WNK lysine deficient protein kinase 2 | Wnk family | IUPHAR/BPS Guide to PHARMACOLOGY

Top ▲

WNK lysine deficient protein kinase 2

Target not currently curated in GtoImmuPdb

Target id: 2281

Nomenclature: WNK lysine deficient protein kinase 2

Abbreviated Name: WNK2

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

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 2217 9q22.3 WNK2 WNK lysine deficient protein kinase 2
Mouse - 2059 13 B1 Wnk2 WNK lysine deficient protein kinase 2
Rat - 2063 17p14 Wnk2 WNK lysine deficient protein kinase 2
Previous and Unofficial Names
SDCCAG43, PRKWNK2 | serologically defined colon cancer antigen 43
Database Links
BRENDA
ChEMBL Target
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 Value Parameter Reference
compound 25 [PMID: 17935989] Hs Inhibition <5.8 pKi 3
pKi <5.8 (Ki >1.518x10-6 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: WNK2/WNK2
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
TGF-beta RI kinase inhibitor Hs Inhibitor Inhibition 49.2 105.0 88.0
GSK-3 inhibitor XIII Hs Inhibitor Inhibition 82.6 74.0 27.0
dasatinib Hs Inhibitor Inhibition 83.9
indirubin derivative E804 Hs Inhibitor Inhibition 85.4 71.0 40.0
isogranulatimide Hs Inhibitor Inhibition 86.6 82.0 43.0
Src kinase inhibitor I Hs Inhibitor Inhibition 88.1 92.0 41.0
Cdk2 inhibitor IV Hs Inhibitor Inhibition 88.6 96.0 48.0
BPIQ-I Hs Inhibitor Inhibition 89.7 105.0 85.0
Cdk4 inhibitor II Hs Inhibitor Inhibition 89.8 86.0 87.0
bohemine Hs Inhibitor Inhibition 90.5 98.0 89.0
Displaying the top 10 most potent ligands  View all ligands in screen »

References

Show »

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. Tao ZF, Chen Z, Bui MH, Kovar P, Johnson E, Bouska J, Zhang H, Rosenberg S, Sowin T, Lin NH. (2007) Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and preliminary pharmacokinetics. Bioorg. Med. Chem. Lett., 17 (23): 6593-601. [PMID:17935989]

How to cite this page

Wnk family: WNK lysine deficient protein kinase 2. Last modified on 16/09/2015. Accessed on 08/12/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2281.