General Information of the Protein
Protein ID
PT06780
Protein Name
LIM domain kinase 1
Gene Name
LIMK1
Secondarily
Gene Name
Limk
Sequence
MRLTLLCCTWREERMGEEGSELPVCASCSQSIYDGQYLQALNADWHADCFRCCECSTSLSHQYYEKDGQLFCKKDYWARYGESCHGCSEHITKGLVMVGGELKYHPECFICLACGNFIGDGDTYTLVEHSKLYCGQCYYQTVVTPVIEQILPDSPGSHLPHTVTLVSIPASAHGKRGLSVSIDPPHGPPGCGTEHSHTVRVQGVDPGCMSPDVKNSIHIGDRILEINGTPIRNVPLDEIDLLIQETSRLLQLTLEHDPHDSLGHGPVSDPSPLASPVHTPSGQAGSSARQKPVLRSCSIDTSPGAGSLVSPASQRKDLGRSESLRVVCRPHRIFRPSDLIHGEVLGKGCFGQAIKVTHRETGEVMVMKELIRFDEETQRTFLKEVKVMRCLEHPNVLKFIGVLYKDKRLNFITEYIKGGTLRGIIKSMDSQYPWSQRVSFAKDIASGMAYLHSMNIIHRDLNSHNCLVRENRNVVVADFGLARLMIDEKGQSEDLRSLKKPDRKKRYTVVGNPYWMAPEMINGRSYDEKVDVFSFGIVLCEIIGRVNADPDYLPRTMDFGLNVRGFLDRYCPPNCPPSFFPITVRCCDLDPEKRPSFVKLEQWLETLRMHLAGHLPLGPQLEQLERGFWETYRRGESSLPAHPEVPD
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Organism
Rattus norvegicus, Rat
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. Activated by upstream kinases including ROCK1, PAK1 and PAK4, which phosphorylate LIMK1 on a threonine residue located in its activation loop. 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. In this way LIMK1 regulates several actin-dependent biological processes including cell motility, cell cycle progression, and differentiation. Phosphorylates TPPP on serine residues, thereby promoting microtubule disassembly. Stimulates axonal outgrowth and may be involved in brain development.
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Uniprot ID
P53669
Ensembl ID
ENSG00000106683
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: CL000238 , A7r5
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0089480
 Compound Info 
1-(4-chlorophenyl)-1-(2-hydroxyethyl)-3-[4-(5-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)phenyl]urea
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C22H20ClN5O2
  1
1
IC50 = 118 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0072235
 Compound Info 
1-(2-hydroxyethyl)-1-(4-methylphenyl)-3-[4-(5-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)phenyl]urea
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C23H23N5O2
  1
1
IC50 = 190 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0089476
 Compound Info 
1-(4-chlorophenyl)-3-[4-(5,6-dimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)-2-fluorophenyl]-1-(2-hydroxyethyl)urea
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C23H21ClFN5O2
  1
1
IC50 = 210 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0072228
 Compound Info 
1-(4-chlorophenyl)-3-[4-(5,6-dimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)-2-fluorophenyl]-1-(2-methoxyethyl)urea
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C24H23ClFN5O2
  1
1
IC50 = 250 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0072229
 Compound Info 
1-(4-chlorophenyl)-1-[2-(dimethylamino)ethyl]-3-[4-(5,6-dimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)-2-fluorophenyl]urea
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C25H26ClFN6O
  1
1
IC50 = 320 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0129804
 Compound Info 
1-(3-chlorophenyl)-1-(2-hydroxyethyl)-3-[4-(5-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)phenyl]urea
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C22H20ClN5O2
  1
1
IC50 = 372 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0210991
 Compound Info 
1-(2-chlorophenyl)-1-(2-hydroxyethyl)-3-[4-(5-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)phenyl]urea
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C22H20ClN5O2
  1
1
IC50 = 420 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
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
  1
1
IC50 = 470 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0071889
 Compound Info 
1-(2-hydroxyethyl)-1-(4-methoxyphenyl)-3-[4-(5-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)phenyl]urea
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C23H23N5O3
  1
1
IC50 = 730 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0072234
 Compound Info 
3-[[2-fluoro-4-(5-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)phenyl]carbamoylamino]-N-propan-2-ylbenzamide
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C24H23FN6O2
  1
1
IC50 = 4000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0058713
 Compound Info 
3-[[4-(5-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)phenyl]carbamoylamino]-N-propan-2-ylbenzamide
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C24H24N6O2
  1
1
IC50 > 1000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
Similar Protein(s) and Bioactivity Statistics
90% Identity
Protein ID Protein Name Protein Organism
PT02178 LIM domain kinase 1 Homo sapiens, Human
 Protein Info