homeodomain interacting protein kinase 1 | HIPK subfamily | IUPHAR/BPS Guide to PHARMACOLOGY

homeodomain interacting protein kinase 1

Target id: 2033

Nomenclature: homeodomain interacting protein kinase 1

Abbreviated Name: HIPK1

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

   GtoImmuPdb view: OFF :     Currently no data for homeodomain interacting protein kinase 1 in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 1210 1p13.1 HIPK1 homeodomain interacting protein kinase 1
Mouse - 1210 3 F3 Hipk1 homeodomain interacting protein kinase 1
Rat - 1211 2 q34 Hipk1 homeodomain interacting protein kinase 1
Previous and Unofficial Names
MYAK | NBAK2 | Nuclear body-associated kinase 2
Database Links
BRENDA
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 Affinity Units Reference
staurosporine Hs Inhibition 5.6 pIC50 4
pIC50 5.6 (IC50 2.639x10-6 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: HIPK1
Ligand Sp. Type Action Affinity Units
sunitinib Hs Inhibitor Inhibition 7.3 pKd
PHA-665752 Hs Inhibitor Inhibition 7.0 pKd
AST-487 Hs Inhibitor Inhibition 6.8 pKd
ruboxistaurin Hs Inhibitor Inhibition 6.6 pKd
A-674563 Hs Inhibitor Inhibition 6.6 pKd
PP-242 Hs Inhibitor Inhibition 6.5 pKd
foretinib Hs Inhibitor Inhibition 6.4 pKd
KW-2449 Hs Inhibitor Inhibition 6.4 pKd
GSK690693 Hs Inhibitor Inhibition 6.3 pKd
bosutinib Hs Inhibitor Inhibition 6.3 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: HIPK1/HIPK1
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
sunitinib Hs Inhibitor Inhibition 71.3
Gö 6983 Hs Inhibitor Inhibition 77.7 88.0 34.0
Gö 6976 Hs Inhibitor Inhibition 81.1 85.0 77.0
ERK inhibitor III Hs Inhibitor Inhibition 81.1 99.0 100.0
isogranulatimide Hs Inhibitor Inhibition 82.6 77.0 58.0
TWS119 Hs Inhibitor Inhibition 82.7 108.0 87.0
GSK-3 inhibitor X Hs Inhibitor Inhibition 83.0 95.0 85.0
GSK-3 inhibitor XIII Hs Inhibitor Inhibition 84.2 95.0 35.0
JAK inhibitor I Hs Inhibitor Inhibition 88.7 84.0 98.0
Flt-3 inhibitor Hs Inhibitor Inhibition 90.2 99.0 105.0
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. Hall MD, Salam NK, Hellawell JL, Fales HM, Kensler CB, Ludwig JA, Szakács G, Hibbs DE, Gottesman MM. (2009) Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells. J. Med. Chem., 52 (10): 3191-204. [PMID:19397322]

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 1. Last modified on 11/09/2015. Accessed on 18/11/2018. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2033.