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Target not currently curated in GtoImmuPdb
Target id: 1555
Nomenclature: calcium/calmodulin-dependent protein kinase II alpha subunit
Abbreviated Name: CaMK2α
Family: CAMK2 family
Gene and Protein Information ![]() |
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Species | TM | AA | Chromosomal Location | Gene Symbol | Gene Name | Reference |
Human | - | 478 | 5q32 | CAMK2A | calcium/calmodulin dependent protein kinase II alpha | |
Mouse | - | 478 | 18 34.41 cM | Camk2a | calcium/calmodulin-dependent protein kinase II alpha | |
Rat | - | 478 | 18q12.1 | Camk2a | calcium/calmodulin-dependent protein kinase II alpha |
Previous and Unofficial Names ![]() |
CaM kinase II alpha subunit | CaMK-II alpha subunit | alpha CaM kinase II | PK2CDD | PKCCD | CaMKII |
Database Links ![]() |
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Alphafold | Q9UQM7 (Hs), P11798 (Mm), P11275 (Rn) |
BRENDA | 2.7.11.17 |
ChEMBL Target | CHEMBL4147 (Hs), CHEMBL2359 (Rn) |
Ensembl Gene | ENSG00000070808 (Hs), ENSMUSG00000024617 (Mm), ENSRNOG00000018712 (Rn) |
Entrez Gene | 815 (Hs), 12322 (Mm), 25400 (Rn) |
Human Protein Atlas | ENSG00000070808 (Hs) |
KEGG Enzyme | 2.7.11.17 |
KEGG Gene | hsa:815 (Hs), mmu:12322 (Mm), rno:25400 (Rn) |
OMIM | 114078 (Hs) |
Pharos | Q9UQM7 (Hs) |
RefSeq Nucleotide | NM_015981 (Hs), NM_177407 (Mm), NM_012920 (Rn) |
RefSeq Protein | NP_057065 (Hs), NP_803126 (Mm), NP_037052 (Rn) |
UniProtKB | Q9UQM7 (Hs), P11798 (Mm), P11275 (Rn) |
Wikipedia | CAMK2A (Hs) |
Selected 3D Structures ![]() |
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Enzyme Reaction ![]() |
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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 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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View species-specific inhibitor tables | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Inhibitor Comments | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
KN-93 is a calmodulin-competitive inhibitor of CaMKII phosphorylating activity [6]. |
DiscoveRx KINOMEscan® screen ![]() |
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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: 2,7 |
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Target used in screen: CAMK2A | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Displaying the top 10 most potent ligands View all ligands in screen » |
EMD Millipore KinaseProfilerTM screen/Reaction Biology Kinase HotspotSM screen ![]() |
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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 |
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Target used in screen: nd/CAMK2a | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Displaying the top 10 most potent ligands View all ligands in screen » |
Immuno Process Associations | |||||||||
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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. Komiya M, Asano S, Koike N, Koga E, Igarashi J, Nakatani S, Isobe Y. (2011) Structure and activity relationship of 2-(substituted benzoyl)-hydroxyindoles as novel CaMKII inhibitors. Bioorg Med Chem Lett, 21 (5): 1456-8. [PMID:21292482]
4. Mirzoeva S, Sawkar A, Zasadzki M, Guo L, Velentza AV, Dunlap V, Bourguignon JJ, Ramstrom H, Haiech J, Van Eldik LJ et al.. (2002) Discovery of a 3-amino-6-phenyl-pyridazine derivative as a new synthetic antineuroinflammatory compound. J Med Chem, 31 (45): 563-6. [PMID:11806708]
5. 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]
6. Sumi M, Kiuchi K, Ishikawa T, Ishii A, Hagiwara M, Nagatsu T, Hidaka H. (1991) The newly synthesized selective Ca2+/calmodulin dependent protein kinase II inhibitor KN-93 reduces dopamine contents in PC12h cells. Biochem Biophys Res Commun, 181 (3): 968-75. [PMID:1662507]
7. 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]
CAMK2 family: calcium/calmodulin-dependent protein kinase II alpha subunit. Last modified on 23/10/2014. Accessed on 17/08/2022. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1555.