CDC like kinase 3 | CLK family | IUPHAR/BPS Guide to PHARMACOLOGY

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CDC like kinase 3

Target id: 1992

Nomenclature: CDC like kinase 3

Abbreviated Name: CLK3

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 3 in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 638 15q24 CLK3 CDC like kinase 3
Mouse - 638 9 C Clk3 CDC-like kinase 3
Rat - 490 8 q24 Clk3 CDC-like kinase 3
Previous and Unofficial Names
dual specificity protein kinase CLK3
Database Links
BRENDA
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
SynPHARM
UniProtKB
Wikipedia
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  Crystal Structure of CLK3
PDB Id:  2EU9
Resolution:  1.53Å
Species:  Human
References:  2
Image of receptor 3D structure from RCSB PDB
Description:  CRYSTAL STRUCTURE OF THE HUMAN CLK3 IN COMPLEX WITH DKI
PDB Id:  2WU6
Resolution:  1.92Å
Species:  Human
References:  6
Image of receptor 3D structure from RCSB PDB
Description:  Crystal Structure of human CDC-like kinase 3 isoform in complex with leucettine L41
PDB Id:  3RAW
Ligand:  leucettine L41
Resolution:  2.09Å
Species:  Human
References:  5
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
leucettine L41 Mm Inhibition 8.4 pIC50 5
pIC50 8.4 (IC50 4.5x10-9 M) [5]
KH-CB19 Hs Inhibition 6.3 pIC50 6
pIC50 6.3 (IC50 5.3x10-7 M) [6]
compound 3b [PMID: 23454515] Mm Inhibition 6.3 pIC50 3
pIC50 6.3 (IC50 5.5x10-7 M) [3]
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: CLK3
Ligand Sp. Type Action Affinity Units
R547 Hs Inhibitor Inhibition 7.9 pKd
A-674563 Hs Inhibitor Inhibition 6.8 pKd
NVP-TAE684 Hs Inhibitor Inhibition 6.7 pKd
bosutinib Hs Inhibitor Inhibition 6.5 pKd
AT-7519 Hs Inhibitor Inhibition 6.4 pKd
BI-2536 Hs Inhibitor Inhibition 6.2 pKd
staurosporine Hs Inhibitor Inhibition 6.0 pKd
alvocidib Hs Inhibitor Inhibition 5.8 pKd
tamatinib Hs Inhibitor Inhibition 5.7 pKd
MLN-8054 Hs Inhibitor Inhibition 5.6 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: 1,7

Key to terms and symbols Click column headers to sort
Target used in screen: CLK3/CLK3
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
Cdk1/2 inhibitor III Hs Inhibitor Inhibition 4.6 -4.0 -5.0
indirubin derivative E804 Hs Inhibitor Inhibition 16.1 58.0 25.0
Gö 6976 Hs Inhibitor Inhibition 23.1 80.0 1.0
IRAK-1/4 inhibitor Hs Inhibitor Inhibition 24.1 55.0 56.0
Flt-3 inhibitor II Hs Inhibitor Inhibition 24.8 69.0 4.0
GSK-3 inhibitor XIII Hs Inhibitor Inhibition 33.8 53.0 15.0
SP600125 Hs Inhibitor Inhibition 38.6 72.0 34.0
Gö 6983 Hs Inhibitor Inhibition 43.6 59.0 45.0
EGFR/ErbB-2/ErbB-4 inhibitor Hs Inhibitor Inhibition 47.1 83.0 125.0
indirubin-3'-monoxime Hs Inhibitor Inhibition 48.2 79.0 54.0
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. Bullock AN, Das S, Debreczeni JE, Rellos P, Fedorov O, Niesen FH, Guo K, Papagrigoriou E, Amos AL, Cho S et al.. (2009) Kinase domain insertions define distinct roles of CLK kinases in SR protein phosphorylation. Structure, 17 (3): 352-62. [PMID:19278650]

3. 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]

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. Debdab M, Carreaux F, Renault S, Soundararajan M, Fedorov O, Filippakopoulos P, Lozach O, Babault L, Tahtouh T, Baratte B et al.. (2011) Leucettines, a class of potent inhibitors of cdc2-like kinases and dual specificity, tyrosine phosphorylation regulated kinases derived from the marine sponge leucettamine B: modulation of alternative pre-RNA splicing. J. Med. Chem., 54 (12): 4172-86. [PMID:21615147]

6. Fedorov O, Huber K, Eisenreich A, Filippakopoulos P, King O, Bullock AN, Szklarczyk D, Jensen LJ, Fabbro D, Trappe J et al.. (2011) Specific CLK inhibitors from a novel chemotype for regulation of alternative splicing. Chem. Biol., 18 (1): 67-76. [PMID:21276940]

7. 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]

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 3. Last modified on 29/01/2016. Accessed on 13/12/2018. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1992.