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

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CDC42 binding protein kinase beta

Target not currently curated in GtoImmuPdb

Target id: 1508

Nomenclature: CDC42 binding protein kinase beta

Abbreviated Name: MRCKβ

Family: GEK subfamily

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 1711 14q32.32 CDC42BPB CDC42 binding protein kinase beta
Mouse - 1713 12 Cdc42bpb CDC42 binding protein kinase beta
Rat - 1713 6q32 Cdc42bpb CDC42 binding protein kinase beta
Previous and Unofficial Names
Cdc42 binding protein kinase beta | MRCK beta | serine/threonine-protein kinase MRCK beta | CDC42 binding protein kinase beta (DMPK-like)
Database Links
BRENDA
CATH/Gene3D
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:  MRCK beta in complex with fasudil
PDB Id:  3TKU
Ligand:  fasudil
Resolution:  2.15Å
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 Value Parameter Reference
A-443654 Hs Inhibition - - 5
[5]
Description: Measured as % inhibition using 1μM compound.
Inhibitor Comments
A-443654 inhibits MRCKβ activity by approximately 94% using 1μM compound [5].
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: 2,6

Key to terms and symbols Click column headers to sort
Target used in screen: MRCKB
Ligand Sp. Type Action Value Parameter
staurosporine Hs Inhibitor Inhibition 7.4 pKd
A-674563 Hs Inhibitor Inhibition 7.0 pKd
foretinib Hs Inhibitor Inhibition 6.5 pKd
nilotinib Hs Inhibitor Inhibition 6.0 pKd
doramapimod Hs Inhibitor Inhibition 6.0 pKd
lestaurtinib Hs Inhibitor Inhibition 6.0 pKd
PD-173955 Hs Inhibitor Inhibition 6.0 pKd
dasatinib Hs Inhibitor Inhibition 5.7 pKd
vandetanib Hs Inhibitor Inhibition 5.6 pKd
SB203580 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: 1,3

Key to terms and symbols Click column headers to sort
Target used in screen: MRCKβ/MRCKb(CDC42BPB)
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
staurosporine Hs Inhibitor Inhibition 2.0 -0.5 0.0
Cdk1/2 inhibitor III Hs Inhibitor Inhibition 48.1 8.0 3.0
alsterpaullone 2-cyanoethyl Hs Inhibitor Inhibition 54.1 9.0 6.0
K-252a Hs Inhibitor Inhibition 78.9 33.0 5.0
VEGF receptor tyrosine kinase inhibitor II Hs Inhibitor Inhibition 79.9 89.0 90.0
Cdk2 inhibitor III Hs Inhibitor Inhibition 82.6 88.0 83.0
PDK1/Akt/Flt dual pathway inhibitor Hs Inhibitor Inhibition 82.6 116.0 88.0
alsterpaullone Hs Inhibitor Inhibition 83.3 48.0 57.0
VEGF receptor 2 kinase inhibitor IV Hs Inhibitor Inhibition 83.4 104.0 92.0
Cdk4 inhibitor Hs Inhibitor Inhibition 84.1 85.0 85.0
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. 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]

4. Heikkila T, Wheatley E, Crighton D, Schroder E, Boakes A, Kaye SJ, Mezna M, Pang L, Rushbrooke M, Turnbull A et al.. (2011) Co-crystal structures of inhibitors with MRCK╬▓, a key regulator of tumor cell invasion. PLoS ONE, 6 (9): e24825. [PMID:21949762]

5. Okuzumi T, Fiedler D, Zhang C, Gray DC, Aizenstein B, Hoffman R, Shokat KM. (2009) Inhibitor hijacking of Akt activation. Nat. Chem. Biol., 5 (7): 484-93. [PMID:19465931]

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 beta. Last modified on 29/01/2016. Accessed on 30/09/2020. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1508.