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Serine/threonine-protein kinase PLK4 Inhibitors (IC50, Ki)

Structure
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Compound Name
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Standard Type
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Standard Values (in nM)
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AxitinibIC5043.0 [1], 46.0 [2]
AxitinibKi4.2 [1]
CFI-400945 (free base)IC502.8 [1]
CFI-400945 (free base)Ki0.26 [1]
3-[(E)-[3-[(E)-2-[4-[(Dimethylamino)methyl]phenyl]ethenyl]indazol-6-ylidene]methyl]-1H-indol-2-olIC502.0 [1], 4.0 [2]
TozasertibKi11.0 [1]
3-[(E)-[3-[(E)-2-Pyridin-4-ylethenyl]indazol-6-ylidene]methyl]-1H-indol-2-olIC502.4 [1], 5.4 [2]
5-Methoxy-3-[(E)-[3-[(E)-2-[6-(4-methylpiperazin-1-yl)pyridin-3-yl]ethenyl]indazol-6-ylidene]methyl]-1H-indol-2-olIC500.61 [1], 7.3 [2]
(2'S,3R)-5-Methoxy-2'-[3-[(E)-2-[4-(morpholin-4-ylmethyl)phenyl]ethenyl]-1H-indazol-6-yl]spiro[1H-indole-3,1'-cyclopropane]-2-oneIC500.9 [1], 2.2 [2]
(2'S,3R)-2'-[3-[(E)-2-Pyridin-3-ylethenyl]-1H-indazol-6-yl]spiro[1H-indole-3,1'-cyclopropane]-2-oneIC501.6 [1], 3.4 [2]
(2'S,3R)-2'-[3-[(E)-2-[4-(Morpholin-4-ylmethyl)phenyl]ethenyl]-1H-indazol-6-yl]spiro[1H-indole-3,1'-cyclopropane]-2-oneIC501.4 [1], 2.3 [2]
(2'S,3R)-5-Methyl-2'-[3-[(E)-2-[4-(morpholin-4-ylmethyl)phenyl]ethenyl]-1H-indazol-6-yl]spiro[1H-indole-3,1'-cyclopropane]-2-oneIC503.1 [1], 7.2 [2]
(2'S,3R)-2'-[3-[(E)-2-[4-(Piperidin-1-ylmethyl)phenyl]ethenyl]-1H-indazol-6-yl]spiro[1H-indole-3,1'-cyclopropane]-2-oneIC500.9 [1], 6.7 [2]
(2'S,3R)-2'-[3-[(E)-2-[4-[(Dimethylamino)methyl]phenyl]ethenyl]-1H-indazol-6-yl]spiro[1H-indole-3,1'-cyclopropane]-2-oneIC500.59 [1], 1.4 [2]
(2'S,3R)-2'-[3-[(E)-2-[4-(Pyrrolidin-1-ylmethyl)phenyl]ethenyl]-1H-indazol-6-yl]spiro[1H-indole-3,1'-cyclopropane]-2-oneIC500.9 [1], 1.3 [2]
(2'S,3R)-5-Methoxy-2'-[3-[(E)-2-[6-(4-methylpiperazin-1-yl)pyridin-3-yl]ethenyl]-1H-indazol-6-yl]spiro[1H-indole-3,1'-cyclopropane]-2-oneIC500.75 [1], 2.2 [2]
(2'S,3R)-2'-[3-[(E)-2-[4-[(Dimethylamino)methyl]phenyl]ethenyl]-1H-indazol-6-yl]-5-methoxyspiro[1H-indole-3,1'-cyclopropane]-2-oneIC500.37 [1], 1.1 [2]
6-(2,4-Difluorophenyl)sulfonyl-2-(1H-indol-5-ylamino)-8-methylpyrido[2,3-d]pyrimidin-7-oneIC5010000.0 [1]
(E)-3-((1H-Indazol-6-yl)methylene)indolin-2-oneIC50290.0 [1]
(E)-3-((1H-Indazol-6-yl)methylene)indolin-2-oneKi22.0 [1]
(2'S,3R)-2'-[3-[(E)-2-[4-[[(2S,6R)-2,6-Dimethylmorpholin-4-yl]methyl]phenyl]ethenyl]-1H-indazol-6-yl]spiro[1H-indole-3,1'-cyclopropane]-2-oneIC507.4 [1]
(2'S,3R)-2'-[3-[(E)-2-[4-[[(2S,6R)-2,6-Dimethylmorpholin-4-yl]methyl]phenyl]ethenyl]-1H-indazol-6-yl]spiro[1H-indole-3,1'-cyclopropane]-2-oneKi0.73 [1]
(1R,2S)-5'-Methoxy-1'-methyl-2-[3-[(E)-2-[4-(morpholin-4-ylmethyl)phenyl]ethenyl]-1H-indazol-6-yl]spiro[cyclopropane-1,3'-indole]-2'-oneIC501.3 [1]
(1R,2S)-5'-Methoxy-1'-methyl-2-[3-[(E)-2-[4-(morpholin-4-ylmethyl)phenyl]ethenyl]-1H-indazol-6-yl]spiro[cyclopropane-1,3'-indole]-2'-oneKi0.1 [1]
Ellagic acidIC502970.0 [1]
Go-6976Ki3.4 [1]
5-Iodo-3-[(3,5-dibromo-4-hydroxyphenyl)methylene]-2-indolinoneIC50230.0 [1]
5-(2-Chlorophenyl)-7-fluoro-1,2-dihydro-8-methoxy-3-methylpyrazolo(3,4-b)(1,4)benzodiazepineKi11.0 [1]
3-(1H-Indol-3-yl)-4-(3,4,5-trimethoxyphenyl)pyrrole-2,5-dioneIC50990.0 [1]
(12E,25E,28E)-5,16,21,32-Tetrabromo-4,20-dihydroxy-12,25-bis(hydroxyimino)-2,18-dioxa-10,27-diazapentacyclo[28.2.2.214,17.13,7.119,23]octatriaconta-1(32),3,5,7(38),14,16,19,21,23(35),28,30,33,36-tridecaene-11,26-dioneIC501900.0 [1]
(2Z)-3-[3-Bromo-5-[3-bromo-5-[(2Z)-3-[2-(3-bromo-4-hydroxyphenyl)ethylamino]-2-hydroxyimino-3-oxopropyl]-2-hydroxyphenyl]-4-hydroxyphenyl]-N-[2-(3-bromo-4-hydroxyphenyl)ethyl]-2-hydroxyiminopropanamideIC504100.0 [1]
4-Amino-5-chloro-6-ethoxy-pyridine-2-carboxylic acid 4-methanesulfonyl-benzylamideKi4300.0 [1]
5-Propan-2-yl-7,8-dihydro-6H-indeno[1,2-b]indole-9,10-dioneIC5035000.0 [1]
1-({4-[(3,4-Dichlorophenyl)methoxy]phenyl}methyl)azetidine-3-carboxylic acidIC5010000.0 [1]
7-(3,5-Dimethyl-1,2-Oxazol-4-Yl)-6-Methoxy-2-Methyl-4-(Quinolin-4-Yl)-9h-Pyrimido[4,5-B]indoleIC503900.0 [1]
2-Pyrrolidin-1-yl-N-[3-(3-sulfamoylphenyl)-1H-indazol-5-yl]-2-thiophen-3-ylacetamideIC5089.0 [1]
7-Chloro-8-(3-hydroxypropoxy)-3-oxo-11,17-dioxa-2,4,20,22-tetrazatricyclo[16.3.1.05,10]docosa-1(21),5,7,9,18(22),19-hexaene-19-carbonitrileKi10000.0 [1]
7-Chloro-8-(3-hydroxypropyl)-3-oxo-11,17-dioxa-2,4,20,22-tetrazatricyclo[16.3.1.05,10]docosa-1(21),5(10),6,8,18(22),19-hexaene-19-carbonitrileKi10000.0 [1]
N-(7-Chloro-19-cyano-3-oxo-11,17-dioxa-2,4,20,22-tetrazatricyclo[16.3.1.05,10]docosa-1(21),5,7,9,18(22),19-hexaen-8-yl)methanesulfonamideKi10000.0 [1]
4-(Prop-2-enoylamino)-N-[4-[(5,8,11-trimethyl-6-oxopyrimido[4,5-b][1,4]benzodiazepin-2-yl)amino]phenyl]benzamideIC5043.5 [1]
3-(6-Methoxy-1H-indol-2-yl)-1H-pyrazolo[4,3-b]pyridineIC503820.0 [1]
4-(1-Methylindol-3-yl)-3-(3,4,5-trimethoxyphenyl)-1,2-dihydropyrrol-5-oneIC509200.0 [1]
4-Amino-N-[4-[(3-fluorophenyl)carbamoylamino]phenyl]pyrrolo[2,1-f][1,2,4]triazine-5-carboxamideIC503.0 [1]
5-(2-Amino-[1,2,4]triazolo[1,5-a]pyridin-7-yl)-N-tert-butylpyridine-3-sulfonamideIC5010000.0 [1]
5-(2-Aminoethyl)-7-(7-(benzo[b]thiophen-2-yl)-1H-indazol-5-yl)-5H-pyrrolo[3,2-d]pyrimidin-2-amineIC50380.0 [1]
(3Z)-3-(4-Hydroxybenzylidene)-1,3-dihydro-2H-indol-2-oneIC50230.0 [1]
2-(Dimethylamino)-2-(2-ethylphenyl)-N-[3-(3-sulfamoylphenyl)-1H-indazol-5-yl]acetamideIC5083.0 [1]
(3Z)-5-Bromo-3-(3-bromo-4,5-dimethoxybenzylidene)-1,3-dihydro-2H-indol-2-oneIC5013000.0 [1]
N-(5-Cyclopropyl-2-methylpyrazol-3-yl)-7-(3,5-dimethyl-1,2-oxazol-4-yl)-6-methoxy-2-methyl-9H-pyrimido[4,5-b]indol-4-amineIC503900.0 [1]
5-(1H-Indol-3-yl)-3-(3,4,5-trimethoxyphenyl)-1H-pyrazin-2-oneIC50100000.0 [1]
(1R,2S)-5'-Methoxy-1'-methyl-2-[3-[(E)-2-[4-[(1S)-1-morpholin-4-ylethyl]phenyl]ethenyl]-1H-indazol-6-yl]spiro[cyclopropane-1,3'-indole]-2'-oneIC501.5 [1]
N-[(R)-Cyclopropyl(pyridin-2-yl)methyl]-3-[4-[(1S,5S)-3-hydroxy-8-azabicyclo[3.2.1]octan-8-yl]phenyl]-1H-indazole-5-carboxamideIC50130.0 [1]
4-(Propanoylamino)-N-[4-[(5,8,11-trimethyl-6-oxopyrimido[4,5-b][1,4]benzodiazepin-2-yl)amino]phenyl]benzamideIC5082.0 [1]
3-[(E)-Benzotriazol-5-ylidenemethyl]-1H-indol-2-olIC502200.0 [1]
3-[(E)-[3-[(E)-2-[4-[(Dimethylamino)methyl]phenyl]ethenyl]indazol-6-ylidene]methyl]-5-methoxy-1H-indol-2-olIC500.32 [1]
3-[(E)-[3-[(E)-2-Pyridin-3-ylethenyl]indazol-6-ylidene]methyl]-1H-indol-2-olIC502.0 [1]
5-Methyl-3-[(E)-[3-[(E)-2-pyridin-4-ylethenyl]indazol-6-ylidene]methyl]-1H-indol-2-olIC501.4 [1]
2-Hydroxy-3-[(E)-indazol-6-ylidenemethyl]-N-methyl-1H-indole-5-carboxamideIC5010000.0 [1]
5-Chloro-3-[(E)-indazol-6-ylidenemethyl]-1H-indol-2-olIC5054.0 [1]
3-[(E)-[3-[(E)-2-[6-(4-Methylpiperazin-1-yl)pyridin-3-yl]ethenyl]indazol-6-ylidene]methyl]-1H-indol-2-olIC501.4 [1]
5-Fluoro-3-[(E)-indazol-6-ylidenemethyl]-1H-indol-2-olIC5060.0 [1]
4-[(E)-2-[(6E)-6-[(2-Hydroxy-1H-indol-3-yl)methylidene]indazol-3-yl]ethenyl]benzoic acidIC500.82 [1]
3-[(E)-[3-[(E)-2-Pyridin-4-ylethenyl]indazol-6-ylidene]methyl]-1H-indole-2,5-diolIC500.9 [1]
5-Methoxy-3-[(E)-[3-[(E)-2-pyridin-4-ylethenyl]indazol-6-ylidene]methyl]-1H-indol-2-olIC500.45 [1]
6-Chloro-3-[(E)-indazol-6-ylidenemethyl]-1H-indol-2-olIC501300.0 [1]
3-[(E)-[3-[(E)-2-Pyridin-2-ylethenyl]indazol-6-ylidene]methyl]-1H-indol-2-olIC5013.0 [1]
5-Chloro-3-[(E)-[3-[(E)-2-pyridin-4-ylethenyl]indazol-6-ylidene]methyl]-1H-indol-2-olIC502.3 [1]
5-Methoxy-3-[(E)-[3-[(E)-2-pyridin-3-ylethenyl]indazol-6-ylidene]methyl]-1H-indol-2-olIC500.48 [1]
N-[2-Hydroxy-3-[(E)-indazol-6-ylidenemethyl]-1H-indol-6-yl]acetamideIC501200.0 [1]
3-[(E)-[3-[(E)-2-Phenylethenyl]indazol-6-ylidene]methyl]-1H-indol-2-olIC5042.0 [1]
3-[(E)-Indazol-6-ylidenemethyl]-5-methoxy-1H-indol-2-olIC5047.0 [1]
3-[(Z)-Indazol-5-ylidenemethyl]-1H-indol-2-olIC50390.0 [1]
5-Fluoro-3-[(Z)-indazol-6-ylidenemethyl]-1H-indol-2-olIC50240.0 [1]
N-[2-Hydroxy-3-[(E)-indazol-6-ylidenemethyl]-1H-indol-5-yl]acetamideIC506300.0 [1]
5-Ethyl-3-[(E)-[3-[(E)-2-pyridin-3-ylethenyl]indazol-6-ylidene]methyl]-1H-indol-2-olIC501.6 [1]
3-[(Z)-Indazol-6-ylidenemethyl]-1H-indol-2-olIC50230.0 [1]
(3Z)-3-[(3-Hydroxyphenyl)methylidene]-1H-indol-2-oneIC50860.0 [1]
3-(1H-Indol-3-yl)-4-(3,4,5-trimethoxyphenyl)-1,2-dihydropyrrol-5-oneIC5010000.0 [1]
3-(1H-Indol-3-yl)-4-(4-methoxyphenyl)-1,5-dihydro-2H-pyrrole-2-oneIC5012000.0 [1]
3-(N-Methyl-1H-indol-3-yl)-4-(4-methoxyphenyl)-1,5-dihydro-2H-pyrrole-2-oneIC5046000.0 [1]
3-[1-(Ethoxymethyl)indol-3-yl]-4-(3,4,5-trimethoxyphenyl)-1,2-dihydropyrrol-5-oneIC5035000.0 [1]
3-[1-[(2-Methylpropan-2-yl)oxymethyl]indol-3-yl]-4-(3,4,5-trimethoxyphenyl)-1,2-dihydropyrrol-5-oneIC5028000.0 [1]
3-[1-[(2,2-Dimethyl-1,3-dioxolan-4-yl)methyl]indol-3-yl]-4-(3,4,5-trimethoxyphenyl)-1,2-dihydropyrrol-5-oneIC5023000.0 [1]
4-(1H-Indol-3-yl)-3-(3,4,5-trimethoxyphenyl)-1,2-dihydropyrrol-5-oneIC507700.0 [1]
3-[1-(Propan-2-yloxymethyl)indol-3-yl]-4-(3,4,5-trimethoxyphenyl)-1,2-dihydropyrrol-5-oneIC5044000.0 [1]
3-[1-(Phenoxymethyl)indol-3-yl]-4-(3,4,5-trimethoxyphenyl)-1,2-dihydropyrrol-5-oneIC509000.0 [1]
3-[1-(2,3-Dihydroxypropyl)indol-3-yl]-4-(3,4,5-trimethoxyphenyl)-1,2-dihydropyrrol-5-oneIC5016000.0 [1]
(18S)-10-[(4-Methylpiperazin-1-yl)methyl]-5,7,14,20,28-pentazapentacyclo[20.3.1.12,6.18,12.014,18]octacosa-1(25),2(28),3,5,8(27),9,11,22(26),23-nonaen-19-oneKi100.0 [1]
(3Z)-5-Bromo-3-[(3-chloro-4-hydroxy-5-methoxyphenyl)methylidene]-1-methylindol-2-oneIC506100.0 [1]
(2'S,3R)-2'-[3-[(E)-2-[4-(1-Propan-2-ylpiperidin-4-yl)oxyphenyl]ethenyl]-1H-indazol-6-yl]spiro[1H-indole-3,1'-cyclopropane]-2-oneIC501.5 [1]
(2'S,3R)-2'-[3-[(E)-2-[3-[[(2R,6S)-2,6-Dimethylmorpholin-4-yl]methyl]phenyl]ethenyl]-1H-indazol-6-yl]spiro[1H-indole-3,1'-cyclopropane]-2-oneIC5020.0 [1]
(1R,2S)-2-[3-[(E)-2-[4-[[(2S,6R)-2,6-Dimethylmorpholin-4-yl]methyl]phenyl]ethenyl]-1H-indazol-6-yl]-5'-methoxy-1'-methylspiro[cyclopropane-1,3'-indole]-2'-oneIC505.7 [1]
(2'S,3R)-5-Methoxy-2'-[3-[(E)-2-[4-[[(2S,6R)-2,4,6-trimethylpiperazin-1-yl]methyl]phenyl]ethenyl]-1H-indazol-6-yl]spiro[1H-indole-3,1'-cyclopropane]-2-oneIC500.39 [1]
(2'S,3R)-2'-[3-[(E)-2-[4-[[(3R,5S)-3,4,5-Trimethylpiperazin-1-yl]methyl]phenyl]ethenyl]-1H-indazol-6-yl]spiro[1H-indole-3,1'-cyclopropane]-2-oneIC500.64 [1]
(2'S,3R)-2'-[3-[(E)-2-[4-(8-Oxa-3-azabicyclo[3.2.1]octan-3-ylmethyl)phenyl]ethenyl]-1H-indazol-6-yl]spiro[1H-indole-3,1'-cyclopropane]-2-oneIC505.2 [1]
(3Z)-5-Bromo-3-[(3,4-dihydroxyphenyl)methylidene]-1H-indol-2-oneIC5013000.0 [1]
(2'S,3R)-2'-[3-[(E)-2-[4-[(Dimethylamino)methyl]phenyl]ethenyl]-1H-indazol-6-yl]-5-methylspiro[1H-indole-3,1'-cyclopropane]-2-oneIC500.71 [1]
(2'S,3R)-2'-[3-[(E)-2-(4-Piperazin-1-ylphenyl)ethenyl]-1H-indazol-6-yl]spiro[1H-indole-3,1'-cyclopropane]-2-oneIC500.9 [1]
(2'S,3R)-2'-[3-[(E)-2-[4-(1,4-Oxazepan-4-ylmethyl)phenyl]ethenyl]-1H-indazol-6-yl]spiro[1H-indole-3,1'-cyclopropane]-2-oneIC501.7 [1]
(2'S,3R)-2'-[3-[(E)-2-[4-(Diethylaminomethyl)phenyl]ethenyl]-1H-indazol-6-yl]spiro[1H-indole-3,1'-cyclopropane]-2-oneIC501.8 [1]
Items per page: 1 - 10 of 100
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References

This online tool may be cited as follows

MLA

"Quest Database™ Serine/threonine-protein kinase PLK4 Inhibitors (IC50, Ki)." AAT Bioquest, Inc., 21 Nov. 2024, https://www.aatbio.com/data-sets/serine-threonine-protein-kinase-plk4-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2024, November 21). Quest Database™ Serine/threonine-protein kinase PLK4 Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/serine-threonine-protein-kinase-plk4-inhibitors-ic50-ki.
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