General Information of the Protein
Protein ID
PT02178
Protein Name
LIM domain kinase 1
Gene Name
LIMK1
Secondarily
Gene Name
LIMK
Sequence
MRLTLLCCTWREERMGEEGSELPVCASCGQRIYDGQYLQALNADWHADCFRCCDCSASLSHQYYEKDGQLFCKKDYWARYGESCHGCSEQITKGLVMVAGELKYHPECFICLTCGTFIGDGDTYTLVEHSKLYCGHCYYQTVVTPVIEQILPDSPGSHLPHTVTLVSIPASSHGKRGLSVSIDPPHGPPGCGTEHSHTVRVQGVDPGCMSPDVKNSIHVGDRILEINGTPIRNVPLDEIDLLIQETSRLLQLTLEHDPHDTLGHGLGPETSPLSSPAYTPSGEAGSSARQKPVLRSCSIDRSPGAGSLGSPASQRKDLGRSESLRVVCRPHRIFRPSDLIHGEVLGKGCFGQAIKVTHRETGEVMVMKELIRFDEETQRTFLKEVKVMRCLEHPNVLKFIGVLYKDKRLNFITEYIKGGTLRGIIKSMDSQYPWSQRVSFAKDIASGMAYLHSMNIIHRDLNSHNCLVRENKNVVVADFGLARLMVDEKTQPEGLRSLKKPDRKKRYTVVGNPYWMAPEMINGRSYDEKVDVFSFGIVLCEIIGRVNADPDYLPRTMDFGLNVRGFLDRYCPPNCPPSFFPITVRCCDLDPEKRPSFVKLEHWLETLRMHLAGHLPLGPQLEQLDRGFWETYRRGESGLPAHPEVPD
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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. Acts downstream of several Rho family GTPase signal transduction pathways (PubMed:10436159, PubMed:11832213, PubMed:12807904, PubMed:15660133, PubMed:16230460, PubMed:18028908, PubMed:22328514, PubMed:23633677). Activated by upstream kinases including ROCK1, PAK1 and PAK4, which phosphorylate LIMK1 on a threonine residue located in its activation loop (PubMed:10436159). LIMK1 subsequently phosphorylates and inactivates the actin binding/depolymerizing factors cofilin-1/CFL1, cofilin-2/CFL2 and destrin/DSTN, thereby preventing the cleavage of filamentous actin (F-actin), and stabilizing the actin cytoskeleton (PubMed:11832213, PubMed:15660133, PubMed:16230460, PubMed:23633677). In this way LIMK1 regulates several actin-dependent biological processes including cell motility, cell cycle progression, and differentiation (PubMed:11832213, PubMed:15660133, PubMed:16230460, PubMed:23633677). Phosphorylates TPPP on serine residues, thereby promoting microtubule disassembly (PubMed:18028908). Stimulates axonal outgrowth and may be involved in brain development (PubMed:18028908).
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Uniprot ID
Primary ID:
P53667

Secondarily ID:
B7Z6I8
D3DXF4
D3DXF5
O15283
Q15820
Q15821
Q75MU3
Q9Y5Q1
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Ensembl ID
ENSG00000106683
HGNC ID
HGNC:6613
Subcellular Location
Cytoplasm
Nucleus
Cytoplasm
Cytoskeleton
Cell projection
Lamellipodium
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
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0495028
 Compound Info 
N-[2-[benzyl-[4-(phenylsulfamoyl)benzoyl]amino]ethyl]-2-(2-methylpropanoylamino)-1,3-thiazole-5-carboxamide
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C30H31N5O5S2
  1
1
IC50 = 9.8 nM
 Bioactivity Info 
   TI
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CP0116716
 Compound Info 
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 = 62 nM
 Bioactivity Info 
   TI
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CP0570991
 Compound Info 
N-benzyl-4-(phenylsulfamoyl)-N-prop-2-ynylbenzamide
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C23H20N2O3S
  1
1
IC50 = 65 nM
 Bioactivity Info 
   TI
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CP0543439
 Compound Info 
N-benzyl-N-[[1-[(2-chlorophenyl)methyl]triazol-4-yl]methyl]-4-(phenylsulfamoyl)benzamide
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C30H26ClN5O3S
  1
1
IC50 = 117 nM
 Bioactivity Info 
   TI
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CP0547624
 Compound Info 
N-benzyl-4-[(3-chlorophenyl)sulfamoyl]-N-prop-2-ynylbenzamide
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C23H19ClN2O3S
  1
1
IC50 = 135 nM
 Bioactivity Info 
   TI
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CP0495025
 Compound Info 
N-benzyl-N-but-3-ynyl-4-(phenylsulfamoyl)benzamide
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C24H22N2O3S
  1
1
IC50 = 158 nM
 Bioactivity Info 
   TI
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CP0495026
 Compound Info 
N-benzyl-N-[(1-benzyltriazol-4-yl)methyl]-4-(phenylsulfamoyl)benzamide
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C30H27N5O3S
  1
1
IC50 = 186 nM
 Bioactivity Info 
   TI
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CP0259778
 Compound Info 
N-benzyl-N-butyl-4-(phenylsulfamoyl)benzamide
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C24H26N2O3S
  1
1
IC50 = 238 nM
 Bioactivity Info 
   TI
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CP0561401
 Compound Info 
N-benzyl-N-(2-phenylethyl)-4-(phenylsulfamoyl)benzamide
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C28H26N2O3S
  1
1
IC50 = 251 nM
 Bioactivity Info 
   TI
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CP0527895
 Compound Info 
N-benzyl-N-[[1-[(3,4-dichlorophenyl)methyl]triazol-4-yl]methyl]-4-(phenylsulfamoyl)benzamide
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C30H25Cl2N5O3S
  1
1
IC50 = 305 nM
 Bioactivity Info 
   TI
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CP0495027
 Compound Info 
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 = 325 nM
 Bioactivity Info 
   TI
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CP0527892
 Compound Info 
N-benzyl-N-[2-(1-benzyltriazol-4-yl)ethyl]-4-(phenylsulfamoyl)benzamide
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C31H29N5O3S
  1
1
IC50 = 472 nM
 Bioactivity Info 
   TI
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CP0527893
 Compound Info 
N-benzyl-4-(phenylsulfamoyl)-N-[[1-(pyridin-4-ylmethyl)triazol-4-yl]methyl]benzamide
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C29H26N6O3S
  1
1
IC50 = 510 nM
 Bioactivity Info 
   TI
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CP0564487
 Compound Info 
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 = 1000 nM
 Bioactivity Info 
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CP0547625
 Compound Info 
N-benzyl-4-[(3-chlorophenyl)sulfamoyl]-N-(2-cyanoethyl)benzamide
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C23H20ClN3O3S
  1
1
IC50 = 1820 nM
 Bioactivity Info 
   TI
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CP0543436
 Compound Info 
N-benzyl-4-(benzylsulfamoyl)benzamide
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C21H20N2O3S
  1
1
IC50 > 25000 nM
 Bioactivity Info 
   TI
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CP0543438
 Compound Info 
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 = 35800 nM
 Bioactivity Info 
   TI
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Cell Line ID: CL000006 , HEK293
 Cell Line Info 
Cell Line ID: CL000017 , HeLa
 Cell Line Info 
Cell Line ID: CL000012 , Sf21
 Cell Line Info 
Cell Line ID: CL000013 , Sf9
 Cell Line Info 
Cell Line ID: CL000142 , ZR-75-1
 Cell Line Info 
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0495028
 Compound Info 
N-[2-[benzyl-[4-(phenylsulfamoyl)benzoyl]amino]ethyl]-2-(2-methylpropanoylamino)-1,3-thiazole-5-carboxamide
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C30H31N5O5S2
  2
1 IC50 = 1.445 nM
2 IC50 = 6.457 nM
CP0266200
 Compound Info 
(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 = 1.995 nM
2 IC50 = 3.2 nM
3 IC50 = 20.89 nM
CP0116716
 Compound Info 
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 = 6.457 nM
2 IC50 = 10 nM
3 IC50 = 70.79 nM
CP0078319
 Compound Info 
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 = 7.413 nM
2 IC50 = 245.47 nM
CP0065872
 Compound Info 
[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
  5
1 IC50 = 12.3 nM
2 IC50 = 24 nM
3 IC50 = 32 nM
4 IC50 = 54 nM
5 IC50 = 295.12 nM
CP0272823
 Compound Info 
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 = 17.78 nM
2 IC50 = 100 nM
CP0052763
 Compound Info 
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 = 43 nM
2 IC50 = 371.54 nM
3 IC50 = 2041.74 nM
CP0762159
 Compound Info 
7-[3-(2H-Tetrazol-5-yl)-phenyl]-benzo[4,5]thieno[3,2-d]pyrimidin-4-ylamine
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C17H11N7S
  1
1 IC50 = 50 nM
CP0061772
 Compound Info 
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 = 54 nM
2 IC50 = 56.23 nM
3 IC50 = 58 nM
4 IC50 = 2290.87 nM
CP0005166
 Compound Info 
BMS-354825
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C22H26ClN7O2S
  4
1 IC50 = 58.88 nM
2 IC50 = 114 nM
3 IC50 = 1023.29 nM
4 Kd = 570 nM
CP0654396
 Compound Info 
3-(4-Amino-benzo[4,5]thieno[3,2-d]pyrimidin-7-yl)-N-(2-morpholin-4-yl-2-oxo-ethyl)-benzamide
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C23H21N5O3S
  1
1 IC50 = 81 nM
CP0259778
 Compound Info 
N-benzyl-N-butyl-4-(phenylsulfamoyl)benzamide
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C24H26N2O3S
  5
1 IC50 = 83.8 nM
2 IC50 = 194.98 nM
3 IC50 = 199.53 nM
4 IC50 = 824 nM
5 Kd = 120 nM
CP0663818
 Compound Info 
1-[3-(4-Amino-benzo[4,5]thieno[3,2-d]pyrimidin-7-yl)-phenyl]-3-ethyl-urea
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C19H17N5OS
  1
1 IC50 = 87 nM
CP0654400
 Compound Info 
Pyrrolidine-1-carboxylic acid [3-(4-amino-benzo[4,5]thieno[3,2-d]pyrimidin-7-yl)-phenyl]-amid
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C21H19N5OS
  1
1 IC50 = 95 nM
CP0697136
 Compound Info 
4-Methyl-piperazine-1-carboxylic acid [3-(4-amino-benzo[4,5]thieno[3,2-d]pyrimidin-7-yl)-phenyl]-amide
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C22H22N6OS
  1
1 IC50 = 95 nM
CP0654395
 Compound Info 
3-(4-Amino-benzo[4,5]thieno[3,2-d]pyrimidin-7-yl)-N-(2-pyridin-3-yl-ethyl)-benzamide
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C24H19N5OS
  1
1 IC50 = 97 nM
CP0843120
 Compound Info 
3-(4-Amino-benzo[4,5]thieno[3,2-d]pyrimidin-7-yl)-benzamide
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C17H12N4OS
  1
1 IC50 = 120 nM
CP0035351
 Compound Info 
(S)-5-fluoro-2-(1-(4-fluorophenyl)ethylamino)-6-(5-methyl-1H-pyrazol-3-ylamino)nicotinonitrile
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C18H16F2N6
  2
1 IC50 = 151.36 nM
2 IC50 = 302 nM
CP0840908
 Compound Info 
PF-477736
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C22H25N7O2
  2
1 IC50 = 173.78 nM
2 IC50 = 812.83 nM
CP0106652
 Compound Info 
GANDOTINIB
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C23H25ClFN7O
  2
1 IC50 = 398.11 nM
2 IC50 = 1047.13 nM
CP0051782
 Compound Info 
1,4,5,6-Tetrahydropyrrolo[3,4-c]pyrazole 18
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C28H35N7O2
  2
1 IC50 = 407.38 nM
2 IC50 = 575.44 nM
CP0576920
 Compound Info 
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 = 794.33 nM
2 IC50 = 3162.28 nM
CP0116325
 Compound Info 
DAMNACANTHAL
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C16H10O5
  1
1 IC50 = 800 nM
CP0127639
 Compound Info 
Chir98014, 20
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C20H17Cl2N9O2
  1
1 IC50 > 10000 nM
CP0575646
 Compound Info 
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
 Compound Info 
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-1 (LIMK-1) )
Target Type Literature-reported Target
Similar Protein(s) and Bioactivity Statistics
90% Identity
Protein ID Protein Name Protein Organism
PT06780 LIM domain kinase 1 Rattus norvegicus, Rat
 Protein Info