02/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2101.