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CDC like kinase 4

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Target id: 1993

Nomenclature: CDC like kinase 4

Abbreviated Name: CLK4

Family: CLK family

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 481 5q35.3 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 Click here for help
dual specificity protein kinase CLK4
Database Links Click here for help
Alphafold Q9HAZ1 (Hs), O35493 (Mm)
BRENDA 2.7.12.1
ChEMBL Target CHEMBL4203 (Hs), CHEMBL1075283 (Mm)
Ensembl Gene ENSG00000113240 (Hs), ENSMUSG00000020385 (Mm), ENSRNOG00000003714 (Rn)
Entrez Gene 57396 (Hs), 12750 (Mm), 287269 (Rn)
Human Protein Atlas ENSG00000113240 (Hs)
KEGG Enzyme 2.7.12.1
KEGG Gene hsa:57396 (Hs), mmu:12750 (Mm), rno:287269 (Rn)
OMIM 607969 (Hs)
Pharos Q9HAZ1 (Hs)
RefSeq Nucleotide NM_020666 (Hs), NM_007714 (Mm), NM_001013041 (Rn)
RefSeq Protein NP_065717 (Hs), NP_031740 (Mm), NP_001013059 (Rn)
UniProtKB Q9HAZ1 (Hs), O35493 (Mm)
Wikipedia CLK4 (Hs)
Enzyme Reaction Click here for help
EC Number: 2.7.12.1

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
compound 17 [PMID: 23642479] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.4 pIC50 4
⤷ pIC50 8.4 (IC50 4x10-9 M) [4]
compound 3b [PMID: 23454515] Small molecule or natural product Click here for species-specific activity table Mm Inhibition 7.2 pIC50 2
⤷ pIC50 7.2 (IC50 6.1x10-8 M) [2]
ML315 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.2 pIC50 4
⤷ pIC50 7.2 (IC50 6.8x10-8 M) [4]
kinase inhibitor 2 [PMID: 30199702] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.1 pIC50 3
⤷ pIC50 7.1 (IC50 8.9x10-8 M) [3]
tomivosertib Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand 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 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: 5,7
Key to terms and symbols Click column headers to sort
Target used in screen: CLK4
Ligand Sp. Type Action Value Parameter
A-674563 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 9.3 pKd
lestaurtinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 8.5 pKd
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.0 pKd
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 7.5 pKd
KW-2449 Small molecule or natural product Hs Inhibitor Inhibition 7.3 pKd
GSK-1838705A Small molecule or natural product Hs Inhibitor Inhibition 7.2 pKd
NVP-TAE684 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.0 pKd
TG-100-115 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.9 pKd
SU-14813 Small molecule or natural product Hs Inhibitor Inhibition 6.6 pKd
AST-487 Small molecule or natural product 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 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
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 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 1.9
dorsomorphin Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 5.7
indirubin derivative E804 Small molecule or natural product Hs Inhibitor Inhibition 6.2
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.6
JAK3 inhibitor VI Small molecule or natural product Hs Inhibitor Inhibition 8.9
PKR inhibitor Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 9.9
K-252a Small molecule or natural product Hs Inhibitor Inhibition 10.4
aminopurvalanol A Small molecule or natural product Hs Inhibitor Inhibition 16.5
SU11652 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 16.8
Cdc2-like kinase inhibitor Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 18.5
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. 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 30/09/2023. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=1993.