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serine/threonine kinase 16

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Target not currently curated in GtoImmuPdb

Target id: 2213

Nomenclature: serine/threonine kinase 16

Abbreviated Name: MPSK1

Family: NAK family

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 305 2q35 STK16 serine/threonine kinase 16
Mouse - 305 1 C4 Stk16 serine/threonine kinase 16
Rat - 305 9q33 Stk16 serine/threonine kinase 16
Previous and Unofficial Names Click here for help
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 Click here for help
Alphafold O75716 (Hs), O88697 (Mm), P57760 (Rn)
BRENDA 2.7.11.1
ChEMBL Target CHEMBL3938 (Hs)
Ensembl Gene ENSG00000115661 (Hs), ENSMUSG00000026201 (Mm), ENSRNOG00000019294 (Rn)
Entrez Gene 8576 (Hs), 20872 (Mm), 286927 (Rn)
Human Protein Atlas ENSG00000115661 (Hs)
KEGG Enzyme 2.7.11.1
KEGG Gene hsa:8576 (Hs), mmu:20872 (Mm), rno:286927 (Rn)
OMIM 604719 (Hs)
Pharos O75716 (Hs)
RefSeq Nucleotide NM_003691 (Hs), NM_011494 (Mm), NM_173142 (Rn)
RefSeq Protein NP_001008910 (Hs), NP_035624 (Mm), NP_775165 (Rn)
UniProtKB O75716 (Hs), O88697 (Mm), P57760 (Rn)
Wikipedia STK16 (Hs)
Selected 3D Structures Click here for help
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 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
compound 13 [PMID: 34333981] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.1 pIC50 3
⤷ pIC50 7.1 (IC50 8.2x10-8 M) [3]
compound 6 [PMID: 34333981] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.1 pIC50 3
⤷ pIC50 7.1 (IC50 8.8x10-8 M) [3]
STK16-IN-1 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 6.5 pIC50 4
⤷ pIC50 6.5 (IC50 2.95x10-7 M) [4]
Description: In an in vitro enzymatic inhibition assay.
compound 27 [PMID: 21123062] Small molecule or natural product Click here for species-specific activity table Hs Inhibition - - 5
⤷ [5]
Description: Measured as % inhibition using 1μM compound.
Inhibitor Comments
STK16 is inhibited by 99% in the presence of 1μM compound 27 [PMID 21123062] [5].
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: 2,6
Key to terms and symbols Click column headers to sort
Target used in screen: STK16
Ligand Sp. Type Action Value Parameter
tamatinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 8.8 pKd
fedratinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 8.2 pKd
JNJ-28312141 Small molecule or natural product Hs Inhibitor Inhibition 7.7 pKd
lestaurtinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 7.7 pKd
KW-2449 Small molecule or natural product Hs Inhibitor Inhibition 7.5 pKd
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 6.6 pKd
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.6 pKd
midostaurin Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.6 pKd
pazopanib Small molecule or natural product Approved drug Hs Inhibitor Inhibition 6.4 pKd
axitinib Small molecule or natural product Approved drug 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
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 Small molecule or natural product Hs Inhibitor Inhibition 12.7
GSK-3 inhibitor XIII Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 24.7
PKR inhibitor Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 28.0
K-252a Small molecule or natural product Hs Inhibitor Inhibition 32.0
Cdk2 inhibitor IV Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 33.6
dorsomorphin Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 40.9
Cdk1/2 inhibitor III Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 42.5
IRAK-1/4 inhibitor Small molecule or natural product Immunopharmacology Ligand Hs Inhibitor Inhibition 43.7
pazopanib Small molecule or natural product Approved drug Hs Inhibitor Inhibition 43.8
JAK3 inhibitor VI Small molecule or natural product 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. 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. 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]

5. 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]

6. 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 08/02/2022. Accessed on 18/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2213.