microtubule affinity regulating kinase 1 | MARK subfamily | IUPHAR/BPS Guide to PHARMACOLOGY

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microtubule affinity regulating kinase 1

Target not currently curated in GtoImmuPdb

Target id: 2097

Nomenclature: microtubule affinity regulating kinase 1

Abbreviated Name: MARK1

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

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 795 1q41 MARK1 microtubule affinity regulating kinase 1
Mouse - 795 1 H5 Mark1 MAP/microtubule affinity regulating kinase 1
Rat - 793 13 q26 Mark1 microtubule affinity regulating kinase 1
Previous and Unofficial Names
Emk3 | Par1c | ELKL motif serine/threonine-protein kinase 3 | MAP/microtubule affinity-regulating kinase 1
Database Links
BRENDA
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
Pharos
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  Structure of the Kinase Associated Domain 1 (KA1) from MARK1 kinase
PDB Id:  3OSE
Resolution:  1.7Å
Species:  Human
References:  5
Enzyme Reaction
EC Number: 2.7.11.1
EC Number: 2.7.11.26

Download all structure-activity data for this target as a CSV file

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
7-hydroxystaurosporine Hs Inhibition 7.6 pIC50 2
pIC50 7.6 (IC50 2.7x10-8 M) [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: 3,6

Key to terms and symbols Click column headers to sort
Target used in screen: MARK1
Ligand Sp. Type Action Value Parameter
staurosporine Hs Inhibitor Inhibition 8.4 pKd
NVP-TAE684 Hs Inhibitor Inhibition 7.5 pKd
lestaurtinib Hs Inhibitor Inhibition 7.1 pKd
midostaurin Hs Inhibitor Inhibition 6.8 pKd
tamatinib Hs Inhibitor Inhibition 6.6 pKd
KW-2449 Hs Inhibitor Inhibition 6.5 pKd
fedratinib Hs Inhibitor Inhibition 6.2 pKd
sunitinib Hs Inhibitor Inhibition 5.9 pKd
SU-14813 Hs Inhibitor Inhibition 5.8 pKd
dovitinib Hs Inhibitor Inhibition 5.6 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: 1,4

Key to terms and symbols Click column headers to sort
Target used in screen: MARK1/MARK1
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
staurosporine Hs Inhibitor Inhibition 0.2 -0.5 0.0
K-252a Hs Inhibitor Inhibition 1.3 0.0 0.0
Cdk1/2 inhibitor III Hs Inhibitor Inhibition 2.7 -1.0 0.0
JAK3 inhibitor VI Hs Inhibitor Inhibition 3.3 1.0 0.0
midostaurin Hs Inhibitor Inhibition 4.1 1.0 0.0
SB 218078 Hs Inhibitor Inhibition 10.4 38.0 29.0
SU11652 Hs Inhibitor Inhibition 18.1 14.0 3.0
PKR inhibitor Hs Inhibitor Inhibition 20.0 9.0 0.0
Gö 6976 Hs Inhibitor Inhibition 20.8 4.0 5.0
dovitinib Hs Inhibitor Inhibition 34.8
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. Busby EC, Leistritz DF, Abraham RT, Karnitz LM, Sarkaria JN. (2000) The radiosensitizing agent 7-hydroxystaurosporine (UCN-01) inhibits the DNA damage checkpoint kinase hChk1. Cancer Res., 60 (8): 2108-12. [PMID:10786669]

3. 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]

4. Gao Y, Davies SP, Augustin M, Woodward A, Patel UA, Kovelman R, Harvey KJ. (2013) A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. Biochem. J., 451 (2): 313-28. [PMID:23398362]

5. Moravcevic K, Mendrola JM, Schmitz KR, Wang YH, Slochower D, Janmey PA, Lemmon MA. (2010) Kinase associated-1 domains drive MARK/PAR1 kinases to membrane targets by binding acidic phospholipids. Cell, 143 (6): 966-77. [PMID:21145462]

6. 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 1. Last modified on 30/03/2016. Accessed on 08/04/2020. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2097.