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CDC42 binding protein kinase alpha

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Target not currently curated in GtoImmuPdb

Target id: 1507

Nomenclature: CDC42 binding protein kinase alpha

Abbreviated Name: MRCKα

Family: GEK subfamily

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 1732 1q42.13 CDC42BPA CDC42 binding protein kinase alpha
Mouse - 1719 1 H4 Cdc42bpa CDC42 binding protein kinase alpha
Rat - 1732 13q26 Cdc42bpa CDC42 binding protein kinase alpha
Previous and Unofficial Names Click here for help
MRCKA | MRCK alpha | serine/threonine-protein kinase MRCK alpha | MRCK | PK428 | CDC42 binding protein kinase alpha (DMPK-like)
Database Links Click here for help
Alphafold Q5VT25 (Hs), Q3UU96 (Mm), O54874 (Rn)
BRENDA 2.7.11.1
CATH/Gene3D 2.30.29.30, 3.90.810.10
ChEMBL Target CHEMBL4516 (Hs)
Ensembl Gene ENSG00000143776 (Hs), ENSMUSG00000026490 (Mm), ENSRNOG00000002841 (Rn)
Entrez Gene 8476 (Hs), 226751 (Mm), 114116 (Rn)
Human Protein Atlas ENSG00000143776 (Hs)
KEGG Enzyme 2.7.11.1
KEGG Gene hsa:8476 (Hs), mmu:226751 (Mm), rno:114116 (Rn)
OMIM 603412 (Hs)
Pharos Q5VT25 (Hs)
RefSeq Nucleotide NM_003607 (Hs), NM_001033285 (Mm), NM_053657 (Rn)
RefSeq Protein NP_003598 (Hs), NP_001028457 (Mm), NP_446109 (Rn)
UniProtKB Q5VT25 (Hs), Q3UU96 (Mm), O54874 (Rn)
Wikipedia CDC42BPA (Hs)
Selected 3D Structures Click here for help
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 Click here for help
EC Number: 2.7.11.1

Download all structure-activity data for this target as a CSV file go icon to follow link

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
RKI-1447 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.5 pIC50 5
⤷ pIC50 8.5 (IC50 2.87x10-9 M) [5]
compound 11d [DOI: 10.1039/c0md00194e] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.1 pIC50 2
⤷ pIC50 7.1 (IC50 7.4x10-8 M) [2]
DiscoveRx KINOMEscan® screen Click here for help
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 Value Parameter
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.2 pKd
A-674563 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.4 pKd
foretinib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.2 pKd
PD-173955 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 5.9 pKd
PI-103 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 5.7 pKd
dasatinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 5.7 pKd
vandetanib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 5.6 pKd
erlotinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition <5.5 pKd
ruboxistaurin Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition <5.5 pKd
crizotinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand 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 Click here for help
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 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 1.7 1.5 0.0
Cdk1/2 inhibitor III Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 54.6 28.0 24.0
SU11652 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 60.0 118.0 113.0
Syk inhibitor Small molecule or natural product Immunopharmacology Ligand Hs Inhibitor Inhibition 70.7 103.0 89.0
alsterpaullone 2-cyanoethyl Small molecule or natural product Hs Inhibitor Inhibition 73.1 35.0 19.0
tozasertib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 75.3
Cdk4 inhibitor III Small molecule or natural product Hs Inhibitor Inhibition 77.6 95.0 91.0
EGFR inhibitor Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 77.7 92.0 115.0
VEGF receptor tyrosine kinase inhibitor III Small molecule or natural product Hs Inhibitor Inhibition 77.8
vatalanib Small molecule or natural product 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. Medchemcomm, 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 19/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1507.