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Serine/threonine-protein kinase PLK1 Inhibitors (IC50, Ki)

Structure
Compound Name
Standard Type
Standard Values (in nM)
BI-2536IC500.83 [1]
BI-2536Ki0.22 [1], 3.0 [2]
[(2R,3S)-3-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-Acetylpyrrolidine-2-carbonyl]amino]-4-methylpentanoyl]amino]-3-[3-(8-phenyloctyl)imidazol-4-yl]propanoyl]amino]-3-hydroxypropanoyl]amino]-4-amino-4-oxobutan-2-yl] dihydrogen phosphateIC5025.0 [1]
StaurosporineIC50540.0 [1]
[(2R,3S)-3-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-Acetylpyrrolidine-2-carbonyl]amino]-4-methylpentanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-3-hydroxypropanoyl]amino]-4-amino-4-oxobutan-2-yl] dihydrogen phosphateIC50300.0 [1], 16000.0 [2], 21500.0 [3], 300000.0 [4]
WortmanninIC505.8 [1], 24.0 [2], 1300.0 [3]
VolasertibIC500.87 [1]
Gsk-461364IC50100.0 [1]
Gsk-461364Ki2.2 [1]
[(2R,3S)-3-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-Acetylpyrrolidine-2-carbonyl]amino]-4-methylpentanoyl]amino]-3-[3-[8-(2-fluoro-6-phenoxyphenyl)octyl]imidazol-4-yl]propanoyl]amino]-3-hydroxypropanoyl]amino]-4-amino-4-oxobutan-2-yl] dihydrogen phosphateIC506.6 [1], 66.0 [2], 127.0 [3]
1-Methyl-8-[5-(4-methylpiperazin-1-yl)-2-(trifluoromethoxy)anilino]-4,5-dihydropyrazolo[4,3-h]quinazoline-3-carboxamideIC501.0 [1], 3.0 [2]
1-Methyl-8-(2-methylanilino)-4,5-dihydropyrazolo[4,3-h]quinazoline-3-carboxamideIC5014.0 [1], 15.0 [2]
4-[2-(2-Hydroxyethoxy)-5-methyl-3-[4-(2H-tetrazol-5-yl)phenyl]phenyl]benzonitrileIC50139000.0 [1], 146000.0 [2], 151000.0 [3]
QuercetinIC505750.0 [1], 64000.0 [2]
2-(4-Morpholinyl)-8-phenyl-4H-1-benzopyran-4-oneIC502000.0 [1], 2100.0 [2]
4-[[(7S)-8-Cyclopentyl-7-ethyl-5-methyl-6-oxo-7H-pteridin-2-yl]amino]-3-methoxy-N-(1-methylpiperidin-4-yl)benzamideIC5032.5 [1]
4-[[(7S)-8-Cyclopentyl-7-ethyl-5-methyl-6-oxo-7H-pteridin-2-yl]amino]-3-methoxy-N-(1-methylpiperidin-4-yl)benzamideKi0.42 [1]
5-(5,6-Dimethoxy-1-benzimidazolyl)-3-[[2-(trifluoromethyl)phenyl]methoxy]-2-thiophenecarboxamideIC502.0 [1]
5-Cyano-7-nitro-3-oxido-1,3-benzothiazol-3-ium-2-carboxamideIC508000.0 [1], 10000.0 [2]
Nms-P937 (nms1286937)IC502.0 [1], 3.0 [2]
8-[2-Methoxy-5-(4-methylpiperazin-1-yl)anilino]-1-methyl-4,5-dihydropyrazolo[4,3-h]quinazoline-3-carboxamideIC507.0 [1], 10.0 [2]
3-[(2-Chlorophenyl)methoxy]-5-(5,6-dimethoxy-1H-1,3-benzodiazol-1-yl)thiophene-2-carboxamideIC502.0 [1]
8-Anilino-1-methyl-4,5-dihydropyrazolo[4,3-h]quinazoline-3-carboxamideIC5068.0 [1]
8-Anilino-N,1-dimethyl-4,5-dihydropyrazolo[4,3-h]quinazoline-3-carboxamideIC504215.0 [1]
4-[4-(4-Methyl-2-methylamino-thiazol-5-YL)-pyrimidin-2-ylamino]-phenolIC5010000.0 [1]
4-[4-(2,4-Dimethyl-thiazol-5-yl)-pyrimidin-2-ylamino]phenolIC505000.0 [1]
5-(1H-Benzimidazol-1-yl)-3-{[2-(trifluoromethyl)benzyl]oxy}thiophene-2-carboxamideIC5015.0 [1], 35.0 [2]
3-[[(2R)-3,3-Dimethylbutan-2-yl]amino]-4-(pyridin-4-ylamino)cyclobut-3-ene-1,2-dioneKi2000.0 [1], 2200.0 [2]
8-Anilino-1-methyl-N-phenyl-4,5-dihydropyrazolo[4,3-h]quinazoline-3-carboxamideIC5010000.0 [1]
Cyclapolin 9IC50500.0 [1], 2400.0 [2]
3-[(E)-[3-[(E)-2-Pyridin-4-ylethenyl]indazol-6-ylidene]methyl]-1H-indol-2-olIC5010000.0 [1], 100000.0 [2]
2-(3-Hydroxy-4-methoxyanilino)-5,7-dihydropyrimido[5,4-d][1]benzazepin-6-oneIC505700.0 [1]
3-Methyl-1-phenyl-N-[(1S)-1-phenylethyl]pyrazolo[4,3-c]pyridin-6-amineIC501301.0 [1]
1-(3-Chlorophenyl)-3-methyl-N-[(1S)-1-phenylethyl]pyrazolo[4,3-c]pyridin-6-amineIC50121.0 [1]
5-(5,6-Dimethoxy-1H-benzimidazol-1-yl)-3-[[4-(methylsulfonyl)phenyl]methoxy]-2-thiophenecarboxamideIC5075.0 [1], 125.89 [2]
(2S,3R)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-Acetylpyrrolidine-2-carbonyl]amino]-4-methylpentanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-3-hydroxypropanoyl]amino]-3-phosphonooxybutanoic acidIC505270.0 [1], 32030.0 [2]
8-(2-Methoxyanilino)-1-methyl-4,5-dihydropyrazolo[4,3-h]quinazoline-3-carboxamideIC5042.0 [1]
8-[5-Amino-2-(trifluoromethoxy)anilino]-1-methyl-4,5-dihydropyrazolo[4,3-h]quinazoline-3-carboxamideIC5060.0 [1], 87.0 [2]
1-Methyl-8-[5-[2-(1-methylpyrrolidin-2-yl)ethylamino]-2-(trifluoromethoxy)anilino]-4,5-dihydropyrazolo[4,3-h]quinazoline-3-carboxamideIC50123.0 [1], 149.0 [2]
1-Methyl-8-(2-(trifluoromethoxy)phenylamino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamideIC50117.0 [1]
6-(2,4-Difluorophenyl)sulfonyl-2-(1H-indol-5-ylamino)-8-methylpyrido[2,3-d]pyrimidin-7-oneIC5010000.0 [1]
N-[(2,6-Dibromo-4-sulfamoylphenyl)carbamothioyl]benzamideIC5039800.0 [1], 95000.0 [2]
[(2R,3S)-3-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-Acetylpyrrolidine-2-carbonyl]amino]-4-methylpentanoyl]amino]-3-[3-[6-[(E)-benzylideneamino]oxyhexyl]imidazol-4-yl]propanoyl]amino]-3-hydroxypropanoyl]amino]-4-amino-4-oxobutan-2-yl] dihydrogen phosphateIC50558.0 [1], 5050.0 [2]
[(2R,3S)-3-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-Acetylpyrrolidine-2-carbonyl]amino]-4-methylpentanoyl]amino]-3-[3-[6-[(Z)-(2-fluoro-6-phenoxyphenyl)methylideneamino]oxyhexyl]imidazol-4-yl]propanoyl]amino]-3-hydroxypropanoyl]amino]-4-amino-4-oxobutan-2-yl] dihydrogen phosphateIC5091.0 [1], 670.0 [2]
[(2R,3S)-3-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-Acetylpyrrolidine-2-carbonyl]amino]-4-methylpentanoyl]amino]-3-[3-[5-[(E)-(2-fluoro-6-phenoxyphenyl)methylideneamino]oxypentyl]imidazol-4-yl]propanoyl]amino]-3-hydroxypropanoyl]amino]-4-amino-4-oxobutan-2-yl] dihydrogen phosphateIC50163.0 [1], 1550.0 [2]
[(2R,3S)-3-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-Acetylpyrrolidine-2-carbonyl]amino]-4-methylpentanoyl]amino]-3-[3-[5-[(E)-benzylideneamino]oxypentyl]imidazol-4-yl]propanoyl]amino]-3-hydroxypropanoyl]amino]-4-amino-4-oxobutan-2-yl] dihydrogen phosphateIC502380.0 [1], 9000.0 [2]
[(2R,3S)-3-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-Acetylpyrrolidine-2-carbonyl]amino]-4-methylpentanoyl]amino]-3-[3-[8-[4-(2-phenylmethoxyethyl)phenyl]octyl]imidazol-4-yl]propanoyl]amino]-3-hydroxypropanoyl]amino]-4-amino-4-oxobutan-2-yl] dihydrogen phosphateIC509.7 [1], 152.0 [2]
[(2R,3S)-3-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-Acetylpyrrolidine-2-carbonyl]amino]-4-methylpentanoyl]amino]-3-[3-[8-[2-fluoro-6-(3-hydroxyphenoxy)phenyl]octyl]imidazol-4-yl]propanoyl]amino]-3-hydroxypropanoyl]amino]-4-amino-4-oxobutan-2-yl] dihydrogen phosphateIC505.5 [1], 188.0 [2]
[(2R,3S)-3-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-Acetylpyrrolidine-2-carbonyl]amino]-4-methylpentanoyl]amino]-3-[3-[8-[2-fluoro-6-(3-phenylmethoxyphenoxy)phenyl]octyl]imidazol-4-yl]propanoyl]amino]-3-hydroxypropanoyl]amino]-4-amino-4-oxobutan-2-yl] dihydrogen phosphateIC5011.2 [1], 862.0 [2]
[(2R,3S)-3-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-Acetylpyrrolidine-2-carbonyl]amino]-4-methylpentanoyl]amino]-3-[3-[8-[4-(2-hydroxyethyl)phenyl]octyl]imidazol-4-yl]propanoyl]amino]-3-hydroxypropanoyl]amino]-4-amino-4-oxobutan-2-yl] dihydrogen phosphateIC505.5 [1], 218.0 [2]
[(1R)-1-[(9S,12S,15S)-15-[[(2S)-2-[[(2S)-1-Acetylpyrrolidine-2-carbonyl]amino]-4-methylpentanoyl]amino]-12-(hydroxymethyl)-8,11,14-trioxo-18-(8-phenyloctyl)-7,10,13,18-tetraza-1-azoniabicyclo[15.2.1]icosa-1(19),17(20)-dien-9-yl]ethyl] dihydrogen phosphateIC506.0 [1], 45.0 [2]
[(1R)-1-[(10S,13S,16S)-16-[[(2S)-2-[[(2S)-1-Acetylpyrrolidine-2-carbonyl]amino]-4-methylpentanoyl]amino]-13-(hydroxymethyl)-9,12,15-trioxo-19-(8-phenyloctyl)-8,11,14,19-tetraza-1-azoniabicyclo[16.2.1]henicosa-1(20),18(21)-dien-10-yl]ethyl] dihydrogen phosphateIC505.0 [1], 44.0 [2]
[(1R)-1-[(8S,11S,14S)-14-[[(2S)-2-[[(2S)-1-Acetylpyrrolidine-2-carbonyl]amino]-4-methylpentanoyl]amino]-11-(hydroxymethyl)-7,10,13-trioxo-17-(8-phenyloctyl)-6,9,12,17-tetraza-1-azoniabicyclo[14.2.1]nonadeca-1(18),16(19)-dien-8-yl]ethyl] dihydrogen phosphateIC5010.0 [1], 160.0 [2]
[(1R)-1-[(9S,12S,15S)-15-Acetamido-12-(hydroxymethyl)-8,11,14-trioxo-18-(8-phenyloctyl)-7,10,13,18-tetraza-1-azoniabicyclo[15.2.1]icosa-1(19),17(20)-dien-9-yl]ethyl] dihydrogen phosphateIC508.0 [1], 370.0 [2]
1-Methyl-8-[5-piperazin-1-yl-2-(trifluoromethoxy)anilino]-4,5-dihydropyrazolo[4,3-h]quinazoline-3-carboxamideIC502.0 [1]
1-Methyl-8-[5-(1-methyl-3,6-dihydro-2H-pyridin-4-yl)-2-(trifluoromethoxy)anilino]-4,5-dihydropyrazolo[4,3-h]quinazoline-3-carboxamideIC503.0 [1], 8.0 [2]
1-Ethenyl-8-[5-(4-methylpiperazin-1-yl)-2-(trifluoromethoxy)anilino]-4,5-dihydropyrazolo[4,3-h]quinazoline-3-carboxamideIC501.0 [1], 6.0 [2]
1-(2-Fluoroethyl)-8-[5-(4-methylpiperazin-1-yl)-2-(trifluoromethoxy)anilino]-4,5-dihydropyrazolo[4,3-h]quinazoline-3-carboxamideIC504.0 [1], 5.0 [2]
1-(2-Chloroethyl)-8-[5-(4-methylpiperazin-1-yl)-2-(trifluoromethoxy)anilino]-4,5-dihydropyrazolo[4,3-h]quinazoline-3-carboxamideIC507.0 [1], 13.0 [2]
ErlotinibIC50100000.0 [1]
Sorafenib tosylateIC5010000.0 [1]
SunitinibIC5010000.0 [1]
LapatinibIC50100000.0 [1]
Ellagic acidIC503340.0 [1]
MorinIC5012600.0 [1]
ThymoquinoneIC502180.0 [1]
AxitinibIC5010000.0 [1]
NintedanibIC5010000.0 [1]
DoramapimodIC5030000.0 [1]
N-[4-[[6-Methoxy-7-[3-(4-morpholinyl)propoxy]-4-quinazolinyl]amino]phenyl]benzamideIC5010000.0 [1]
ReversineIC505000.0 [1]
KenpaulloneIC50100000.0 [1]
Nvp-aew541IC5010000.0 [1]
DanusertibIC503500.0 [1]
ScytoneminIC502000.0 [1]
5-Iodo-3-[(3,5-dibromo-4-hydroxyphenyl)methylene]-2-indolinoneIC504600.0 [1]
RigosertibIC509.0 [1]
4-[[9-Chloro-7-(2,6-difluorophenyl)-5H-pyrimido[5,4-d][2]benzazepin-2-yl]amino]benzoic acidIC5053000.0 [1]
EntrectinibIC5010000.0 [1]
Cfms Receptor Tyrosine Kinase InhibitorIC5024000.0 [1]
Bms-777607IC502000.0 [1]
Azd-1152hqpaKi10000.0 [1]
2-(Pyridin-4-yl)-6,7-dihydro-1H-pyrrolo[3,2-c]pyridin-4(5H)-oneIC50980.0 [1]
Tak-285IC5010000.0 [1]
MilciclibIC5010000.0 [1]
4-Methyl-5-(2-((4-morpholinophenyl)amino)-pyrimidin-4-yl)thiazol-2-amineKi10000.0 [1]
Aminofurazanyl-azabenzimidazole 6nIC5010000.0 [1]
Pha-793887IC5010000.0 [1]
CFI-400945 (free base)IC5050000.0 [1]
TCS JNK 5aIC5010000.0 [1]
NorlichexanthoneIC5075700.0 [1]
CID 44556162IC5010000.0 [1]
N6-Cyclohexyl-N2-(2-methyl-4-morpholinophenyl)-9H-purine-2,6-diamineIC505000.0 [1]
CID 53357478IC502.0 [1]
PoloxinIC5029400.0 [1]
JNK Inhibitor VIIIKi8900.0 [1]
IKK-3 InhibitorIC50794.33 [1]
CID 11634725Ki4000.0 [1]
CID 25015677IC504.0 [1]
3-(1H-Indol-3-yl)-4-(3,4,5-trimethoxyphenyl)pyrrole-2,5-dioneIC50100000.0 [1]



References

This online tool may be cited as follows

MLA

"Quest Database™ Serine/threonine-protein kinase PLK1 Inhibitors (IC50, Ki)." AAT Bioquest, Inc.21 Dec2024https://www.aatbio.com/data-sets/serine-threonine-protein-kinase-plk1-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2024December 21). Quest Database™ Serine/threonine-protein kinase PLK1 Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/serine-threonine-protein-kinase-plk1-inhibitors-ic50-ki.
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