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homeodomain interacting protein kinase 4

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Target not currently curated in GtoImmuPdb

Target id: 2036

Nomenclature: homeodomain interacting protein kinase 4

Abbreviated Name: HIPK4

Family: HIPK subfamily

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 616 19q13.2 HIPK4 homeodomain interacting protein kinase 4
Mouse - 616 7 A3 Hipk4 homeodomain interacting protein kinase 4
Rat - 616 1q21 Hipk4 homeodomain interacting protein kinase 4
Database Links Click here for help
Alphafold Q8NE63 (Hs), Q3V016 (Mm), Q4V793 (Rn)
BRENDA 2.7.11.1
ChEMBL Target CHEMBL1075167 (Hs)
Ensembl Gene ENSG00000160396 (Hs), ENSMUSG00000040424 (Mm), ENSRNOG00000020835 (Rn)
Entrez Gene 147746 (Hs), 233020 (Mm), 308449 (Rn)
Human Protein Atlas ENSG00000160396 (Hs)
KEGG Enzyme 2.7.11.1
KEGG Gene hsa:147746 (Hs), mmu:233020 (Mm), rno:308449 (Rn)
OMIM 611712 (Hs)
Pharos Q8NE63 (Hs)
RefSeq Nucleotide NM_144685 (Hs), NM_001033315 (Mm), NM_001024776 (Rn)
RefSeq Protein NP_653286 (Hs), NP_001028487 (Mm), NP_001019947 (Rn)
UniProtKB Q8NE63 (Hs), Q3V016 (Mm), Q4V793 (Rn)
Wikipedia HIPK4 (Hs)
Enzyme Reaction Click here for help
EC Number: 2.7.11.1
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: 2-3
Key to terms and symbols Click column headers to sort
Target used in screen: HIPK4
Ligand Sp. Type Action Value Parameter
foretinib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 9.3 pKd
sorafenib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 8.5 pKd
AST-487 Small molecule or natural product Hs Inhibitor Inhibition 8.4 pKd
linifanib Small molecule or natural product Hs Inhibitor Inhibition 7.3 pKd
barasertib-hQPA Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.0 pKd
bosutinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.9 pKd
lestaurtinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.8 pKd
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 6.8 pKd
fedratinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 6.7 pKd
gefitinib Small molecule or natural product Approved drug Ligand has a PDB structure 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 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
Key to terms and symbols Click column headers to sort
Target used in screen: nd/HIPK1
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
sorafenib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 4.9
SB 218078 Small molecule or natural product Hs Inhibitor Inhibition 29.1
Cdk1/2 inhibitor III Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 50.6
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 55.3
JAK3 inhibitor VI Small molecule or natural product Hs Inhibitor Inhibition 58.7
SU11652 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 61.7
AG1478 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 64.4
K-252a Small molecule or natural product Hs Inhibitor Inhibition 65.4
JNJ-7706621 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 67.7
bosutinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 74.6
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. 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 4. Last modified on 18/08/2014. Accessed on 12/09/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2036.