microtubule affinity regulating kinase 3 | MARK subfamily | IUPHAR/BPS Guide to PHARMACOLOGY

microtubule affinity regulating kinase 3

Target id: 2099

Nomenclature: microtubule affinity regulating kinase 3

Abbreviated Name: MARK3

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 3 in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 753 14q32.3 MARK3 microtubule affinity regulating kinase 3
Mouse - 744 12 F1-2 Mark3 MAP/microtubule affinity regulating kinase 3
Rat - 797 6 q32 Mark3 microtubule affinity regulating kinase 3
Previous and Unofficial Names
CTAK1 | Cdc25C-associated protein kinase 1 | ELKL motif kinase 2 | EMK2 | Par-1a | Protein kinase STK10 | MAP/microtubule affinity-regulating kinase 3
Database Links
BRENDA
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:  Kinase and Ubiquitin-associated domains of MARK3/Par-1
PDB Id:  2QNJ
Resolution:  2.7Å
Species:  Human
References:  4
Enzyme Reaction
EC Number: 2.7.11.1

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 Affinity Units Reference
compound 17d [PMID: 23099093] Hs Inhibition 7.9 pIC50 3
pIC50 7.9 (IC50 1.2x10-8 M) [3]
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: 2,5

Key to terms and symbols Click column headers to sort
Target used in screen: MARK3
Ligand Sp. Type Action Affinity Units
staurosporine Hs Inhibitor Inhibition 8.5 pKd
NVP-TAE684 Hs Inhibitor Inhibition 7.9 pKd
midostaurin Hs Inhibitor Inhibition 7.7 pKd
lestaurtinib Hs Inhibitor Inhibition 7.3 pKd
fedratinib Hs Inhibitor Inhibition 6.5 pKd
sunitinib Hs Inhibitor Inhibition 6.4 pKd
PD-173955 Hs Inhibitor Inhibition 6.1 pKd
SU-14813 Hs Inhibitor Inhibition 6.0 pKd
KW-2449 Hs Inhibitor Inhibition 5.9 pKd
tamatinib Hs Inhibitor Inhibition 5.7 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/MARK3
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
Cdk1/2 inhibitor III Hs Inhibitor Inhibition 0.3
staurosporine Hs Inhibitor Inhibition 0.7
K-252a Hs Inhibitor Inhibition 1.8
JAK3 inhibitor VI Hs Inhibitor Inhibition 3.9
midostaurin Hs Inhibitor Inhibition 4.8
SU11652 Hs Inhibitor Inhibition 7.9
SB 218078 Hs Inhibitor Inhibition 8.5
Gö 6976 Hs Inhibitor Inhibition 13.9
PKR inhibitor Hs Inhibitor Inhibition 21.3
isogranulatimide Hs Inhibitor Inhibition 29.8
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. 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. McIver EG, Bryans J, Birchall K, Chugh J, Drake T, Lewis SJ, Osborne J, Smiljanic-Hurley E, Tsang W, Kamal A et al.. (2012) Synthesis and structure-activity relationships of a novel series of pyrimidines as potent inhibitors of TBK1/IKK╬Á kinases. Bioorg. Med. Chem. Lett., 22 (23): 7169-73. [PMID:23099093]

4. Murphy JM, Korzhnev DM, Ceccarelli DF, Briant DJ, Zarrine-Afsar A, Sicheri F, Kay LE, Pawson T. (2007) Conformational instability of the MARK3 UBA domain compromises ubiquitin recognition and promotes interaction with the adjacent kinase domain. Proc. Natl. Acad. Sci. U.S.A., 104 (36): 14336-41. [PMID:17726107]

5. 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 3. Last modified on 30/03/2016. Accessed on 19/11/2018. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2099.