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NIMA related kinase 3

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Target id: 2118

Nomenclature: NIMA related kinase 3

Abbreviated Name: NEK3

Family: NIMA (never in mitosis gene a)- related kinase (NEK) family

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 506 13q14.3 NEK3 NIMA related kinase 3
Mouse - 511 8 11.07 cM Nek3 NIMA (never in mitosis gene a)-related expressed kinase 3
Rat - 468 16q12.5 Nek3 NIMA-related kinase 3
Previous and Unofficial Names Click here for help
HSPK36 | phosphorylase B kinase kinase | NIMA-related kinase 3
Database Links Click here for help
Alphafold P51956 (Hs), Q9R0A5 (Mm)
BRENDA 2.7.11.1
ChEMBL Target CHEMBL5679 (Hs)
Ensembl Gene ENSG00000136098 (Hs), ENSMUSG00000031478 (Mm), ENSRNOG00000012757 (Rn)
Entrez Gene 4752 (Hs), 23954 (Mm), 306576 (Rn)
Human Protein Atlas ENSG00000136098 (Hs)
KEGG Enzyme 2.7.11.1
KEGG Gene hsa:4752 (Hs), mmu:23954 (Mm), rno:306576 (Rn)
OMIM 604044 (Hs)
Pharos P51956 (Hs)
RefSeq Nucleotide NM_002498 (Hs), NM_001162947 (Mm), XM_224971 (Rn)
RefSeq Protein NP_002489 (Hs), NP_001156419 (Mm), XP_224971 (Rn)
UniProtKB P51956 (Hs), Q9R0A5 (Mm)
Wikipedia NEK3 (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 4
⤷ pKi <5.8 (Ki >1.667x10-6 M) [4]
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: NEK3
Ligand Sp. Type Action Value Parameter
tamatinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.8 pKd
fedratinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 6.2 pKd
BI-2536 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.1 pKd
KW-2449 Small molecule or natural product Hs Inhibitor Inhibition 6.0 pKd
ruxolitinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.0 pKd
neratinib Small molecule or natural product Approved drug Hs Inhibitor Inhibition 5.6 pKd
SB203580 Small molecule or natural product Immunopharmacology Ligand Hs Inhibitor Inhibition <5.5 pKd
ruboxistaurin Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition <5.5 pKd
erlotinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition <5.5 pKd
linifanib Small molecule or natural product Hs Inhibitor Inhibition <5.5 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: 1,3
Key to terms and symbols Click column headers to sort
Target used in screen: NEK3/NEK3
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
Cdk1/2 inhibitor III Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 19.6 6.0 3.0
Tpl2 kinase inhibitor Small molecule or natural product Hs Inhibitor Inhibition 56.0 37.0 46.0
TWS119 Small molecule or natural product Hs Inhibitor Inhibition 57.5 42.0 23.0
Syk inhibitor Small molecule or natural product Immunopharmacology Ligand Hs Inhibitor Inhibition 66.2 72.0 19.0
Cdk2 inhibitor IV Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 69.4 47.0 18.0
JAK inhibitor I Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 74.4 92.0 46.0
EGFR/ErbB-2/ErbB-4 inhibitor Small molecule or natural product Hs Inhibitor Inhibition 76.2 107.0 84.0
GSK-3beta inhibitor VIII Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 78.6 74.0 96.0
PKR inhibitor Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 80.2 102.0 32.0
Cdc2-like kinase inhibitor Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 82.5 81.0 91.0
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. 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. 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]

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]

How to cite this page

NIMA (never in mitosis gene a)- related kinase (NEK) family: NIMA related kinase 3. Last modified on 29/01/2016. Accessed on 25/10/2025. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=2118.