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homeodomain interacting protein kinase 3

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Target id: 2035

Nomenclature: homeodomain interacting protein kinase 3

Abbreviated Name: HIPK3

Family: HIPK subfamily

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 1215 11p13 HIPK3 homeodomain interacting protein kinase 3
Mouse - 1192 2 E2 Hipk3 homeodomain interacting protein kinase 3
Rat - 1191 3q32 Hipk3 homeodomain interacting protein kinase 3
Previous and Unofficial Names Click here for help
ANPK | DYRK6 | FIST3
Database Links Click here for help
Alphafold Q9H422 (Hs), Q9ERH7 (Mm), O88850 (Rn)
BRENDA 2.7.11.1
ChEMBL Target CHEMBL4577 (Hs)
Ensembl Gene ENSG00000110422 (Hs), ENSMUSG00000027177 (Mm), ENSRNOG00000011358 (Rn)
Entrez Gene 10114 (Hs), 15259 (Mm), 83617 (Rn)
Human Protein Atlas ENSG00000110422 (Hs)
KEGG Enzyme 2.7.11.1
KEGG Gene hsa:10114 (Hs), mmu:15259 (Mm), rno:83617 (Rn)
OMIM 604424 (Hs)
Pharos Q9H422 (Hs)
RefSeq Nucleotide NM_001048200 (Hs), NM_001145824 (Mm), NM_031787 (Rn)
RefSeq Protein NP_001041665 (Hs), NP_001139296 (Mm), NP_113975 (Rn)
UniProtKB Q9H422 (Hs), Q9ERH7 (Mm), O88850 (Rn)
Wikipedia HIPK3 (Hs)
Enzyme Reaction Click here for help
EC Number: 2.7.11.1

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
silmitasertib Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.3 pIC50 4
⤷ pIC50 7.3 (IC50 4.5x10-8 M) [4]
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: 2,5
Key to terms and symbols Click column headers to sort
Target used in screen: HIPK3
Ligand Sp. Type Action Value Parameter
AST-487 Small molecule or natural product Hs Inhibitor Inhibition 8.4 pKd
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 7.4 pKd
foretinib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.4 pKd
PHA-665752 Small molecule or natural product Hs Inhibitor Inhibition 7.2 pKd
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.1 pKd
ruboxistaurin Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.1 pKd
SU-14813 Small molecule or natural product Hs Inhibitor Inhibition 7.1 pKd
A-674563 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.0 pKd
PP-242 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.9 pKd
GSK690693 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.7 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: 1,3
Key to terms and symbols Click column headers to sort
Target used in screen: HIPK3/HIPK3
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
Gö 6976 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 29.8 31.0 28.0
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 47.3
SB 218078 Small molecule or natural product Hs Inhibitor Inhibition 49.9 -2.0 -2.0
SU11652 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 50.8 9.0 -5.0
Flt-3 inhibitor III Small molecule or natural product Hs Inhibitor Inhibition 64.8 78.0 31.0
GSK-3 inhibitor IX Small molecule or natural product Hs Inhibitor Inhibition 64.8 73.0 88.0
indirubin derivative E804 Small molecule or natural product Hs Inhibitor Inhibition 66.2 70.0 56.0
JAK3 inhibitor VI Small molecule or natural product Hs Inhibitor Inhibition 66.4 10.0 0.0
isogranulatimide Small molecule or natural product Hs Inhibitor Inhibition 66.9 61.0 42.0
JAK3 inhibitor II Small molecule or natural product Hs Inhibitor Inhibition 67.7 95.0 92.0
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. Pierre F, Chua PC, O'Brien SE, Siddiqui-Jain A, Bourbon P, Haddach M, Michaux J, Nagasawa J, Schwaebe MK, Stefan E et al.. (2011) Discovery and SAR of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the treatment of cancer. J Med Chem, 54 (2): 635-54. [PMID:21174434]

5. 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

HIPK subfamily: homeodomain interacting protein kinase 3. Last modified on 17/02/2015. Accessed on 18/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=2035.