doublecortin like kinase 2 | DCAMKL family | IUPHAR/BPS Guide to PHARMACOLOGY

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doublecortin like kinase 2

Target not currently curated in GtoImmuPdb

Target id: 2006

Nomenclature: doublecortin like kinase 2

Abbreviated Name: DCAMKL2

Family: DCAMKL family

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

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 766 4q31.3 DCLK2 doublecortin like kinase 2
Mouse - 771 3 F1 Dclk2 doublecortin-like kinase 2
Rat - 767 2 q34 Dclk2 doublecortin-like kinase 2
Previous and Unofficial Names
CaMK-like CREB regulatory kinase 2 | CLICK2 | CLICK-II | DCK2 | doublecortin and CaM kinase-like 2
Database Links
BRENDA
CATH/Gene3D
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Enzyme Reaction
EC Number: 2.7.11.1

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 Value Parameter Reference
XMD8-92 Hs Inhibition 6.7 pKd 5
pKd 6.7 (Kd 1.9x10-7 M) [5]
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: 2,4

Key to terms and symbols Click column headers to sort
Target used in screen: DCAMKL2
Ligand Sp. Type Action Value Parameter
NVP-TAE684 Hs Inhibitor Inhibition 7.8 pKd
staurosporine Hs Inhibitor Inhibition 7.1 pKd
crizotinib Hs Inhibitor Inhibition 6.4 pKd
ruxolitinib Hs Inhibitor Inhibition 6.1 pKd
fedratinib Hs Inhibitor Inhibition 6.1 pKd
PHA-665752 Hs Inhibitor Inhibition 6.0 pKd
BMS-387032 Hs Inhibitor Inhibition 6.0 pKd
AT-7519 Hs Inhibitor Inhibition 5.6 pKd
sunitinib Hs Inhibitor Inhibition 5.6 pKd
SB203580 Hs Inhibitor Inhibition <5.5 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: DCAMKL2/DCAMKL2
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
staurosporine Hs Inhibitor Inhibition 11.0 5.5 2.5
Cdk1/2 inhibitor III Hs Inhibitor Inhibition 40.4 13.0 2.0
JAK inhibitor I Hs Inhibitor Inhibition 65.8 38.0 27.0
PKR inhibitor Hs Inhibitor Inhibition 69.8 55.0 17.0
SU6656 Hs Inhibitor Inhibition 72.0 55.0 55.0
K-252a Hs Inhibitor Inhibition 74.4 75.0 41.0
isogranulatimide Hs Inhibitor Inhibition 82.3 96.0 85.0
SU11652 Hs Inhibitor Inhibition 82.8 68.0 24.0
fasudil Hs Inhibitor Inhibition 83.9 120.0 105.0
Gö 6976 Hs Inhibitor Inhibition 84.7 56.0 60.0
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. Yang Q, Deng X, Lu B, Cameron M, Fearns C, Patricelli MP, Yates 3rd JR, Gray NS, Lee JD. (2010) Pharmacological inhibition of BMK1 suppresses tumor growth through promyelocytic leukemia protein. Cancer Cell, 18 (3): 258-67. [PMID:20832753]

How to cite this page

DCAMKL family: doublecortin like kinase 2. Last modified on 29/01/2016. Accessed on 24/02/2020. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2006.