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STE20 like kinase

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Target not currently curated in GtoImmuPdb

Target id: 2200

Nomenclature: STE20 like kinase

Abbreviated Name: SLK

Family: SLK subfamily

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 1235 10q24.33-q25.1 SLK STE20 like kinase
Mouse - 1233 19 C3-D1 Slk STE20-like kinase
Rat - 1206 1q54 Slk STE20-like kinase
Previous and Unofficial Names Click here for help
Etk4 | STE20-related kinase | STK2 | STE20-like kinase
Database Links Click here for help
Alphafold Q9H2G2 (Hs), O54988 (Mm), O08815 (Rn)
BRENDA 2.7.11.1
ChEMBL Target CHEMBL4202 (Hs), CHEMBL2176844 (Mm)
Ensembl Gene ENSG00000065613 (Hs), ENSMUSG00000025060 (Mm), ENSRNOG00000011339 (Rn)
Entrez Gene 9748 (Hs), 20874 (Mm), 54308 (Rn)
Human Protein Atlas ENSG00000065613 (Hs)
KEGG Enzyme 2.7.11.1
KEGG Gene hsa:9748 (Hs), mmu:20874 (Mm), rno:54308 (Rn)
Pharos Q9H2G2 (Hs)
RefSeq Nucleotide NM_014720 (Hs), NM_001164639 (Mm), NM_019349 (Rn)
RefSeq Protein NP_055535 (Hs), NP_001158111 (Mm), NP_062222 (Rn)
UniProtKB Q9H2G2 (Hs), O54988 (Mm), O08815 (Rn)
Wikipedia SLK (Hs)
Selected 3D Structures Click here for help
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 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
RN486 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.4 pKd 6
⤷ pKd 7.4 (Kd 4.3x10-8 M) [6]
danusertib Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.2 pIC50 3
⤷ pIC50 6.2 (IC50 6.21x10-7 M) [3]
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: 2,5
Key to terms and symbols Click column headers to sort
Target used in screen: SLK
Ligand Sp. Type Action Value Parameter
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 10.6 pKd
foretinib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.5 pKd
bosutinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 8.3 pKd
KW-2449 Small molecule or natural product Hs Inhibitor Inhibition 7.9 pKd
crizotinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 7.7 pKd
NVP-TAE684 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.7 pKd
cediranib Small molecule or natural product Hs Inhibitor Inhibition 7.7 pKd
AST-487 Small molecule or natural product Hs Inhibitor Inhibition 7.6 pKd
erlotinib Small molecule or natural product Approved drug Ligand has a PDB structure 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
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/SLK(STK2)
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 1.8
Cdk1/2 inhibitor III Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 4.6
PDGF RTK inhibitor Small molecule or natural product Hs Inhibitor Inhibition 6.2
K-252a Small molecule or natural product Hs Inhibitor Inhibition 7.9
SU11274 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 13.6
JNJ-7706621 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 19.1
bosutinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 21.6
SU6656 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 23.4
SB 218078 Small molecule or natural product Hs Inhibitor Inhibition 26.0
Syk inhibitor Small molecule or natural product Immunopharmacology Ligand Hs Inhibitor Inhibition 28.6
Displaying the top 10 most potent ligands  View all ligands in screen »
Immuno Process Associations
Immuno Process:  Cytokine production & signalling

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 16/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetoimmunopharmacology.org/GRAC/ObjectDisplayForward?objectId=2200.