salt inducible kinase 1 | QIK subfamily | IUPHAR/BPS Guide to PHARMACOLOGY

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salt inducible kinase 1

Target not currently curated in GtoImmuPdb

Target id: 2197

Nomenclature: salt inducible kinase 1

Abbreviated Name: SIK

Family: QIK 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 - 783 21q22.3 SIK1 salt inducible kinase 1
Mouse - 779 17 B1 Sik1 salt inducible kinase 1
Rat - 776 20 p12 Sik1 salt-inducible kinase 1
Previous and Unofficial Names
Msk | myocardial SNF1-like kinase | protein kinase KID2 | Snf1lk | SNF1LK
Database Links
BRENDA
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
Pharos
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
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
HG-9-91-01 Hs Inhibition 9.0 pIC50 1
pIC50 9.0 (IC50 9.2x10-10 M) [1]
dasatinib Hs Inhibition >8.5 pIC50 5
pIC50 >8.5 (IC50 <3x10-9 M) [5]
bosutinib Hs Inhibition >8.5 pIC50 5
pIC50 >8.5 (IC50 <3x10-9 M) [5]
compound 2c [PMID: 24900538] Hs Inhibition 8.3 pIC50 6
pIC50 8.3 (IC50 5.5x10-9 M) [6]
ARN-3236 Hs Inhibition 7.7 pIC50 4
pIC50 7.7 (IC50 2.16x10-8 M) [4]
Description: In an in vitro enzymatic assay.
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: 2,7

Key to terms and symbols Click column headers to sort
Target used in screen: SIK
Ligand Sp. Type Action Value Parameter
staurosporine Hs Inhibitor Inhibition 8.7 pKd
dasatinib Hs Inhibitor Inhibition 8.4 pKd
PD-173955 Hs Inhibitor Inhibition 8.2 pKd
NVP-TAE684 Hs Inhibitor Inhibition 7.8 pKd
bosutinib Hs Inhibitor Inhibition 7.5 pKd
fedratinib Hs Inhibitor Inhibition 7.4 pKd
tamatinib Hs Inhibitor Inhibition 7.3 pKd
lestaurtinib Hs Inhibitor Inhibition 7.1 pKd
foretinib Hs Inhibitor Inhibition 6.8 pKd
midostaurin Hs Inhibitor Inhibition 6.8 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: 3...

Key to terms and symbols Click column headers to sort
Target used in screen: SIK/nd
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
Cdk1/2 inhibitor III Hs Inhibitor Inhibition -2.0 -2.0
K-252a Hs Inhibitor Inhibition 0.0 0.0
staurosporine Hs Inhibitor Inhibition 1.0 0.0
PDGF receptor tyrosine kinase inhibitor IV Hs Inhibitor Inhibition 4.0 5.0
midostaurin Hs Inhibitor Inhibition 4.0 2.0
TWS119 Hs Inhibitor Inhibition 8.0 2.0
Gö 6976 Hs Inhibitor Inhibition 9.0 24.0
GSK-3 inhibitor IX Hs Inhibitor Inhibition 18.0 8.0
CGP74514A Hs Inhibitor Inhibition 20.0 0.0
Syk inhibitor Hs Inhibitor Inhibition 24.0 11.0
Displaying the top 10 most potent ligands  View all ligands in screen »

References

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1. Clark K, MacKenzie KF, Petkevicius K, Kristariyanto Y, Zhang J, Choi HG, Peggie M, Plater L, Pedrioli PG, McIver E et al.. (2012) Phosphorylation of CRTC3 by the salt-inducible kinases controls the interconversion of classically activated and regulatory macrophages. Proc. Natl. Acad. Sci. U.S.A., 109 (42): 16986-91. [PMID:23033494]

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. 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]

4. Lombardi MS, Gilliéron C, Dietrich D, Gabay C. (2016) SIK inhibition in human myeloid cells modulates TLR and IL-1R signaling and induces an anti-inflammatory phenotype. J. Leukoc. Biol., 99 (5): 711-21. [PMID:26590148]

5. Ozanne J, Prescott AR, Clark K. (2015) The clinically approved drugs dasatinib and bosutinib induce anti-inflammatory macrophages by inhibiting the salt-inducible kinases. Biochem. J., 465 (2): 271-9. [PMID:25351958]

6. Wang T, Lamb ML, Block MH, Davies AM, Han Y, Hoffmann E, Ioannidis S, Josey JA, Liu ZY, Lyne PD et al.. (2012) Discovery of Disubstituted Imidazo[4,5-b]pyridines and Purines as Potent TrkA Inhibitors. ACS Med Chem Lett, 3 (9): 705-9. [PMID:24900538]

7. 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

QIK subfamily: salt inducible kinase 1. Last modified on 23/05/2017. Accessed on 03/04/2020. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2197.