Top ▲

calcium/calmodulin-dependent protein kinase II delta subunit

Click here for help

Target id: 1558

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

Abbreviated Name: CaMK2δ

Family: CAMK2 family

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 499 4q26 CAMK2D calcium/calmodulin dependent protein kinase II delta
Mouse - 499 3 G1 Camk2d calcium/calmodulin-dependent protein kinase II, delta
Rat - 533 2q42 Camk2d calcium/calmodulin-dependent protein kinase II delta
Previous and Unofficial Names Click here for help
caM kinase II subunit delta | CAMK1 | Camk2 | Camki | caMK-II subunit delta | CAMKD | calcium/calmodulin-dependent protein kinase II
Database Links Click here for help
Alphafold Q13557 (Hs), Q6PHZ2 (Mm), P15791 (Rn)
BRENDA 2.7.11.17
ChEMBL Target CHEMBL2801 (Hs), CHEMBL4296090 (Rn)
Ensembl Gene ENSG00000145349 (Hs), ENSMUSG00000053819 (Mm), ENSRNOG00000011589 (Rn)
Entrez Gene 817 (Hs), 108058 (Mm), 24246 (Rn)
Human Protein Atlas ENSG00000145349 (Hs)
KEGG Enzyme 2.7.11.17
KEGG Gene hsa:817 (Hs), mmu:108058 (Mm), rno:24246 (Rn)
OMIM 607708 (Hs)
Pharos Q13557 (Hs)
RefSeq Nucleotide NM_001221 (Hs), NM_001025439 (Mm), NM_012519 (Rn)
RefSeq Protein NP_001212 (Hs), NP_001020609 (Mm), NP_001020610 (Mm), NP_076302 (Mm), NP_036651 (Rn)
UniProtKB Q13557 (Hs), Q6PHZ2 (Mm), P15791 (Rn)
Wikipedia CAMK2D (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 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 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
compound 15b [PMID: 18334293] Small molecule or natural product Primary target of this compound Hs Inhibition 8.1 pIC50 6
⤷ pIC50 8.1 (IC50 9x10-9 M) [6]
compound 27 [PMID: 18337095] Small molecule or natural product Primary target of this compound Hs Inhibition 8.0 pIC50 5
⤷ pIC50 8.0 (IC50 1x10-8 M) [5]
MELK-TI Small molecule or natural product Click here for species-specific activity table 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 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: 2,8
Key to terms and symbols Click column headers to sort
Target used in screen: CAMK2D
Ligand Sp. Type Action Value Parameter
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 9.5 pKd
lestaurtinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 8.1 pKd
midostaurin Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 7.4 pKd
ruxolitinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 7.1 pKd
A-674563 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.6 pKd
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 6.4 pKd
NVP-TAE684 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.2 pKd
fedratinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 6.2 pKd
GSK-461364A Small molecule or natural product Hs Inhibitor Inhibition 6.2 pKd
SU-14813 Small molecule or natural product 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 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: CaMKIIδ/CAMK2d
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
K-252a Small molecule or natural product Hs Inhibitor Inhibition 2.6 0.0 1.0
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 3.1 0.5 0.0
SB 218078 Small molecule or natural product Hs Inhibitor Inhibition 7.0 -1.0 5.0
SU11652 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.2 3.0 1.0
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 11.6
Cdk1/2 inhibitor III Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 15.6 0.0 0.0
midostaurin Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 17.3 5.0 1.0
Gö 6976 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 20.3 1.0 1.0
GSK-3 inhibitor IX Small molecule or natural product Hs Inhibitor Inhibition 23.0 1.0 2.0
indirubin derivative E804 Small molecule or natural product Hs Inhibitor Inhibition 29.1 6.0 1.0
Displaying the top 10 most potent ligands  View all ligands in screen »
Immuno Process Associations
Immuno Process:  Inflammation
Immuno Process:  Cytokine production & signalling

References

Show »

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 10/10/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=1558.