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calcium/calmodulin dependent protein kinase ID

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Target id: 1953

Nomenclature: calcium/calmodulin dependent protein kinase ID

Abbreviated Name: CaMK1-delta

Family: CAMK1 family

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 385 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 Click here for help
CaM kinase I delta
Database Links Click here for help
Alphafold Q8IU85 (Hs), Q8BW96 (Mm)
BRENDA 2.7.11.17
ChEMBL Target CHEMBL5073 (Hs)
Ensembl Gene ENSG00000183049 (Hs), ENSMUSG00000039145 (Mm), ENSRNOG00000017882 (Rn)
Entrez Gene 57118 (Hs), 227541 (Mm), 307124 (Rn)
Human Protein Atlas ENSG00000183049 (Hs)
KEGG Enzyme 2.7.11.17
KEGG Gene hsa:57118 (Hs), mmu:227541 (Mm), rno:307124 (Rn)
OMIM 607957 (Hs)
Pharos Q8IU85 (Hs)
RefSeq Nucleotide NM_020397 (Hs), NM_177343 (Mm), NM_001107365 (Rn)
RefSeq Protein NP_065130 (Hs), NP_796317 (Mm), NP_001100835 (Rn)
UniProtKB Q8IU85 (Hs), Q8BW96 (Mm)
Wikipedia CAMK1D (Hs)
Selected 3D Structures Click here for help
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 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
bosutinib Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 7.0 pIC50 4
⤷ pIC50 7.0 (IC50 9.2x10-8 M) [4]
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: 2,5
Key to terms and symbols Click column headers to sort
Target used in screen: CAMK1D
Ligand Sp. Type Action Value Parameter
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 9.0 pKd
lestaurtinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 7.3 pKd
ruxolitinib Small molecule or natural product Approved drug 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 6.7 pKd
NVP-TAE684 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.6 pKd
fedratinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 6.3 pKd
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 6.3 pKd
KW-2449 Small molecule or natural product Hs Inhibitor Inhibition 6.3 pKd
bosutinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.3 pKd
midostaurin Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand 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 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: CaMKIδ/CAMK1d
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 0.9 3.0 1.0
bosutinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 16.6
K-252a Small molecule or natural product Hs Inhibitor Inhibition 24.4 5.0 0.0
SB 218078 Small molecule or natural product Hs Inhibitor Inhibition 33.6 89.0 94.0
LY 294002 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 47.9 93.0 83.0
Lck inhibitor Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 50.3 98.0 55.0
SU11652 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 60.2 42.0 6.0
Syk inhibitor II Small molecule or natural product Immunopharmacology Ligand Hs Inhibitor Inhibition 61.1 41.0 6.0
PD98059 Small molecule or natural product Hs Inhibitor Inhibition 65.3 123.0 120.0
GF109203X Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 68.0 63.0 10.0
Displaying the top 10 most potent ligands  View all ligands in screen »
Immuno Process Associations
Immuno Process:  Inflammation
Immuno Process:  Immune regulation
Immuno Process:  Chemotaxis & migration

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 19/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=1953.