STE20 like kinase | SLK subfamily | IUPHAR/BPS Guide to PHARMACOLOGY

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STE20 like kinase

Target not currently curated in GtoImmuPdb

Target id: 2200

Nomenclature: STE20 like kinase

Abbreviated Name: SLK

Family: SLK subfamily

Annotation status:  image of an orange circle Annotated and awaiting review. Please contact us if you can help with reviewing.  » Email us

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 1235 10q25.1 SLK STE20 like kinase
Mouse - 1202 19 D2 Slk STE20-like kinase
Rat - 1203 1 q54 Slk STE20-like kinase
Previous and Unofficial Names
Etk4 | STE20-related kinase | STK2 | STE20-like kinase
Database Links
BRENDA
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of STE20-like kinase (unliganded form).
PDB Id:  2JFM
Resolution:  2.85Å
Species:  Human
References:  4
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of human STE20-like kinase bound to 5-amino-3-((4-(aminosulfonyl)phenyl)amino)-n-(2,6-difluorophenyl)-1h-1,2,4-triazole-1-carbothioamide.
PDB Id:  2J51
Resolution:  2.1Å
Species:  Human
References:  4
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
RN486 Hs Inhibition 7.4 pKd 6
pKd 7.4 (Kd 4.3x10-8 M) [6]
danusertib Hs Inhibition 6.2 pIC50 3
pIC50 6.2 (IC50 6.21x10-7 M) [3]
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: SLK
Ligand Sp. Type Action Value Parameter
staurosporine Hs Inhibitor Inhibition 10.6 pKd
foretinib Hs Inhibitor Inhibition 8.5 pKd
bosutinib Hs Inhibitor Inhibition 8.3 pKd
KW-2449 Hs Inhibitor Inhibition 7.9 pKd
crizotinib Hs Inhibitor Inhibition 7.7 pKd
NVP-TAE684 Hs Inhibitor Inhibition 7.7 pKd
cediranib Hs Inhibitor Inhibition 7.7 pKd
AST-487 Hs Inhibitor Inhibition 7.6 pKd
erlotinib Hs Inhibitor Inhibition 7.6 pKd
tamatinib Hs Inhibitor Inhibition 7.5 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/SLK(STK2)
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
staurosporine Hs Inhibitor Inhibition 1.8
Cdk1/2 inhibitor III Hs Inhibitor Inhibition 4.6
PDGF RTK inhibitor Hs Inhibitor Inhibition 6.2
K-252a Hs Inhibitor Inhibition 7.9
SU11274 Hs Inhibitor Inhibition 13.6
JNJ-7706621 Hs Inhibitor Inhibition 19.1
bosutinib Hs Inhibitor Inhibition 21.6
SU6656 Hs Inhibitor Inhibition 23.4
SB 218078 Hs Inhibitor Inhibition 26.0
Syk inhibitor Hs Inhibitor Inhibition 28.6
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. Fancelli D, Moll J, Varasi M, Bravo R, Artico R, Berta D, Bindi S, Cameron A, Candiani I, Cappella P et al.. (2006) 1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazoles: identification of a potent Aurora kinase inhibitor with a favorable antitumor kinase inhibition profile. J. Med. Chem., 49 (24): 7247-51. [PMID:17125279]

4. Pike AC, Rellos P, Niesen FH, Turnbull A, Oliver AW, Parker SA, Turk BE, Pearl LH, Knapp S. (2008) Activation segment dimerization: a mechanism for kinase autophosphorylation of non-consensus sites. EMBO J., 27 (4): 704-14. [PMID:18239682]

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]

6. Xu D, Kim Y, Postelnek J, Vu MD, Hu DQ, Liao C, Bradshaw M, Hsu J, Zhang J, Pashine A et al.. (2012) RN486, a selective Bruton's tyrosine kinase inhibitor, abrogates immune hypersensitivity responses and arthritis in rodents. J. Pharmacol. Exp. Ther., 341 (1): 90-103. [PMID:22228807]

How to cite this page

SLK subfamily: STE20 like kinase. Last modified on 29/01/2016. Accessed on 21/07/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2200.