NIMA related kinase 11 | NIMA (never in mitosis gene a)- related kinase (NEK) family | IUPHAR/BPS Guide to PHARMACOLOGY

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NIMA related kinase 11

Target not currently curated in GtoImmuPdb

Target id: 2116

Nomenclature: NIMA related kinase 11

Abbreviated Name: NEK11

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

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 599 3q22.1 NEK11 NIMA related kinase 11
Mouse - 628 9 F1 Nek11 NIMA (never in mitosis gene a)-related expressed kinase 11
Rat - 507 8 q32 Nek11 NIMA-related kinase 11
Previous and Unofficial Names
NIMA-related kinase 11
Database Links
BRENDA
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
Pharos
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 4
pKi <5.8 (Ki >1.549x10-6 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: NEK11
Ligand Sp. Type Action Value Parameter
tamatinib Hs Inhibitor Inhibition 6.8 pKd
PLX-4720 Hs Inhibitor Inhibition 6.7 pKd
dasatinib Hs Inhibitor Inhibition 6.3 pKd
bosutinib Hs Inhibitor Inhibition 6.2 pKd
Ki-20227 Hs Inhibitor Inhibition 6.0 pKd
fedratinib Hs Inhibitor Inhibition 5.9 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: NEK11/NEK11
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
dasatinib Hs Inhibitor Inhibition 21.7
staurosporine Hs Inhibitor Inhibition 37.0 43.0 7.5
SB 218078 Hs Inhibitor Inhibition 60.6 91.0 87.0
purvalanol A Hs Inhibitor Inhibition 67.1 59.0 38.0
SKF-86002 Hs Inhibitor Inhibition 71.4 77.0 83.0
purvalanol A Hs Inhibitor Inhibition 73.6 59.0 38.0
Ro-32-0432 Hs Inhibitor Inhibition 74.1
Src kinase inhibitor I Hs Inhibitor Inhibition 74.8 100.0 105.0
PKCbeta inhibitor Hs Inhibitor Inhibition 75.6 59.0 44.0
SC-68376 Hs Inhibitor Inhibition 76.7 81.0 85.0
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 11. Last modified on 29/01/2016. Accessed on 01/06/2020. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2116.