Information on EC 2.7.11.21 - polo kinase

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The expected taxonomic range for this enzyme is: Eukaryota

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
REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
phospho group transfer
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
diverse strains
-
-
Manually annotated by BRENDA team
Saccharomyces pombe
-
-
-
Manually annotated by BRENDA team
-
UniProt
Manually annotated by BRENDA team
-
-
-
Manually annotated by BRENDA team
-
-
-
Manually annotated by BRENDA team
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
malfunction
physiological function
SUBSTRATE
PRODUCT                       
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
ATP + 5FAM-RALMEASFADQAR-NH2
ADP + phosphorylated 5FAM-RALMEASFADQAR-NH2
show the reaction diagram
substrate peptide, based on human Cdc25C, used in biochemical activity assay
-
-
?
ATP + 85kDa microtubule-associated protein
ADP + phosphorylated 85kDa microtubule-associated protein
show the reaction diagram
ATP + a protein
ADP + a phosphoprotein
show the reaction diagram
ATP + abnormal spindle pole protein
ADP + phosphorylated abnormal spindle pole protein
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 + Bem3
ADP + phosphorylated Bem3
show the reaction diagram
-
bound by the polo-box domain of Cdc5
-
-
?
ATP + beta-casein
ADP + phosphorylated beta-casein
show the reaction diagram
-
-
-
-
?
ATP + beta-tubulin
ADP + phosphorylated beta-tubulin
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 + a phosphorylated casein
show the reaction diagram
-
activity assay
-
-
?
ATP + casein
ADP + phosphocasein
show the reaction diagram
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 + Cdc25
ADP + phosphorylated Cdc25
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 + Cdh1
ADP + phosphorylated Cdh1
show the reaction diagram
-
-
-
-
?
ATP + centromeric protein PBIP1
ADP + phosphorylated centromeric protein PBIP1
show the reaction diagram
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 + claspin
ADP + phosphorylated claspin
show the reaction diagram
ATP + cohesin
ADP + phosphorylated cohesin
show the reaction diagram
ATP + cyclin B
ADP + phosphorylated cyclin B
show the reaction diagram
ATP + cyclin B1
ADP + phosphorylated cyclin B
show the reaction diagram
-
phosphorylation at S101, not at S113 in the cytoplasmic retention sequence
-
-
?
ATP + Ecm25
ADP + phosphorylated Ecm25
show the reaction diagram
-
bound by the polo-box domain of Cdc5
-
-
?
ATP + Ect2
ADP + phosphorylated Ect2
show the reaction diagram
-
-
-
-
?
ATP + Emi2
ADP + phosphorylated Emi2
show the reaction diagram
ATP + Fkh2p
ADP + phosphorylated Fkh2p
show the reaction diagram
-
Fkh2p is only poorly phosphorylated by Cdc5p, Fkh2p has a function in nucleating the formation of a Fkh2p-Ndd1p-Cdc5p complex on CLB2 cluster promoters, and the subsequent Cdc5p-dependent phosphorylation of Ndd1p at Ser 85
-
-
?
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
ATP + histone H1 kinase
ADP + phosphorylated histone H1 kinase
show the reaction diagram
-
activation
-
-
?
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 + Mad3
ADP + phosphorylated Mad3
show the reaction diagram
ATP + MEI-S332 protein
ADP + phosphorylated MEI-S332 protein
show the reaction diagram
ATP + MEX-5
ADP + phosphorylated MEX-5
show the reaction diagram
-
-
-
-
?
ATP + Mid1p
ADP + phosphorylated Mid1p
show the reaction diagram
ATP + Myt1
ADP + phosphorylated Myt1
show the reaction diagram
ATP + Ndd1p
ADP + phosphorylated Ndd1p
show the reaction diagram
-
phosphorylation of Ser 85, phosphorylation is required for the normal temporal expression of cell-cycle-regulated genes such as CLB2 and SWI5 in G2/M phase
-
-
?
ATP + Nud1
ADP + phosphorylated Nud1
show the reaction diagram
-
Cdc5 and Cdc28 activities are required for proper phosphorylation of Nud1
-
-
?
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 + 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 + protein p110
ADP + ?
show the reaction diagram
-
-
-
-
?
ATP + Rom2
ADP + phosphorylated Rom2
show the reaction diagram
-
bound by the polo-box domain of Cdc5
-
-
?
ATP + Sac7
ADP + phosphorylated Sac7
show the reaction diagram
-
bound by the polo-box domain of Cdc5
-
-
?
ATP + SCC1 cohesin
ADP + phosphorylated SCC1 cohesin
show the reaction diagram
-
-
-
-
?
ATP + Slk19
ADP + phosphorylated Slk19
show the reaction diagram
-
Cdc5 and Cdc28 activities are required for proper phosphorylation of Slk19
-
-
?
ATP + Stu2
ADP + phosphorylated Stu2
show the reaction diagram
-
Cdc5 and Cdc28 activities are required for proper phosphorylation of Stu2
-
-
?
ATP + SYK tyrosine kinase
ADP + phosphorylated SYK tyrosine kinase
show the reaction diagram
-
-
-
-
?
ATP + TbCentrin2
ADP + ?
show the reaction diagram
-
-
-
-
?
ATP + TPSDSLIYDDGLS
ADP + phosphorylated TPSDSLIYDDGLS
show the reaction diagram
-
-
-
?
ATP + TRF1
ADP + phosphorylated TRF1
show the reaction diagram
ATP + Tus1
ADP + phosphorylated Tus1
show the reaction diagram
-
bound by the polo-box domain of Cdc5
-
-
?
ATP + viral phosphoprotein P
ADP + phosphorylated viral phosphoprotein P
show the reaction diagram
-
PLK1 directly phosphorylates viral phosphoprotein P of paramyxovirus in vitro
-
-
?
ATP + Wee1
ADP + phosphorylated Wee1
show the reaction diagram
-
-
-
-
?
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
ATP + 85kDa microtubule-associated protein
ADP + phosphorylated 85kDa microtubule-associated protein
show the reaction diagram
-
protein is released from microtubules after phosphorylation
-
-
?
ATP + a protein
ADP + a phosphoprotein
show the reaction diagram
ATP + abnormal spindle pole protein
ADP + phosphorylated abnormal spindle pole protein
show the reaction diagram
-
i.e. abnormal spindle pole protein, activation of abnormal spindle pole protein by phosphorylation
-
-
?
ATP + beta-tubulin
ADP + phosphorylated beta-tubulin
show the reaction diagram
-
the enzyme is required for beta-tubulin recruitment to the centrosome
-
-
?
ATP + BubR1
ADP + phosphorylated BubR1
show the reaction diagram
-
S676 is an in vivo Plk1 phosphorylation site in BubR1
-
-
?
ATP + casein
ADP + phosphorylated casein
show the reaction diagram
-
kinase assay
-
-
?
ATP + Cdc25C
ADP + phosphorylated Cdc25C
show the reaction diagram
-
phosphorylation by Plk1 on Ser198 in a nuclear export signal sequence promoting its nuclear translocation, inhibition of Cdc25 activation resulting in a delay in Cdc2 activation
-
-
?
ATP + Chk2
ADP + phosphorylated Chk2
show the reaction diagram
ATP + claspin
ADP + phosphorylated claspin
show the reaction diagram
-
Plx1 is involved in alleviating DNA replication checkpoint response by inactivation of claspin through phosphorylation
-
-
?
ATP + cohesin
ADP + phosphorylated cohesin
show the reaction diagram
-
phosphorylation by Cdc5 required for removal of cohesin from chromosomes
-
-
?
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 + cyclin B1
ADP + phosphorylated cyclin B
show the reaction diagram
-
phosphorylation at S101, not at S113 in the cytoplasmic retention sequence
-
-
?
ATP + Emi2
ADP + phosphorylated Emi2
show the reaction diagram
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 + Mad3
ADP + phosphorylated Mad3
show the reaction diagram
-
phosphorylation of Mad3 isozymes at 5 serine residues, S222, S380, S466, S504, and especially at S268, during spindle checkpoint activation, Mad3 is an inhibitor of Cdc20/APC ubiquitin ligase, overview
-
-
?
ATP + MEI-S332 protein
ADP + phosphorylated MEI-S332 protein
show the reaction diagram
ATP + Mid1p
ADP + phosphorylated Mid1p
show the reaction diagram
-
required for positioning of division sites in cytokinesis
-
-
?
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 + 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 + Rom2
ADP + phosphorylated Rom2
show the reaction diagram
-
bound by the polo-box domain of Cdc5
-
-
?
ATP + TRF1
ADP + phosphorylated TRF1
show the reaction diagram
-
the cell-cycle-dependent TRF1 recruitment to telomere chromatin is regulated by the enzyme, TRF1 binds the telomere via the telomeric repeats, process overview
-
-
?
ATP + Tus1
ADP + phosphorylated Tus1
show the reaction diagram
-
bound by the polo-box domain of Cdc5
-
-
?
additional information
?
-
METALS and IONS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
Ca2+
-
Emi2 only associates with Plx1 after Ca2+ addition, Ca2+-induced Emi2-Plx1 association in cytostatic factor extract relies mostly on the 192RSST motif, whereas the 333RLST motif contributes only slightly to Plx1 binding
INHIBITORS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(3-[5-methyl-2-[(3,4,5-trimethoxyphenyl)amino]imidazo[5,1-f][1,2,4]triazin-7-yl]phenyl)(phenyl)methanone
-
-
(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
-
; good selectivity over Plk-1 (193-fold), good permeability and moderate microsomal stability. When dosed orally in rats, the inhibitor demonstrates a 41-45% reduction of pS129-a-synuclein levels in the cerebral cortex
(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
-
;
(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
-
;
(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-fluorophenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
-
-
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-(2-methoxyphenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
-
-
1-(3,5-dichlorophenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
-
-
1-(3,5-dimethylphenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
-
-
1-(3-bromo-5-chlorophenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
-
-
1-(3-chlorophenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
-
-
1-(3-fluorophenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
-
-
1-(3-methoxyphenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
-
-
1-(4-fluorophenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
-
-
1-(4-methoxyphenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
-
-
1-(5-methyl-2-trifluoro-methyl-furan-3-yl)-3-(5-[2-[6-(1H-[1,2,4]triazol-3-ylamino)-pyrimidin-4-ylamino]-ethyl]-thiazol-2-yl)urea
-
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-[3-(3-aminopropyl)phenyl]-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
-
-
1-[3-(dimethylamino)phenyl]-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
-
-
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-(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-[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-(1-[2-chloro-4-[(3-hydroxypyrrolidin-1-yl)methyl]phenyl]ethoxy)-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
-
-
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-methyl-6-[[(1S)-1-phenylethyl]amino]-1H-pyrazolo[4,3-c]pyridin-1-yl)benzonitrile
-
-
3-(3-methylphenyl)-N-[(1S)-1-phenylethyl]isoxazolo[5,4-c]pyridin-5-amine
; >0.01
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-methyl-1-(2-methylphenyl)-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
-
-
3-methyl-1-(3-methylphenyl)-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
-
-
3-methyl-1-(4-methylphenyl)-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
-
-
3-methyl-1-phenyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
-
-
3-methyl-1-[3-(1-methylethyl)phenyl]-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
-
-
3-methyl-1-[3-(methylsulfonyl)phenyl]-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
-
-
3-phenyl-N-[(1S)-1-phenylethyl]isoxazolo[5,4-c]pyridin-5-amine
-
3-[(1R)-1-(2-chloro-4-[[(1-methylethyl)amino]methyl]phenyl)ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
-
-
3-[(1R)-1-(2-chloro-4-[[(2-hydroxy-1,1-dimethylethyl)amino]methyl]phenyl)ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
-
-
3-[(1R)-1-(2-chloro-4-[[(2-hydroxyethyl)amino]methyl]phenyl)ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
-
-
3-[(1R)-1-(2-chloro-4-[[(3-hydroxypropyl)amino]methyl]phenyl)ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
-
-
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-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
-
-
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-[6-(hydroxymethyl)imidazo[1,2-a]pyridin-3-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-[(1R)-1-[2-(hydroxymethyl)phenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
-
-
3-[(1R)-1-[2-chloro-4-(hydroxymethyl)phenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
-
-
3-[(1R)-1-[2-chloro-4-[(1,1-dioxidothiomorpholin-4-yl)methyl]phenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
-
-
3-[(1R)-1-[2-chloro-4-[(3-oxopiperazin-1-yl)methyl]phenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
-
-
3-[(1R)-1-[2-chloro-4-[(4-fluoropiperidin-1-yl)methyl]phenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
-
-
3-[(1R)-1-[2-chloro-4-[(4-hydroxypiperidin-1-yl)methyl]phenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
-
-
3-[(1R)-1-[2-chloro-4-[(4-methylpiperazin-1-yl)methyl]phenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
-
-
3-[(1R)-1-[2-chloro-4-[(cyclopentylamino)methyl]phenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
-
-
3-[(1R)-1-[2-chloro-4-[(cyclopropylamino)methyl]phenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
-
-
3-[(1R)-1-[2-chloro-4-[(dimethylamino)methyl]phenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
-
-
3-[(1R)-1-[2-chloro-4-[(ethylamino)methyl]phenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
-
-
3-[(1R)-1-[2-chloro-4-[(methylamino)methyl]phenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
-
-
3-[(1R)-1-[4-[(tert-butylamino)methyl]-2-(difluoromethoxy)phenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
-
tested in rat xenograft model
3-[(1R)-1-[4-[(tert-butylamino)methyl]-2-(difluoromethyl)phenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
-
-
3-[(1R)-1-[4-[(tert-butylamino)methyl]-2-chlorophenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
-
-
3-[(1R)-1-[4-[(tert-butylamino)methyl]-2-cyclopropylphenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
-
-
3-[(1R)-1-[4-[(tert-butylamino)methyl]-2-fluorophenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
-
-
3-[(1R)-1-[4-[(tert-butylamino)methyl]-2-methylphenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
-
-
3-[(1S)-1-(2-chlorophenyl)ethoxy]-5-(5,6-dimethoxy-1H-benzimidazol-1-yl)thiophene-2-carboxamide
-
-
3-[(1S)-1-(2-chlorophenyl)ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
-
-
3-[(2-chlorobenzyl)oxy]-5-(5,6-dimethoxy-1H-benzimidazol-1-yl)thiophene-2-carboxamide
-
-
3-[(2-chlorobenzyl)oxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
-
-
3-[1-(2-chlorophenyl)ethoxy]-5-[7-(hydroxymethyl)imidazo[1,2-a]pyridin-3-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-chloro-5-(hydroxymethyl)phenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
-
-
3-[3-(3-methyl-6-[[(1S)-1-phenylethyl]amino]-1H-pyrazolo[4,3-c]pyridin-1-yl)phenyl]propanamide
-
-
3-[3-(3-methyl-6-[[(1S)-1-phenylethyl]amino]-1H-pyrazolo[4,3-c]pyridin-1-yl)phenyl]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-[(5-methyl-7-phenylimidazo[5,1-f][1,2,4]triazin-2-yl)amino]benzenesulfonamide
-
-
4-[7-ethyl-2-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5-methyl-6-oxo-6,7-dihydropteridin-8(5H)-yl]benzonitrile
-
;
5-(1-methyl-1H-imidazol-5-yl)-3-[[2-(trifluoromethyl)benzyl]oxy]thiophene-2-carboxamide
-
-
5-(1H-benzimidazol-1-yl)-3-[[2-(trifluoromethyl)benzyl]oxy]thiophene-2-carboxamide
-
-
5-(2-amino-1,3-thiazol-5-yl)-3-[[2-(trifluoromethyl)benzyl]oxy]thiophene-2-carboxamide
-
-
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
-
i.e. GW843682X, inhibition of PLK1 activity abrogates mitotic activation of AMP-activated protein kinasealpha through direct or indirect mechanisms
-
5-(5,6-dimethoxy-1H-benzimidazol-1-yl)-3-[[2-(trifluoromethyl)benzyl]oxy]thiophene-2-carboxamide
-
-
5-(5,6-dimethoxy-1H-benzimidazole-1-yl)-3-[2-(trifluoromethyl)-benzyloxy]-thiophene-2-carboxamide
-
GW843682X
5-(6-methoxy-1H-benzimidazol-1-yl)-3-[(1R)-1-[2-(trifluoromethyl)phenyl]ethoxy]thiophene-2-carboxamide
-
-
5-imidazo[1,2-a]pyridin-3-yl-3-[[2-(trifluoromethyl)benzyl]oxy]thiophene-2-carboxamide
-
-
5-methyl-7-(2-nitrophenyl)-N-(3,4,5-trimethoxyphenyl)imidazo[5,1-f][1,2,4]triazin-2-amine
-
-
5-methyl-7-(3-phenoxyphenyl)-N-(3,4,5-trimethoxyphenyl)imidazo[5,1-f][1,2,4]triazin-2-amine
-
-
5-methyl-7-phenyl-N-(2-pyridin-4-ylethyl)imidazo[5,1-f][1,2,4]triazin-2-amine
-
>0.010
5-methyl-7-phenyl-N-(3,4,5-trimethoxyphenyl)imidazo[5,1-f][1,2,4]triazin-2-amine
-
-
5-methyl-7-phenyl-N-[3-(trifluoromethyl)phenyl]imidazo[5,1-f][1,2,4]triazin-2-amine
-
>0.010
5-methyl-7-phenylimidazo[5,1-f][1,2,4]triazin-2-amine
-
>0.010
5-methyl-7-[3-(trifluoromethyl)phenyl]-N-(3,4,5-trimethoxyphenyl)imidazo[5,1-f][1,2,4]triazin-2-amine
-
-
5-methyl-7-[4-(trifluoromethyl)phenyl]-N-(3,4,5-trimethoxyphenyl)imidazo[5,1-f][1,2,4]triazin-2-amine
-
-
5-methyl-N,7-diphenylimidazo[5,1-f][1,2,4]triazin-2-amine
-
-
5-methyl-N-(3-morpholin-4-ylpropyl)-7-phenylimidazo[5,1-f][1,2,4]triazin-2-amine
-
>0.010
5-methyl-N-(4-nitrophenyl)-7-phenylimidazo[5,1-f][1,2,4]triazin-2-amine
-
-
5-pyrazolo[1,5-a]pyridin-3-yl-3-[[2-(trifluoromethyl)benzyl]oxy]thiophene-2-carboxamide
-
-
5-[2-(phenylamino)-1,3-thiazol-5-yl]-3-[[2-(trifluoromethyl)benzyl]oxy]thiophene-2-carboxamide
-
-
5-[2-[(phenylcarbonyl)amino]-1,3-thiazol-5-yl]-3-[[2-(trifluoromethyl)benzyl]oxy]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-(2-bromophenyl)-5-methyl-N-(3,4,5-trimethoxyphenyl)imidazo[5,1-f][1,2,4]triazin-2-amine
-
-
7-(2-methoxyphenyl)-5-methyl-N-(3,4,5-trimethoxyphenyl)imidazo[5,1-f][1,2,4]triazin-2-amine
-
-
7-(3-bromophenyl)-5-methyl-N-(3,4,5-trimethoxyphenyl)imidazo[5,1-f][1,2,4]triazin-2-amine
-
-
7-(4-fluorophenyl)-5-methyl-N-(3,4,5-trimethoxyphenyl)imidazo[5,1-f][1,2,4]triazin-2-amine
-
-
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
-
;
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
-
selective inhibition of PLK4 relative to PLK1-3
AMPPNP
-
-
ataxia-telangiectasia mutant
-
i.e. ATM, inhibits p53 phosphorylation by Plk1 in vivo
-
BAY 439006
-
selective inhibition of PLK4 relative to PLK1-3
BI 2536
BI-2536
BI2536
BI6727
-
-
-
CHIR-258
-
; selectivity profile of PLK2/4 over PLK1/3; selectivity profile of PLK2/4 over PLK1/3
CP 547632
-
selective inhibition of PLK4 relative to PLK1-3
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
-
-
genistein
-
decreases Plk1 expression
GO 6976
-
; loses PLK1 activity by at least an order of magnitude, relative to staurosporine; loses PLK2 activity by at least an order of magnitude, relative to staurosporine; loses PLK3 activity by at least an order of magnitude, relative to staurosporine
GSK 461364
-
-
GSK461364
-
-
GSK461364A
GW843682
-
-
-
GW843682X
H-1152
-
selective inhibition of PLK4 relative to PLK1-3
HMN-214
-
-
-
imatinib
-
selective inhibition of PLK4 relative to PLK1-3
indirubin
-
decreases Plk1 expression
LY294002
Map205
-
Map205 can stabilize Polo and inhibit its cellular activity in vivo
-
matrimony
-
the matrimony protein acts as a negative regulator of polo during the later stages of G2 arrest during meiosis
-
methyl 2-[(3-carbamoyl-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazolin-8-yl)amino]benzoate
-
-
-
N,1-dimethyl-8-(phenylamino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
N-(2-hydroxyethyl)-3-[3-(3-methyl-6-[[(1S)-1-phenylethyl]amino]-1H-pyrazolo[4,3-c]pyridin-1-yl)phenyl]propanamide
-
-
N-(3,4-dimethoxyphenyl)-5-methyl-7-phenylimidazo[5,1-f][1,2,4]triazin-2-amine
-
-
N-(3-methoxyphenyl)-5-methyl-7-phenylimidazo[5,1-f][1,2,4]triazin-2-amine
-
-
N-(4-methoxyphenyl)-5-methyl-7-phenylimidazo[5,1-f][1,2,4]triazin-2-amine
-
-
N-benzyl-5-methyl-7-phenylimidazo[5,1-f][1,2,4]triazin-2-amine
-
-
N-cyclohexyl-5-methyl-7-phenylimidazo[5,1-f][1,2,4]triazin-2-amine
-
>0.010
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-(3-methyl-6-[[(1S)-1-phenylethyl]amino]-1H-pyrazolo[4,3-c]pyridin-1-yl)phenyl]-2-phenylacetamide
-
-
N-[4-[(6-chloropyridin-3-yl)methoxy]-3-methoxybenzyl]-2-(3,4-dimethoxyphenyl)ethanamine
-
SBE13
N-[4-[2-(dimethylamino)ethoxy]phenyl]-5-methyl-7-phenylimidazo[5,1-f][1,2,4]triazin-2-amine
-
-
ON-01910
-
-
-
ON01910.Na
-
-
-
ONO1910
-
; does not significantly impacting Plk3 activity in vitro; inhibits Plk1 activity without significantly impacting Plk3 activity in vitro
PHA-680626
-
; selective against Plk1
Purpurogallin
-
polo box inhibitor
quercetin
scytonemin
silibinin
-
decreases Plk1 expression
staurosporine
SU11248
-
selective inhibition of PLK4 relative to PLK1-3
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
-
polo box inhibitor
trichostatin A
-
decreases Plk1 expression
Vanillin
-
decreases Plk1 expression
VX-680
-
selective inhibition of PLK4 relative to PLK1-3
Wortmannin
additional information
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
aurora A
basic fibroblast growth factor
-
bFGF, extracellular stimuli to induce NS-1 cell differentiation
-
Bora
-
Plk1 activity is increased upon phosphorylation at threonine-210 by Aurora A in conjunction with Bora
-
dibutyryl cAMP
-
dbcAMP, extracellular stimuli to induce NS-1 cell differentiation
forskolin
-
extracellular stimuli to induce NS-1 cell differentiation
interleukin-6
-
IL-6, extracellular stimuli to induce NS-1 cell differentiation
nerve growth factor
-
NGF, extracellular stimuli to induce NS-1 cell differentiation
-
nocodazole
-
-
okadaic acid
-
-
pituitary adenylate cyclase-activating polypeptide 38
-
PACAP38, extracellular stimuli to induce NS-1 cell differentiation
-
additional information
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.0002 - 0.0076
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
0.00085
4-amino-5-fluoro-3-[6-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]quinolin-2-ol
-
-
0.0000042 - 0.02
AG-013736
0.00024 - 0.03
BAY 439006
0.000001 - 0.02
BI 2536
0.0014 - 0.02
CHIR-258
0.00012 - 0.02
CP 547632
0.0000034 - 0.019
GO 6976
0.0000005
GSK461364A
-
Ki, apparent dissociation constant, less than 0.0000005
0.00012 - 0.02
H-1152
0.0022 - 0.02
imatinib
0.0061 - 0.02
LY294002
0.02
N-methyl-2-({3-[(E)-2-(pyridin-2-yl)ethenyl]-2H-indazol-6-yl}sulfanyl)benzenecarboximidic acid
-
;
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 - 0.02
PP1
0.0000026 - 0.0012
staurosporine
0.0003 - 0.02
SU11248
0.02
VX-680
-
-
0.0015 - 0.02
Wortmannin
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.00041
(3-[5-methyl-2-[(3,4,5-trimethoxyphenyl)amino]imidazo[5,1-f][1,2,4]triazin-7-yl]phenyl)(phenyl)methanone
Mammalia
-
-
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
-
22C, 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, 25C
-
0.004516
1-(2-fluorophenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
Danio rerio
-
-
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
0.01445
1-(2-methoxyphenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
Danio rerio
-
-
0.000641
1-(3,5-dichlorophenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
Danio rerio
-
-
0.000149
1-(3,5-dimethylphenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
Danio rerio
-
-
0.000274
1-(3-bromo-5-chlorophenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
Danio rerio
-
-
0.000121
1-(3-chlorophenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
Danio rerio
-
-
0.000464
1-(3-fluorophenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
Danio rerio
-
-
0.005928
1-(3-methoxyphenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
Danio rerio
-
-
0.003241
1-(4-fluorophenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
Danio rerio
-
-
0.000703
1-(4-methoxyphenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
Danio rerio
-
-
0.000143
1-cyclohexyl-8-(phenylamino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Homo sapiens
-
pH 7.9, 25C
-
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, 25C
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, 25C
-
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, 25C
-
0.01
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
Homo sapiens
-
larger than 0.010, pH 7.9, 25C
-
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, 25C
-
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, 25C
-
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, 25C
-
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, 25C
-
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, 25C
0.01
1-methyl-N-phenyl-8-(phenylamino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
0.000059
1-[3-(3-aminopropyl)phenyl]-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
Danio rerio
-
-
0.000977
1-[3-(dimethylamino)phenyl]-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
Danio rerio
-
-
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
0.00271
2-[2-(4-fluorophenyl)-1H-imidazol-1-yl]-5,7,7-trimethyl-8-(propan-2-yl)-7,8-dihydropteridin-6(5H)-one
Homo sapiens
-
22C, 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
0.00002
3-(1-[2-chloro-4-[(3-hydroxypyrrolidin-1-yl)methyl]phenyl]ethoxy)-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
Mammalia
-
-
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
-
0.000412
3-(3-methyl-6-[[(1S)-1-phenylethyl]amino]-1H-pyrazolo[4,3-c]pyridin-1-yl)benzonitrile
Danio rerio
-
-
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
0.007685
3-methyl-1-(2-methylphenyl)-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
Danio rerio
-
-
0.000474
3-methyl-1-(3-methylphenyl)-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
Danio rerio
-
-
0.004528
3-methyl-1-(4-methylphenyl)-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
Danio rerio
-
-
0.001301
3-methyl-1-phenyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
Danio rerio
-
-
0.001476
3-methyl-1-[3-(1-methylethyl)phenyl]-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
Danio rerio
-
-
0.000225
3-methyl-1-[3-(methylsulfonyl)phenyl]-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
Danio rerio
-
-
0.001616
3-phenyl-N-[(1S)-1-phenylethyl]isoxazolo[5,4-c]pyridin-5-amine
Homo sapiens
Q9H4B4
-
0.000028
3-[(1R)-1-(2-chloro-4-[[(1-methylethyl)amino]methyl]phenyl)ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
Mammalia
-
-
0.000023
3-[(1R)-1-(2-chloro-4-[[(2-hydroxy-1,1-dimethylethyl)amino]methyl]phenyl)ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
Mammalia
-
-
0.000021
3-[(1R)-1-(2-chloro-4-[[(2-hydroxyethyl)amino]methyl]phenyl)ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
Mammalia
-
-
0.000019
3-[(1R)-1-(2-chloro-4-[[(3-hydroxypropyl)amino]methyl]phenyl)ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
Mammalia
-
-
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
0.000061 - 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
0.000007
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
Mammalia
-
-
0.0000073
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-[6-(hydroxymethyl)imidazo[1,2-a]pyridin-3-yl]thiophene-2-carboxamide
Mammalia
-
-
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
0.000088
3-[(1R)-1-[2-(hydroxymethyl)phenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
Mammalia
-
-
0.0000049
3-[(1R)-1-[2-chloro-4-(hydroxymethyl)phenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
Mammalia
-
-
0.000016
3-[(1R)-1-[2-chloro-4-[(1,1-dioxidothiomorpholin-4-yl)methyl]phenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
Mammalia
-
-
0.000012
3-[(1R)-1-[2-chloro-4-[(3-oxopiperazin-1-yl)methyl]phenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
Mammalia
-
-
0.000013
3-[(1R)-1-[2-chloro-4-[(4-fluoropiperidin-1-yl)methyl]phenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
Mammalia
-
-
0.000027
3-[(1R)-1-[2-chloro-4-[(4-hydroxypiperidin-1-yl)methyl]phenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
Mammalia
-
-
0.000017
3-[(1R)-1-[2-chloro-4-[(4-methylpiperazin-1-yl)methyl]phenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
Mammalia
-
-
0.000025
3-[(1R)-1-[2-chloro-4-[(cyclopentylamino)methyl]phenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
Mammalia
-
-
0.000012
3-[(1R)-1-[2-chloro-4-[(cyclopropylamino)methyl]phenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
Mammalia
-
-
0.000022
3-[(1R)-1-[2-chloro-4-[(dimethylamino)methyl]phenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
Mammalia
-
-
0.000021
3-[(1R)-1-[2-chloro-4-[(ethylamino)methyl]phenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
Mammalia
-
-
0.000016
3-[(1R)-1-[2-chloro-4-[(methylamino)methyl]phenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
Mammalia
-
-
0.0000098
3-[(1R)-1-[4-[(tert-butylamino)methyl]-2-(difluoromethoxy)phenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
Mammalia
-
-
0.00002
3-[(1R)-1-[4-[(tert-butylamino)methyl]-2-(difluoromethyl)phenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
Mammalia
-
-
0.000021
3-[(1R)-1-[4-[(tert-butylamino)methyl]-2-chlorophenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
Mammalia
-
-
0.00021
3-[(1R)-1-[4-[(tert-butylamino)methyl]-2-cyclopropylphenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
Mammalia
-
-
0.000046
3-[(1R)-1-[4-[(tert-butylamino)methyl]-2-fluorophenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
Mammalia
-
-
0.00015
3-[(1R)-1-[4-[(tert-butylamino)methyl]-2-methylphenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
Mammalia
-
-
0.00003 - 0.000994
3-[(1S)-1-(2-chlorophenyl)ethoxy]-5-(5,6-dimethoxy-1H-benzimidazol-1-yl)thiophene-2-carboxamide
0.0003
3-[(1S)-1-(2-chlorophenyl)ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
Mammalia
-
-
0.000002 - 0.00114
3-[(2-chlorobenzyl)oxy]-5-(5,6-dimethoxy-1H-benzimidazol-1-yl)thiophene-2-carboxamide
0.000035
3-[(2-chlorobenzyl)oxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
Mammalia
-
-
0.000092
3-[1-(2-chlorophenyl)ethoxy]-5-[7-(hydroxymethyl)imidazo[1,2-a]pyridin-3-yl]thiophene-2-carboxamide
Mammalia
-
-
0.007479
3-[1-(5-[[(1S)-1-phenylethyl]amino]isoxazolo[5,4-c]pyridin-3-yl)piperidin-3-yl]propanamide
Homo sapiens
Q9H4B4
-
0.000039
3-[1-[2-chloro-5-(hydroxymethyl)phenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
Mammalia
-
-
0.000032
3-[3-(3-methyl-6-[[(1S)-1-phenylethyl]amino]-1H-pyrazolo[4,3-c]pyridin-1-yl)phenyl]propanamide
Danio rerio
-
-
0.000021
3-[3-(3-methyl-6-[[(1S)-1-phenylethyl]amino]-1H-pyrazolo[4,3-c]pyridin-1-yl)phenyl]propanoic acid
Danio rerio
-
-
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
-
-
-
0.00274
4-[(5-methyl-7-phenylimidazo[5,1-f][1,2,4]triazin-2-yl)amino]benzenesulfonamide
Mammalia
-
-
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
0.00043
5-(1-methyl-1H-imidazol-5-yl)-3-[[2-(trifluoromethyl)benzyl]oxy]thiophene-2-carboxamide
Mammalia
-
-
0.000035
5-(1H-benzimidazol-1-yl)-3-[[2-(trifluoromethyl)benzyl]oxy]thiophene-2-carboxamide
Mammalia
-
-
0.003
5-(2-amino-1,3-thiazol-5-yl)-3-[[2-(trifluoromethyl)benzyl]oxy]thiophene-2-carboxamide
Mammalia
-
larger than 0.003
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
0.0000022 - 0.0013
5-(5,6-dimethoxy-1H-benzimidazole-1-yl)-3-[2-(trifluoromethyl)-benzyloxy]-thiophene-2-carboxamide
0.000003 - 0.000476
5-(6-methoxy-1H-benzimidazol-1-yl)-3-[(1R)-1-[2-(trifluoromethyl)phenyl]ethoxy]thiophene-2-carboxamide
0.000022
5-imidazo[1,2-a]pyridin-3-yl-3-[[2-(trifluoromethyl)benzyl]oxy]thiophene-2-carboxamide
Mammalia
-
-
0.00198
5-methyl-7-(2-nitrophenyl)-N-(3,4,5-trimethoxyphenyl)imidazo[5,1-f][1,2,4]triazin-2-amine
Mammalia
-
-
0.0005
5-methyl-7-(3-phenoxyphenyl)-N-(3,4,5-trimethoxyphenyl)imidazo[5,1-f][1,2,4]triazin-2-amine
Mammalia
-
-
0.01
5-methyl-7-phenyl-N-(2-pyridin-4-ylethyl)imidazo[5,1-f][1,2,4]triazin-2-amine
Mammalia
-
>0.010
0.00004
5-methyl-7-phenyl-N-(3,4,5-trimethoxyphenyl)imidazo[5,1-f][1,2,4]triazin-2-amine
Mammalia
-
-
0.01
5-methyl-7-phenyl-N-[3-(trifluoromethyl)phenyl]imidazo[5,1-f][1,2,4]triazin-2-amine
0.00003
5-methyl-7-[3-(trifluoromethyl)phenyl]-N-(3,4,5-trimethoxyphenyl)imidazo[5,1-f][1,2,4]triazin-2-amine
Mammalia
-
-