histone H3 associated protein kinase | Haspin family | IUPHAR/BPS Guide to PHARMACOLOGY

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histone H3 associated protein kinase

Target not currently curated in GtoImmuPdb

Target id: 2028

Nomenclature: histone H3 associated protein kinase

Abbreviated Name: Haspin

Family: Haspin family

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 - 798 17p13 HASPIN histone H3 associated protein kinase
Mouse - 754 11 B4 Haspin histone H3 associated protein kinase
Previous and Unofficial Names
Germ cell-specific gene 2 protein | Haploid germ cell-specific nuclear protein kinase | haspin | Serine/threonine-protein kinase haspin | germ cell associated 2 (haspin) | germ cell-specific gene 2 | GSG2 | germ cell associated 2, haspin | Gsg2
Database Links
BRENDA
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of haspin kinase
PDB Id:  2WB8
Resolution:  2.15Å
Species:  Human
References:  4
Image of receptor 3D structure from RCSB PDB
Description:  Crystal Structure of Human Haspin with an Imidazo-pyridazine ligand
PDB Id:  3F2N
Resolution:  1.8Å
Species:  Human
References: 
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
SGI-1776 Hs Inhibition 7.5 pIC50 2
pIC50 7.5 (IC50 3.4x10-8 M) [2]
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: Haspin/Haspin
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
PKR inhibitor Hs Inhibitor Inhibition 5.7 3.0 1.0
staurosporine Hs Inhibitor Inhibition 6.9 1.0 2.5
PKR inhibitor, negative control Hs Inhibitor Inhibition 8.7 12.0 1.0
K-252a Hs Inhibitor Inhibition 10.2 8.0 5.0
SB 218078 Hs Inhibitor Inhibition 18.5 50.0 22.0
JAK3 inhibitor VI Hs Inhibitor Inhibition 22.5 9.0 1.0
Cdc2-like kinase inhibitor Hs Inhibitor Inhibition 25.0 17.0 4.0
Gö 6976 Hs Inhibitor Inhibition 27.2 11.0 8.0
JNK inhibitor V Hs Inhibitor Inhibition 31.0 36.0 -2.0
indirubin derivative E804 Hs Inhibitor Inhibition 32.8 13.0 11.0
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. Drygin D, Haddach M, Pierre F, Ryckman DM. (2012) Potential use of selective and nonselective Pim kinase inhibitors for cancer therapy. J. Med. Chem., 55 (19): 8199-208. [PMID:22924342]

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. Villa F, Capasso P, Tortorici M, Forneris F, de Marco A, Mattevi A, Musacchio A. (2009) Crystal structure of the catalytic domain of Haspin, an atypical kinase implicated in chromatin organization. Proc. Natl. Acad. Sci. U.S.A., 106 (48): 20204-9. [PMID:19918049]

How to cite this page

Haspin family: histone H3 associated protein kinase. Last modified on 23/05/2017. Accessed on 22/07/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2028.