calcium/calmodulin-dependent protein kinase II beta subunit | CAMK2 family | IUPHAR/BPS Guide to PHARMACOLOGY

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calcium/calmodulin-dependent protein kinase II beta subunit

Target id: 1556

Nomenclature: calcium/calmodulin-dependent protein kinase II beta subunit

Abbreviated Name: CaMK2β

Family: CAMK2 family

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 calcium/calmodulin-dependent protein kinase II beta subunit in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 666 7p14.3-p14.1 CAMK2B calcium/calmodulin dependent protein kinase II beta
Mouse - 542 11 Camk2b calcium/calmodulin-dependent protein kinase II, beta
Rat - 589 14q21 Camk2b calcium/calmodulin-dependent protein kinase II beta
Previous and Unofficial Names
CaM kinase II beta subunit | proline rich calmodulin-dependent protein kinase | caMK-II subunit beta | Ck2b | CAM2 | CAMKB | calcium/calmodulin-dependent protein kinase II
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:  Crystal structure of human calcium/calmodulin-dependent protein kinase IIB isoform 1 (CAMK2B)
PDB Id:  3BHH
Resolution:  2.4Å
Species:  Human
References: 
Enzyme Reaction
EC Number: 2.7.11.17

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
staurosporine Hs Inhibition >10.0 pIC50 4
pIC50 >10.0 (IC50 <1x10-10 M) [4]
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: CAMK2B
Ligand Sp. Type Action Affinity Units
staurosporine Hs Inhibitor Inhibition 8.9 pKd
lestaurtinib Hs Inhibitor Inhibition 7.2 pKd
midostaurin Hs Inhibitor Inhibition 6.7 pKd
ruxolitinib Hs Inhibitor Inhibition 6.5 pKd
R547 Hs Inhibitor Inhibition 6.1 pKd
A-674563 Hs Inhibitor Inhibition 6.0 pKd
sunitinib Hs Inhibitor Inhibition 5.8 pKd
NVP-TAE684 Hs Inhibitor Inhibition 5.7 pKd
SU-14813 Hs Inhibitor Inhibition 5.6 pKd
GSK-461364A 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: 1,3

Key to terms and symbols Click column headers to sort
Target used in screen: CaMKIIβ/CAMK2b
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
staurosporine Hs Inhibitor Inhibition 1.6 -1.0 1.0
K-252a Hs Inhibitor Inhibition 4.8 0.0 -1.0
Cdk1/2 inhibitor III Hs Inhibitor Inhibition 9.5 5.0 -1.0
SB 218078 Hs Inhibitor Inhibition 9.9 32.0 32.0
SU11652 Hs Inhibitor Inhibition 27.3 8.0 1.0
JAK3 inhibitor VI Hs Inhibitor Inhibition 29.5 13.0 2.0
PKR inhibitor Hs Inhibitor Inhibition 40.8 13.0 3.0
sunitinib Hs Inhibitor Inhibition 46.7
Gö 6976 Hs Inhibitor Inhibition 51.3 11.0 10.0
casein kinase II inhibitor III Hs Inhibitor Inhibition 56.1 78.0 39.0
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. Hall MD, Salam NK, Hellawell JL, Fales HM, Kensler CB, Ludwig JA, Szakács G, Hibbs DE, Gottesman MM. (2009) Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells. J. Med. Chem., 52 (10): 3191-204. [PMID:19397322]

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

CAMK2 family: calcium/calmodulin-dependent protein kinase II beta subunit. Last modified on 13/02/2015. Accessed on 11/12/2018. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1556.