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serine/threonine kinase 17a

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Target not currently curated in GtoImmuPdb

Target id: 2214

Nomenclature: serine/threonine kinase 17a

Abbreviated Name: DRAK1

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 - 414 7p13 STK17A serine/threonine kinase 17a
Previous and Unofficial Names Click here for help
death-associated protein kinase-related 1
Database Links Click here for help
Alphafold Q9UEE5 (Hs)
BRENDA 2.7.11.1
ChEMBL Target CHEMBL4525 (Hs)
Ensembl Gene ENSG00000164543 (Hs)
Entrez Gene 9263 (Hs)
Human Protein Atlas ENSG00000164543 (Hs)
KEGG Enzyme 2.7.11.1
KEGG Gene hsa:9263 (Hs)
OMIM 604726 (Hs)
Pharos Q9UEE5 (Hs)
RefSeq Nucleotide NM_004760 (Hs)
RefSeq Protein NP_004751 (Hs)
UniProtKB Q9UEE5 (Hs)
Wikipedia STK17A (Hs)
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
AT-9283 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.0 pIC50 5
⤷ pIC50 8.0 (IC50 1x10-8 M) [5]
compound 7 [PMID: 34333981] Small molecule or natural product Hs Inhibition 6.9 pIC50 3
⤷ pIC50 6.9 (IC50 1.26x10-7 M) [3]
tomivosertib Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 6.9 pIC50 7
⤷ pIC50 6.9 (IC50 1.3x10-7 M) [7]
Description: Biochemical inhibition assay.
BAY-985 Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 6.5 pIC50 6
⤷ pIC50 6.5 (IC50 3.11x10-7 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: DRAK1
Ligand Sp. Type Action Value Parameter
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 9.0 pKd
KW-2449 Small molecule or natural product Hs Inhibitor Inhibition 8.5 pKd
lestaurtinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 8.5 pKd
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.8 pKd
SU-14813 Small molecule or natural product Hs Inhibitor Inhibition 7.6 pKd
tamatinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 7.5 pKd
MLN-8054 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.7 pKd
JNJ-28312141 Small molecule or natural product Hs Inhibitor Inhibition 6.6 pKd
neratinib Small molecule or natural product Approved drug Hs Inhibitor Inhibition 6.5 pKd
BMS-387032 Small molecule or natural product Ligand has a PDB structure 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 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: 1,4
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 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 3.1 1.0 -0.5
K-252a Small molecule or natural product Hs Inhibitor Inhibition 4.1 0.0 1.0
JAK3 inhibitor VI Small molecule or natural product Hs Inhibitor Inhibition 5.2 1.0 0.0
JAK inhibitor I Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.4 0.0 0.0
PKR inhibitor Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.8 1.0 1.0
SB 218078 Small molecule or natural product Hs Inhibitor Inhibition 8.6 16.0 8.0
Cdk1/2 inhibitor III Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 11.1 1.0 4.0
SU11652 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 16.1 3.0 2.0
indirubin derivative E804 Small molecule or natural product Hs Inhibitor Inhibition 22.5 5.0 3.0
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure 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. Drewry DH, Annor-Gyamfi JK, Wells CI, Pickett JE, Dederer V, Preuss F, Mathea S, Axtman AD. (2022) Identification of Pyrimidine-Based Lead Compounds for Understudied Kinases Implicated in Driving Neurodegeneration. J Med Chem, 65 (2): 1313-1328. [PMID:34333981]

4. 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]

5. 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]

6. 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/IKKε Inhibitor. J Med Chem, 63 (2): 601-612. DOI: 10.1021/acs.jmedchem.9b01460 [PMID:31859507]

7. 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]

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: serine/threonine kinase 17a. Last modified on 08/02/2022. Accessed on 20/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2214.