General Information of the Protein
Protein ID
PT01074
Protein Name
Serine/threonine-protein kinase Nek2
Secondarily
Protein Name
HSPK 21
Never in mitosis A-related kinase 2
NimA-like protein kinase 1
Gene Name
NEK2
Secondarily
Gene Name
NEK2A
NLK1
Sequence
MPSRAEDYEVLYTIGTGSYGRCQKIRRKSDGKILVWKELDYGSMTEAEKQMLVSEVNLLRELKHPNIVRYYDRIIDRTNTTLYIVMEYCEGGDLASVITKGTKERQYLDEEFVLRVMTQLTLALKECHRRSDGGHTVLHRDLKPANVFLDGKQNVKLGDFGLARILNHDTSFAKTFVGTPYYMSPEQMNRMSYNEKSDIWSLGCLLYELCALMPPFTAFSQKELAGKIREGKFRRIPYRYSDELNEIITRMLNLKDYHRPSVEEILENPLIADLVADEQRRNLERRGRQLGEPEKSQDSSPVLSELKLKEIQLQERERALKAREERLEQKEQELCVRERLAEDKLARAENLLKNYSLLKERKFLSLASNPELLNLPSSVIKKKVHFSGESKENIMRSENSESQLTSKSKCKDLKKRLHAAQLRAQALSDIEKNYQLKSRQILGMR
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Kinase
>
Protein Kinase
>
Other protein kinase group
>
Other protein kinase NEK family
Function
Protein kinase which is involved in the control of centrosome separation and bipolar spindle formation in mitotic cells and chromatin condensation in meiotic cells. Regulates centrosome separation (essential for the formation of bipolar spindles and high-fidelity chromosome separation) by phosphorylating centrosomal proteins such as CROCC, CEP250 and NINL, resulting in their displacement from the centrosomes. Regulates kinetochore microtubule attachment stability in mitosis via phosphorylation of NDC80. Involved in regulation of mitotic checkpoint protein complex via phosphorylation of CDC20 and MAD2L1. Plays an active role in chromatin condensation during the first meiotic division through phosphorylation of HMGA2. Phosphorylates: PPP1CC; SGO1; NECAB3 and NPM1. Essential for localization of MAD2L1 to kinetochore and MAPK1 and NPM1 to the centrosome. Phosphorylates CEP68 and CNTLN directly or indirectly (PubMed:24554434). NEK2-mediated phosphorylation of CEP68 promotes CEP68 dissociation from the centrosome and its degradation at the onset of mitosis (PubMed:25704143). Involved in the regulation of centrosome disjunction (PubMed:26220856). Phosphorylates CCDC102B either directly or indirectly which causes CCDC102B to dissociate from the centrosome and allows for centrosome separation (PubMed:30404835).
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Uniprot ID
Primary ID:
P51955

Secondarily ID:
Q53FD6
Q5I1Z9
Q5VXZ1
Q6NZX8
Q7Z634
Q86XH2
Q96QN9
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Ensembl ID
ENSG00000117650
HGNC ID
HGNC:7745
Subcellular Location
Nucleus
Nucleus
Nucleolus
Cytoplasm
Cytoplasm
Cytoskeleton
Microtubule organizing center
Centrosome
Cytoplasm
Cytoskeleton
Spindle pole
Chromosome
Centromere
Kinetochore
Chromosome
Centromere
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000012 , Sf21
Compound ID Compound Name Compound Formula
CP0073455
4-[7-[1-[2-(dimethylamino)ethyl]pyrazol-4-yl]imidazo[1,2-a]pyridin-3-yl]-2-[(3-fluorophenyl)methoxy]benzamide
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C28H27FN6O2
 1
1
IC50 = 1 nM
   TI
   LI
   LO
   TS
CP0370695
4-[7-[1-[2-(dimethylamino)ethyl]pyrazol-4-yl]imidazo[1,2-a]pyridin-3-yl]-2-phenylmethoxybenzamide
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C28H28N6O2
 1
1
IC50 = 3 nM
   TI
   LI
   LO
   TS
CP0513258
4-[7-[1-[2-(dimethylamino)ethyl]pyrazol-4-yl]imidazo[1,2-a]pyridin-3-yl]-2-[[3-(trifluoromethyl)phenyl]methoxy]benzamide
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C29H27F3N6O2
 1
1
IC50 = 7 nM
   TI
   LI
   LO
   TS
CP0267288
4-[7-[1-[2-(dimethylamino)ethyl]pyrazol-4-yl]imidazo[1,2-a]pyridin-3-yl]-2-[(2-fluorophenyl)methoxy]benzamide
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C28H27FN6O2
 1
1
IC50 = 87 nM
   TI
   LI
   LO
   TS
CP0492110
4-[7-[1-[2-(dimethylamino)ethyl]pyrazol-4-yl]imidazo[1,2-a]pyridin-3-yl]-2-[[4-(trifluoromethyl)phenyl]methoxy]benzamide
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C29H27F3N6O2
 1
1
IC50 = 386 nM
   TI
   LI
   LO
   TS
CP0409583
4-[7-[1-[2-(dimethylamino)ethyl]pyrazol-4-yl]imidazo[1,2-a]pyridin-3-yl]-2-[[2-(trifluoromethyl)phenyl]methoxy]benzamide
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C29H27F3N6O2
 1
1
IC50 = 478 nM
   TI
   LI
   LO
   TS
CP0476157
4-[7-(1-methylpiperidin-4-yl)oxyimidazo[1,2-a]pyridin-3-yl]-2-[(1R)-1-[2-(trifluoromethyl)phenyl]ethoxy]benzamide
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C29H29F3N4O3
 1
1
IC50 = 591 nM
   TI
   LI
   LO
   TS
CP0575501
4-[7-(1-methylpiperidin-4-yl)oxyimidazo[1,2-a]pyridin-3-yl]-2-phenylmethoxybenzamide
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C27H28N4O3
 1
1
IC50 = 808 nM
   TI
   LI
   LO
   TS
CP0541794
4-[7-(1-methylpiperidin-4-yl)oxyimidazo[1,2-a]pyridin-3-yl]-2-[[2-(trifluoromethyl)phenyl]methoxy]benzamide
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C28H27F3N4O3
 1
1
IC50 = 838 nM
   TI
   LI
   LO
   TS
CP0539210
4-[7-[1-[2-(dimethylamino)ethyl]pyrazol-4-yl]imidazo[1,2-a]pyridin-3-yl]-2-[(1R)-1-[2-(trifluoromethyl)phenyl]ethoxy]benzamide
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C30H29F3N6O2
 1
1
IC50 = 927 nM
   TI
   LI
   LO
   TS
CP0398996
tert-butyl 4-[3-[4-carbamoyl-3-[[2-(trifluoromethyl)phenyl]methoxy]phenyl]imidazo[1,2-a]pyridin-7-yl]oxypiperidine-1-carboxylate
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C32H33F3N4O5
 1
1
IC50 = 1037 nM
   TI
   LI
   LO
   TS
CP0551634
4-[7-(4-methylpiperazin-1-yl)imidazo[1,2-a]pyridin-3-yl]-2-[(1R)-1-[2-(trifluoromethyl)phenyl]ethoxy]benzamide
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C28H28F3N5O2
 1
1
IC50 = 1190 nM
   TI
   LI
   LO
   TS
CP0392000
N-(2-aminoethyl)-4-[7-(4-methylpiperazin-1-yl)imidazo[1,2-a]pyridin-3-yl]-2-[[2-(trifluoromethyl)phenyl]methoxy]benzamide
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C29H31F3N6O2
 1
1
IC50 = 1300 nM
   TI
   LI
   LO
   TS
CP0539211
4-[7-(1-methylpiperidin-4-yl)oxyimidazo[1,2-a]pyridin-3-yl]-2-[1-[2-(trifluoromethyl)phenyl]ethoxy]benzamide
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C29H29F3N4O3
 1
1
IC50 = 1600 nM
   TI
   LI
   LO
   TS
CP0541792
4-[7-(4-methylpiperazin-1-yl)imidazo[1,2-a]pyridin-3-yl]-2-[1-[2-(trifluoromethyl)phenyl]ethoxy]benzamide
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C28H28F3N5O2
 1
1
IC50 = 2170 nM
   TI
   LI
   LO
   TS
CP0541791
4-[7-(4-methylpiperazin-1-yl)imidazo[1,2-a]pyridin-3-yl]-2-[[2-(trifluoromethyl)phenyl]methoxy]benzamide
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C27H26F3N5O2
 1
1
IC50 = 2400 nM
   TI
   LI
   LO
   TS
CP0575533
4-[7-(4-methylpiperazin-1-yl)imidazo[1,2-a]pyridin-3-yl]-2-phenylmethoxybenzamide
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C26H27N5O2
 1
1
IC50 = 3210 nM
   TI
   LI
   LO
   TS
CP0478237
N-hydroxy-4-[7-(4-methylpiperazin-1-yl)imidazo[1,2-a]pyridin-3-yl]-2-[[2-(trifluoromethyl)phenyl]methoxy]benzamide
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C27H26F3N5O3
 1
1
IC50 = 10000 nM
   TI
   LI
   LO
   TS
CP0535546
4-[7-(1-methylpiperidin-4-yl)oxyimidazo[1,2-a]pyridin-3-yl]-2-[(1S)-1-[2-(trifluoromethyl)phenyl]ethoxy]benzamide
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C29H29F3N4O3
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0072678
5-(1,3-benzodioxol-5-yl)-7-[[(2R)-1-ethenylsulfonylpyrrolidin-2-yl]methyl]pyrrolo[2,3-d]pyrimidin-4-amine
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C20H21N5O4S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0478239
4-[7-(4-methylpiperazin-1-yl)imidazo[1,2-a]pyridin-3-yl]-2-[[2-(trifluoromethyl)phenyl]methoxy]benzoic acid
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C27H25F3N4O3
 1
1
IC50 = 10030 nM
   TI
   LI
   LO
   TS
CP0968789
4-(7-(piperidin-4-yloxy)imidazo[1,2-a]pyridin-3-yl)-2-(2-(trifluoromethyl)benzyloxy)benzamide 2,2,2-trifluoroacetate
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C29H26F6N4O5
 1
1
IC50 = 10030 nM
   TI
   LI
   LO
   TS
CP0492111
tert-butyl 4-[3-[4-carbamoyl-3-[(1R)-1-[2-(trifluoromethyl)phenyl]ethoxy]phenyl]imidazo[1,2-a]pyridin-7-yl]oxypiperidine-1-carboxylate
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C33H35F3N4O5
 1
1
IC50 = 11190 nM
   TI
   LI
   LO
   TS
CP0564704
2-methoxy-4-[7-(4-methylpiperazin-1-yl)imidazo[1,2-a]pyridin-3-yl]benzamide
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C20H23N5O2
 1
1
IC50 = 19280 nM
   TI
   LI
   LO
   TS
CP0541793
methyl 4-[7-(4-methylpiperazin-1-yl)imidazo[1,2-a]pyridin-3-yl]-2-[1-[2-(trifluoromethyl)phenyl]ethoxy]benzoate
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C29H29F3N4O3
 1
1
IC50 = 42600 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0092308
4-[2-amino-5-[4-[(dimethylamino)methyl]thiophen-2-yl]pyridin-3-yl]-2-[(Z,2R)-5,5,5-trifluoropent-3-en-2-yl]oxybenzamide
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C24H25F3N4O2S
 1
1 IC50 = 22 nM
CP0114044
4-[2-amino-5-[4-[(dimethylamino)methyl]thiophen-2-yl]pyridin-3-yl]-2-[(1R)-1-[2-(trifluoromethyl)phenyl]ethoxy]benzamide
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C28H27F3N4O2S
 1
1 IC50 = 37 nM
CP0642709
(Z)-N-(3-((2-Ethyl-4-methyl-1H-imidazol-5-yl)methylene)-2-oxoindolin-5-yl)propiolamide
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C18H16N4O2
 1
1 IC50 = 770 nM
Clinical Information about the Protein
Target 1 ( NIMA-related kinase 2 (NEK2) )
Target Type Literature-reported Target