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death associated protein kinase 3

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Target id: 2004

Nomenclature: death associated protein kinase 3

Abbreviated Name: DAPK3

Family: Death-associated kinase (DAPK) family

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 454 19p13.3 DAPK3 death associated protein kinase 3
Mouse - 448 10 39.72 cM Dapk3 death-associated protein kinase 3
Rat - 448 7q11 Dapk3 death-associated protein kinase 3
Previous and Unofficial Names Click here for help
DAP-like kinase | Death-associated like kinase | ZIP kinase
Database Links Click here for help
Alphafold O43293 (Hs), O54784 (Mm), O88764 (Rn)
BRENDA 2.7.11.1
ChEMBL Target CHEMBL2468 (Hs)
Ensembl Gene ENSG00000167657 (Hs), ENSMUSG00000034974 (Mm), ENSRNOG00000020383 (Rn)
Entrez Gene 1613 (Hs), 13144 (Mm), 64391 (Rn)
Human Protein Atlas ENSG00000167657 (Hs)
KEGG Enzyme 2.7.11.1
KEGG Gene hsa:1613 (Hs), mmu:13144 (Mm), rno:64391 (Rn)
OMIM 603289 (Hs)
Pharos O43293 (Hs)
RefSeq Nucleotide NM_001348 (Hs), NM_001190473 (Mm), NM_022546 (Rn)
RefSeq Protein NP_001339 (Hs), NP_001177402 (Mm), NP_071991 (Rn)
UniProtKB O43293 (Hs), O54784 (Mm), O88764 (Rn)
Wikipedia DAPK3 (Hs)
Selected 3D Structures Click here for help
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 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
silmitasertib Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.8 pIC50 7
⤷ pIC50 7.8 (IC50 1.7x10-8 M) [7]
URMC-099 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.8 pIC50 4
⤷ pIC50 6.8 (IC50 1.5x10-7 M) [4]
DAPK inhibitor 13 Small molecule or natural product Hs Inhibition 6.6 pIC50 6
⤷ pIC50 6.6 (IC50 2.53x10-7 M) [6]
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: 2,8
Key to terms and symbols Click column headers to sort
Target used in screen: DAPK3
Ligand Sp. Type Action Value Parameter
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 9.0 pKd
fedratinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 8.9 pKd
tamatinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 7.9 pKd
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 7.7 pKd
PP-242 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.4 pKd
lestaurtinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 7.1 pKd
ruxolitinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 7.1 pKd
BI-2536 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.9 pKd
SU-14813 Small molecule or natural product Hs Inhibitor Inhibition 6.8 pKd
KW-2449 Small molecule or natural product 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: 1,3
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 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 1.9 1.5 -1.0
JAK inhibitor I Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 2.2 0.0 2.0
SB 218078 Small molecule or natural product Hs Inhibitor Inhibition 24.6 80.0 78.0
K-252a Small molecule or natural product Hs Inhibitor Inhibition 27.2 12.0 2.0
isogranulatimide Small molecule or natural product Hs Inhibitor Inhibition 29.6 27.0 30.0
STO609 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 51.3 60.0 14.0
SU11652 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 54.3 44.0 17.0
GSK-3 inhibitor XIII Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 57.5 46.0 13.0
Cdk4 inhibitor Small molecule or natural product Hs Inhibitor Inhibition 62.9 102.0 91.0
indirubin derivative E804 Small molecule or natural product Hs Inhibitor Inhibition 66.6 63.0 54.0
Displaying the top 10 most potent ligands  View all ligands in screen »
Immuno Process Associations
Immuno Process:  Inflammation
Immuno Process:  Cytokine production & signalling

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 09/10/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=2004.