CDC42 binding protein kinase alpha | GEK subfamily | IUPHAR/BPS Guide to PHARMACOLOGY

CDC42 binding protein kinase alpha

Target id: 1507

Nomenclature: CDC42 binding protein kinase alpha

Abbreviated Name: MRCKα

Family: GEK 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 CDC42 binding protein kinase alpha in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 1719 1q42.11 CDC42BPA CDC42 binding protein kinase alpha
Mouse - 1732 1 Cdc42bpa CDC42 binding protein kinase alpha
Rat - 1732 13q26 Cdc42bpa CDC42 binding protein kinase alpha
Previous and Unofficial Names
MRCKA | MRCK alpha | serine/threonine-protein kinase MRCK alpha | MRCK | PK428 | CDC42 binding protein kinase alpha (DMPK-like)
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 CDC42 binding protein kinase alpha (MRCK alpha)
PDB Id:  4AW2
Resolution:  1.7Å
Species:  Rat
References: 
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
RKI-1447 Hs Inhibition 8.5 pIC50 5
pIC50 8.5 (IC50 2.87x10-9 M) [5]
compound 11d [DOI: 10.1039/c0md00194e] Hs Inhibition 7.1 pIC50 2
pIC50 7.1 (IC50 7.4x10-8 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: MRCKA
Ligand Sp. Type Action Affinity Units
staurosporine Hs Inhibitor Inhibition 7.2 pKd
A-674563 Hs Inhibitor Inhibition 6.4 pKd
foretinib Hs Inhibitor Inhibition 6.2 pKd
PD-173955 Hs Inhibitor Inhibition 5.9 pKd
PI-103 Hs Inhibitor Inhibition 5.7 pKd
dasatinib Hs Inhibitor Inhibition 5.7 pKd
vandetanib Hs Inhibitor Inhibition 5.6 pKd
erlotinib Hs Inhibitor Inhibition <5.5 pKd
ruboxistaurin Hs Inhibitor Inhibition <5.5 pKd
crizotinib 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: 1,4

Key to terms and symbols Click column headers to sort
Target used in screen: MRCKα/MRCKa(CDC42BPA)
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
staurosporine Hs Inhibitor Inhibition 1.7 1.5 0.0
Cdk1/2 inhibitor III Hs Inhibitor Inhibition 54.6 28.0 24.0
SU11652 Hs Inhibitor Inhibition 60.0 118.0 113.0
Syk inhibitor Hs Inhibitor Inhibition 70.7 103.0 89.0
alsterpaullone 2-cyanoethyl Hs Inhibitor Inhibition 73.1 35.0 19.0
tozasertib Hs Inhibitor Inhibition 75.3
Cdk4 inhibitor III Hs Inhibitor Inhibition 77.6 95.0 91.0
EGFR inhibitor Hs Inhibitor Inhibition 77.7 92.0 115.0
VEGF receptor tyrosine kinase inhibitor III Hs Inhibitor Inhibition 77.8
vatalanib Hs Inhibitor Inhibition 78.3
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. Chen YT, Vojkovsky T, Fang X, Pocas JR, Grant W, Handy AMW, Schroter T, LoGrasso P, Bannister TD, Feng Y. (2011) Asymmetric synthesis of potent chroman-based Rho kinase (ROCK-II) inhibitors. Med Chem Commun, 2: 73-75.

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. Pireddu R, Forinash KD, Sun NN, Martin MP, Sung SS, Alexander B, Zhu JY, Guida WC, Schönbrunn E, Sebti SM et al.. (2012) Pyridylthiazole-based ureas as inhibitors of Rho associated protein kinases (ROCK1 and 2). Medchemcomm, 3 (6): 699-709. [PMID:23275831]

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

GEK subfamily: CDC42 binding protein kinase alpha. Last modified on 29/01/2016. Accessed on 17/11/2018. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1507.