death associated protein kinase 3 | Death-associated kinase (DAPK) family | IUPHAR/BPS Guide to PHARMACOLOGY

death associated protein kinase 3

Target id: 2004

Nomenclature: death associated protein kinase 3

Abbreviated Name: DAPK3

Family: Death-associated kinase (DAPK) family

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 death associated protein kinase 3 in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 454 19p13.3 DAPK3 death associated protein kinase 3
Mouse - 448 10 C1 Dapk3 death-associated protein kinase 3
Rat - 448 7 q11 Dapk3 death-associated protein kinase 3
Previous and Unofficial Names
DAP-like kinase | Death-associated like kinase | ZIP kinase
Database Links
BRENDA
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 human death associated protein kinase 3 (DAPK3) in complex with a beta-carboline ligand
PDB Id:  3BHY
Resolution:  1.24Å
Species:  Human
References:  5
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
silmitasertib Hs Inhibition 7.8 pIC50 7
pIC50 7.8 (IC50 1.7x10-8 M) [7]
URMC-099 Hs Inhibition 6.8 pIC50 4
pIC50 6.8 (IC50 1.5x10-7 M) [4]
DAPK inhibitor 13 Hs Inhibition 6.6 pIC50 6
pIC50 6.6 (IC50 2.53x10-7 M) [6]
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: 2,8

Key to terms and symbols Click column headers to sort
Target used in screen: DAPK3
Ligand Sp. Type Action Affinity Units
staurosporine Hs Inhibitor Inhibition 9.0 pKd
fedratinib Hs Inhibitor Inhibition 8.9 pKd
tamatinib Hs Inhibitor Inhibition 7.9 pKd
sunitinib Hs Inhibitor Inhibition 7.7 pKd
PP-242 Hs Inhibitor Inhibition 7.4 pKd
lestaurtinib Hs Inhibitor Inhibition 7.1 pKd
ruxolitinib Hs Inhibitor Inhibition 7.1 pKd
BI-2536 Hs Inhibitor Inhibition 6.9 pKd
SU-14813 Hs Inhibitor Inhibition 6.8 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: 1,3

Key to terms and symbols Click column headers to sort
Target used in screen: ZIPK/ZIPK(DAPK3)
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
staurosporine Hs Inhibitor Inhibition 1.9 1.5 -1.0
JAK inhibitor I Hs Inhibitor Inhibition 2.2 0.0 2.0
SB 218078 Hs Inhibitor Inhibition 24.6 80.0 78.0
K-252a Hs Inhibitor Inhibition 27.2 12.0 2.0
isogranulatimide Hs Inhibitor Inhibition 29.6 27.0 30.0
STO609 Hs Inhibitor Inhibition 51.3 60.0 14.0
SU11652 Hs Inhibitor Inhibition 54.3 44.0 17.0
GSK-3 inhibitor XIII Hs Inhibitor Inhibition 57.5 46.0 13.0
Cdk4 inhibitor Hs Inhibitor Inhibition 62.9 102.0 91.0
indirubin derivative E804 Hs Inhibitor Inhibition 66.6 63.0 54.0
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. Goodfellow VS, Loweth CJ, Ravula SB, Wiemann T, Nguyen T, Xu Y, Todd DE, Sheppard D, Pollack S, Polesskaya O et al.. (2013) Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3. J. Med. Chem., 56 (20): 8032-48. [PMID:24044867]

5. Huber K, Brault L, Fedorov O, Gasser C, Filippakopoulos P, Bullock AN, Fabbro D, Trappe J, Schwaller J, Knapp S et al.. (2012) 7,8-dichloro-1-oxo-β-carbolines as a versatile scaffold for the development of potent and selective kinase inhibitors with unusual binding modes. J. Med. Chem., 55 (1): 403-13. [PMID:22136433]

6. Okamoto M, Takayama K, Shimizu T, Muroya A, Furuya T. (2010) Structure-activity relationship of novel DAPK inhibitors identified by structure-based virtual screening. Bioorg. Med. Chem., 18 (7): 2728-34. [PMID:20206532]

7. Pierre F, Chua PC, O'Brien SE, Siddiqui-Jain A, Bourbon P, Haddach M, Michaux J, Nagasawa J, Schwaebe MK, Stefan E et al.. (2011) Discovery and SAR of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the treatment of cancer. J. Med. Chem., 54 (2): 635-54. [PMID:21174434]

8. 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

Death-associated kinase (DAPK) family: death associated protein kinase 3. Last modified on 19/01/2017. Accessed on 14/11/2018. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2004.