serine/threonine kinase 17a | Death-associated kinase (DAPK) family | IUPHAR Guide to IMMUNOPHARMACOLOGY

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serine/threonine kinase 17a

Target not currently curated in GtoImmuPdb

Target id: 2214

Nomenclature: serine/threonine kinase 17a

Abbreviated Name: DRAK1

Family: Death-associated kinase (DAPK) family

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 414 7p13 STK17A serine/threonine kinase 17a
Previous and Unofficial Names
death-associated protein kinase-related 1
Database Links
BRENDA
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
Pharos
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
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
AT-9283 Hs Inhibition 8.0 pIC50 4
pIC50 8.0 (IC50 1x10-8 M) [4]
tomivosertib Hs Inhibition 6.9 pIC50 6
pIC50 6.9 (IC50 1.3x10-7 M) [6]
Description: Biochemical inhibition assay.
BAY-985 Hs Inhibition 6.5 pIC50 5
pIC50 6.5 (IC50 3.11x10-7 M) [5]
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: DRAK1
Ligand Sp. Type Action Value Parameter
sunitinib Hs Inhibitor Inhibition 9.0 pKd
KW-2449 Hs Inhibitor Inhibition 8.5 pKd
lestaurtinib Hs Inhibitor Inhibition 8.5 pKd
staurosporine Hs Inhibitor Inhibition 7.8 pKd
SU-14813 Hs Inhibitor Inhibition 7.6 pKd
tamatinib Hs Inhibitor Inhibition 7.5 pKd
MLN-8054 Hs Inhibitor Inhibition 6.7 pKd
JNJ-28312141 Hs Inhibitor Inhibition 6.6 pKd
neratinib Hs Inhibitor Inhibition 6.5 pKd
BMS-387032 Hs Inhibitor Inhibition 6.4 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: DRAK1/DRAK1(STK17A)
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
staurosporine Hs Inhibitor Inhibition 3.1 1.0 -0.5
K-252a Hs Inhibitor Inhibition 4.1 0.0 1.0
JAK3 inhibitor VI Hs Inhibitor Inhibition 5.2 1.0 0.0
JAK inhibitor I Hs Inhibitor Inhibition 6.4 0.0 0.0
PKR inhibitor Hs Inhibitor Inhibition 6.8 1.0 1.0
SB 218078 Hs Inhibitor Inhibition 8.6 16.0 8.0
Cdk1/2 inhibitor III Hs Inhibitor Inhibition 11.1 1.0 4.0
SU11652 Hs Inhibitor Inhibition 16.1 3.0 2.0
indirubin derivative E804 Hs Inhibitor Inhibition 22.5 5.0 3.0
sunitinib Hs Inhibitor Inhibition 26.7
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. Howard S, Berdini V, Boulstridge JA, Carr MG, Cross DM, Curry J, Devine LA, Early TR, Fazal L, Gill AL et al.. (2009) Fragment-based discovery of the pyrazol-4-yl urea (AT9283), a multitargeted kinase inhibitor with potent aurora kinase activity. J. Med. Chem., 52 (2): 379-88. [PMID:19143567]

5. Lefranc J, Schulze VK, Hillig RC, Briem H, Prinz F, Mengel A, Heinrich T, Balint J, Rengachari S, Irlbacher H et al.. (2020) Discovery of BAY-985, a Highly Selective TBK1/IKK╬Á Inhibitor. J. Med. Chem., 63 (2): 601-612. DOI: 10.1021/acs.jmedchem.9b01460 [PMID:31859507]

6. Reich SH, Sprengeler PA, Chiang GG, Appleman JR, Chen J, Clarine J, Eam B, Ernst JT, Han Q, Goel VK et al.. (2018) Structure-based Design of Pyridone-Aminal eFT508 Targeting Dysregulated Translation by Selective Mitogen-activated Protein Kinase Interacting Kinases 1 and 2 (MNK1/2) Inhibition. J. Med. Chem., 61 (8): 3516-3540. [PMID:29526098]

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: serine/threonine kinase 17a. Last modified on 15/01/2020. Accessed on 25/09/2020. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetoimmunopharmacology.org/GRAC/ObjectDisplayForward?objectId=2214.