CDC like kinase 4 | CLK family | IUPHAR/BPS Guide to PHARMACOLOGY

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CDC like kinase 4

Target not currently curated in GtoImmuPdb

Target id: 1993

Nomenclature: CDC like kinase 4

Abbreviated Name: CLK4

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

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 481 5q35 CLK4 CDC like kinase 4
Mouse - 481 11 B1.3 Clk4 CDC like kinase 4
Rat - 301 10 q22 Clk4 CDC-like kinase 4
Previous and Unofficial Names
dual specificity protein kinase CLK4
Database Links
BRENDA
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Enzyme Reaction
EC Number: 2.7.12.1

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 Parameter Reference
compound 17 [PMID: 23642479] Hs Inhibition 8.4 pIC50 4
pIC50 8.4 (IC50 4x10-9 M) [4]
compound 3b [PMID: 23454515] Mm Inhibition 7.2 pIC50 2
pIC50 7.2 (IC50 6.1x10-8 M) [2]
ML315 Hs Inhibition 7.2 pIC50 4
pIC50 7.2 (IC50 6.8x10-8 M) [4]
kinase inhibitor 2 [PMID: 30199702] Hs Inhibition 7.1 pIC50 3
pIC50 7.1 (IC50 8.9x10-8 M) [3]
tomivosertib Hs Inhibition 6.1 pIC50 6
pIC50 6.1 (IC50 7.9x10-7 M) [6]
Description: Biochemical inhibition assay.
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: 5,7

Key to terms and symbols Click column headers to sort
Target used in screen: CLK4
Ligand Sp. Type Action Affinity Parameter
A-674563 Hs Inhibitor Inhibition 9.3 pKd
lestaurtinib Hs Inhibitor Inhibition 8.5 pKd
staurosporine Hs Inhibitor Inhibition 8.0 pKd
sunitinib Hs Inhibitor Inhibition 7.5 pKd
KW-2449 Hs Inhibitor Inhibition 7.3 pKd
GSK-1838705A Hs Inhibitor Inhibition 7.2 pKd
NVP-TAE684 Hs Inhibitor Inhibition 7.0 pKd
TG-100-115 Hs Inhibitor Inhibition 6.9 pKd
SU-14813 Hs Inhibitor Inhibition 6.6 pKd
AST-487 Hs Inhibitor Inhibition 6.5 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

Key to terms and symbols Click column headers to sort
Target used in screen: nd/CLK4
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
Cdk1/2 inhibitor III Hs Inhibitor Inhibition 1.9
dorsomorphin Hs Inhibitor Inhibition 5.7
indirubin derivative E804 Hs Inhibitor Inhibition 6.2
staurosporine Hs Inhibitor Inhibition 6.6
JAK3 inhibitor VI Hs Inhibitor Inhibition 8.9
PKR inhibitor Hs Inhibitor Inhibition 9.9
K-252a Hs Inhibitor Inhibition 10.4
aminopurvalanol A Hs Inhibitor Inhibition 16.5
SU11652 Hs Inhibitor Inhibition 16.8
Cdc2-like kinase inhibitor Hs Inhibitor Inhibition 18.5
Displaying the top 10 most potent ligands  View all ligands in screen »

References

Show »

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. Compain G, Oumata N, Clarhaut J, Péraudeau E, Renoux B, Galons H, Papot S. (2018) A β-glucuronidase-responsive albumin-binding prodrug for potential selective kinase inhibitor-based cancer chemotherapy. Eur J Med Chem, 158: 1-6. [PMID:30199702]

4. 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]

5. 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]

6. Reich SH, Sprengeler PA, Chiang GG, Appleman JR, Chen J, Clarine J, Eam B, Ernst JT, Han Q, Goel VK et al.. (2018) Structure-based Design of Pyridone-Aminal eFT508 Targeting Dysregulated Translation by Selective Mitogen-activated Protein Kinase Interacting Kinases 1 and 2 (MNK1/2) Inhibition. J. Med. Chem., 61 (8): 3516-3540. [PMID:29526098]

7. 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 4. Last modified on 10/01/2019. Accessed on 23/04/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1993.