CDC like kinase 2

Target id: 1991

Nomenclature: CDC like kinase 2

Abbreviated Name: CLK2

Family: CLK 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 CDC like kinase 2 in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 498 1q21 CLK2 CDC like kinase 2
Mouse - 498 3 F1 Clk2 CDC-like kinase 2
Rat - 500 2 q34 Clk2 CDC-like kinase 2
Previous and Unofficial Names
dual specificity protein kinase CLK2
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:  Structure of human CDC2-like kinase 2 (CLK2)
PDB Id:  3NR9
Resolution:  2.89Å
Species:  Human
References: 
Enzyme Reaction
EC Number: 2.7.12.1

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 Affinity Units Reference
compound 17 [PMID: 23642479] Hs Inhibition 7.6 pIC50 3
pIC50 7.6 (IC50 2.3x10-8 M) [3]
Cdc2-like kinase inhibitor Mm Inhibition 6.7 pIC50 5
pIC50 6.7 (IC50 2x10-7 M) [5]
compound 3b [PMID: 23454515] Mm Inhibition 6.7 pIC50 2
pIC50 6.7 (IC50 2.1x10-7 M) [2]
ML315 Hs Inhibition 6.6 pIC50 3
pIC50 6.6 (IC50 2.31x10-7 M) [3]
Takinib Hs Inhibition 6.4 pIC50 7
pIC50 6.4 (IC50 4.3x10-7 M) [7]
View species-specific inhibitor tables
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: 4,8

Key to terms and symbols Click column headers to sort
Target used in screen: CLK2
Ligand Sp. Type Action Affinity Units
A-674563 Hs Inhibitor Inhibition 9.3 pKd
staurosporine Hs Inhibitor Inhibition 8.1 pKd
GSK-1838705A Hs Inhibitor Inhibition 7.8 pKd
sunitinib Hs Inhibitor Inhibition 7.7 pKd
TG-100-115 Hs Inhibitor Inhibition 7.4 pKd
lestaurtinib Hs Inhibitor Inhibition 7.4 pKd
R547 Hs Inhibitor Inhibition 7.1 pKd
NVP-TAE684 Hs Inhibitor Inhibition 7.1 pKd
KW-2449 Hs Inhibitor Inhibition 7.0 pKd
SU-14813 Hs Inhibitor Inhibition 6.8 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: 1,6

Key to terms and symbols Click column headers to sort
Target used in screen: CLK2/CLK2
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
JAK3 inhibitor VI Hs Inhibitor Inhibition 0.3 1.0 1.0
staurosporine Hs Inhibitor Inhibition 3.7 1.0 1.0
Cdk1/2 inhibitor III Hs Inhibitor Inhibition 3.8 -2.0 2.0
K-252a Hs Inhibitor Inhibition 4.4 1.0 4.0
SU11274 Hs Inhibitor Inhibition 5.1 7.0 2.0
PKR inhibitor Hs Inhibitor Inhibition 10.0 8.0 3.0
sunitinib Hs Inhibitor Inhibition 13.6
PKCbeta inhibitor Hs Inhibitor Inhibition 14.7 8.0 2.0
SU11652 Hs Inhibitor Inhibition 15.8 9.0 1.0
aminopurvalanol A Hs Inhibitor Inhibition 17.7 7.0 1.0
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. Burgy G, Tahtouh T, Durieu E, Foll-Josselin B, Limanton E, Meijer L, Carreaux F, Bazureau JP. (2013) Chemical synthesis and biological validation of immobilized protein kinase inhibitory Leucettines. Eur J Med Chem, 62: 728-37. [PMID:23454515]

3. Coombs TC, Tanega C, Shen M, Wang JL, Auld DS, Gerritz SW, Schoenen FJ, Thomas CJ, Aubé J. (2013) Small-molecule pyrimidine inhibitors of the cdc2-like (Clk) and dual specificity tyrosine phosphorylation-regulated (Dyrk) kinases: development of chemical probe ML315. Bioorg. Med. Chem. Lett., 23 (12): 3654-61. [PMID:23642479]

4. 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]

5. Fedorov O, Marsden B, Pogacic V, Rellos P, Müller S, Bullock AN, Schwaller J, Sundström M, Knapp S. (2007) A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. Proc. Natl. Acad. Sci. U.S.A., 104 (51): 20523-8. [PMID:18077363]

6. 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]

7. Totzke J, Gurbani D, Raphemot R, Hughes PF, Bodoor K, Carlson DA, Loiselle DR, Bera AK, Eibschutz LS, Perkins MM et al.. (2017) Takinib, a Selective TAK1 Inhibitor, Broadens the Therapeutic Efficacy of TNF-α Inhibition for Cancer and Autoimmune Disease. Cell Chem Biol, 24 (8): 1029-1039.e7. [PMID:28820959]

8. 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

CLK family: CDC like kinase 2. Last modified on 23/08/2017. Accessed on 15/07/2018. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1991.