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NIMA related kinase 11

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Target id: 2116

Nomenclature: NIMA related kinase 11

Abbreviated Name: NEK11

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 - 645 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 Click here for help
NIMA-related kinase 11
Database Links Click here for help
Alphafold Q8NG66 (Hs), Q8C0Q4 (Mm)
BRENDA 2.7.11.1
ChEMBL Target CHEMBL5638 (Hs)
Ensembl Gene ENSG00000114670 (Hs), ENSMUSG00000035032 (Mm), ENSRNOG00000042432 (Rn)
Entrez Gene 79858 (Hs), 208583 (Mm), 315978 (Rn)
Human Protein Atlas ENSG00000114670 (Hs)
KEGG Enzyme 2.7.11.1
KEGG Gene hsa:79858 (Hs), mmu:208583 (Mm), rno:315978 (Rn)
OMIM 609779 (Hs)
Pharos Q8NG66 (Hs)
RefSeq Nucleotide NM_001146003 (Hs), NM_172461 (Mm), NM_001108182 (Rn)
RefSeq Protein NP_001139475 (Hs), NP_766049 (Mm), NP_001101652 (Rn)
UniProtKB Q8NG66 (Hs), Q8C0Q4 (Mm)
Wikipedia NEK11 (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 >1.549x10-6 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: NEK11
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
PLX-4720 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.7 pKd
dasatinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.3 pKd
bosutinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.2 pKd
Ki-20227 Small molecule or natural product Hs Inhibitor Inhibition 6.0 pKd
fedratinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 5.9 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: NEK11/NEK11
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
dasatinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 21.7
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 37.0 43.0 7.5
SB 218078 Small molecule or natural product Hs Inhibitor Inhibition 60.6 91.0 87.0
purvalanol A Small molecule or natural product Hs Inhibitor Inhibition 67.1 59.0 38.0
SKF-86002 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 71.4 77.0 83.0
purvalanol A Small molecule or natural product Hs Inhibitor Inhibition 73.6 59.0 38.0
Ro-32-0432 Small molecule or natural product Hs Inhibitor Inhibition 74.1
Src kinase inhibitor I Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 74.8 100.0 105.0
PKCbeta inhibitor Small molecule or natural product Hs Inhibitor Inhibition 75.6 59.0 44.0
SC-68376 Small molecule or natural product 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 25/04/2025. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=2116.