NIMA related kinase 6 | NIMA (never in mitosis gene a)- related kinase (NEK) family | IUPHAR/BPS Guide to PHARMACOLOGY

NIMA related kinase 6

Target id: 2121

Nomenclature: NIMA related kinase 6

Abbreviated Name: NEK6

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 6 in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 347 9q33.3-q34.11 NEK6 NIMA related kinase 6
Mouse - 313 2 B Nek6 NIMA (never in mitosis gene a)-related expressed kinase 6
Rat - 313 3 q11 Nek6 NIMA-related kinase 6
Previous and Unofficial Names
NIMA-related kinase 6
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 22 [PMID: 20462760] Hs Inhibition - - 5
[5]
Description: Measured as % inhibition using 3μM compound.
Inhibitor Comments
3μM compound 22 [PMID 20462760] abolishes NEK6 activity [5].
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: 2,4

Key to terms and symbols Click column headers to sort
Target used in screen: NEK6
Ligand Sp. Type Action Affinity Units
tamatinib Hs Inhibitor Inhibition 8.2 pKd
fedratinib Hs Inhibitor Inhibition 6.9 pKd
KW-2449 Hs Inhibitor Inhibition 6.9 pKd
SU-14813 Hs Inhibitor Inhibition 6.2 pKd
NVP-TAE684 Hs Inhibitor Inhibition 5.9 pKd
dovitinib Hs Inhibitor Inhibition 5.8 pKd
AST-487 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
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: NEK6/NEK6
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
Cdk1/2 inhibitor III Hs Inhibitor Inhibition 78.8 89.0 44.0
JAK inhibitor I Hs Inhibitor Inhibition 82.5 85.0 103.0
tofacitinib Hs Inhibitor Inhibition 83.2
dovitinib Hs Inhibitor Inhibition 84.5
bosutinib Hs Inhibitor Inhibition 85.3
dasatinib Hs Inhibitor Inhibition 86.2
tandutinib Hs Inhibitor Inhibition 87.4
fascaplysin Hs Inhibitor Inhibition 87.8 109.0 104.0
staurosporine Hs Inhibitor Inhibition 88.6 92.0 88.0
isogranulatimide Hs Inhibitor Inhibition 88.7 98.0 90.0
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. 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]

5. Wu F, Büttner FH, Chen R, Hickey E, Jakes S, Kaplita P, Kashem MA, Kerr S, Kugler S, Paw Z et al.. (2010) Substituted 2H-isoquinolin-1-one as potent Rho-Kinase inhibitors. Part 1: Hit-to-lead account. Bioorg. Med. Chem. Lett., 20 (11): 3235-9. [PMID:20462760]

How to cite this page

NIMA (never in mitosis gene a)- related kinase (NEK) family: NIMA related kinase 6. Last modified on 29/01/2016. Accessed on 18/11/2018. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2121.