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

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calcium/calmodulin-dependent protein kinase II delta subunit

Target not currently curated in GtoImmuPdb

Target id: 1558

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

Abbreviated Name: CaMK2δ

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

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 499 4q26 CAMK2D calcium/calmodulin dependent protein kinase II delta
Mouse - 512 3 Camk2d calcium/calmodulin-dependent protein kinase II, delta
Rat - 533 2 q42-q43 Camk2d calcium/calmodulin-dependent protein kinase II delta
Previous and Unofficial Names
caM kinase II subunit delta | CAMK1 | Camk2 | Camki | caMK-II subunit delta | CAMKD | calcium/calmodulin-dependent protein kinase II
Database Links
BRENDA
ChEMBL Target
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 II DELTA ISOFORM 1, CAMKD
PDB Id:  2VN9
Resolution:  2.3Å
Species:  Human
References:  7
Image of receptor 3D structure from RCSB PDB
Description:  CRYSTAL STRUCTURE OF SU6656-BOUND CALCIUM/CALMODULIN-DEPENDENT PROTEIN KINASE II DELTA IN COMPLEX WITH CALMODULIN
PDB Id:  2WEL
Resolution:  1.9Å
Species:  Human
References:  7
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 Value Parameter Reference
compound 15b [PMID: 18334293] Hs Inhibition 8.1 pIC50 6
pIC50 8.1 (IC50 9x10-9 M) [6]
compound 27 [PMID: 18337095] Hs Inhibition 8.0 pIC50 5
pIC50 8.0 (IC50 1x10-8 M) [5]
MELK-TI Hs Inhibition 6.1 pIC50 4
pIC50 6.1 (IC50 8.1x10-7 M) [4]
Description: Measured in a MIllipore kinase screening panel assay
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: 2,8

Key to terms and symbols Click column headers to sort
Target used in screen: CAMK2D
Ligand Sp. Type Action Value Parameter
staurosporine Hs Inhibitor Inhibition 9.5 pKd
lestaurtinib Hs Inhibitor Inhibition 8.1 pKd
midostaurin Hs Inhibitor Inhibition 7.4 pKd
ruxolitinib Hs Inhibitor Inhibition 7.1 pKd
A-674563 Hs Inhibitor Inhibition 6.6 pKd
sunitinib Hs Inhibitor Inhibition 6.4 pKd
NVP-TAE684 Hs Inhibitor Inhibition 6.2 pKd
fedratinib Hs Inhibitor Inhibition 6.2 pKd
GSK-461364A Hs Inhibitor Inhibition 6.2 pKd
SU-14813 Hs Inhibitor Inhibition 6.1 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: CaMKIIδ/CAMK2d
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
K-252a Hs Inhibitor Inhibition 2.6 0.0 1.0
staurosporine Hs Inhibitor Inhibition 3.1 0.5 0.0
SB 218078 Hs Inhibitor Inhibition 7.0 -1.0 5.0
SU11652 Hs Inhibitor Inhibition 7.2 3.0 1.0
sunitinib Hs Inhibitor Inhibition 11.6
Cdk1/2 inhibitor III Hs Inhibitor Inhibition 15.6 0.0 0.0
midostaurin Hs Inhibitor Inhibition 17.3 5.0 1.0
Gö 6976 Hs Inhibitor Inhibition 20.3 1.0 1.0
GSK-3 inhibitor IX Hs Inhibitor Inhibition 23.0 1.0 2.0
indirubin derivative E804 Hs Inhibitor Inhibition 29.1 6.0 1.0
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. Johnson CN, Berdini V, Beke L, Bonnet P, Brehmer D, Coyle JE, Day PJ, Frederickson M, Freyne EJ, Gilissen RA et al.. (2014) Fragment-based discovery of type I inhibitors of maternal embryonic leucine zipper kinase. ACS Med Chem Lett, 6 (1): 25-30. [PMID:25589925]

5. Lu Q, Chen Z, Perumattam J, Wang DX, Liang W, Xu YJ, Do S, Bonaga L, Higaki J, Dong H et al.. (2008) Aryl-indolyl maleimides as inhibitors of CaMKIIdelta. Part 3: Importance of the indole orientation. Bioorg. Med. Chem. Lett., 18 (7): 2399-403. [PMID:18337095]

6. Mavunkel B, Xu YJ, Goyal B, Lim D, Lu Q, Chen Z, Wang DX, Higaki J, Chakraborty I, Liclican A et al.. (2008) Pyrimidine-based inhibitors of CaMKIIdelta. Bioorg. Med. Chem. Lett., 18 (7): 2404-8. [PMID:18334293]

7. Rellos P, Pike AC, Niesen FH, Salah E, Lee WH, von Delft F, Knapp S. (2010) Structure of the CaMKIIdelta/calmodulin complex reveals the molecular mechanism of CaMKII kinase activation. PLoS Biol., 8 (7): e1000426. [PMID:20668654]

8. 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 delta subunit. Last modified on 07/11/2016. Accessed on 15/11/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1558.