calcium/calmodulin dependent protein kinase ID | CAMK1 family | IUPHAR/BPS Guide to PHARMACOLOGY

calcium/calmodulin dependent protein kinase ID

Target id: 1953

Nomenclature: calcium/calmodulin dependent protein kinase ID

Abbreviated Name: CaMK1-delta

Family: CAMK1 family

Annotation status:  image of an orange circle Annotated and awaiting review. Please contact us if you can help with reviewing.  » Email us

   GtoImmuPdb view: OFF :     Currently no data for calcium/calmodulin dependent protein kinase ID in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 357 10p13 CAMK1D calcium/calmodulin dependent protein kinase ID
Mouse - 385 2 A1 Camk1d calcium/calmodulin-dependent protein kinase ID
Rat - 385 17q12.3 Camk1d calcium/calmodulin-dependent protein kinase ID
Previous and Unofficial Names
CaM kinase I delta
Database Links
BRENDA
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 calmodulin-dependent protein kinase 1D
PDB Id:  2JC6
Resolution:  2.3Å
Species:  Human
References: 
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 Affinity Units Reference
bosutinib Hs Inhibition 7.0 pIC50 4
pIC50 7.0 (IC50 9.2x10-8 M) [4]
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: 2,5

Key to terms and symbols Click column headers to sort
Target used in screen: CAMK1D
Ligand Sp. Type Action Affinity Units
staurosporine Hs Inhibitor Inhibition 9.0 pKd
lestaurtinib Hs Inhibitor Inhibition 7.3 pKd
ruxolitinib Hs Inhibitor Inhibition 6.9 pKd
tamatinib Hs Inhibitor Inhibition 6.7 pKd
NVP-TAE684 Hs Inhibitor Inhibition 6.6 pKd
fedratinib Hs Inhibitor Inhibition 6.3 pKd
sunitinib Hs Inhibitor Inhibition 6.3 pKd
KW-2449 Hs Inhibitor Inhibition 6.3 pKd
bosutinib Hs Inhibitor Inhibition 6.3 pKd
midostaurin Hs Inhibitor Inhibition 6.2 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: CaMKIδ/CAMK1d
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
staurosporine Hs Inhibitor Inhibition 0.9 3.0 1.0
bosutinib Hs Inhibitor Inhibition 16.6
K-252a Hs Inhibitor Inhibition 24.4 5.0 0.0
SB 218078 Hs Inhibitor Inhibition 33.6 89.0 94.0
LY 294002 Hs Inhibitor Inhibition 47.9 93.0 83.0
Lck inhibitor Hs Inhibitor Inhibition 50.3 98.0 55.0
SU11652 Hs Inhibitor Inhibition 60.2 42.0 6.0
Syk inhibitor II Hs Inhibitor Inhibition 61.1 41.0 6.0
PD98059 Hs Inhibitor Inhibition 65.3 123.0 120.0
GF109203X Hs Inhibitor Inhibition 68.0 63.0 10.0
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. Remsing Rix LL, Rix U, Colinge J, Hantschel O, Bennett KL, Stranzl T, Müller A, Baumgartner C, Valent P, Augustin M et al.. (2009) Global target profile of the kinase inhibitor bosutinib in primary chronic myeloid leukemia cells. Leukemia, 23 (3): 477-85. [PMID:19039322]

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

CAMK1 family: calcium/calmodulin dependent protein kinase ID. Last modified on 13/02/2017. Accessed on 14/11/2018. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1953.