death associated protein kinase 1 | Death-associated kinase (DAPK) family | IUPHAR/BPS Guide to PHARMACOLOGY

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death associated protein kinase 1

Target not currently curated in GtoImmuPdb

Target id: 2002

Nomenclature: death associated protein kinase 1

Abbreviated Name: DAPK1

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

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 1430 9q34.1 DAPK1 death associated protein kinase 1
Mouse - 1430 13 B2 Dapk1 death associated protein kinase 1
Rat - 1430 17 p14 Dapk1 death associated protein kinase 1
Previous and Unofficial Names
DAP kinase 1 | DAP-Kinase | death-associated protein kinase 1
Database Links
BRENDA
CATH/Gene3D
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
SynPHARM
UniProtKB
Wikipedia
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  1.5A X-RAY STRUCTURE OF APO FORM OF A CATALYTIC DOMAIN OF DEATH-ASSOCIATED PROTEIN KINASE
PDB Id:  1JKS
Resolution:  1.5Å
Species:  Human
References:  6
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of death associated protein kinase complexed with AMPPNP
PDB Id:  3EHA
Resolution:  1.6Å
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 Value Parameter Reference
staurosporine Hs Inhibition 9.3 pIC50 4
pIC50 9.3 (IC50 5x10-10 M) [4]
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: 2,7

Key to terms and symbols Click column headers to sort
Target used in screen: DAPK1
Ligand Sp. Type Action Value Parameter
staurosporine Hs Inhibitor Inhibition 8.9 pKd
fedratinib Hs Inhibitor Inhibition 7.8 pKd
tamatinib Hs Inhibitor Inhibition 7.3 pKd
ruxolitinib Hs Inhibitor Inhibition 7.1 pKd
lestaurtinib Hs Inhibitor Inhibition 7.1 pKd
PP-242 Hs Inhibitor Inhibition 7.0 pKd
sunitinib Hs Inhibitor Inhibition 6.9 pKd
SU-14813 Hs Inhibitor Inhibition 6.6 pKd
KW-2449 Hs Inhibitor Inhibition 6.4 pKd
BI-2536 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
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: DAPK1/DAPK1
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
JAK inhibitor I Hs Inhibitor Inhibition 3.0 8.0 3.0
staurosporine Hs Inhibitor Inhibition 3.6 6.0 0.5
isogranulatimide Hs Inhibitor Inhibition 26.6 57.0 41.0
K-252a Hs Inhibitor Inhibition 29.0 48.0 10.0
SB 218078 Hs Inhibitor Inhibition 32.7 49.0 60.0
GSK-3 inhibitor XIII Hs Inhibitor Inhibition 39.1 59.0 17.0
STO609 Hs Inhibitor Inhibition 40.9 79.0 47.0
SU11652 Hs Inhibitor Inhibition 47.7 75.0 31.0
sunitinib Hs Inhibitor Inhibition 66.9
GTP-14564 Hs Inhibitor Inhibition 71.0 94.0 98.0
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. McNamara LK, Watterson DM, Brunzelle JS. (2009) Structural insight into nucleotide recognition by human death-associated protein kinase. Acta Crystallogr. D Biol. Crystallogr., 65 (Pt 3): 241-8. [PMID:19237746]

6. Tereshko V, Teplova M, Brunzelle J, Watterson DM, Egli M. (2001) Crystal structures of the catalytic domain of human protein kinase associated with apoptosis and tumor suppression. Nat. Struct. Biol., 8 (10): 899-907. [PMID:11573098]

7. 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 1. Last modified on 30/03/2016. Accessed on 19/11/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2002.