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homeodomain interacting protein kinase 1

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Target id: 2033

Nomenclature: homeodomain interacting protein kinase 1

Abbreviated Name: HIPK1

Family: HIPK subfamily

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 1210 1p13.2 HIPK1 homeodomain interacting protein kinase 1
Mouse - 1210 3 F2.2 Hipk1 homeodomain interacting protein kinase 1
Rat - 1211 2q34 Hipk1 homeodomain interacting protein kinase 1
Previous and Unofficial Names Click here for help
MYAK | NBAK2 | Nuclear body-associated kinase 2
Database Links Click here for help
Alphafold Q86Z02 (Hs), O88904 (Mm), A4L9P5 (Rn)
BRENDA 2.7.11.1
ChEMBL Target CHEMBL5427 (Hs)
Ensembl Gene ENSG00000163349 (Hs), ENSMUSG00000008730 (Mm), ENSRNOG00000019333 (Rn)
Entrez Gene 204851 (Hs), 15257 (Mm), 365895 (Rn)
Human Protein Atlas ENSG00000163349 (Hs)
KEGG Enzyme 2.7.11.1
KEGG Gene hsa:204851 (Hs), mmu:15257 (Mm), rno:365895 (Rn)
OMIM 608003 (Hs)
Pharos Q86Z02 (Hs)
RefSeq Nucleotide NM_198268 (Hs), NM_010432 (Mm), NM_001100986 (Rn)
RefSeq Protein NP_938009 (Hs), NP_034562 (Mm), NP_001094456 (Rn)
UniProtKB Q86Z02 (Hs), O88904 (Mm), A4L9P5 (Rn)
Wikipedia HIPK1 (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
staurosporine Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 5.6 pIC50 4
⤷ pIC50 5.6 (IC50 2.639x10-6 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: HIPK1
Ligand Sp. Type Action Value Parameter
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 7.3 pKd
PHA-665752 Small molecule or natural product Hs Inhibitor Inhibition 7.0 pKd
AST-487 Small molecule or natural product Hs Inhibitor Inhibition 6.8 pKd
ruboxistaurin Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.6 pKd
A-674563 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.6 pKd
PP-242 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.5 pKd
foretinib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.4 pKd
KW-2449 Small molecule or natural product Hs Inhibitor Inhibition 6.4 pKd
GSK690693 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.3 pKd
bosutinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand 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 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: HIPK1/HIPK1
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 71.3
Gö 6983 Small molecule or natural product Hs Inhibitor Inhibition 77.7 88.0 34.0
Gö 6976 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 81.1 85.0 77.0
ERK inhibitor III Small molecule or natural product Hs Inhibitor Inhibition 81.1 99.0 100.0
isogranulatimide Small molecule or natural product Hs Inhibitor Inhibition 82.6 77.0 58.0
TWS119 Small molecule or natural product Hs Inhibitor Inhibition 82.7 108.0 87.0
GSK-3 inhibitor X Small molecule or natural product Hs Inhibitor Inhibition 83.0 95.0 85.0
GSK-3 inhibitor XIII Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 84.2 95.0 35.0
JAK inhibitor I Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 88.7 84.0 98.0
Flt-3 inhibitor Small molecule or natural product 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 30/10/2025. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=2033.