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calcium/calmodulin-dependent protein kinase II beta subunit

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Target not currently curated in GtoImmuPdb

Target id: 1556

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

Abbreviated Name: CaMK2β

Family: CAMK2 family

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 666 7p13 CAMK2B calcium/calmodulin dependent protein kinase II beta
Mouse - 542 11 3.89 cM Camk2b calcium/calmodulin-dependent protein kinase II, beta
Rat - 542 14q21 Camk2b calcium/calmodulin-dependent protein kinase II beta
Previous and Unofficial Names Click here for help
CaM kinase II beta subunit | proline rich calmodulin-dependent protein kinase | caMK-II subunit beta | Ck2b | CAMKB | CAM2 | calcium/calmodulin-dependent protein kinase II
Database Links Click here for help
Alphafold Q13554 (Hs), P28652 (Mm), P08413 (Rn)
BRENDA 2.7.11.17
ChEMBL Target CHEMBL4121 (Hs), CHEMBL2610 (Rn)
Ensembl Gene ENSG00000058404 (Hs), ENSMUSG00000057897 (Mm), ENSRNOG00000052080 (Rn)
Entrez Gene 816 (Hs), 12323 (Mm), 24245 (Rn)
Human Protein Atlas ENSG00000058404 (Hs)
KEGG Enzyme 2.7.11.17
KEGG Gene hsa:816 (Hs), mmu:12323 (Mm), rno:24245 (Rn)
OMIM 607707 (Hs)
Pharos Q13554 (Hs)
RefSeq Nucleotide NM_001220 (Hs), NM_007595 (Mm), NM_001042354 (Rn)
RefSeq Protein NP_001211 (Hs), NP_001167524 (Mm), NP_001167525 (Mm), NP_031621 (Mm), NP_001035813 (Rn)
UniProtKB Q13554 (Hs), P28652 (Mm), P08413 (Rn)
Wikipedia CAMK2B (Hs)
Selected 3D Structures Click here for help
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 Click here for help
EC Number: 2.7.11.17

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
staurosporine Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition >10.0 pIC50 4
⤷ pIC50 >10.0 (IC50 <1x10-10 M) [4]
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: 2,5
Key to terms and symbols Click column headers to sort
Target used in screen: CAMK2B
Ligand Sp. Type Action Value Parameter
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.9 pKd
lestaurtinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 7.2 pKd
midostaurin Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.7 pKd
ruxolitinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.5 pKd
R547 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.1 pKd
A-674563 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.0 pKd
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 5.8 pKd
NVP-TAE684 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 5.7 pKd
SU-14813 Small molecule or natural product Hs Inhibitor Inhibition 5.6 pKd
GSK-461364A Small molecule or natural product 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: 1,3
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 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 1.6 -1.0 1.0
K-252a Small molecule or natural product Hs Inhibitor Inhibition 4.8 0.0 -1.0
Cdk1/2 inhibitor III Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 9.5 5.0 -1.0
SB 218078 Small molecule or natural product Hs Inhibitor Inhibition 9.9 32.0 32.0
SU11652 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 27.3 8.0 1.0
JAK3 inhibitor VI Small molecule or natural product Hs Inhibitor Inhibition 29.5 13.0 2.0
PKR inhibitor Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 40.8 13.0 3.0
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 46.7
Gö 6976 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 51.3 11.0 10.0
casein kinase II inhibitor III Small molecule or natural product Hs Inhibitor Inhibition 56.1 78.0 39.0
Displaying the top 10 most potent ligands  View all ligands in screen »
Immuno Process Associations
Immuno Process:  Inflammation
Immuno Process:  Cytokine production & signalling

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 18/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1556.