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WNK lysine deficient protein kinase 2

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Target id: 2281

Nomenclature: WNK lysine deficient protein kinase 2

Abbreviated Name: WNK2

Family: Wnk family

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 2297 9q22.31 WNK2 WNK lysine deficient protein kinase 2
Mouse - 2149 13 25.07 cM Wnk2 WNK lysine deficient protein kinase 2
Rat - 2063 17p14 Wnk2 WNK lysine deficient protein kinase 2
Previous and Unofficial Names Click here for help
SDCCAG43, PRKWNK2 | serologically defined colon cancer antigen 43
Database Links Click here for help
Alphafold Q9Y3S1 (Hs), Q3UH66 (Mm)
BRENDA 2.7.11.1
ChEMBL Target CHEMBL5639 (Hs)
Ensembl Gene ENSG00000165238 (Hs), ENSMUSG00000037989 (Mm), ENSRNOG00000016684 (Rn)
Entrez Gene 65268 (Hs), 75607 (Mm), 306811 (Rn)
Human Protein Atlas ENSG00000165238 (Hs)
KEGG Enzyme 2.7.11.1
KEGG Gene hsa:65268 (Hs), mmu:75607 (Mm), rno:306811 (Rn)
OMIM 606249 (Hs)
Pharos Q9Y3S1 (Hs)
RefSeq Nucleotide NM_006648 (Hs), NM_029361 (Mm), NM_001191556 (Rn)
RefSeq Protein NP_006639 (Hs), NP_083637 (Mm), NP_001178485 (Rn)
UniProtKB Q9Y3S1 (Hs), Q3UH66 (Mm)
Wikipedia WNK2 (Hs)
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
compound 25 [PMID: 17935989] Small molecule or natural product Click here for species-specific activity table Hs Inhibition <5.8 pKi 3
⤷ pKi <5.8 (Ki >1.518x10-6 M) [3]
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: 1-2
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 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 49.2 105.0 88.0
GSK-3 inhibitor XIII Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 82.6 74.0 27.0
dasatinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 83.9
indirubin derivative E804 Small molecule or natural product Hs Inhibitor Inhibition 85.4 71.0 40.0
isogranulatimide Small molecule or natural product Hs Inhibitor Inhibition 86.6 82.0 43.0
Src kinase inhibitor I Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 88.1 92.0 41.0
Cdk2 inhibitor IV Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 88.6 96.0 48.0
BPIQ-I Small molecule or natural product Hs Inhibitor Inhibition 89.7 105.0 85.0
Cdk4 inhibitor II Small molecule or natural product Hs Inhibitor Inhibition 89.8 86.0 87.0
bohemine Small molecule or natural product Hs Inhibitor Inhibition 90.5 98.0 89.0
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. 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 02/11/2025. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=2281.