General Information of the Protein
Protein ID
PT01347
Protein Name
LIM domain kinase 2
Gene Name
LIMK2
Sequence
MSALAGEDVWRCPGCGDHIAPSQIWYRTVNETWHGSCFRCSECQDSLTNWYYEKDGKLYCPKDYWGKFGEFCHGCSLLMTGPFMVAGEFKYHPECFACMSCKVIIEDGDAYALVQHATLYCGKCHNEVVLAPMFERLSTESVQEQLPYSVTLISMPATTEGRRGFSVSVESACSNYATTVQVKEVNRMHISPNNRNAIHPGDRILEINGTPVRTLRVEEVEDAISQTSQTLQLLIEHDPVSQRLDQLRLEARLAPHMQNAGHPHALSTLDTKENLEGTLRRRSLRRSNSISKSPGPSSPKEPLLFSRDISRSESLRCSSSYSQQIFRPCDLIHGEVLGKGFFGQAIKVTHKATGKVMVMKELIRCDEETQKTFLTEVKVMRSLDHPNVLKFIGVLYKDKKLNLLTEYIEGGTLKDFLRSMDPFPWQQKVRFAKGIASGMAYLHSMCIIHRDLNSHNCLIKLDKTVVVADFGLSRLIVEERKRAPMEKATTKKRTLRKNDRKKRYTVVGNPYWMAPEMLNGKSYDETVDIFSFGIVLCEIIGQVYADPDCLPRTLDFGLNVKLFWEKFVPTDCPPAFFPLAAICCRLEPESRPAFSKLEDSFEALSLYLGELGIPLPAELEELDHTVSMQYGLTRDSPP
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Kinase
>
Protein Kinase
>
TKL protein kinase group
>
TKL protein kinase LISK family
>
TKL protein kinase LIMK subfamily
Function
Serine/threonine-protein kinase that plays an essential role in the regulation of actin filament dynamics (PubMed:10436159, PubMed:11018042). Acts downstream of several Rho family GTPase signal transduction pathways (PubMed:10436159, PubMed:11018042). Involved in astral microtubule organization and mitotic spindle orientation during early stages of mitosis by mediating phosphorylation of TPPP (PubMed:22328514). Displays serine/threonine-specific phosphorylation of myelin basic protein and histone (MBP) in vitro (PubMed:8537403). Suppresses ciliogenesis via multiple pathways; phosphorylation of CFL1, suppression of directional trafficking of ciliary vesicles to the ciliary base, and by facilitating YAP1 nuclear localization where it acts as a transcriptional corepressor of the TEAD4 target genes AURKA and PLK1 (PubMed:25849865).
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Uniprot ID
Primary ID:
P53671

Secondarily ID:
A8K6H5
Q7KZ80
Q7L3H5
Q96E10
Q99464
Q9UFU0
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Ensembl ID
ENSG00000182541
HGNC ID
HGNC:6614
Subcellular Location
Cytoplasm
Cytoskeleton
Spindle
Cytoplasm
Cytoskeleton
Microtubule organizing center
Centrosome
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: CL000025 , HEK-293T
Compound ID Compound Name Compound Formula
CP0495028
N-[2-[benzyl-[4-(phenylsulfamoyl)benzoyl]amino]ethyl]-2-(2-methylpropanoylamino)-1,3-thiazole-5-carboxamide
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C30H31N5O5S2
 1
1
IC50 = 13 nM
   TI
   LI
   LO
   TS
CP0116716
N-[5-[2-(2,6-dichlorophenyl)-5-(difluoromethyl)pyrazol-3-yl]-1,3-thiazol-2-yl]-2-methylpropanamide
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C17H14Cl2F2N4OS
 1
1
IC50 = 17 nM
   TI
   LI
   LO
   TS
CP0543439
N-benzyl-N-[[1-[(2-chlorophenyl)methyl]triazol-4-yl]methyl]-4-(phenylsulfamoyl)benzamide
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C30H26ClN5O3S
 1
1
IC50 = 61 nM
   TI
   LI
   LO
   TS
CP0570991
N-benzyl-4-(phenylsulfamoyl)-N-prop-2-ynylbenzamide
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C23H20N2O3S
 1
1
IC50 = 65 nM
   TI
   LI
   LO
   TS
CP0495025
N-benzyl-N-but-3-ynyl-4-(phenylsulfamoyl)benzamide
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C24H22N2O3S
 1
1
IC50 = 67 nM
   TI
   LI
   LO
   TS
CP0495026
N-benzyl-N-[(1-benzyltriazol-4-yl)methyl]-4-(phenylsulfamoyl)benzamide
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C30H27N5O3S
 1
1
IC50 = 87 nM
   TI
   LI
   LO
   TS
CP0527895
N-benzyl-N-[[1-[(3,4-dichlorophenyl)methyl]triazol-4-yl]methyl]-4-(phenylsulfamoyl)benzamide
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C30H25Cl2N5O3S
 1
1
IC50 = 90 nM
   TI
   LI
   LO
   TS
CP0259778
N-benzyl-N-butyl-4-(phenylsulfamoyl)benzamide
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C24H26N2O3S
 1
1
IC50 = 91 nM
   TI
   LI
   LO
   TS
CP0561401
N-benzyl-N-(2-phenylethyl)-4-(phenylsulfamoyl)benzamide
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C28H26N2O3S
 1
1
IC50 = 92 nM
   TI
   LI
   LO
   TS
CP0527893
N-benzyl-4-(phenylsulfamoyl)-N-[[1-(pyridin-4-ylmethyl)triazol-4-yl]methyl]benzamide
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C29H26N6O3S
 1
1
IC50 = 118 nM
   TI
   LI
   LO
   TS
CP0527892
N-benzyl-N-[2-(1-benzyltriazol-4-yl)ethyl]-4-(phenylsulfamoyl)benzamide
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C31H29N5O3S
 1
1
IC50 = 121 nM
   TI
   LI
   LO
   TS
CP0547624
N-benzyl-4-[(3-chlorophenyl)sulfamoyl]-N-prop-2-ynylbenzamide
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C23H19ClN2O3S
 1
1
IC50 = 161 nM
   TI
   LI
   LO
   TS
CP0495027
N-benzyl-N-[[1-[(2-methyl-1,3-thiazol-4-yl)methyl]triazol-4-yl]methyl]-4-(phenylsulfamoyl)benzamide
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C28H26N6O3S2
 1
1
IC50 = 323 nM
   TI
   LI
   LO
   TS
CP0547625
N-benzyl-4-[(3-chlorophenyl)sulfamoyl]-N-(2-cyanoethyl)benzamide
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C23H20ClN3O3S
 1
1
IC50 = 440 nM
   TI
   LI
   LO
   TS
CP0564487
N-benzyl-N-[[1-(imidazo[1,2-a]pyrimidin-2-ylmethyl)triazol-4-yl]methyl]-4-(phenylsulfamoyl)benzamide
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C30H26N8O3S
 1
1
IC50 = 573 nM
   TI
   LI
   LO
   TS
CP0543438
N-benzyl-N-[[1-[(2-oxo-1,3-oxazolidin-5-yl)methyl]triazol-4-yl]methyl]-4-(phenylsulfamoyl)benzamide
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C27H26N6O5S
 1
1
IC50 = 23900 nM
   TI
   LI
   LO
   TS
CP0543436
N-benzyl-4-(benzylsulfamoyl)benzamide
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C21H20N2O3S
 1
1
IC50 > 25000 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0266200
(S)-3-(2-methyl-4-(5-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperazine-1-carboxamido)phenyl dimethylcarbamate
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C22H27N7O3
 3
1 IC50 = 1.2 nM
2 IC50 = 1.82 nM
3 IC50 = 20.89 nM
CP0065872
[3-[[4-(aminomethyl)-1-(5-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carbonyl]amino]phenyl] N,N-dimethylcarbamate
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C23H29N7O3
 6
1 IC50 = 1.6 nM
2 IC50 = 4.3 nM
3 IC50 = 7.5 nM
4 IC50 = 10.72 nM
5 IC50 = 309.03 nM
6 Kd < 1000 nM
CP0495028
N-[2-[benzyl-[4-(phenylsulfamoyl)benzoyl]amino]ethyl]-2-(2-methylpropanoylamino)-1,3-thiazole-5-carboxamide
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C30H31N5O5S2
 2
1 IC50 = 5.495 nM
2 IC50 = 7.079 nM
CP0443258
(S)-N-(3-(isopropylcarbamoyl)phenyl)-2-methyl-4-(5-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperazine-1-carboxamide
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C23H29N7O2
 1
1 IC50 = 5.5 nM
CP0576920
2-benzyl-6-[(3S)-8-chloro-5-methyl-4-oxo-2,3-dihydro-1,5-benzoxazepin-3-yl]-7-oxo-4,5-dihydropyrazolo[3,4-c]pyridine-3-carboxamide
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C24H22ClN5O4
 2
1 IC50 = 6.31 nM
2 IC50 = 7.943 nM
CP0272822
N-benzyl-N-ethyl-4-(phenylsulfamoyl)benzamide
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C22H22N2O3S
 2
1 IC50 = 6.457 nM
2 IC50 = 12.59 nM
CP0550920
N-benzyl-N-(2-cyanoethyl)-4-(phenylsulfamoyl)benzamide
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C23H21N3O3S
 2
1 IC50 = 7.244 nM
2 IC50 = 8.913 nM
CP0078319
6-(2,4-dichlorophenyl)-8-ethyl-2-(3-fluoro-4-piperazin-1-ylanilino)pyrido[2,3-d]pyrimidin-7-one
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C25H23Cl2FN6O
 2
1 IC50 = 13.49 nM
2 IC50 = 512.86 nM
CP0259778
N-benzyl-N-butyl-4-(phenylsulfamoyl)benzamide
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C24H26N2O3S
 3
1 IC50 = 14.45 nM
2 IC50 = 15.49 nM
3 IC50 = 15.5 nM
CP0052763
1-(2-hydroxyethyl)-3-[4-(5-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)phenyl]-1-phenylurea
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C22H21N5O2
 3
1 IC50 = 24 nM
2 IC50 = 1905.46 nM
3 IC50 > 10000 nM
CP0272823
N-[5-[2-(2,6-dichlorophenyl)-5-(difluoromethyl)pyrazol-3-yl]-1,3-thiazol-2-yl]cyclopropanecarboxamide
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C17H12Cl2F2N4OS
 2
1 IC50 = 30.2 nM
2 IC50 = 275.42 nM
CP0116716
N-[5-[2-(2,6-dichlorophenyl)-5-(difluoromethyl)pyrazol-3-yl]-1,3-thiazol-2-yl]-2-methylpropanamide
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C17H14Cl2F2N4OS
 3
1 IC50 = 33.11 nM
2 IC50 = 85 nM
3 IC50 = 338.84 nM
CP0061772
1-ethyl-3-[5-[6-(4-methoxy-2,6-dimethylphenyl)-2-pyrazin-2-ylpyrimidin-4-yl]-1,3-thiazol-2-yl]urea
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C23H23N7O2S
 4
1 IC50 = 38 nM
2 IC50 = 134.9 nM
3 IC50 = 696 nM
4 IC50 = 707.95 nM
CP0343733
N-benzyl-N-methyl-4-[(3-methylphenyl)sulfamoyl]benzamide
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C22H22N2O3S
 2
1 IC50 = 199.53 nM
2 IC50 = 269.15 nM
CP0005166
BMS-354825
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C22H26ClN7O2S
 3
1 IC50 = 223.87 nM
2 IC50 = 1513.56 nM
3 Kd = 86 nM
CP0035351
(S)-5-fluoro-2-(1-(4-fluorophenyl)ethylamino)-6-(5-methyl-1H-pyrazol-3-ylamino)nicotinonitrile
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C18H16F2N6
 2
1 IC50 = 1949.84 nM
2 IC50 = 6606.93 nM
CP0840908
PF-477736
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C22H25N7O2
 2
1 IC50 = 3388.44 nM
2 IC50 > 10000 nM
CP0106652
GANDOTINIB
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C23H25ClFN7O
 2
1 IC50 = 6025.6 nM
2 IC50 > 10000 nM
CP0051782
1,4,5,6-Tetrahydropyrrolo[3,4-c]pyrazole 18
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C28H35N7O2
 2
1 IC50 = 7943.28 nM
2 IC50 > 10000 nM
CP0127639
Chir98014, 20
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C20H17Cl2N9O2
 1
1 IC50 > 10000 nM
CP0575646
3-methyl-N-[3-[[3-(trifluoromethyl)phenyl]carbamoyl]phenyl]-1,2-oxazole-5-carboxamide
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C19H14F3N3O3
 1
1 IC50 > 10000 nM
CP0543436
N-benzyl-4-(benzylsulfamoyl)benzamide
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C21H20N2O3S
 1
1 IC50 > 50000 nM
Clinical Information about the Protein
Target 1 ( LIM domain kinase-2 (LIMK-2) )
Target Type Literature-reported Target