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CDC42 binding protein kinase beta

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Target not currently curated in GtoImmuPdb

Target id: 1508

Nomenclature: CDC42 binding protein kinase beta

Abbreviated Name: MRCKβ

Family: GEK subfamily

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 1711 14q32.32 CDC42BPB CDC42 binding protein kinase beta
Mouse - 1713 12 60.94 cM Cdc42bpb CDC42 binding protein kinase beta
Rat - 1713 6q32 Cdc42bpb CDC42 binding protein kinase beta
Previous and Unofficial Names Click here for help
Cdc42 binding protein kinase beta | MRCK beta | serine/threonine-protein kinase MRCK beta | CDC42 binding protein kinase beta (DMPK-like)
Database Links Click here for help
Alphafold Q9Y5S2 (Hs), Q7TT50 (Mm), Q7TT49 (Rn)
BRENDA 2.7.11.1
CATH/Gene3D 2.130.10.10, 2.30.29.30, 3.90.810.10
ChEMBL Target CHEMBL5052 (Hs)
Ensembl Gene ENSG00000198752 (Hs), ENSMUSG00000021279 (Mm), ENSRNOG00000009675 (Rn)
Entrez Gene 9578 (Hs), 217866 (Mm), 113960 (Rn)
Human Protein Atlas ENSG00000198752 (Hs)
KEGG Enzyme 2.7.11.1
KEGG Gene hsa:9578 (Hs), mmu:217866 (Mm), rno:113960 (Rn)
OMIM 614062 (Hs)
Pharos Q9Y5S2 (Hs)
RefSeq Nucleotide NM_006035 (Hs), NM_183016 (Mm), NM_053620 (Rn)
RefSeq Protein NP_006026 (Hs), NP_898837 (Mm), NP_446072 (Rn)
UniProtKB Q9Y5S2 (Hs), Q7TT50 (Mm), Q7TT49 (Rn)
Wikipedia CDC42BPB (Hs)
Selected 3D Structures Click here for help
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 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
A-443654 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure 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 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: 2,6
Key to terms and symbols Click column headers to sort
Target used in screen: MRCKB
Ligand Sp. Type Action Value Parameter
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.4 pKd
A-674563 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.0 pKd
foretinib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.5 pKd
nilotinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 6.0 pKd
doramapimod Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.0 pKd
lestaurtinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.0 pKd
PD-173955 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.0 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
SB203580 Small molecule or natural product Immunopharmacology Ligand 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 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: 1,3
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 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 2.0 -0.5 0.0
Cdk1/2 inhibitor III Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 48.1 8.0 3.0
alsterpaullone 2-cyanoethyl Small molecule or natural product Hs Inhibitor Inhibition 54.1 9.0 6.0
K-252a Small molecule or natural product Hs Inhibitor Inhibition 78.9 33.0 5.0
VEGF receptor tyrosine kinase inhibitor II Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 79.9 89.0 90.0
Cdk2 inhibitor III Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 82.6 88.0 83.0
PDK1/Akt/Flt dual pathway inhibitor Small molecule or natural product Hs Inhibitor Inhibition 82.6 116.0 88.0
alsterpaullone Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 83.3 48.0 57.0
VEGF receptor 2 kinase inhibitor IV Small molecule or natural product Hs Inhibitor Inhibition 83.4 104.0 92.0
Cdk4 inhibitor Small molecule or natural product 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 MRCKβ, 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 16/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1508.