serine/threonine kinase 16 | NAK family | IUPHAR/BPS Guide to PHARMACOLOGY

serine/threonine kinase 16

Target id: 2213

Nomenclature: serine/threonine kinase 16

Abbreviated Name: MPSK1

Family: NAK 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 serine/threonine kinase 16 in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 305 2q35 STK16 serine/threonine kinase 16
Mouse - 305 1 C3 Stk16 serine/threonine kinase 16
Rat - 305 9 q33 Stk16 serine/threonine kinase 16
Previous and Unofficial Names
EDPK | Embryo-Derived Protein Kinase | Krct | MPSK | myristoylated and palmitoylated serine/threonine-protein kinase | protein kinase PKL12 | TGF-beta-stimulated factor 1 | TSF-1
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 the human serine-threonine kinase 16 in complex with staurosporine.
PDB Id:  2BUJ
Ligand:  staurosporine
Resolution:  2.6Å
Species:  Human
References: 
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
STK16-IN-1 Hs Inhibition 6.5 pIC50 3
pIC50 6.5 (IC50 2.95x10-7 M) [3]
Description: In an in vitro enzymatic inhibition assay.
compound 27 [PMID: 21123062] Hs Inhibition - - 4
[4]
Description: Measured as % inhibition using 1μM compound.
Inhibitor Comments
STK16 is inhibited by 99% in the presence of 1μM compound 27 [PMID 21123062] [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: 2,5

Key to terms and symbols Click column headers to sort
Target used in screen: STK16
Ligand Sp. Type Action Affinity Units
tamatinib Hs Inhibitor Inhibition 8.8 pKd
fedratinib Hs Inhibitor Inhibition 8.2 pKd
JNJ-28312141 Hs Inhibitor Inhibition 7.7 pKd
lestaurtinib Hs Inhibitor Inhibition 7.7 pKd
KW-2449 Hs Inhibitor Inhibition 7.5 pKd
sunitinib Hs Inhibitor Inhibition 6.6 pKd
staurosporine Hs Inhibitor Inhibition 6.6 pKd
midostaurin Hs Inhibitor Inhibition 6.6 pKd
pazopanib Hs Inhibitor Inhibition 6.4 pKd
axitinib 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

Key to terms and symbols Click column headers to sort
Target used in screen: nd/STK16
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
indirubin derivative E804 Hs Inhibitor Inhibition 12.7
GSK-3 inhibitor XIII Hs Inhibitor Inhibition 24.7
PKR inhibitor Hs Inhibitor Inhibition 28.0
K-252a Hs Inhibitor Inhibition 32.0
Cdk2 inhibitor IV Hs Inhibitor Inhibition 33.6
dorsomorphin Hs Inhibitor Inhibition 40.9
Cdk1/2 inhibitor III Hs Inhibitor Inhibition 42.5
IRAK-1/4 inhibitor Hs Inhibitor Inhibition 43.7
pazopanib Hs Inhibitor Inhibition 43.8
JAK3 inhibitor VI Hs Inhibitor Inhibition 44.3
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. Liu F, Wang J, Yang X, Li B, Wu H, Qi S, Chen C, Liu X, Yu K, Wang W et al.. (2016) Discovery of a Highly Selective STK16 Kinase Inhibitor. ACS Chem. Biol., 11 (6): 1537-43. [PMID:27082499]

4. Weinberg LR, Albom MS, Angeles TS, Husten J, Lisko JG, McHugh RJ, Milkiewicz KL, Murthy S, Ott GR, Theroff JP et al.. (2011) Fused bicyclic derivatives of 2,4-diaminopyrimidine as c-Met inhibitors. Bioorg. Med. Chem. Lett., 21 (1): 164-7. [PMID:21123062]

5. 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

NAK family: serine/threonine kinase 16. Last modified on 27/10/2017. Accessed on 26/09/2018. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2213.