WNK lysine deficient protein kinase 3 | Wnk family | IUPHAR/BPS Guide to PHARMACOLOGY

WNK lysine deficient protein kinase 3

Target id: 2282

Nomenclature: WNK lysine deficient protein kinase 3

Abbreviated Name: WNK3

Family: Wnk family

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

   GtoImmuPdb view: OFF :     Currently no data for WNK lysine deficient protein kinase 3 in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 1800 Xp11.22 WNK3 WNK lysine deficient protein kinase 3
Mouse - 1757 X F3 Wnk3 WNK lysine deficient protein kinase 3
Rat - 1691 Xq21 Wnk3 WNK lysine deficient protein kinase 3
Previous and Unofficial Names
PRKWNK3
Database Links
BRENDA
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
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 Affinity Units Reference
compound 2c [PMID: 24900538] Hs Inhibition 7.0 pIC50 3
pIC50 7.0 (IC50 9.98x10-8 M) [3]
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: 1-2

Key to terms and symbols Click column headers to sort
Target used in screen: WNK3/WNK3
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
K-252a Hs Inhibitor Inhibition 60.3 70.0 8.0
staurosporine Hs Inhibitor Inhibition 73.6 83.5 40.0
Flt-3 inhibitor II Hs Inhibitor Inhibition 74.6 88.0 44.0
GSK-3 inhibitor XIII Hs Inhibitor Inhibition 74.9 74.0 31.0
aminopurvalanol A Hs Inhibitor Inhibition 76.9 88.0 37.0
compound 52 [PMID: 9677190] Hs Inhibitor Inhibition 77.7 88.0 57.0
dorsomorphin Hs Inhibitor Inhibition 78.1 107.0 91.0
isogranulatimide Hs Inhibitor Inhibition 79.1 74.0 45.0
indirubin derivative E804 Hs Inhibitor Inhibition 79.7 76.0 50.0
Cdk2 inhibitor IV Hs Inhibitor Inhibition 80.6 90.0 63.0
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. 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]

3. 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]

How to cite this page

Wnk family: WNK lysine deficient protein kinase 3. Last modified on 20/02/2015. Accessed on 17/11/2018. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2282.