NIMA related kinase 3 | NIMA (never in mitosis gene a)- related kinase (NEK) family | IUPHAR/BPS Guide to PHARMACOLOGY

NIMA related kinase 3

Target id: 2118

Nomenclature: NIMA related kinase 3

Abbreviated Name: NEK3

Family: NIMA (never in mitosis gene a)- related kinase (NEK) 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 NIMA related kinase 3 in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 506 13q14.2-q21.1 NEK3 NIMA related kinase 3
Mouse - 511 8 A2 Nek3 NIMA (never in mitosis gene a)-related expressed kinase 3
Rat - 468 16q12.5 Nek3 NIMA-related kinase 3
Previous and Unofficial Names
HSPK36 | phosphorylase B kinase kinase | NIMA-related kinase 3
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 25 [PMID: 17935989] Hs Inhibition <5.8 pKi 4
pKi <5.8 (Ki >1.667x10-6 M) [4]
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: 2,5

Key to terms and symbols Click column headers to sort
Target used in screen: NEK3
Ligand Sp. Type Action Affinity Units
tamatinib Hs Inhibitor Inhibition 6.8 pKd
fedratinib Hs Inhibitor Inhibition 6.2 pKd
BI-2536 Hs Inhibitor Inhibition 6.1 pKd
KW-2449 Hs Inhibitor Inhibition 6.0 pKd
ruxolitinib Hs Inhibitor Inhibition 6.0 pKd
neratinib Hs Inhibitor Inhibition 5.6 pKd
SB203580 Hs Inhibitor Inhibition <5.5 pKd
ruboxistaurin Hs Inhibitor Inhibition <5.5 pKd
erlotinib Hs Inhibitor Inhibition <5.5 pKd
GSK690693 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
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 Hs Inhibitor Inhibition 19.6 6.0 3.0
Tpl2 kinase inhibitor Hs Inhibitor Inhibition 56.0 37.0 46.0
TWS119 Hs Inhibitor Inhibition 57.5 42.0 23.0
Syk inhibitor Hs Inhibitor Inhibition 66.2 72.0 19.0
Cdk2 inhibitor IV Hs Inhibitor Inhibition 69.4 47.0 18.0
JAK inhibitor I Hs Inhibitor Inhibition 74.4 92.0 46.0
EGFR/ErbB-2/ErbB-4 inhibitor Hs Inhibitor Inhibition 76.2 107.0 84.0
GSK-3beta inhibitor VIII Hs Inhibitor Inhibition 78.6 74.0 96.0
PKR inhibitor Hs Inhibitor Inhibition 80.2 102.0 32.0
Cdc2-like kinase inhibitor 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 17/11/2018. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2118.