homeodomain interacting protein kinase 3 | HIPK subfamily | IUPHAR/BPS Guide to PHARMACOLOGY

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homeodomain interacting protein kinase 3

Target not currently curated in GtoImmuPdb

Target id: 2035

Nomenclature: homeodomain interacting protein kinase 3

Abbreviated Name: HIPK3

Family: HIPK subfamily

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 - 1194 11p13 HIPK3 homeodomain interacting protein kinase 3
Mouse - 1191 2 E2 Hipk3 homeodomain interacting protein kinase 3
Rat - 1191 3 q32 Hipk3 homeodomain interacting protein kinase 3
Previous and Unofficial Names
ANPK | DYRK6 | FIST3
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: 2.7.11.1

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 Value Parameter Reference
silmitasertib Hs Inhibition 7.3 pIC50 4
pIC50 7.3 (IC50 4.5x10-8 M) [4]
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: 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 Hs Inhibitor Inhibition 8.4 pKd
sunitinib Hs Inhibitor Inhibition 7.4 pKd
foretinib Hs Inhibitor Inhibition 7.4 pKd
PHA-665752 Hs Inhibitor Inhibition 7.2 pKd
staurosporine Hs Inhibitor Inhibition 7.1 pKd
ruboxistaurin Hs Inhibitor Inhibition 7.1 pKd
SU-14813 Hs Inhibitor Inhibition 7.1 pKd
A-674563 Hs Inhibitor Inhibition 7.0 pKd
PP-242 Hs Inhibitor Inhibition 6.9 pKd
GSK690693 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
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 Hs Inhibitor Inhibition 29.8 31.0 28.0
sunitinib Hs Inhibitor Inhibition 47.3
SB 218078 Hs Inhibitor Inhibition 49.9 -2.0 -2.0
SU11652 Hs Inhibitor Inhibition 50.8 9.0 -5.0
Flt-3 inhibitor III Hs Inhibitor Inhibition 64.8 78.0 31.0
GSK-3 inhibitor IX Hs Inhibitor Inhibition 64.8 73.0 88.0
indirubin derivative E804 Hs Inhibitor Inhibition 66.2 70.0 56.0
JAK3 inhibitor VI Hs Inhibitor Inhibition 66.4 10.0 0.0
isogranulatimide Hs Inhibitor Inhibition 66.9 61.0 42.0
JAK3 inhibitor II 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 18/09/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2035.