microtubule affinity regulating kinase 4 | MARK subfamily | IUPHAR/BPS Guide to PHARMACOLOGY

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microtubule affinity regulating kinase 4

Target id: 2100

Nomenclature: microtubule affinity regulating kinase 4

Abbreviated Name: MARK4

Family: MARK subfamily

Annotation status:  image of an orange circle Annotated and awaiting review. Please contact us if you can help with reviewing.  » Email us

   GtoImmuPdb view: OFF :     Currently no data for microtubule affinity regulating kinase 4 in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 688 19q13.2 MARK4 microtubule affinity regulating kinase 4
Mouse - 752 7 A3 Mark4 MAP/microtubule affinity regulating kinase 4
Rat - 752 1q21 Mark4 microtubule affinity regulating kinase 4
Previous and Unofficial Names
MAP/microtubule affinity-regulating kinase like 1 | MARKL1 | MAP/microtubule affinity-regulating kinase 4
Database Links
BRENDA
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Enzyme Reaction
EC Number: 2.7.11.1
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: MARK4
Ligand Sp. Type Action Affinity Units
staurosporine Hs Inhibitor Inhibition 8.3 pKd
NVP-TAE684 Hs Inhibitor Inhibition 7.9 pKd
tamatinib Hs Inhibitor Inhibition 7.1 pKd
lestaurtinib Hs Inhibitor Inhibition 6.9 pKd
KW-2449 Hs Inhibitor Inhibition 6.7 pKd
midostaurin Hs Inhibitor Inhibition 6.4 pKd
fedratinib Hs Inhibitor Inhibition 6.0 pKd
dovitinib Hs Inhibitor Inhibition 5.8 pKd
SU-14813 Hs Inhibitor Inhibition 5.7 pKd
SB203580 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/MARK4
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
staurosporine Hs Inhibitor Inhibition 0.0
K-252a Hs Inhibitor Inhibition 0.9
JAK3 inhibitor VI Hs Inhibitor Inhibition 1.6
Cdk1/2 inhibitor III Hs Inhibitor Inhibition 2.3
midostaurin Hs Inhibitor Inhibition 3.2
SB 218078 Hs Inhibitor Inhibition 5.3
SU11652 Hs Inhibitor Inhibition 7.2
Gö 6976 Hs Inhibitor Inhibition 10.8
PKR inhibitor Hs Inhibitor Inhibition 12.8
sunitinib Hs Inhibitor Inhibition 24.7
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. 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

MARK subfamily: microtubule affinity regulating kinase 4. Last modified on 30/03/2016. Accessed on 21/11/2018. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2100.