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calcium/calmodulin dependent protein kinase I

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Target id: 1952

Nomenclature: calcium/calmodulin dependent protein kinase I

Abbreviated Name: CaMK1-alpha

Family: CAMK1 family

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 370 3p25.3 CAMK1 calcium/calmodulin dependent protein kinase I
Mouse - 374 6 52.75 cM Camk1 calcium/calmodulin-dependent protein kinase I
Rat - 374 4q42 Camk1 calcium/calmodulin-dependent protein kinase I
Previous and Unofficial Names Click here for help
Gaip | caM kinase I alpha | caMKI-alpha | G alpha interacting protein | regulator of G-protein signalling 19
Database Links Click here for help
Alphafold Q14012 (Hs), Q91YS8 (Mm), Q63450 (Rn)
BRENDA 2.7.11.17
ChEMBL Target CHEMBL2493 (Hs)
Ensembl Gene ENSG00000134072 (Hs), ENSMUSG00000030272 (Mm), ENSRNOG00000021781 (Rn)
Entrez Gene 8536 (Hs), 52163 (Mm), 171503 (Rn)
Human Protein Atlas ENSG00000134072 (Hs)
KEGG Enzyme 2.7.11.17
KEGG Gene hsa:8536 (Hs), mmu:52163 (Mm), rno:171503 (Rn)
OMIM 604998 (Hs)
Pharos Q14012 (Hs)
RefSeq Nucleotide NM_003656 (Hs), NM_133926 (Mm), NM_134468 (Rn)
RefSeq Protein NP_003647 (Hs), NP_598687 (Mm), NP_604463 (Rn)
UniProtKB Q14012 (Hs), Q91YS8 (Mm), Q63450 (Rn)
Wikipedia CAMK1 (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 I apo form
PDB Id:  4FGB
Resolution:  2.6Å
Species:  Human
References:  5
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of human calcium/calmodulin-dependent protein kinase I 1-315 in complex with ATP
PDB Id:  4FG8
Resolution:  2.2Å
Species:  Human
References:  5
Enzyme Reaction Click here for help
EC Number: 2.7.11.17
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: 2,4
Key to terms and symbols Click column headers to sort
Target used in screen: CAMK1
Ligand Sp. Type Action Value Parameter
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.6 pKd
lestaurtinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.9 pKd
tamatinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.6 pKd
ruxolitinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.3 pKd
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 6.0 pKd
NVP-TAE684 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.0 pKd
tofacitinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 5.9 pKd
KW-2449 Small molecule or natural product Hs Inhibitor Inhibition 5.8 pKd
fedratinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 5.8 pKd
PLX-4720 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 5.7 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: CaMKI/CAMK1a
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 2.2 1.5 2.5
K-252a Small molecule or natural product Hs Inhibitor Inhibition 26.5 6.0 1.0
Syk inhibitor II Small molecule or natural product Immunopharmacology Ligand Hs Inhibitor Inhibition 60.9 20.0 -5.0
PDK1/Akt/Flt dual pathway inhibitor Small molecule or natural product Hs Inhibitor Inhibition 68.7 107.0 100.0
bosutinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 68.9
SB 218078 Small molecule or natural product Hs Inhibitor Inhibition 69.7 63.0 48.0
compound 52 [PMID: 9677190] Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 71.2 87.0 71.0
Chk2 inhibitor II Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 72.5 94.0 92.0
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 75.2
Cdk4 inhibitor II Small molecule or natural product Hs Inhibitor Inhibition 75.2 96.0 77.0
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. 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]

5. Zha M, Zhong C, Ou Y, Han L, Wang J, Ding J. (2012) Crystal structures of human CaMKIα reveal insights into the regulation mechanism of CaMKI. PLoS ONE, 7 (9): e44828. [PMID:23028635]

How to cite this page

CAMK1 family: calcium/calmodulin dependent protein kinase I. Last modified on 13/02/2017. Accessed on 18/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=1952.