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serine/threonine kinase 33

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Target not currently curated in GtoImmuPdb

Target id: 2221

Nomenclature: serine/threonine kinase 33

Abbreviated Name: STK33

Family: CAMK-unique family

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 514 11p15.4 STK33 serine/threonine kinase 33
Mouse - 491 7 57.21 cM Stk33 serine/threonine kinase 33
Rat - - 1 q33 Stk33 serine/threonine kinase 33
Database Links Click here for help
Alphafold Q9BYT3 (Hs), Q924X7 (Mm)
BRENDA 2.7.11.1
ChEMBL Target CHEMBL6005 (Hs)
Ensembl Gene ENSG00000130413 (Hs), ENSMUSG00000031027 (Mm), ENSRNOG00000014590 (Rn)
Entrez Gene 65975 (Hs), 117229 (Mm), 690861 (Rn)
Human Protein Atlas ENSG00000130413 (Hs)
KEGG Enzyme 2.7.11.1
KEGG Gene hsa:65975 (Hs), mmu:117229 (Mm), rno:690861 (Rn)
OMIM 607670 (Hs)
Pharos Q9BYT3 (Hs)
RefSeq Nucleotide NM_030906 (Hs), NM_054103 (Mm)
RefSeq Protein NP_112168 (Hs), NP_473444 (Mm)
UniProtKB Q9BYT3 (Hs), Q924X7 (Mm)
Wikipedia STK33 (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
compound 1 [PMID: 21742770] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.1 pIC50 2
⤷ pIC50 8.1 (IC50 7x10-9 M) [2]
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: 3,5
Key to terms and symbols Click column headers to sort
Target used in screen: STK33
Ligand Sp. Type Action Value Parameter
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.7 pKd
NVP-TAE684 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.5 pKd
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 7.8 pKd
lestaurtinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 7.6 pKd
bosutinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 7.4 pKd
GSK-1838705A Small molecule or natural product Hs Inhibitor Inhibition 7.2 pKd
foretinib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.0 pKd
SU-14813 Small molecule or natural product Hs Inhibitor Inhibition 6.9 pKd
KW-2449 Small molecule or natural product Hs Inhibitor Inhibition 6.8 pKd
midostaurin Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.7 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: STK33/STK33
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 10.7 1.0 -1.0
K-252a Small molecule or natural product Hs Inhibitor Inhibition 12.5 7.0 0.0
SB 218078 Small molecule or natural product Hs Inhibitor Inhibition 12.7 106.0 99.0
JAK3 inhibitor VI Small molecule or natural product Hs Inhibitor Inhibition 15.0 24.0 4.0
SU11652 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 20.6 33.0 6.0
indirubin derivative E804 Small molecule or natural product Hs Inhibitor Inhibition 22.3 37.0 7.0
Gö 6976 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 26.5 6.0 14.0
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 31.8
Cdk1/2 inhibitor III Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 35.1 77.0 26.0
PKR inhibitor Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 35.7 62.0 25.0
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. Babij C, Zhang Y, Kurzeja RJ, Munzli A, Shehabeldin A, Fernando M, Quon K, Kassner PD, Ruefli-Brasse AA, Watson VJ et al.. (2011) STK33 kinase activity is nonessential in KRAS-dependent cancer cells. Cancer Res, 71 (17): 5818-26. [PMID:21742770]

3. 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]

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. 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

CAMK-unique family: serine/threonine kinase 33. Last modified on 19/02/2015. Accessed on 16/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetoimmunopharmacology.org/GRAC/ObjectDisplayForward?objectId=2221.