Information on EC 2.7.11.21 - polo kinase and Organism(s) Homo sapiens and UniProt Accession O00444

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Homo sapiens
UNIPROT: O00444


The taxonomic range for the selected organisms is: Homo sapiens

The enzyme appears in selected viruses and cellular organisms

EC NUMBER
COMMENTARY hide
2.7.11.21
-
RECOMMENDED NAME
GeneOntology No.
polo kinase
-
REACTION
REACTION DIAGRAM
COMMENTARY hide
ORGANISM
UNIPROT
LITERATURE
ATP + a protein = ADP + a phosphoprotein
show the reaction diagram
SYSTEMATIC NAME
IUBMB Comments
ATP:protein phosphotransferase (spindle-pole-dependent)
The enzyme associates with the spindle pole during mitosis and is thought to play an important role in the dynamic function of the mitotic spindle during chromosome segregation. The human form of the enzyme, Plk1, does not phosphorylate histone H1, enolase and phosvitin but it can phosphorylate myelin basic protein and microtubule-associated protein MAP-2, although to a lesser extent than casein [2].
CAS REGISTRY NUMBER
COMMENTARY hide
149433-93-2
Polo kinase
ORGANISM
COMMENTARY hide
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
-
SwissProt
Manually annotated by BRENDA team
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
malfunction
-
heterozygosity of Plk4 does not lead to polyploidization and centrosome amplification
physiological function
-
polo-like kinase 4 controls centriole duplication but does not directly regulate cytokinesis
evolution
malfunction
metabolism
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cell cycle-dependent regulation of the PBIP1-CENP-Q complex involving the enzyme, overview
physiological function
additional information
-
in Plk1, the phosphopeptide binds to a shallow cleft formed between polo box 1 (PB1) and polo box 2 (PB2), which are clamped together by the Polo-cap
SUBSTRATE
PRODUCT                       
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
ATP + TPSDSLIYDDGLS
ADP + phosphorylated TPSDSLIYDDGLS
show the reaction diagram
-
-
-
?
ATP + 20S proteasome
ADP + phosphorylated S20 proteasome
show the reaction diagram
-
phosphorylation by Plk1 enhances the proteolytic activity
-
-
?
ATP + 3F3/2 kinase
ADP + phosphorylated 3F3/2 kinase
show the reaction diagram
ATP + 53BP1
ADP + phosphorylated 53BP1
show the reaction diagram
ATP + a protein
ADP + a phosphoprotein
show the reaction diagram
ATP + alpha-casein
ADP + phosphorylated alpha-casein
show the reaction diagram
ATP + Bcl-xL
ADP + phosphorylated Bcl-xL
show the reaction diagram
-
-
-
-
?
ATP + Brd4
ADP + phosphorylated Brd4
show the reaction diagram
-
the E2 binding domain of Brd4 is phosphorylated by Plk1 in vitro
-
-
?
ATP + BubR1
ADP + phosphorylated BubR1
show the reaction diagram
ATP + casein
ADP + phosphocasein
show the reaction diagram
-
substrate in biochemical activity assay
-
-
?
ATP + casein
ADP + phosphorylated casein
show the reaction diagram
ATP + casein
ATP + phosphorylated casein
show the reaction diagram
-
-
-
-
?
ATP + Cdc14A
ADP + phosphorylated Cdc14A
show the reaction diagram
-
-
-
-
?
ATP + Cdc25A
ADP + phosphorylated Cdc25A
show the reaction diagram
-
-
-
-
?
ATP + Cdc25C
ADP + phosphorylated Cdc25
show the reaction diagram
-
-
-
-
?
ATP + Cdc25C
ADP + phosphorylated Cdc25C
show the reaction diagram
ATP + CENP-Q
ADP + phosphorylated CENP-Q
show the reaction diagram
ATP + centromeric protein PBIP1
ADP + phosphorylated centromeric protein PBIP1
show the reaction diagram
-
Plk1 phosphorylates PBIP1 at T78, GST-PBIPtide is used as in vitro substrate
-
-
?
ATP + Chk2
ADP + phosphorylated Chk2
show the reaction diagram
ATP + cJun peptide
ADP + phosphorylated cJun peptide
show the reaction diagram
strong preference of PLK1 versus PLK2 and PLK3
-
-
?
ATP + CLASP
ADP + phosphorylated CLASP
show the reaction diagram
-
-
-
-
?
ATP + cyclin B
ADP + phosphorylated cyclin B
show the reaction diagram
ATP + Ect2
ADP + phosphorylated Ect2
show the reaction diagram
-
-
-
-
?
ATP + gammaBD of IKKbeta
ADP + phosphorylated gammaBD of IKKbeta
show the reaction diagram
-
Plk1 phosphorylates serines 733, 740 and 750 in the IKKgammaNEMO-binding domain, gammaBD, of IKKbeta
-
-
?
ATP + giantin
ADP + phosphorylated giantin
show the reaction diagram
-
-
-
-
?
ATP + Hice1 subunit of Augmin complex
ADP + phosphorylated Hice1 subunit of Augmin complex
show the reaction diagram
ATP + histone H1
ADP + phosphorylated histone H1
show the reaction diagram
-
substrate used in kinase assay
-
-
?
ATP + HsCdc14A
ADP + phosphorylated HsCdc14A
show the reaction diagram
-
HsCdc14A binds to PLK1 via its C-terminus, phosphorylation partially releases the auto-inhibition of HsCdc14A, PLK1-mediated phospho-regulation promotes HsCdc14A phosphatase activity
-
-
?
ATP + kinesin-like protein 2
ADP + phosphorylated kinesin-like protein 2
show the reaction diagram
ATP + Mad1
ADP + phosphorylated Mad1
show the reaction diagram
-
the results suggest that Plk1 is influential of Mad1 phosphorylation, Mad1, mitotic arrest deficiency protein 1
-
-
?
ATP + MEX-5
ADP + phosphorylated MEX-5
show the reaction diagram
-
-
-
-
?
ATP + mitotic centromere-associated kinesin
ADP + phosphorylated mitotic centromere-associated kinesin
show the reaction diagram
ATP + Myt1
ADP + phosphorylated Myt1
show the reaction diagram
ATP + NudC
ADP + phosphorylated kinesin-like protein 2
show the reaction diagram
-
i.e. nuclear distribution protein C, Plk1 phosphorylates Ser274 and Ser326
-
-
?
ATP + p125
ADP + phosphorylated p125
show the reaction diagram
ATP + p53
ADP + phosphorylated p53
show the reaction diagram
ATP + PBIP1
ADP + phosphorylated PBIP1
show the reaction diagram
ATP + Pin1
ADP + phosphorylated Pin1
show the reaction diagram
ATP + Plk1 polo box 1-derived peptide
ADP + phosphorylated Plk1 polo box 1-derived peptide
show the reaction diagram
-
synthetic substrate
-
-
?
ATP + PLKtide
ADP + phosphorylated PLKtide
show the reaction diagram
ATP + protein
ADP + phosphoprotein
show the reaction diagram
ATP + protein MAVS
ADP + phosphorylated protein MAVS
show the reaction diagram
-
phosphorylation of the mitochondria-bound adapter protein MAVS, MAVS, mitochondrial antiviral signaling
-
-
?
ATP + SCC1 cohesin
ADP + phosphorylated SCC1 cohesin
show the reaction diagram
-
-
-
-
?
ATP + SCFFbw7 ubiquitin ligase
ADP + phosphorylated SCFFbw7 ubiquitin ligase
show the reaction diagram
-
-
-
-
?
ATP + SYK tyrosine kinase
ADP + phosphorylated SYK tyrosine kinase
show the reaction diagram
-
-
-
-
?
ATP + viral phosphoprotein P
ADP + phosphorylated viral phosphoprotein P
show the reaction diagram
-
PLK1 directly phosphorylates viral phosphoprotein P of paramyxovirus in vitro
-
-
?
additional information
?
-
NATURAL SUBSTRATES
NATURAL PRODUCTS
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
ATP + 20S proteasome
ADP + phosphorylated S20 proteasome
show the reaction diagram
-
phosphorylation by Plk1 enhances the proteolytic activity
-
-
?
ATP + 3F3/2 kinase
ADP + phosphorylated 3F3/2 kinase
show the reaction diagram
-
the enzyme creates the 3F3/2 kinase phosphoepitope on mitotic kinetichores, depletion of enzyme in M phase cell extract leads to loss of 3F3/2 kinase activity
-
-
?
ATP + 53BP1
ADP + phosphorylated 53BP1
show the reaction diagram
-
53BP1 is phosphorylated by Plk1 in mitosis
-
-
?
ATP + a protein
ADP + a phosphoprotein
show the reaction diagram
ATP + BubR1
ADP + phosphorylated BubR1
show the reaction diagram
ATP + casein
ADP + phosphorylated casein
show the reaction diagram
-
kinase assay
-
-
?
ATP + Cdc25C
ADP + phosphorylated Cdc25C
show the reaction diagram
ATP + CENP-Q
ADP + phosphorylated CENP-Q
show the reaction diagram
-
-
-
-
?
ATP + Chk2
ADP + phosphorylated Chk2
show the reaction diagram
ATP + CLASP
ADP + phosphorylated CLASP
show the reaction diagram
-
-
-
-
?
ATP + cyclin B
ADP + phosphorylated cyclin B
show the reaction diagram
-
phosphorylation at S126, S128, S133, and S147 for nuclear translocation of cyclin B
-
-
?
ATP + giantin
ADP + phosphorylated giantin
show the reaction diagram
-
-
-
-
?
ATP + Hice1 subunit of Augmin complex
ADP + phosphorylated Hice1 subunit of Augmin complex
show the reaction diagram
-
via the formation of the Nedd1-Plk1 complex and subsequent Augmin phosphorylation, Plk1 regulates spindle microtubule-based microtubule nucleation to accomplish normal bipolar spindle formation and mitotic progression
-
-
?
ATP + kinesin-like protein 2
ADP + phosphorylated kinesin-like protein 2
show the reaction diagram
-
Plk1, essential for cytokinesis
-
-
?
ATP + mitotic centromere-associated kinesin
ADP + phosphorylated mitotic centromere-associated kinesin
show the reaction diagram
-
i.e. MCAK, residue S621 in MCAK is the major phosphorylation site of Plk1, residues S632/S633 are also phoshorylated by Plk1. S632/S633 phosphorylation significantly enhances the microtubule depolymerizing activity of MCAK in vivo and in vitro
-
-
?
ATP + Myt1
ADP + phosphorylated Myt1
show the reaction diagram
-
phosphorylation of Myt1 during M phase
-
-
?
ATP + NudC
ADP + phosphorylated kinesin-like protein 2
show the reaction diagram
-
i.e. nuclear distribution protein C, Plk1 phosphorylates Ser274 and Ser326
-
-
?
ATP + p125
ADP + phosphorylated p125
show the reaction diagram
-
peptide fragment of DNA polymerase delta, phosphorylation at Ser60 by Plk3
-
-
?
ATP + p53
ADP + phosphorylated p53
show the reaction diagram
ATP + PBIP1
ADP + phosphorylated PBIP1
show the reaction diagram
ATP + Pin1
ADP + phosphorylated Pin1
show the reaction diagram
-
Plk1-mediated phosphorylation at Ser65 stabilizes Pin1 by inhibiting its ubiquitination in cells
-
-
?
ATP + protein
ADP + phosphoprotein
show the reaction diagram
ATP + SCFFbw7 ubiquitin ligase
ADP + phosphorylated SCFFbw7 ubiquitin ligase
show the reaction diagram
-
-
-
-
?
additional information
?
-
METALS and IONS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
INHIBITORS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
AG-013736
-
selective inhibition of PLK4 relative to PLK1-3
BAY 439006
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selective inhibition of PLK4 relative to PLK1-3
BI 2536
-
-
CHIR-258
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selectivity profile of PLK2/4 over PLK1/3
CP 547632
-
selective inhibition of PLK4 relative to PLK1-3
GO 6976
-
-
H-1152
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selective inhibition of PLK4 relative to PLK1-3
imatinib
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selective inhibition of PLK4 relative to PLK1-3
LY294002
-
selective inhibition of PLK4 relative to PLK1-3
staurosporine
-
specific for PLK4
SU11248
-
selective inhibition of PLK4 relative to PLK1-3
VX-680
-
selective inhibition of PLK4 relative to PLK1-3
Wortmannin
-
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(-)-epigallocatechin
-
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(1R)-1-[(3S,6S,9S,12S,15S)-19-(6-[[2-(1-acetyl-1H-indol-3-yl)ethyl]amino]-6-oxohexyl)-3-carbamoyl-9-(hydroxymethyl)-12-(1H-imidazol-5-ylmethyl)-15-(2-methylpropyl)-5,8,11,14,17,20-hexaoxo-1-thia-4,7,10,13,16,19-hexaazacyclohenicosan-6-yl]ethyl phosphate
-
PL-116
-
(1R)-1-[(3S,6S,9S,12S,15S)-19-(6-[[2-(1-acetyl-1H-indol-3-yl)ethyl]amino]-6-oxohexyl)-3-carbamoyl-9-(hydroxymethyl)-15-(2-methylpropyl)-5,8,11,14,17,20-hexaoxo-12-[[1-(9-phenylnonyl)-1H-imidazol-5-yl]methyl]-1-thia-4,7,10,13,16,19-hexaazacyclohenicosan-6-yl]ethyl phosphate
-
PL-120
(2Z)-2-(5-bromo-2-methoxybenzylidene)-6-methyl-7H-[1,3]thiazolo[3,2-b][1,2,4]triazine-3,7(2H)-dione
-
-
(3S)-4-amino-4-oxo-3-([[2-(4-phenylbutyl)-1-(2-phenylethyl)-1H-benzimidazol-5-yl]carbonyl]amino)butan-2-yl phosphate
-
-
(4E)-4-(hydroxyimino)-5-methyl-2-(propan-2-yl)cyclohexa-2,5-dien-1-one
(4E)-5-methyl-4-[[(2-methylbenzoyl)oxy]imino]-2-(propan-2-yl)cyclohexa-2,5-dien-1-one
-
-
(4E)-5-methyl-4-{[(2-methylbenzoyl)oxy]imino}-2-(propan-2-yl)cyclohexa-2,5-dien-1-one
(4R)-1-acetyl-4-(4-phenylbutoxy)prolyl-L-leucyl-L-histidyl-L-seryl-O-phosphono-L-threoninamide
-
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(4R)-1-acetyl-4-[[(E)-(3-phenylpropylidene)amino]oxy]prolyl-L-leucyl-L-histidyl-L-seryl-O-phosphono-L-threoninamide
-
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(7R)-2-[5-(2,4-difluorophenyl)-1H-pyrazol-4-yl]-7-ethyl-5-methyl-8-(1-methyl-1H-pyrazol-4-yl)-7,8-dihydropteridin-6(5H)-one
-
-
(7R)-7-ethyl-2-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5-methyl-8-(1-methyl-1H-pyrazol-3-yl)-7,8-dihydropteridin-6(5H)-one
(7R)-7-ethyl-2-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5-methyl-8-(1-methyl-1H-pyrazol-4-yl)-7,8-dihydropteridin-6(5H)-one
-
-
(7R)-7-ethyl-2-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5-methyl-8-(1-methyl-1H-pyrazol-5-yl)-7,8-dihydropteridin-6(5H)-one
-
-
(7R)-7-ethyl-2-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5-methyl-8-(1H-pyrazol-4-yl)-7,8-dihydropteridin-6(5H)-one
-
-
(7R)-7-ethyl-2-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5-methyl-8-(3,3,3-trifluoropropyl)-7,8-dihydropteridin-6(5H)-one
-
-
(7R)-7-ethyl-2-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5-methyl-8-(oxetan-3-yl)-7,8-dihydropteridin-6(5H)-one
-
-
(7R)-7-ethyl-2-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5-methyl-8-[(3S)-tetrahydrofuran-3-yl]-7,8-dihydropteridin-6(5H)-one
-
-
(7R)-7-ethyl-5-methyl-2-(2-phenyl-1H-imidazol-1-yl)-8-(3,3,3-trifluoropropyl)-7,8-dihydropteridin-6(5H)-one
-
-
(7R)-7-ethyl-5-methyl-2-(2-phenyl-1H-imidazol-1-yl)-8-(propan-2-yl)-7,8-dihydropteridin-6(5H)-one
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(7R)-7-ethyl-5-methyl-2-(2-phenyl-1H-imidazol-1-yl)-8-(pyrimidin-5-yl)-7,8-dihydropteridin-6(5H)-one
-
-
(7R)-7-ethyl-5-methyl-2-(2-phenyl-1H-imidazol-1-yl)-8-[(3R)-tetrahydrofuran-3-yl]-7,8-dihydropteridin-6(5H)-one
-
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(7R)-7-ethyl-5-methyl-2-(2-phenyl-1H-imidazol-1-yl)-8-[(3S)-tetrahydrofuran-3-yl]-7,8-dihydropteridin-6(5H)-one
-
-
(7R)-7-ethyl-5-methyl-8-(1H-pyrazol-4-yl)-2-[5-(1,3-thiazol-2-yl)-1H-pyrazol-4-yl]-7,8-dihydropteridin-6(5H)-one
-
-
(7R)-7-ethyl-5-methyl-8-(tetrahydro-2H-pyran-4-yl)-2-[5-(1,3-thiazol-2-yl)-1H-pyrazol-4-yl]-7,8-dihydropteridin-6(5H)-one
-
-
(7R)-7-ethyl-5-methyl-8-(tetrahydrofuran-3-yl)-2-[5-(1,3-thiazol-2-yl)-1H-pyrazol-4-yl]-7,8-dihydropteridin-6(5H)-one
-
-
(7R)-8-(3,3-difluorocyclobutyl)-7-ethyl-2-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5-methyl-7,8-dihydropteridin-6(5H)-one
-
-
(R)-4-[(8-cyclopentyl-7-ethyl-5,6,7,8-tetrahydro-5-methyl-6-oxo-2-pteridinyl)amino]-3-methoxy-N-(1-methyl-4-piperidinyl)benzamide
-
i.e. BI2536
1-(1-methylpiperidin-4-yl)-8-(phenylamino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
1-(2-hydroxyethyl)-2-(2-[[5-(4-methylpiperazin-1-yl)-2-(trifluoromethoxy)phenyl]amino]pyrimidin-4-yl)-1,5,6,7-tetrahydro-4H-pyrrolo[3,2-c]pyridin-4-one
-
-
1-(2-hydroxyethyl)-5-(2-[[5-(4-methylpiperazin-1-yl)-2-(trifluoromethoxy)phenyl]amino]pyrimidin-4-yl)-1H-pyrrole-3-carboxamide
-
-
1-(26-oxo-2,5,8,11,14,17,20,23-octaoxahexacosan-26-yl)-L-prolyl-L-leucyl-3-(8-phenyloctyl)-L-histidyl-L-seryl-(3R)-4-phosphono-L-valinamide
-
-
1-acetyl-L-prolyl-L-leucyl-3-(8-phenyloctyl)-L-histidyl-L-seryl-O-phosphono-L-threoninamide
-
-
1-acetyl-L-prolyl-L-leucyl-3-[3-(2-hydroxyethyl)-1-(8-phenyloctyl)-1H-imidazol-3-ium-5-yl]-L-alanyl-L-seryl-O-phosphono-L-threoninamide
-
-
1-acetyl-L-prolyl-L-leucyl-3-[3-(2-hydroxyethyl)-1-(8-phenyloctyl)-1H-imidazol-3-ium-5-yl]-L-alanyl-L-seryl-O-[[[(2,2-dimethylpropanoyl)oxy]methoxy](hydroxy)phosphoryl]-L-threoninamide
-
-
1-cyclohexyl-8-(phenylamino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
1-methyl-2-(2-[[5-(4-methylpiperazin-1-yl)-2-(trifluoromethoxy)phenyl]amino]pyrimidin-4-yl)-1,5,6,7-tetrahydro-4H-pyrrolo[3,2-c]pyridin-4-one
-
high levels of selectivity on a panel of unrelated kinases, as well as against PLK2 and PLK3 isoforms, acceptable oral bioavailability in mice making this inhibitor a suitable candidate for further in vivo activity studies
1-methyl-5-(2-[[5-(4-methylpiperazin-1-yl)-2-(trifluoromethoxy)phenyl]amino]pyrimidin-4-yl)-1H-pyrrole-3-carboxamide
-
high levels of selectivity on a panel of unrelated kinases, as well as against PLK2 and PLK3 isoforms, acceptable oral bioavailability in mice making this inhibitor a suitable candidate for further in vivo activity studies
1-methyl-5-(2-[[5-(piperazin-1-yl)-2-(trifluoromethoxy)phenyl]amino]pyrimidin-4-yl)-1H-pyrrole-3-carboxamide
-
-
1-methyl-8-(phenylamino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
1-methyl-8-(phenylamino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxylic acid
-
-
1-methyl-8-[(2-methylphenyl)amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
1-methyl-8-[(2-nitrophenyl)amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
1-methyl-8-[(2-phenoxyphenyl)amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
1-methyl-8-[(2-sulfamoylphenyl)amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
1-methyl-8-[(3-nitrophenyl)amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
1-methyl-8-[(4-nitrophenyl)amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
1-methyl-8-[[2-(methylamino)phenyl]amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
1-methyl-8-[[2-(methylsulfanyl)phenyl]amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
1-methyl-8-[[2-(phenylamino)phenyl]amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
1-methyl-8-[[2-(phenylcarbonyl)phenyl]amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
1-methyl-8-[[2-(phenylsulfanyl)phenyl]amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
1-methyl-8-[[2-(propan-2-yl)phenyl]amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
1-methyl-8-[[2-(trifluoromethyl)phenyl]amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
1-methyl-8-[[3-(trifluoromethyl)phenyl]amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
1-methyl-8-[[4-(trifluoromethyl)phenyl]amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
1-methyl-N-phenyl-8-(phenylamino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
1-phenyl-8-(phenylamino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
1-[2-hydroxy-3-(4-methylpiperazin-1-yl)propyl]-1H-indole-3-carboxylic acid
-
-
1-[2-hydroxy-3-(piperidin-1-yl)propyl]-1H-indole-3-carboxylic acid
-
-
1-[2-hydroxy-3-(pyrrolidin-1-yl)propyl]-1H-indole-3-carboxylic acid
-
-
1-[3-(diethylamino)-2-hydroxypropyl]-1H-indole-3-carboxylic acid
-
-
2'-(2-hydroxyethoxy)-5'-methyl-(1,1':3',1''-terphenyl)-4,4''-dinitrile
-
0.3 mM, 11% inhibition, full-length enzyme Plk1 with the mutation T210D in the active-site loop of kinase domain
2'-(2-hydroxyethoxy)-5'-methyl-(1,1':3':1''-terphenyl)-4''-(1H-tetrazol-5-yl)-4-nitrile
-
0.3 mM, 66% inhibition, full-length enzyme Plk1 with the mutation T210D in the active-site loop of kinase domain
2'-(2-hydroxyethoxy)-5'-methyl-[1,1':3',1''-terphenyl]-3,3'',5,5''-tetrafluoro-4,4''-diol
-
0.3 mM, 61% inhibition, full-length enzyme Plk1 with the mutation T210D in the active-site loop of kinase domain
2'-(2-hydroxyethoxy)-5'-methyl-[1,1':3',1''-terphenyl]-4,4''-diacetic acid
-
0.3 mM, 53% inhibition, full-length enzyme Plk1 with the mutation T210D in the active-site loop of kinase domain
2'-(2-hydroxyethoxy)-5'-methyl-[1,1':3',1''-terphenyl]-4,4''-dicarboxylic acid
-
0.3 mM, 14% inhibition, full-length enzyme Plk1 with the mutation T210D in the active-site loop of kinase domain
2'-(2-hydroxyethoxy)-5'-methyl-[1,1':3',1''-terphenyl]-4,4''-dipropionic acid
-
0.3 mM, 26% inhibition, full-length enzyme Plk1 with the mutation T210D in the active-site loop of kinase domain
2'-hydroxy-5'-methyl-[1,1':3',1''-terphenyl]-4,4''-dicarboxylic acid
-
0.3 mM, 36% inhibition, full-length enzyme Plk1 with the mutation T210D in the active-site loop of kinase domain
2'-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5'-methyl-8'-(propan-2-yl)-5',8'-dihydro-6'H-spiro[cyclobutane-1,7'-pteridin]-6'-one
-
-
2,3,4,6-tetrahydroxy-5H-benzo[7]annulen-5-one
-
HeLa cells treated with purpurogallin exhibit delayed onset of mitosis and prolonged mitosis progression
2-(2-[[5-(4-methylpiperazin-1-yl)-2-(trifluoromethoxy)phenyl]amino]pyrimidin-4-yl)-1-(2,2,2-trifluoroethyl)-1,5,6,7-tetrahydro-4H-pyrrolo[3,2-c]pyridin-4-one
-
-
2-cyano-3-hydroxy-3-methyl-N-[4-(trifluoromethoxy)phenyl]-propenamide
-
LFM-A12
2-methyl-5-(propan-2-yl)cyclohexa-2,5-diene-1,4-dione
2-[(3-cyano-6-methoxyquinolin-2-yl)sulfanyl]-N-(2-methoxy-5-methylphenyl)acetamide
-
i.e. I2
2-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5,7,7-trimethyl-8-(propan-2-yl)-7,8-dihydropteridin-6(5H)-one
-
-
2-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5-methyl-7-(2,2,2-trifluoroethyl)-8-(3,3,3-trifluoropropyl)-7,8-dihydropteridin-6(5H)-one
-
-
2-[5'-methyl-4,4''-ditetrazol-5-yl-(1,1':3',1''-terphenyl)-2'-oxy]ethanol
-
0.3 mM, 47% inhibition, full-length enzyme Plk1 with the mutation T210D in the active-site loop of kinase domain
3-(1,3-benzodioxol-5-yl)-N-[(1S)-1-phenylethyl]isoxazolo[5,4-c]pyridin-5-amine
-
3-(2-methylcyclohexyl)-N-[(1S)-1-phenylethyl]isoxazolo[5,4-c]pyridin-5-amine
-
3-(3,4-dimethoxyphenyl)-N-[(1S)-1-phenylethyl]isoxazolo[5,4-c]pyridin-5-amine
-
3-(3,4-dimethylphenyl)-N-[(1S)-1-phenylethyl]isoxazolo[5,4-c]pyridin-5-amine
-
3-(3-chlorophenyl)-N-[(1S)-1-phenylethyl]isoxazolo[5,4-c]pyridin-5-amine
-
3-(3-methylphenyl)-N-[(1S)-1-phenylethyl]isoxazolo[5,4-c]pyridin-5-amine
3-(4-methylphenyl)-N-[(1S)-1-phenylethyl]isoxazolo[5,4-c]pyridin-5-amine
-
3-(4-methylthiophen-3-yl)-N-[(1S)-1-phenylethyl]isoxazolo[5,4-c]pyridin-5-amine
-
3-benzyl-N-[(1S)-1-phenylethyl]isoxazolo[5,4-c]pyridin-5-amine
>0.020
3-phenyl-N-[(1S)-1-phenylethyl]isoxazolo[5,4-c]pyridin-5-amine
-
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-(5,6-dimethoxy-1H-benzimidazol-1-yl)thiophene-2-carboxamide
-
-
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-(6-methoxy-1H-benzimidazol-1-yl)thiophene-2-carboxamide
-
-
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-(6-[[(2R)-2,3-dihydroxypropyl]oxy]-1H-benzimidazol-1-yl)thiophene-2-carboxamide
-
-
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-(6-[[(2R)-2-hydroxy-3-pyrrolidin-1-ylpropyl]oxy]-1H-benzimidazol-1-yl)thiophene-2-carboxamide
-
-
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-(6-[[(4R)-1-methylazepan-4-yl]oxy]-1H-benzimidazol-1-yl)thiophene-2-carboxamide
-
-
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-(6-[[(4S)-1-methylazepan-4-yl]oxy]-1H-benzimidazol-1-yl)thiophene-2-carboxamide
-
-
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-[6-[(1-methylpiperidin-4-yl)methoxy]-1H-benzimidazol-1-yl]thiophene-2-carboxamide
-
-
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-[6-[(1-methylpiperidin-4-yl)oxy]-1H-benzimidazol-1-yl]thiophene-2-carboxamide
-
-
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-[6-[3-(dimethylamino)propoxy]-1H-benzimidazol-1-yl]thiophene-2-carboxamide
-
-
3-[(1S)-1-(2-chlorophenyl)ethoxy]-5-(5,6-dimethoxy-1H-benzimidazol-1-yl)thiophene-2-carboxamide
-
-
3-[(2-chlorobenzyl)oxy]-5-(5,6-dimethoxy-1H-benzimidazol-1-yl)thiophene-2-carboxamide
-
-
3-[1-(5-[[(1S)-1-phenylethyl]amino]isoxazolo[5,4-c]pyridin-3-yl)piperidin-3-yl]propanamide
-
3-[1-[2-hydroxy-3-(piperidin-1-yl)propyl]-1H-indol-3-yl]propanoic acid
-
-
3-[1-[2-hydroxy-3-(pyrrolidin-1-yl)propyl]-1H-indol-3-yl]propanoic acid
-
-
3-[3-chloro-5-(5-[[(1S)-1-phenylethyl]amino]isoxazolo[5,4-c]pyridin-3-yl)phenyl]propan-1-ol
-
3-[3-chloro-5-(5-[[(1S)-1-phenylethyl]amino]isoxazolo[5,4-c]pyridin-3-yl)phenyl]propanamide
-
4-((R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,7,8-tetrahydro-pteridin-2-ylamino)-3-methoxy-N-(1-methyl-piperidin-4-yl)-benzamide
-
BI 2536
4-amino-5-fluoro-3-[6-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]quinolin-2-ol
-
selectivity profile of PLK2/4 over PLK1/3
4-[7-ethyl-2-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5-methyl-6-oxo-6,7-dihydropteridin-8(5H)-yl]benzonitrile
-
-
5-(2-[[5-(4-methylpiperazin-1-yl)-2-(trifluoromethoxy)phenyl]amino]pyrimidin-4-yl)-1-(2,2,2-trifluoroethyl)-1H-pyrrole-3-carboxamide
-
-
5-(2-[[5-(4-methylpiperazin-1-yl)-2-(trifluoromethoxy)phenyl]amino]pyrimidin-4-yl)-1-[2-(tetrahydro-2H-pyran-4-yloxy)ethyl]-1H-pyrrole-3-carboxamide
-
-
5-(5,6-dimethoxy-1H-benzimidazol-1-yl)-3-[2-(trifluoromethyl)-benzyloxy]-thiophene-2-carboxamide
-
-
5-(5,6-dimethoxy-1H-benzimidazol-1-yl)-3-[2-(trifluoromethyl)-benzyl]oxythiophene-2-carboxamide
-
GW843682X
5-(5,6-dimethoxy-1H-benzimidazol-1-yl)-3-[[2-(trifluoromethyl)benzyl]oxy]thiophene-2-carboxamide
-
-
5-(5,6-dimethoxy-1H-benzimidazol-1-yl)-3-{[2-(trifluoromethyl)phenyl]methoxy}thiophene-2-carboxamide
-
i.e. GW843682X, inhibition of PLK1 activity abrogates mitotic activation of AMP-activated protein kinasealpha through direct or indirect mechanisms
5-(6-methoxy-1H-benzimidazol-1-yl)-3-[(1R)-1-[2-(trifluoromethyl)phenyl]ethoxy]thiophene-2-carboxamide
-
-
5-[6-(piperidin-4-yloxy)-1H-benzimidazol-1-yl]-3-[(1R)-1-[2-(trifluoromethyl)phenyl]ethoxy]thiophene-2-carboxamide
-
-
5-[6-[(1-methylpiperidin-4-yl)methoxy]-1H-benzimidazol-1-yl]-3-[(1R)-1-[2-(trifluoromethyl)phenyl]ethoxy]thiophene-2-carboxamide
-
-
5-[6-[(1-methylpiperidin-4-yl)oxy]-1H-benzimidazol-1-yl]-3-[(1R)-1-[2-(trifluoromethyl)phenyl]ethoxy]thiophene-2-carboxamide
-
-
7-ethyl-2-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5,7-dimethyl-8-(3,3,3-trifluoropropyl)-7,8-dihydropteridin-6(5H)-one
-
-
7-ethyl-2-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5-methyl-8-(1H-pyrazol-3-yl)-7,8-dihydropteridin-6(5H)-one
-
-
7-ethyl-5-methyl-8-(1-methyl-1H-pyrazol-4-yl)-2-[5-(1,3-thiazol-2-yl)-1H-pyrazol-4-yl]-7,8-dihydropteridin-6(5H)-one
-
-
7-ethyl-5-methyl-8-(1-methyl-1H-pyrazol-4-yl)-2-[5-(pyridin-2-yl)-1H-pyrazol-4-yl]-7,8-dihydropteridin-6(5H)-one
-
-
7-ethyl-5-methyl-8-phenyl-2-(2-phenyl-1H-imidazol-1-yl)-7,8-dihydropteridin-6(5H)-one
-
-
7-ethyl-8-(4-fluorophenyl)-2-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5-methyl-7,8-dihydropteridin-6(5H)-one
-
-
71-FDPPLHSpTA-79
-
a PBIP1-derived phosphopeptide, the N-terminal phenylalanine sits in the hydrophobic pocket
-
8-(3,3-difluorocyclopentyl)-7-ethyl-2-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5-methyl-7,8-dihydropteridin-6(5H)-one
-
-
8-(biphenyl-2-ylamino)-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
8-(phenylamino)-1-(2,2,2-trifluoroethyl)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
8-(phenylamino)-1-(propan-2-yl)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
8-(phenylamino)-1-[2-(piperidin-1-yl)ethyl]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
8-(phenylamino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
8-[(2-acetylphenyl)amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
8-[(2-aminophenyl)amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
8-[(2-benzylphenyl)amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
8-[(2-carbamoylphenyl)amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
8-[(2-fluorophenyl)amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
8-[(2-methoxyphenyl)amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
8-[(3-acetylphenyl)amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
8-[(3-methoxyphenyl)amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
8-[(4-acetylphenyl)amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
8-[(4-methoxyphenyl)amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
8-[[2-(acetylamino)phenyl]amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
8-[[2-acetyl-3-(4-methylpiperazin-1-yl)phenyl]amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
8-[[2-acetyl-4-(4-methylpiperazin-1-yl)phenyl]amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
8-[[2-acetyl-5-(4-methylpiperazin-1-yl)phenyl]amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
8-[[2-methoxy-4-(4-methylpiperazin-1-yl)phenyl]amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
8-[[2-methoxy-5-(4-methylpiperazin-1-yl)phenyl]amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
AG-013736
-
-
AMPPNP
-
-
ataxia-telangiectasia mutant
-
i.e. ATM, inhibits p53 phosphorylation by Plk1 in vivo
-
BAY 439006
-
-
BI 2536
BI 6727
BI-2536
BI6727
-
-
BTO-1
CHIR-258
CJ-054
-
-
-
CP 547632
-
-
cyclapolin 1
-
-
cyclic (-CH2-CO-Pro-Leu-His-Ser-pThr-Cys-S-)
-
-
cyclic [-CH2-CO-N[2-(1H-indol-3-yl)ethyl]-CH2-CO-Leu-His-Ser-pThr-NH-CH[CONH2]-CH2-S-]
-
-
cyclic [-CH2-CO-N[3-[[2-(1H-indol-3-yl)ethyl]amino]-3-oxopropyl]-CH2-CO-Leu-His-Ser-p-Thr-NH-CH[CONH2]-CH2-S-]
-
-
cyclic [-CH2-CO-N[6-[[2-(1-acetyl-1H-indol-3-yl)ethyl]amino]-6-oxohexyl]-CH2-CO-Leu-His-Ser-pThr-NH-CH[CONH2]-CH2-S-]
-
-
cyclic [-CH2-CO-N[6-[[2-(1-acetyl-1H-indol-3-yl)ethyl]amino]-6-oxohexyl]-CH2-CO-Leu-His[N3-(8-phenyloctyl)]-Ser-pThr-NH-CH[CONH2]-CH2-S-]
-
-
DAP81
-
-
ethyl 1-methyl-8-(phenylamino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxylate
-
-
GO 6976
GSK461364
-
-
GSK461364A
GW843682
-
-
GW843682X
H-1152
-
-
hesperadin
-
almost complete inhibition
-
imatinib
-
-
LY294002
-
-
MAGPMQSpTPLNGAKK
-
the peptide inhibitor blocks the interaction between the Plk1 PBD and Cdc25C
-
methyl 2-[(3-carbamoyl-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazolin-8-yl)amino]benzoate
-
-
morin
-
-
N,1-dimethyl-8-(phenylamino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-2-methylbenzamide
-
-
N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-2-nitrobenzamide
-
-
N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-4-chlorobenzylaniline
-
-
N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-4-methoxybenzamide
-
-
N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-4-methoxybenzylaniline
-
-
N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-4-methylbenzamide
-
-
N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-4-methylbenzylaniline
-
-
N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-4-nitrobenzamide
-
-
N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-4-nitrobenzylaniline
-
-
N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-acetamide
-
-
N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-benzamide
-
-
N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-benzylaniline
-
-
N-(2-(3-(1H-indol-1-yl)propoxy)phenyl)-2-methylbenzamide
-
-
N-(2-(3-(1H-indol-1-yl)propoxy)phenyl)-2-nitrobenzamide
-
-
N-(2-(3-(1H-indol-1-yl)propoxy)phenyl)-4-methoxybenzamide
-
a highly selective inhibitor of Plk1, in vitro kinase inhibitory profile of 5i, overview
N-(2-(3-(1H-indol-1-yl)propoxy)phenyl)-4-nitrobenzamide
-
-
N-(2-(3-(1H-indol-1-yl)propoxy)phenyl)acetamide
-
-
N-(2-(3-(1H-indol-1-yl)propoxy)phenyl)benzamide
-
-
N-(2-(3-(1H-indol-1-yl)propoxy)phenyl)benzylaniline
-
-
N-(3-(2-[(7-[4-[(4-[[(7S)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,7,8-tetrahydropteridin-2-yl]amino]-3-methoxybenzoyl)amino]piperidin-1-yl]heptanoyl)amino]ethoxy)propanoyl)glycyl-L-prolyl-L-leucyl-L-histidyl-L-seryl-O-phosphono-L-threonyl-L-alaninamide
-
-
-
N-(3-(4-[(7-[4-[(4-[[(7S)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,7,8-tetrahydropteridin-2-yl]amino]-3-methoxybenzoyl)amino]piperidin-1-yl]heptanoyl)amino]butoxy)propanoyl)glycyl-L-prolyl-L-leucyl-L-histidyl-L-seryl-O-phosphono-L-threonyl-L-alaninamide
-
-
-
N-(3-[2-[(7-[4-[(4-[[(7S)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,7,8-tetrahydropteridin-2-yl]amino]-3-methoxybenzoyl)amino]piperidin-1-yl]heptanoyl)amino]ethoxy]propanoyl)glycyl-L-prolyl-L-leucyl-L-histidyl-L-seryl-O-phosphono-L-threonyl-L-alaninamide}
-
-
-
N-(47-{4-[(4-{[(7S)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,7,8-tetrahydropteridin-2-yl]amino}-3-methoxybenzoyl)amino]piperidin-1-yl}-41-oxo-4,7,10,13,16,19,22,25,28,31,34,37-dodecaoxa-40-azaheptatetracontan-1-oyl)glycyl-L-prolyl-L-leucyl-L-histidyl-L-seryl-O-phosphono-L-threonyl-L-alaninamide
-
-
N-(71-[4-[(4-[[(7S)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,7,8-tetrahydropteridin-2-yl]amino]-3-methoxybenzoyl)amino]piperidin-1-yl]-65-oxo-4,7,10,13,16,19,22,25,28,31,34,37,40,43,46,49,52,55,58,61-icosaoxa-64-azahenheptacontan-1-oyl)glycyl-L-prolyl-L-leucyl-L-histidyl-L-seryl-O-phosphono-L-threonyl-L-alaninamide
-
-
N-acetyl-N-(6-phenylhexyl)glycyl-L-leucyl-L-histidyl-L-seryl-O-phosphono-L-threoninamide
-
-
N-adamantylacetyl-L-prolyl-L-leucyl-L-histidyl-L-seryl-O-phosphono-L-threonyl-L-methioninamide
-
i.e PL-55, PLHSpT-based peptide
N-cyclopentyl-1-methyl-8-(phenylamino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
N-cyclopropyl-1-methyl-8-(phenylamino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
N-[(1S)-1-phenylethyl]-3-thiophen-2-ylisoxazolo[5,4-c]pyridin-5-amine
-
N-[2-methoxy-5-({[(E)-2-(2,4,6-trimethoxyphenyl)ethenyl]sulfonyl}methyl)phenyl]glycine
N-[3-(1-benzothiophen-2-yl)propanoyl]-alpha-aspartyl-L-prolyl-L-prolyl-L-leucyl-L-histidyl-L-seryl-O-phosphono-L-threonyl-L-alaninamide
-
-
N-[4-[(6-chloropyridin-3-yl)methoxy]-3-methoxybenzyl]-2-(3,4-dimethoxyphenyl)ethanamine
-
SBE13
NMS-P937
-
inhibition via binding in the ATP-binding site
-
ON-01910
-
-
ON01910.Na
-
-
ONO1910
PHA-680626
PL-42
-
(MeO)3PhCH2PLHSpTM
-
PL-49
-
cyclohexylmethyl-PLHSpTM
-
quercetin
-
-
RNA
-
RNA interference abrogates centrosome maturation, spindle bipolarization, and silencing of the spindle assembly checkpoint
RNAi
-
SBE13
scytonemin
-
-
shRNA
-
-
-
siRNA
-
staurosporine
-
-
SU11248
-
-
tert-butyl 1-methyl-2-(2-[[5-(4-methylpiperazin-1-yl)-2-(trifluoromethoxy)phenyl]amino]pyrimidin-4-yl)-4-oxo-1,4,6,7-tetrahydro-5H-pyrrolo[3,2-c]pyridine-5-carboxylate
-
-
thymoquinone
-
-
Volasertib
-
BI6727, inhibition via binding in the ATP-binding site
-
VX-680
-
-
Wortmannin
[1-[2-hydroxy-3-(4-methylpiperazin-1-yl)propyl]-1H-indol-3-yl]acetic acid
-
a highly selective inhibitor of Plk1, poor inhibition of Plk2 and Plk3
[1-[2-hydroxy-3-(morpholin-4-yl)propyl]-1H-indol-3-yl]acetic acid
-
-
[1-[2-hydroxy-3-(piperidin-1-yl)propyl]-1H-indol-3-yl]acetic acid
-
-
[1-[2-hydroxy-3-(pyrrolidin-1-yl)propyl]-1H-indol-3-yl]acetic acid
-
-
[1-[3-(diethylamino)-2-hydroxypropyl]-1H-indol-3-yl]acetic acid
-
-
additional information
-
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
aurora A
-
-
-
nocodazole
-
-
okadaic acid
-
-
additional information
-
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.001
ATP
-
-
0.0002 - 0.0055
ATP
0.0006 - 0.0008
Cdc25C
-
TURNOVER NUMBER [1/s]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.0019 - 0.019
ATP
0.0049 - 0.0376
Cdc25C
-
Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.0000042
AG-013736
-
-
0.00024
BAY 439006
-
-
0.02
BI 2536
-
-
0.0014
CHIR-258
-
-
0.00012
CP 547632
-
-
0.0000034
GO 6976
-
-
0.00012
H-1152
-
-
0.0022
imatinib
-
-
0.02
LY294002
-
-
0.000011
N-[4-({4-[(Z)-(5-methyl-1,2-dihydro-3H-pyrazol-3-ylidene)amino]-6-(4-methylpiperazin-1-yl)pyrimidin-2-yl}sulfanyl)phenyl]cyclopropanecarboxamide
-
-
0.00079
PP1
-
-
0.0000026
staurosporine
-
-
0.0003
SU11248
-
-
0.02
Wortmannin
-
-
0.00085
4-amino-5-fluoro-3-[6-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]quinolin-2-ol
-
-
0.02
AG-013736
-
-
0.02 - 0.03
BAY 439006
0.000001
BI 2536
-
time-dependent inhibition
0.02
CHIR-258
-
-
0.02
CP 547632
-
-
0.008 - 0.019
GO 6976
0.0000005
GSK461364A
-
Ki, apparent dissociation constant, less than 0.0000005
0.02
H-1152
-
-
0.018 - 0.02
imatinib
0.0061 - 0.016
LY294002
0.02
N-methyl-2-({3-[(E)-2-(pyridin-2-yl)ethenyl]-2H-indazol-6-yl}sulfanyl)benzenecarboximidic acid
-
-
0.02
PP1
-
-
0.00015 - 0.0012
staurosporine
0.0093 - 0.02
SU11248
0.02
VX-680
-
-
0.0015 - 0.003
Wortmannin
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.00256
(1R)-1-[(3S,6S,9S,12S,15S)-19-(6-[[2-(1-acetyl-1H-indol-3-yl)ethyl]amino]-6-oxohexyl)-3-carbamoyl-9-(hydroxymethyl)-12-(1H-imidazol-5-ylmethyl)-15-(2-methylpropyl)-5,8,11,14,17,20-hexaoxo-1-thia-4,7,10,13,16,19-hexaazacyclohenicosan-6-yl]ethyl phosphate
Homo sapiens
-
pH and temperature not specified in the publication
-
0.00108
(1R)-1-[(3S,6S,9S,12S,15S)-19-(6-[[2-(1-acetyl-1H-indol-3-yl)ethyl]amino]-6-oxohexyl)-3-carbamoyl-9-(hydroxymethyl)-15-(2-methylpropyl)-5,8,11,14,17,20-hexaoxo-12-[[1-(9-phenylnonyl)-1H-imidazol-5-yl]methyl]-1-thia-4,7,10,13,16,19-hexaazacyclohenicosan-6-yl]ethyl phosphate
Homo sapiens
-
pH and temperature not specified in the publication
0.0032
(2Z)-2-(5-bromo-2-methoxybenzylidene)-6-methyl-7H-[1,3]thiazolo[3,2-b][1,2,4]triazine-3,7(2H)-dione
Homo sapiens
-
pH and temperature not specified in the publication
0.0045
(3S)-4-amino-4-oxo-3-([[2-(4-phenylbutyl)-1-(2-phenylethyl)-1H-benzimidazol-5-yl]carbonyl]amino)butan-2-yl phosphate
Homo sapiens
-
pH and temperature not specified in the publication
0.00114 - 0.00136
(4E)-5-methyl-4-[[(2-methylbenzoyl)oxy]imino]-2-(propan-2-yl)cyclohexa-2,5-dien-1-one
0.000014
(4R)-1-acetyl-4-(4-phenylbutoxy)prolyl-L-leucyl-L-histidyl-L-seryl-O-phosphono-L-threoninamide
Homo sapiens
-
pH and temperature not specified in the publication
122
(4R)-1-acetyl-4-[[(E)-(3-phenylpropylidene)amino]oxy]prolyl-L-leucyl-L-histidyl-L-seryl-O-phosphono-L-threoninamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000103 - 0.00126
(7R)-2-[5-(2,4-difluorophenyl)-1H-pyrazol-4-yl]-7-ethyl-5-methyl-8-(1-methyl-1H-pyrazol-4-yl)-7,8-dihydropteridin-6(5H)-one
0.000007 - 0.00135
(7R)-7-ethyl-2-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5-methyl-8-(1-methyl-1H-pyrazol-3-yl)-7,8-dihydropteridin-6(5H)-one
0.000021 - 0.00327
(7R)-7-ethyl-2-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5-methyl-8-(1-methyl-1H-pyrazol-4-yl)-7,8-dihydropteridin-6(5H)-one
0.000532 - 0.0288
(7R)-7-ethyl-2-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5-methyl-8-(1-methyl-1H-pyrazol-5-yl)-7,8-dihydropteridin-6(5H)-one
0.000012 - 0.00867
(7R)-7-ethyl-2-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5-methyl-8-(1H-pyrazol-4-yl)-7,8-dihydropteridin-6(5H)-one
0.000042 - 0.00355
(7R)-7-ethyl-2-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5-methyl-8-(3,3,3-trifluoropropyl)-7,8-dihydropteridin-6(5H)-one
0.00104
(7R)-7-ethyl-2-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5-methyl-8-(oxetan-3-yl)-7,8-dihydropteridin-6(5H)-one
Homo sapiens
-
22°C, pH not specified in the publication
0.000033 - 0.00753
(7R)-7-ethyl-2-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5-methyl-8-[(3S)-tetrahydrofuran-3-yl]-7,8-dihydropteridin-6(5H)-one
0.000009 - 0.00025
(7R)-7-ethyl-5-methyl-2-(2-phenyl-1H-imidazol-1-yl)-8-(3,3,3-trifluoropropyl)-7,8-dihydropteridin-6(5H)-one
0.000025 - 0.00087
(7R)-7-ethyl-5-methyl-2-(2-phenyl-1H-imidazol-1-yl)-8-(propan-2-yl)-7,8-dihydropteridin-6(5H)-one
0.000044 - 0.00776
(7R)-7-ethyl-5-methyl-2-(2-phenyl-1H-imidazol-1-yl)-8-(pyrimidin-5-yl)-7,8-dihydropteridin-6(5H)-one
0.000021 - 0.00048
(7R)-7-ethyl-5-methyl-2-(2-phenyl-1H-imidazol-1-yl)-8-[(3R)-tetrahydrofuran-3-yl]-7,8-dihydropteridin-6(5H)-one
0.000008 - 0.00038
(7R)-7-ethyl-5-methyl-2-(2-phenyl-1H-imidazol-1-yl)-8-[(3S)-tetrahydrofuran-3-yl]-7,8-dihydropteridin-6(5H)-one
0.000092 - 0.00303
(7R)-7-ethyl-5-methyl-8-(1H-pyrazol-4-yl)-2-[5-(1,3-thiazol-2-yl)-1H-pyrazol-4-yl]-7,8-dihydropteridin-6(5H)-one
0.000036 - 0.00025
(7R)-7-ethyl-5-methyl-8-(tetrahydro-2H-pyran-4-yl)-2-[5-(1,3-thiazol-2-yl)-1H-pyrazol-4-yl]-7,8-dihydropteridin-6(5H)-one
0.000039 - 0.00141
(7R)-7-ethyl-5-methyl-8-(tetrahydrofuran-3-yl)-2-[5-(1,3-thiazol-2-yl)-1H-pyrazol-4-yl]-7,8-dihydropteridin-6(5H)-one
0.000012 - 0.00939
(7R)-8-(3,3-difluorocyclobutyl)-7-ethyl-2-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5-methyl-7,8-dihydropteridin-6(5H)-one
0.01
1-(1-methylpiperidin-4-yl)-8-(phenylamino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
-
larger than 0.010, pH 7.9, 25°C
0.000102
1-(2-hydroxyethyl)-2-(2-[[5-(4-methylpiperazin-1-yl)-2-(trifluoromethoxy)phenyl]amino]pyrimidin-4-yl)-1,5,6,7-tetrahydro-4H-pyrrolo[3,2-c]pyridin-4-one
Homo sapiens
-
pH and temperature not specified in the publication
0.000151
1-(2-hydroxyethyl)-5-(2-[[5-(4-methylpiperazin-1-yl)-2-(trifluoromethoxy)phenyl]amino]pyrimidin-4-yl)-1H-pyrrole-3-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.38
1-(26-oxo-2,5,8,11,14,17,20,23-octaoxahexacosan-26-yl)-L-prolyl-L-leucyl-3-(8-phenyloctyl)-L-histidyl-L-seryl-(3R)-4-phosphono-L-valinamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0000025 - 0.000017
1-acetyl-L-prolyl-L-leucyl-3-(8-phenyloctyl)-L-histidyl-L-seryl-O-phosphono-L-threoninamide
Homo sapiens
-
pH and temperature not specified in the publication
0.085
1-acetyl-L-prolyl-L-leucyl-3-[3-(2-hydroxyethyl)-1-(8-phenyloctyl)-1H-imidazol-3-ium-5-yl]-L-alanyl-L-seryl-O-phosphono-L-threoninamide
Homo sapiens
-
pH and temperature not specified in the publication
0.055
1-acetyl-L-prolyl-L-leucyl-3-[3-(2-hydroxyethyl)-1-(8-phenyloctyl)-1H-imidazol-3-ium-5-yl]-L-alanyl-L-seryl-O-[[[(2,2-dimethylpropanoyl)oxy]methoxy](hydroxy)phosphoryl]-L-threoninamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000143
1-cyclohexyl-8-(phenylamino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
-
pH 7.9, 25°C
0.000009
1-methyl-2-(2-[[5-(4-methylpiperazin-1-yl)-2-(trifluoromethoxy)phenyl]amino]pyrimidin-4-yl)-1,5,6,7-tetrahydro-4H-pyrrolo[3,2-c]pyridin-4-one
Homo sapiens
-
pH and temperature not specified in the publication
0.000015
1-methyl-5-(2-[[5-(4-methylpiperazin-1-yl)-2-(trifluoromethoxy)phenyl]amino]pyrimidin-4-yl)-1H-pyrrole-3-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000018
1-methyl-5-(2-[[5-(piperazin-1-yl)-2-(trifluoromethoxy)phenyl]amino]pyrimidin-4-yl)-1H-pyrrole-3-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000009 - 0.000068
1-methyl-8-(phenylamino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
0.00011
1-methyl-8-(phenylamino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxylic acid
Homo sapiens
-
pH 7.9, 25°C
0.000002 - 0.000015
1-methyl-8-[(2-methylphenyl)amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
0.000488
1-methyl-8-[(2-nitrophenyl)amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
-
pH 7.9, 25°C
0.000051 - 0.002666
1-methyl-8-[(2-phenoxyphenyl)amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
0.003733
1-methyl-8-[(2-sulfamoylphenyl)amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
-
pH 7.9, 25°C
0.01
1-methyl-8-[(3-nitrophenyl)amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
-
larger than 0.010, pH 7.9, 25°C
0.01
1-methyl-8-[(4-nitrophenyl)amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
-
larger than 0.010, pH 7.9, 25°C
0.000011 - 0.00011
1-methyl-8-[[2-(methylamino)phenyl]amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
0.000014 - 0.000097
1-methyl-8-[[2-(methylsulfanyl)phenyl]amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
0.000949
1-methyl-8-[[2-(phenylamino)phenyl]amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
-
pH 7.9, 25°C
0.001969
1-methyl-8-[[2-(phenylcarbonyl)phenyl]amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
-
pH 7.9, 25°C
0.002033
1-methyl-8-[[2-(phenylsulfanyl)phenyl]amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
-
pH 7.9, 25°C
0.000146 - 0.000509
1-methyl-8-[[2-(propan-2-yl)phenyl]amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
0.000095 - 0.000432
1-methyl-8-[[2-(trifluoromethyl)phenyl]amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
0.000051
1-methyl-8-[[3-(trifluoromethyl)phenyl]amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
-
pH 7.9, 25°C
0.000872
1-methyl-8-[[4-(trifluoromethyl)phenyl]amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
-
pH 7.9, 25°C
0.01
1-methyl-N-phenyl-8-(phenylamino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
-
larger than 0.010, pH 7.9, 25°C
0.01
1-phenyl-8-(phenylamino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
-
larger than 0.010, pH 7.9, 25°C
0.00347
1-[2-hydroxy-3-(4-methylpiperazin-1-yl)propyl]-1H-indole-3-carboxylic acid
Homo sapiens
-
pH 7.5, 30°C
0.0021
1-[2-hydroxy-3-(piperidin-1-yl)propyl]-1H-indole-3-carboxylic acid
Homo sapiens
-
pH 7.5, 30°C
0.00484
1-[2-hydroxy-3-(pyrrolidin-1-yl)propyl]-1H-indole-3-carboxylic acid
Homo sapiens
-
pH 7.5, 30°C
0.00191
1-[3-(diethylamino)-2-hydroxypropyl]-1H-indole-3-carboxylic acid
Homo sapiens
-
pH 7.5, 30°C
0.00115 - 0.0253
2'-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5'-methyl-8'-(propan-2-yl)-5',8'-dihydro-6'H-spiro[cyclobutane-1,7'-pteridin]-6'-one
0.000028
2-(2-[[5-(4-methylpiperazin-1-yl)-2-(trifluoromethoxy)phenyl]amino]pyrimidin-4-yl)-1-(2,2,2-trifluoroethyl)-1,5,6,7-tetrahydro-4H-pyrrolo[3,2-c]pyridin-4-one
Homo sapiens
-
pH and temperature not specified in the publication
0.00218
2-methyl-5-(propan-2-yl)cyclohexa-2,5-diene-1,4-dione
Homo sapiens
-
pH 7.5, 30°C
0.00271
2-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5,7,7-trimethyl-8-(propan-2-yl)-7,8-dihydropteridin-6(5H)-one
Homo sapiens
-
22°C, pH not specified in the publication
0.00012 - 0.00348
2-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5-methyl-7-(2,2,2-trifluoroethyl)-8-(3,3,3-trifluoropropyl)-7,8-dihydropteridin-6(5H)-one
0.000004 - 0.000214
3-(1,3-benzodioxol-5-yl)-N-[(1S)-1-phenylethyl]isoxazolo[5,4-c]pyridin-5-amine
0.005689
3-(2-methylcyclohexyl)-N-[(1S)-1-phenylethyl]isoxazolo[5,4-c]pyridin-5-amine
Homo sapiens
Q9H4B4
-
0.004927
3-(3,4-dimethoxyphenyl)-N-[(1S)-1-phenylethyl]isoxazolo[5,4-c]pyridin-5-amine
Homo sapiens
Q9H4B4
-
0.00033
3-(3,4-dimethylphenyl)-N-[(1S)-1-phenylethyl]isoxazolo[5,4-c]pyridin-5-amine
Homo sapiens
Q9H4B4
-
0.000625
3-(3-chlorophenyl)-N-[(1S)-1-phenylethyl]isoxazolo[5,4-c]pyridin-5-amine
Homo sapiens
Q9H4B4
-
0.000549 - 0.01
3-(3-methylphenyl)-N-[(1S)-1-phenylethyl]isoxazolo[5,4-c]pyridin-5-amine
0.00117
3-(4-methylphenyl)-N-[(1S)-1-phenylethyl]isoxazolo[5,4-c]pyridin-5-amine
Homo sapiens
Q9H4B4
-
0.000779
3-(4-methylthiophen-3-yl)-N-[(1S)-1-phenylethyl]isoxazolo[5,4-c]pyridin-5-amine
Homo sapiens
Q9H4B4
-
0.02
3-benzyl-N-[(1S)-1-phenylethyl]isoxazolo[5,4-c]pyridin-5-amine
Homo sapiens
Q9H4B4
>0.020
0.001616
3-phenyl-N-[(1S)-1-phenylethyl]isoxazolo[5,4-c]pyridin-5-amine
Homo sapiens
Q9H4B4
-
0.0000008 - 0.000025
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-(5,6-dimethoxy-1H-benzimidazol-1-yl)thiophene-2-carboxamide
0.000001 - 0.000321
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-(6-methoxy-1H-benzimidazol-1-yl)thiophene-2-carboxamide
0.000001 - 0.000073
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-(6-[[(2R)-2,3-dihydroxypropyl]oxy]-1H-benzimidazol-1-yl)thiophene-2-carboxamide
0.000003 - 0.00061
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-(6-[[(2R)-2-hydroxy-3-pyrrolidin-1-ylpropyl]oxy]-1H-benzimidazol-1-yl)thiophene-2-carboxamide
0.000004 - 0.00025
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-(6-[[(4R)-1-methylazepan-4-yl]oxy]-1H-benzimidazol-1-yl)thiophene-2-carboxamide
0.000003 - 0.00024
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-(6-[[(4S)-1-methylazepan-4-yl]oxy]-1H-benzimidazol-1-yl)thiophene-2-carboxamide
0.000006 - 0.0011
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-[6-[(1-methylpiperidin-4-yl)methoxy]-1H-benzimidazol-1-yl]thiophene-2-carboxamide
0.000002 - 0.00063
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-[6-[(1-methylpiperidin-4-yl)oxy]-1H-benzimidazol-1-yl]thiophene-2-carboxamide
0.000004 - 0.00046
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-[6-[3-(dimethylamino)propoxy]-1H-benzimidazol-1-yl]thiophene-2-carboxamide
0.00003 - 0.000994
3-[(1S)-1-(2-chlorophenyl)ethoxy]-5-(5,6-dimethoxy-1H-benzimidazol-1-yl)thiophene-2-carboxamide
0.000002 - 0.00114
3-[(2-chlorobenzyl)oxy]-5-(5,6-dimethoxy-1H-benzimidazol-1-yl)thiophene-2-carboxamide
0.007479
3-[1-(5-[[(1S)-1-phenylethyl]amino]isoxazolo[5,4-c]pyridin-3-yl)piperidin-3-yl]propanamide
Homo sapiens
Q9H4B4
-
0.00571
3-[1-[2-hydroxy-3-(piperidin-1-yl)propyl]-1H-indol-3-yl]propanoic acid
Homo sapiens
-
pH 7.5, 30°C
0.0029
3-[1-[2-hydroxy-3-(pyrrolidin-1-yl)propyl]-1H-indol-3-yl]propanoic acid
Homo sapiens
-
pH 7.5, 30°C
0.000099
3-[3-chloro-5-(5-[[(1S)-1-phenylethyl]amino]isoxazolo[5,4-c]pyridin-3-yl)phenyl]propan-1-ol
Homo sapiens
Q9H4B4
-
0.000051 - 0.001382
3-[3-chloro-5-(5-[[(1S)-1-phenylethyl]amino]isoxazolo[5,4-c]pyridin-3-yl)phenyl]propanamide
0.00000083
4-((R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,7,8-tetrahydro-pteridin-2-ylamino)-3-methoxy-N-(1-methyl-piperidin-4-yl)-benzamide
Homo sapiens
-
-
0.000031 - 0.00376
4-[7-ethyl-2-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5-methyl-6-oxo-6,7-dihydropteridin-8(5H)-yl]benzonitrile
0.0000018
5-(2-[[5-(4-methylpiperazin-1-yl)-2-(trifluoromethoxy)phenyl]amino]pyrimidin-4-yl)-1-(2,2,2-trifluoroethyl)-1H-pyrrole-3-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000272
5-(2-[[5-(4-methylpiperazin-1-yl)-2-(trifluoromethoxy)phenyl]amino]pyrimidin-4-yl)-1-[2-(tetrahydro-2H-pyran-4-yloxy)ethyl]-1H-pyrrole-3-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000002 - 0.000009
5-(5,6-dimethoxy-1H-benzimidazol-1-yl)-3-[[2-(trifluoromethyl)benzyl]oxy]thiophene-2-carboxamide
0.000003 - 0.000476
5-(6-methoxy-1H-benzimidazol-1-yl)-3-[(1R)-1-[2-(trifluoromethyl)phenyl]ethoxy]thiophene-2-carboxamide
0.000003 - 0.00035
5-[6-(piperidin-4-yloxy)-1H-benzimidazol-1-yl]-3-[(1R)-1-[2-(trifluoromethyl)phenyl]ethoxy]thiophene-2-carboxamide
0.000007 - 0.00055
5-[6-[(1-methylpiperidin-4-yl)methoxy]-1H-benzimidazol-1-yl]-3-[(1R)-1-[2-(trifluoromethyl)phenyl]ethoxy]thiophene-2-carboxamide
0.000002 - 0.00027
5-[6-[(1-methylpiperidin-4-yl)oxy]-1H-benzimidazol-1-yl]-3-[(1R)-1-[2-(trifluoromethyl)phenyl]ethoxy]thiophene-2-carboxamide
0.00003 - 0.00716
7-ethyl-2-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5,7-dimethyl-8-(3,3,3-trifluoropropyl)-7,8-dihydropteridin-6(5H)-one
0.000009 - 0.00342
7-ethyl-2-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5-methyl-8-(1H-pyrazol-3-yl)-7,8-dihydropteridin-6(5H)-one
0.00013 - 0.00182
7-ethyl-5-methyl-8-(1-methyl-1H-pyrazol-4-yl)-2-[5-(1,3-thiazol-2-yl)-1H-pyrazol-4-yl]-7,8-dihydropteridin-6(5H)-one
0.000168 - 0.00182
7-ethyl-5-methyl-8-(1-methyl-1H-pyrazol-4-yl)-2-[5-(pyridin-2-yl)-1H-pyrazol-4-yl]-7,8-dihydropteridin-6(5H)-one
0.000017 - 0.00283
7-ethyl-5-methyl-8-phenyl-2-(2-phenyl-1H-imidazol-1-yl)-7,8-dihydropteridin-6(5H)-one
0.000015 - 0.00234
7-ethyl-8-(4-fluorophenyl)-2-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5-methyl-7,8-dihydropteridin-6(5H)-one
0.000013 - 0.00032
8-(3,3-difluorocyclopentyl)-7-ethyl-2-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5-methyl-7,8-dihydropteridin-6(5H)-one
0.001565
8-(biphenyl-2-ylamino)-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
-
pH 7.9, 25°C
0.000006
8-(phenylamino)-1-(2,2,2-trifluoroethyl)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
-
pH 7.9, 25°C
0.00043
8-(phenylamino)-1-(propan-2-yl)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
-
pH 7.9, 25°C
0.01
8-(phenylamino)-1-[2-(piperidin-1-yl)ethyl]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
-
larger than 0.010, pH 7.9, 25°C
0.000248
8-(phenylamino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
-
pH 7.9, 25°C
0.000103 - 0.000346
8-[(2-acetylphenyl)amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
0.000012 - 0.00015
8-[(2-aminophenyl)amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
0.000943
8-[(2-benzylphenyl)amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
-
pH 7.9, 25°C
0.002076
8-[(2-carbamoylphenyl)amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
-
pH 7.9, 25°C
0.000027 - 0.000125
8-[(2-fluorophenyl)amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
0.000013 - 0.000042
8-[(2-methoxyphenyl)amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
0.0001
8-[(3-acetylphenyl)amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
-
pH 7.9, 25°C
0.000135
8-[(3-methoxyphenyl)amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
-
pH 7.9, 25°C
0.000197
8-[(4-acetylphenyl)amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
-
pH 7.9, 25°C
0.000256
8-[(4-methoxyphenyl)amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
-
pH 7.9, 25°C
0.000049 - 0.002523
8-[[2-(acetylamino)phenyl]amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
0.002051 - 0.01
8-[[2-acetyl-3-(4-methylpiperazin-1-yl)phenyl]amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
0.000464 - 0.01
8-[[2-acetyl-4-(4-methylpiperazin-1-yl)phenyl]amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
0.000109 - 0.01
8-[[2-acetyl-5-(4-methylpiperazin-1-yl)phenyl]amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
0.00004 - 0.000082
8-[[2-methoxy-4-(4-methylpiperazin-1-yl)phenyl]amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
0.000007 - 0.00045
8-[[2-methoxy-5-(4-methylpiperazin-1-yl)phenyl]amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
0.14 - 0.166
AMPPNP
0.00000083
BI 2536
0.00000087
BI 6727
Homo sapiens
-
pH 7.5, 30°C
0.0008
BI-2536
Homo sapiens
-
-
0.0000008
BI2536
Homo sapiens
-
-
0.00000087
BI6727
Homo sapiens
-
-
0.008
BTO-1
Homo sapiens
-
-
0.0098
cyclic (-CH2-CO-Pro-Leu-His-Ser-pThr-Cys-S-)
Homo sapiens
-
25°C, pH not specified in the publication
0.0085
cyclic [-CH2-CO-N[2-(1H-indol-3-yl)ethyl]-CH2-CO-Leu-His-Ser-pThr-NH-CH[CONH2]-CH2-S-]
Homo sapiens
-
25°C, pH not specified in the publication
0.0048
cyclic [-CH2-CO-N[3-[[2-(1H-indol-3-yl)ethyl]amino]-3-oxopropyl]-CH2-CO-Leu-His-Ser-p-Thr-NH-CH[CONH2]-CH2-S-]
Homo sapiens
-
25°C, pH not specified in the publication
0.0026
cyclic [-CH2-CO-N[6-[[2-(1-acetyl-1H-indol-3-yl)ethyl]amino]-6-oxohexyl]-CH2-CO-Leu-His-Ser-pThr-NH-CH[CONH2]-CH2-S-]
Homo sapiens
-
25°C, pH not specified in the publication
0.0011
cyclic [-CH2-CO-N[6-[[2-(1-acetyl-1H-indol-3-yl)ethyl]amino]-6-oxohexyl]-CH2-CO-Leu-His[N3-(8-phenyloctyl)]-Ser-pThr-NH-CH[CONH2]-CH2-S-]
Homo sapiens
-
25°C, pH not specified in the publication
0.01
ethyl 1-methyl-8-(phenylamino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxylate
Homo sapiens
-
larger than 0.010, pH7.9, 25°C
0.00000005
GSK461364A
Homo sapiens
-
less than 50 nM
0.00525
LY294002
Homo sapiens
-
-
0.001117
methyl 2-[(3-carbamoyl-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazolin-8-yl)amino]benzoate
Homo sapiens
-
pH 7.9, 25°C
0.0126
morin
Homo sapiens
-
-
0.004215
N,1-dimethyl-8-(phenylamino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
-
pH 7.9, 25°C
0.0026
N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-2-methylbenzamide
Homo sapiens
-
pH 7.5, 30°C
0.01
N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-2-nitrobenzamide
Homo sapiens
-
pH 7.5, 30°C
0.00322
N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-4-chlorobenzylaniline
Homo sapiens
-
pH 7.5, 30°C
0.00093
N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-4-methoxybenzamide
Homo sapiens
-
pH 7.5, 30°C
0.00205
N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-4-methoxybenzylaniline
Homo sapiens
-
pH 7.5, 30°C
0.00709
N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-4-methylbenzamide
Homo sapiens
-
pH 7.5, 30°C
0.00466
N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-4-methylbenzylaniline
Homo sapiens
-
pH 7.5, 30°C
0.01
N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-4-nitrobenzamide
Homo sapiens
-
pH 7.5, 30°C
0.01
N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-4-nitrobenzylaniline
Homo sapiens
-
pH 7.5, 30°C
0.00683
N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-acetamide
Homo sapiens
-
pH 7.5, 30°C
0.00633
N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-benzamide
Homo sapiens
-
pH 7.5, 30°C
0.00948
N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-benzylaniline
Homo sapiens
-
pH 7.5, 30°C
0.00559
N-(2-(3-(1H-indol-1-yl)propoxy)phenyl)-2-methylbenzamide
Homo sapiens
-
pH 7.5, 30°C
0.01
N-(2-(3-(1H-indol-1-yl)propoxy)phenyl)-2-nitrobenzamide
Homo sapiens
-
pH 7.5, 30°C
0.00068
N-(2-(3-(1H-indol-1-yl)propoxy)phenyl)-4-methoxybenzamide
Homo sapiens
-
pH 7.5, 30°C
0.01
N-(2-(3-(1H-indol-1-yl)propoxy)phenyl)-4-nitrobenzamide
Homo sapiens
-
pH 7.5, 30°C
0.0047
N-(2-(3-(1H-indol-1-yl)propoxy)phenyl)acetamide
Homo sapiens
-
pH 7.5, 30°C
0.01
N-(2-(3-(1H-indol-1-yl)propoxy)phenyl)benzamide
Homo sapiens
-
pH 7.5, 30°C
0.00702
N-(2-(3-(1H-indol-1-yl)propoxy)phenyl)benzylaniline
Homo sapiens
-
pH 7.5, 30°C
0.00082
N-adamantylacetyl-L-prolyl-L-leucyl-L-histidyl-L-seryl-O-phosphono-L-threonyl-L-methioninamide
Homo sapiens
-
pH and temperature not specified in the publication
0.01
N-cyclopentyl-1-methyl-8-(phenylamino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
-
larger than 0.010, pH 7.9, 25°C
0.01
N-cyclopropyl-1-methyl-8-(phenylamino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
-
larger than 0.010, pH 7.9, 25°C
0.003007
N-[(1S)-1-phenylethyl]-3-thiophen-2-ylisoxazolo[5,4-c]pyridin-5-amine
Homo sapiens
Q9H4B4
-
0.00025
N-[3-(1-benzothiophen-2-yl)propanoyl]-alpha-aspartyl-L-prolyl-L-prolyl-L-leucyl-L-histidyl-L-seryl-O-phosphono-L-threonyl-L-alaninamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0000002
N-[4-[(6-chloropyridin-3-yl)methoxy]-3-methoxybenzyl]-2-(3,4-dimethoxyphenyl)ethanamine
Homo sapiens
-
-
0.000009 - 0.01
ONO1910
0.00034 - 0.00053
PHA-680626
0.0018
PL-42
Homo sapiens
-
pH and temperature not specified in the publication
-
0.00036
PL-49
Homo sapiens
-
pH and temperature not specified in the publication
-
0.064
quercetin
Homo sapiens
-
-
0.0000002
SBE13
Homo sapiens
-
immunoprecipitated Plk1 from HeLa cells
0.002
scytonemin
Homo sapiens
-
-
0.000817
tert-butyl 1-methyl-2-(2-[[5-(4-methylpiperazin-1-yl)-2-(trifluoromethoxy)phenyl]amino]pyrimidin-4-yl)-4-oxo-1,4,6,7-tetrahydro-5H-pyrrolo[3,2-c]pyridine-5-carboxylate
Homo sapiens
-
pH and temperature not specified in the publication
0.00218
thymoquinone
Homo sapiens
-
pH 7.5, 30°C
0.000024
Wortmannin
Homo sapiens
-
-
0.00188
[1-[2-hydroxy-3-(4-methylpiperazin-1-yl)propyl]-1H-indol-3-yl]acetic acid
Homo sapiens
-
pH 7.5, 30°C
0.00096
[1-[2-hydroxy-3-(morpholin-4-yl)propyl]-1H-indol-3-yl]acetic acid
Homo sapiens
-
pH 7.5, 30°C
0.00041
[1-[2-hydroxy-3-(piperidin-1-yl)propyl]-1H-indol-3-yl]acetic acid
Homo sapiens
-
pH 7.5, 30°C
0.00013
[1-[2-hydroxy-3-(pyrrolidin-1-yl)propyl]-1H-indol-3-yl]acetic acid
Homo sapiens
-
pH 7.5, 30°C
0.00264
[1-[3-(diethylamino)-2-hydroxypropyl]-1H-indol-3-yl]acetic acid
Homo sapiens
-
pH 7.5, 30°C
additional information
additional information
Homo sapiens
-
IC50 values for cell growth inhibition of HeLa and MCF-7 cells
-
SPECIFIC ACTIVITY [µmol/min/mg]
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
additional information
-
activity of wild-type and mutant GST-tagged or His6-tagged Plk3 with p125
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
7.6
-
in vitro kinase assay
7.9
-
kinase assay
8
-
in vitro kinase assay
TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
23
-
kinase assay
25
-
kinase assay
SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
SOURCE
-
anaplastic thyroid carcinoma cell line
Manually annotated by BRENDA team
-
squamous A-253 cell
Manually annotated by BRENDA team
-
anaplastic thyroid carcinoma cell line
Manually annotated by BRENDA team
-
anaplastic thyroid carcinoma cell line
Manually annotated by BRENDA team
-
increased requirement for Plk1 in comparison to normal cells
Manually annotated by BRENDA team
-
skin epidermis
Manually annotated by BRENDA team
-
is highly expressed, on average 2.7-fold higher mRNA expression levels than in normal organs excluding testis, promoter activity 18.9 higher than in normal lung and renal cells
Manually annotated by BRENDA team
-
osteoblast cell
Manually annotated by BRENDA team
-
osteoblast cell
Manually annotated by BRENDA team
-
osteosarcoma cell line
Manually annotated by BRENDA team