homeodomain interacting protein kinase 2 | HIPK subfamily | IUPHAR/BPS Guide to PHARMACOLOGY

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homeodomain interacting protein kinase 2

Target not currently curated in GtoImmuPdb

Target id: 2034

Nomenclature: homeodomain interacting protein kinase 2

Abbreviated Name: HIPK2

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 - 1198 7q32-q34 HIPK2 homeodomain interacting protein kinase 2
Mouse - 1196 6 B Hipk2 homeodomain interacting protein kinase 2
Rat - 1195 4 q22 Hipk2 homeodomain interacting protein kinase 2
Previous and Unofficial Names
Nbak1 | Nuclear body-associated kinase 1 | Stank
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
compound 5b [PMID: 24900464] Hs Inhibition >8.5 pIC50 4
pIC50 >8.5 (IC50 <3x10-9 M) [4]
compound 1a [PMID: 24900749] Hs Inhibition 7.4 pIC50 3
pIC50 7.4 (IC50 4x10-8 M) [3]
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: 2,6

Key to terms and symbols Click column headers to sort
Target used in screen: HIPK2
Ligand Sp. Type Action Value Parameter
AST-487 Hs Inhibitor Inhibition 8.1 pKd
sunitinib Hs Inhibitor Inhibition 7.5 pKd
SU-14813 Hs Inhibitor Inhibition 7.0 pKd
PHA-665752 Hs Inhibitor Inhibition 6.9 pKd
ruboxistaurin Hs Inhibitor Inhibition 6.8 pKd
staurosporine Hs Inhibitor Inhibition 6.7 pKd
foretinib Hs Inhibitor Inhibition 6.7 pKd
A-674563 Hs Inhibitor Inhibition 6.7 pKd
PI-103 Hs Inhibitor Inhibition 6.5 pKd
KW-2449 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: 1,5

Key to terms and symbols Click column headers to sort
Target used in screen: HIPK2/HIPK2
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
SU11652 Hs Inhibitor Inhibition 20.0 6.0 1.0
SB 218078 Hs Inhibitor Inhibition 32.6 42.0 26.0
sunitinib Hs Inhibitor Inhibition 41.3
JAK3 inhibitor VI Hs Inhibitor Inhibition 60.3 8.0 0.0
Cdk1/2 inhibitor III Hs Inhibitor Inhibition 62.1 12.0 0.0
dorsomorphin Hs Inhibitor Inhibition 70.8 62.0 14.0
JNJ-7706621 Hs Inhibitor Inhibition 72.8 48.0 6.0
Syk inhibitor II Hs Inhibitor Inhibition 76.4 93.0 90.0
GF109203X Hs Inhibitor Inhibition 77.5 69.0 21.0
AG 1296 Hs Inhibitor Inhibition 78.7 96.0 97.0
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. Dowling JE, Alimzhanov M, Bao L, Block MH, Chuaqui C, Cooke EL, Denz CR, Hird A, Huang S, Larsen NA et al.. (2013) Structure and Property Based Design of Pyrazolo[1,5-a]pyrimidine Inhibitors of CK2 Kinase with Activity in Vivo. ACS Med Chem Lett, 4 (8): 800-5. [PMID:24900749]

4. Dowling JE, Chuaqui C, Pontz TW, Lyne PD, Larsen NA, Block MH, Chen H, Su N, Wu A, Russell D et al.. (2012) Potent and Selective Inhibitors of CK2 Kinase Identified through Structure-Guided Hybridization. ACS Med Chem Lett, 3 (4): 278-83. [PMID:24900464]

5. 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]

6. 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 2. Last modified on 17/02/2015. Accessed on 17/09/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2034.