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Compile Data Set for Download or QSAR

Found 329 hits Enz. Inhib. hit(s) with Target = 'Polo-Like Kinase 3'   
Target
(Institution)
LigandTarget
Links
Ligand
Links
Trg + Lig
Links
Ki
nM
ΔG°
kJ/mole
IC50
nM
Kd
nM
EC50/IC50
nM
koff
s-1
kon
M-1s-1
pHTemp
°C
Serine/threonine-protein kinase PLK3


(Homo sapiens (human))
BDBM50362988
PNG
(CHEMBL1945500)
Show SMILES CN(C)CCCc1cc(Cl)cc(Nc2ncc3CC(=S)Nc4cc(Cl)ccc4-c3n2)c1
Show InChI InChI=1S/C23H23Cl2N5S/c1-30(2)7-3-4-14-8-17(25)11-18(9-14)27-23-26-13-15-10-21(31)28-20-12-16(24)5-6-19(20)22(15)29-23/h5-6,8-9,11-13H,3-4,7,10H2,1-2H3,(H,28,31)(H,26,27,29)
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n/an/a 5n/an/an/an/an/an/a



Millennium Pharmaceuticals, Inc.

Curated by ChEMBL


Assay Description
Inhibition of PLK3


J Med Chem 55: 197-208 (2012)

More data for this
Ligand-Target Pair
Serine/threonine-protein kinase PLK3


(Homo sapiens (human))
BDBM50362985
PNG
(CHEMBL1945502)
Show SMILES COc1ccc(Nc2ncc3CC(=S)Nc4cc(Cl)ccc4-c3n2)cc1CCCN(C)C
Show InChI InChI=1S/C24H26ClN5OS/c1-30(2)10-4-5-15-11-18(7-9-21(15)31-3)27-24-26-14-16-12-22(32)28-20-13-17(25)6-8-19(20)23(16)29-24/h6-9,11,13-14H,4-5,10,12H2,1-3H3,(H,28,32)(H,26,27,29)
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n/an/a 5n/an/an/an/an/an/a



Millennium Pharmaceuticals, Inc.

Curated by ChEMBL


Assay Description
Inhibition of PLK3


J Med Chem 55: 197-208 (2012)

More data for this
Ligand-Target Pair
Serine/threonine-protein kinase PLK3


(Homo sapiens (human))
BDBM50323110
PNG
((R)-5-(5-(2-aminopyrimidin-4-yl)-1H-benzo[d]imidaz...)
Show SMILES C[C@@H](Oc1cc(sc1C(N)=O)-n1cnc2cc(ccc12)-c1ccnc(N)n1)c1ccccc1C(F)(F)F
Show InChI InChI=1S/C25H19F3N6O2S/c1-13(15-4-2-3-5-16(15)25(26,27)28)36-20-11-21(37-22(20)23(29)35)34-12-32-18-10-14(6-7-19(18)34)17-8-9-31-24(30)33-17/h2-13H,1H3,(H2,29,35)(H2,30,31,33)/t13-/m1/s1
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n/an/a 5n/an/an/an/an/an/a



GlaxoSmithKline

Curated by ChEMBL


Assay Description
Inhibition of full lungth PLK3 by SPA assay


Bioorg Med Chem Lett 20: 4587-92 (2010)

More data for this
Ligand-Target Pair
Serine/threonine-protein kinase PLK3


(Homo sapiens (human))
BDBM50323109
PNG
((R)-3-(1-(2-chlorophenyl)ethoxy)-5-(5-(1-methyl-1H...)
Show SMILES C[C@@H](Oc1cc(sc1C(N)=O)-n1cnc2cc(ccc12)-c1cnn(C)c1)c1ccccc1Cl
Show InChI InChI=1S/C24H20ClN5O2S/c1-14(17-5-3-4-6-18(17)25)32-21-10-22(33-23(21)24(26)31)30-13-27-19-9-15(7-8-20(19)30)16-11-28-29(2)12-16/h3-14H,1-2H3,(H2,26,31)/t14-/m1/s1
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n/an/a 6n/an/an/an/an/an/a



GlaxoSmithKline

Curated by ChEMBL


Assay Description
Inhibition of full lungth PLK3 by SPA assay


Bioorg Med Chem Lett 20: 4587-92 (2010)

More data for this
Ligand-Target Pair
Serine/threonine-protein kinase PLK3


(Homo sapiens (human))
BDBM50323122
PNG
((R)-5-(5-(1-methyl-1H-pyrazol-4-yl)-1H-benzo[d]imi...)
Show SMILES C[C@@H](Oc1cc(sc1C(N)=O)-n1cnc2cc(ccc12)-c1cnn(C)c1)c1ccccc1C(F)(F)F
Show InChI InChI=1S/C25H20F3N5O2S/c1-14(17-5-3-4-6-18(17)25(26,27)28)35-21-10-22(36-23(21)24(29)34)33-13-30-19-9-15(7-8-20(19)33)16-11-31-32(2)12-16/h3-14H,1-2H3,(H2,29,34)/t14-/m1/s1
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GlaxoSmithKline

Curated by ChEMBL


Assay Description
Inhibition of full lungth PLK3 by SPA assay


Bioorg Med Chem Lett 20: 4587-92 (2010)

More data for this
Ligand-Target Pair
Serine/threonine-protein kinase PLK3


(Homo sapiens (human))
BDBM50318085
PNG
(1-Methyl-8-[(2-methylphenyl)amino]-4,5-dihydro-1H-...)
Show SMILES Cc1ccccc1Nc1ncc2CCc3c(nn(C)c3-c2n1)C(N)=O
Show InChI InChI=1S/C18H18N6O/c1-10-5-3-4-6-13(10)21-18-20-9-11-7-8-12-15(17(19)25)23-24(2)16(12)14(11)22-18/h3-6,9H,7-8H2,1-2H3,(H2,19,25)(H,20,21,22)
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n/an/a 6n/an/an/an/an/an/a



Nerviano Medical Sciences Srl

Curated by ChEMBL


Assay Description
Inhibition of Plk3 assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting


J Med Chem 53: 3532-51 (2010)

More data for this
Ligand-Target Pair
Serine/threonine-protein kinase PLK3


(Homo sapiens (human))
BDBM28206
PNG
(3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-(5,6-dimethoxy...)
Show SMILES COc1cc2ncn(-c3cc(O[C@H](C)c4ccccc4Cl)c(s3)C(N)=O)c2cc1OC
Show InChI InChI=1S/C22H20ClN3O4S/c1-12(13-6-4-5-7-14(13)23)30-19-10-20(31-21(19)22(24)27)26-11-25-15-8-17(28-2)18(29-3)9-16(15)26/h4-12H,1-3H3,(H2,24,27)/t12-/m1/s1
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n/an/a 6n/an/an/an/a7.222



GSK



Assay Description
The compound inhibitory activity was determined by incubation with purified PLK enzyme and biotinylated peptide substrate in the presence ATP/[gamma-...


Bioorg Med Chem Lett 19: 1694-7 (2009)

More data for this
Ligand-Target Pair
Polo-Like Kinase 3


(Homo sapiens (human))
BDBM26514
PNG
(4-{[(7R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,...)
Show SMILES CC[C@H]1N(C2CCCC2)c2nc(Nc3ccc(cc3)C(=O)NC3CCN(C)CC3)ncc2N(C)C1=O
Show InChI InChI=1S/C27H37N7O2/c1-4-22-26(36)33(3)23-17-28-27(31-24(23)34(22)21-7-5-6-8-21)30-19-11-9-18(10-12-19)25(35)29-20-13-15-32(2)16-14-20/h9-12,17,20-22H,4-8,13-16H2,1-3H3,(H,29,35)(H,28,30,31)/t22-/m1/s1
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n/an/a 6.70n/an/an/an/a7.522



Pfizer



Assay Description
Percent inhibition and IC50 values were determined with ATP concentrations at apparent Km using the Invitrogen SelectScreen Kinase Profiling Service ...


Chem Biol Drug Des 70: 540-6 (2007)

More data for this
Ligand-Target Pair
Serine/threonine-protein kinase PLK3


(Homo sapiens (human))
BDBM50362986
PNG
(CHEMBL1945501)
Show SMILES CN(C)CCCc1cc(Nc2ncc3CC(=S)Nc4cc(Cl)ccc4-c3n2)ccc1F
Show InChI InChI=1S/C23H23ClFN5S/c1-30(2)9-3-4-14-10-17(6-8-19(14)25)27-23-26-13-15-11-21(31)28-20-12-16(24)5-7-18(20)22(15)29-23/h5-8,10,12-13H,3-4,9,11H2,1-2H3,(H,28,31)(H,26,27,29)
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n/an/a 7n/an/an/an/an/an/a



Millennium Pharmaceuticals, Inc.

Curated by ChEMBL


Assay Description
Inhibition of PLK3


J Med Chem 55: 197-208 (2012)

More data for this
Ligand-Target Pair
Serine/threonine-protein kinase PLK3


(Homo sapiens (human))
BDBM50323113
PNG
((R)-5-(5-(pyridin-4-yl)-1H-benzo[d]imidazol-1-yl)-...)
Show SMILES C[C@@H](Oc1cc(sc1C(N)=O)-n1cnc2cc(ccc12)-c1ccncc1)c1ccccc1C(F)(F)F
Show InChI InChI=1S/C26H19F3N4O2S/c1-15(18-4-2-3-5-19(18)26(27,28)29)35-22-13-23(36-24(22)25(30)34)33-14-32-20-12-17(6-7-21(20)33)16-8-10-31-11-9-16/h2-15H,1H3,(H2,30,34)/t15-/m1/s1
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n/an/a 8n/an/an/an/an/an/a



GlaxoSmithKline

Curated by ChEMBL


Assay Description
Inhibition of full lungth PLK3 by SPA assay


Bioorg Med Chem Lett 20: 4587-92 (2010)

More data for this
Ligand-Target Pair
Serine/threonine-protein kinase PLK3


(Homo sapiens (human))
BDBM25120
PNG
(5-(5,6-dimethoxy-1H-1,3-benzodiazol-1-yl)-3-{[2-(t...)
Show SMILES COc1cc2ncn(-c3cc(OCc4ccccc4C(F)(F)F)c(s3)C(N)=O)c2cc1OC
Show InChI InChI=1S/C22H18F3N3O4S/c1-30-16-7-14-15(8-17(16)31-2)28(11-27-14)19-9-18(20(33-19)21(26)29)32-10-12-5-3-4-6-13(12)22(23,24)25/h3-9,11H,10H2,1-2H3,(H2,26,29)
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n/an/a 9n/an/an/an/a7.222



GSK



Assay Description
The compound inhibitory activity was determined by incubation with purified PLK enzyme and biotinylated peptide substrate in the presence ATP/[gamma-...


Bioorg Med Chem Lett 19: 1018-21 (2009)

More data for this
Ligand-Target Pair
Serine/threonine-protein kinase PLK3


(Homo sapiens (human))
BDBM50362984
PNG
(CHEMBL1945801)
Show SMILES CN(C)CCCc1cc(Nc2ncc3CC(=S)Nc4cc(Cl)ccc4-c3n2)ccc1C(F)(F)F
Show InChI InChI=1S/C24H23ClF3N5S/c1-33(2)9-3-4-14-10-17(6-8-19(14)24(26,27)28)30-23-29-13-15-11-21(34)31-20-12-16(25)5-7-18(20)22(15)32-23/h5-8,10,12-13H,3-4,9,11H2,1-2H3,(H,31,34)(H,29,30,32)
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Millennium Pharmaceuticals, Inc.

Curated by ChEMBL


Assay Description
Inhibition of PLK3


J Med Chem 55: 197-208 (2012)

More data for this
Ligand-Target Pair
Serine/threonine-protein kinase PLK3


(Homo sapiens (human))
BDBM28178
PNG
(3-[(2-chlorophenyl)methoxy]-5-(5,6-dimethoxy-1H-1,...)
Show SMILES COc1cc2ncn(-c3cc(OCc4ccccc4Cl)c(s3)C(N)=O)c2cc1OC
Show InChI InChI=1S/C21H18ClN3O4S/c1-27-16-7-14-15(8-17(16)28-2)25(11-24-14)19-9-18(20(30-19)21(23)26)29-10-12-5-3-4-6-13(12)22/h3-9,11H,10H2,1-2H3,(H2,23,26)
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n/an/a 9n/an/an/an/a7.222



GSK



Assay Description
The compound inhibitory activity was determined by incubation with purified PLK enzyme and biotinylated peptide substrate in the presence ATP/[gamma-...


Bioorg Med Chem Lett 19: 1694-7 (2009)

More data for this
Ligand-Target Pair
Serine/threonine-protein kinase PLK3


(Homo sapiens (human))
BDBM50329197
PNG
(3-((R)-1-((2S,6R)-2,6-dimethylmorpholino)ethyl)-N-...)
Show SMILES C[C@@H](N1C[C@H](C)O[C@H](C)C1)c1cc(Nc2nc(C)cn3c(cnc23)-c2cn[nH]c2)sn1
Show InChI InChI=1S/C21H26N8OS/c1-12-9-29-18(16-6-23-24-7-16)8-22-21(29)20(25-12)26-19-5-17(27-31-19)15(4)28-10-13(2)30-14(3)11-28/h5-9,13-15H,10-11H2,1-4H3,(H,23,24)(H,25,26)/t13-,14+,15-/m1/s1
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n/an/a>10n/an/an/an/an/an/a



Merck Research Laboratories

Curated by ChEMBL


Assay Description
Inhibition of PLK3


Bioorg Med Chem Lett 20: 6739-43 (2010)

More data for this
Ligand-Target Pair
Serine/threonine-protein kinase PLK3


(Homo sapiens (human))
BDBM50323107
PNG
((R)-3-(1-(2-chlorophenyl)ethoxy)-5-(5-(pyridin-4-y...)
Show SMILES C[C@@H](Oc1cc(sc1C(N)=O)-n1cnc2cc(ccc12)-c1ccncc1)c1ccccc1Cl
Show InChI InChI=1S/C25H19ClN4O2S/c1-15(18-4-2-3-5-19(18)26)32-22-13-23(33-24(22)25(27)31)30-14-29-20-12-17(6-7-21(20)30)16-8-10-28-11-9-16/h2-15H,1H3,(H2,27,31)/t15-/m1/s1
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n/an/a 10n/an/an/an/an/an/a



GlaxoSmithKline

Curated by ChEMBL


Assay Description
Inhibition of full lungth PLK3 by SPA assay


Bioorg Med Chem Lett 20: 4587-92 (2010)

More data for this
Ligand-Target Pair
Serine/threonine-protein kinase PLK3


(Homo sapiens (human))
BDBM50318061
PNG
(1-Methyl-8-{[2-(methylamino)phenyl]amino}-4,5-dihy...)
Show SMILES CNc1ccccc1Nc1ncc2CCc3c(nn(C)c3-c2n1)C(N)=O
Show InChI InChI=1S/C18H19N7O/c1-20-12-5-3-4-6-13(12)22-18-21-9-10-7-8-11-15(17(19)26)24-25(2)16(11)14(10)23-18/h3-6,9,20H,7-8H2,1-2H3,(H2,19,26)(H,21,22,23)
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n/an/a 11n/an/an/an/an/an/a



Nerviano Medical Sciences Srl

Curated by ChEMBL


Assay Description
Inhibition of Plk3 assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting


J Med Chem 53: 3532-51 (2010)

More data for this
Ligand-Target Pair
Serine/threonine-protein kinase PLK3


(Homo sapiens (human))
BDBM50362982
PNG
(CHEMBL1945170)
Show SMILES CN(C)CCCc1cccc(Nc2ncc3CC(=S)Nc4cc(Cl)ccc4-c3n2)c1
Show InChI InChI=1S/C23H24ClN5S/c1-29(2)10-4-6-15-5-3-7-18(11-15)26-23-25-14-16-12-21(30)27-20-13-17(24)8-9-19(20)22(16)28-23/h3,5,7-9,11,13-14H,4,6,10,12H2,1-2H3,(H,27,30)(H,25,26,28)
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n/an/a 12n/an/an/an/an/an/a



Millennium Pharmaceuticals, Inc.

Curated by ChEMBL


Assay Description
Inhibition of PLK3


J Med Chem 55: 197-208 (2012)

More data for this
Ligand-Target Pair
Serine/threonine-protein kinase PLK3


(Homo sapiens (human))
BDBM50323123
PNG
((R)-3-(1-(2-chlorophenyl)ethoxy)-5-(6-(1-methyl-1H...)
Show SMILES C[C@@H](Oc1cc(sc1C(N)=O)-n1cnc2ccc(cc12)-c1cnn(C)c1)c1ccccc1Cl
Show InChI InChI=1S/C24H20ClN5O2S/c1-14(17-5-3-4-6-18(17)25)32-21-10-22(33-23(21)24(26)31)30-13-27-19-8-7-15(9-20(19)30)16-11-28-29(2)12-16/h3-14H,1-2H3,(H2,26,31)/t14-/m1/s1
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n/an/a 13n/an/an/an/an/an/a



GlaxoSmithKline

Curated by ChEMBL


Assay Description
Inhibition of full lungth PLK3 by SPA assay


Bioorg Med Chem Lett 20: 4587-92 (2010)

More data for this
Ligand-Target Pair
Serine/threonine-protein kinase PLK3


(Homo sapiens (human))
BDBM50318074
PNG
(8-[(2-Aminophenyl)amino]-1-methyl-4,5-dihydro-1H-p...)
Show SMILES Cn1nc(C(N)=O)c2CCc3cnc(Nc4ccccc4N)nc3-c12
Show InChI InChI=1S/C17H17N7O/c1-24-15-10(14(23-24)16(19)25)7-6-9-8-20-17(22-13(9)15)21-12-5-3-2-4-11(12)18/h2-5,8H,6-7,18H2,1H3,(H2,19,25)(H,20,21,22)
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n/an/a 13n/an/an/an/an/an/a



Nerviano Medical Sciences Srl

Curated by ChEMBL


Assay Description
Inhibition of Plk3 assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting


J Med Chem 53: 3532-51 (2010)

More data for this
Ligand-Target Pair
Serine/threonine-protein kinase PLK3


(Homo sapiens (human))
BDBM50318081
PNG
(8-[(2-Methoxyphenyl)amino]-1-methyl-4,5-dihydro-1H...)
Show SMILES COc1ccccc1Nc1ncc2CCc3c(nn(C)c3-c2n1)C(N)=O
Show InChI InChI=1S/C18H18N6O2/c1-24-16-11(15(23-24)17(19)25)8-7-10-9-20-18(22-14(10)16)21-12-5-3-4-6-13(12)26-2/h3-6,9H,7-8H2,1-2H3,(H2,19,25)(H,20,21,22)
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n/an/a 13n/an/an/an/an/an/a



Nerviano Medical Sciences Srl

Curated by ChEMBL


Assay Description
Inhibition of Plk3 assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting


J Med Chem 53: 3532-51 (2010)

More data for this
Ligand-Target Pair
Polo-Like Kinase 3


(Homo sapiens (human))
BDBM25121
PNG
(4-{[(7R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,...)
Show SMILES CC[C@H]1N(C2CCCC2)c2nc(Nc3ccc(cc3OC)C(=O)NC3CCN(C)CC3)ncc2N(C)C1=O
Show InChI InChI=1S/C28H39N7O3/c1-5-22-27(37)34(3)23-17-29-28(32-25(23)35(22)20-8-6-7-9-20)31-21-11-10-18(16-24(21)38-4)26(36)30-19-12-14-33(2)15-13-19/h10-11,16-17,19-20,22H,5-9,12-15H2,1-4H3,(H,30,36)(H,29,31,32)/t22-/m1/s1
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n/an/a 13.6n/an/an/an/a7.522



Pfizer



Assay Description
Percent inhibition and IC50 values were determined with ATP concentrations at apparent Km using the Invitrogen SelectScreen Kinase Profiling Service ...


Chem Biol Drug Des 70: 540-6 (2007)

More data for this
Ligand-Target Pair
Serine/threonine-protein kinase PLK3


(Homo sapiens (human))
BDBM31532
PNG
(pyrazolo[4,3-h]quinazoline-3-carboxamide, 1)
Show SMILES Cn1nc(C(N)=O)c2CCc3cnc(Nc4ccccc4)nc3-c12
Show InChI InChI=1S/C17H16N6O/c1-23-15-12(14(22-23)16(18)24)8-7-10-9-19-17(21-13(10)15)20-11-5-3-2-4-6-11/h2-6,9H,7-8H2,1H3,(H2,18,24)(H,19,20,21)
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n/an/a 14n/an/an/an/an/an/a



Nerviano Medical Sciences Srl

Curated by ChEMBL


Assay Description
Inhibition of Plk3 assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting


J Med Chem 53: 3532-51 (2010)

More data for this
Ligand-Target Pair
Serine/threonine-protein kinase PLK3


(Homo sapiens (human))
BDBM50323116
PNG
((R)-5-(5-(pyridin-3-yl)-1H-benzo[d]imidazol-1-yl)-...)
Show SMILES C[C@@H](Oc1cc(sc1C(N)=O)-n1cnc2cc(ccc12)-c1cccnc1)c1ccccc1C(F)(F)F
Show InChI InChI=1S/C26H19F3N4O2S/c1-15(18-6-2-3-7-19(18)26(27,28)29)35-22-12-23(36-24(22)25(30)34)33-14-32-20-11-16(8-9-21(20)33)17-5-4-10-31-13-17/h2-15H,1H3,(H2,30,34)/t15-/m1/s1
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n/an/a 16n/an/an/an/an/an/a



GlaxoSmithKline

Curated by ChEMBL


Assay Description
Inhibition of full lungth PLK3 by SPA assay


Bioorg Med Chem Lett 20: 4587-92 (2010)

More data for this
Ligand-Target Pair
Serine/threonine-protein kinase PLK3


(Homo sapiens (human))
BDBM50318076
PNG
(1-Methyl-8-{[2-(methylsulfanyl)phenyl]amino}-4,5-d...)
Show SMILES CSc1ccccc1Nc1ncc2CCc3c(nn(C)c3-c2n1)C(N)=O
Show InChI InChI=1S/C18H18N6OS/c1-24-16-11(15(23-24)17(19)25)8-7-10-9-20-18(22-14(10)16)21-12-5-3-4-6-13(12)26-2/h3-6,9H,7-8H2,1-2H3,(H2,19,25)(H,20,21,22)
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n/an/a 16n/an/an/an/an/an/a



Nerviano Medical Sciences Srl

Curated by ChEMBL


Assay Description
Inhibition of Plk3 assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting


J Med Chem 53: 3532-51 (2010)

More data for this
Ligand-Target Pair
Serine/threonine-protein kinase PLK3


(Homo sapiens (human))
BDBM50323114
PNG
((R)-5-(6-(pyridin-4-yl)-1H-benzo[d]imidazol-1-yl)-...)
Show SMILES C[C@@H](Oc1cc(sc1C(N)=O)-n1cnc2ccc(cc12)-c1ccncc1)c1ccccc1C(F)(F)F
Show InChI InChI=1S/C26H19F3N4O2S/c1-15(18-4-2-3-5-19(18)26(27,28)29)35-22-13-23(36-24(22)25(30)34)33-14-32-20-7-6-17(12-21(20)33)16-8-10-31-11-9-16/h2-15H,1H3,(H2,30,34)/t15-/m1/s1
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n/an/a 16n/an/an/an/an/an/a



GlaxoSmithKline

Curated by ChEMBL


Assay Description
Inhibition of full lungth PLK3 by SPA assay


Bioorg Med Chem Lett 20: 4587-92 (2010)

More data for this
Ligand-Target Pair
Serine/threonine-protein kinase PLK3


(Homo sapiens (human))
BDBM50362981
PNG
(CHEMBL1945171)
Show SMILES CN(C)CCCc1ccc(C)c(Nc2ncc3CC(=S)Nc4cc(Cl)ccc4-c3n2)c1
Show InChI InChI=1S/C24H26ClN5S/c1-15-6-7-16(5-4-10-30(2)3)11-20(15)28-24-26-14-17-12-22(31)27-21-13-18(25)8-9-19(21)23(17)29-24/h6-9,11,13-14H,4-5,10,12H2,1-3H3,(H,27,31)(H,26,28,29)
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n/an/a 18n/an/an/an/an/an/a



Millennium Pharmaceuticals, Inc.

Curated by ChEMBL


Assay Description
Inhibition of PLK3


J Med Chem 55: 197-208 (2012)

More data for this
Ligand-Target Pair
Polo-Like Kinase 3


(Homo sapiens (human))
BDBM24933
PNG
(2-amino-isoxazolopyridine, 9 | 3-(2H-1,3-benzodiox...)
Show SMILES C[C@H](Nc1cc2c(noc2cn1)-c1ccc2OCOc2c1)c1ccccc1
Show InChI InChI=1S/C21H17N3O3/c1-13(14-5-3-2-4-6-14)23-20-10-16-19(11-22-20)27-24-21(16)15-7-8-17-18(9-15)26-12-25-17/h2-11,13H,12H2,1H3,(H,22,23)/t13-/m0/s1
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n/an/a 24n/an/an/an/a7.230



Sunesis Pharmaceuticals



Assay Description
An IMAP fluorescence polarization-based assay format (Molecular Devices) was used to determine the ability of compounds to inhibit the phosphorylatio...


Bioorg Med Chem Lett 18: 5186-9 (2008)

More data for this
Ligand-Target Pair
Serine/threonine-protein kinase PLK3


(Homo sapiens (human))
BDBM50323115
PNG
((R)-3-(1-(2-chlorophenyl)ethoxy)-5-(6-(pyridin-4-y...)
Show SMILES C[C@@H](Oc1cc(sc1C(N)=O)-n1cnc2ccc(cc12)-c1ccncc1)c1ccccc1Cl
Show InChI InChI=1S/C25H19ClN4O2S/c1-15(18-4-2-3-5-19(18)26)32-22-13-23(33-24(22)25(27)31)30-14-29-20-7-6-17(12-21(20)30)16-8-10-28-11-9-16/h2-15H,1H3,(H2,27,31)/t15-/m1/s1
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n/an/a 25n/an/an/an/an/an/a



GlaxoSmithKline

Curated by ChEMBL


Assay Description
Inhibition of full lungth PLK3 by SPA assay


Bioorg Med Chem Lett 20: 4587-92 (2010)

More data for this
Ligand-Target Pair
Serine/threonine-protein kinase PLK3


(Homo sapiens (human))
BDBM50275752
PNG
(5-methyl-7-(3-(trifluoromethyl)phenyl)-N-(3,4,5-tr...)
Show SMILES COc1cc(Nc2ncc3c(C)nc(-c4cccc(c4)C(F)(F)F)n3n2)cc(OC)c1OC
Show InChI InChI=1S/C22H20F3N5O3/c1-12-16-11-26-21(28-15-9-17(31-2)19(33-4)18(10-15)32-3)29-30(16)20(27-12)13-6-5-7-14(8-13)22(23,24)25/h5-11H,1-4H3,(H,28,29)
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n/an/a 30n/an/an/an/an/an/a



GlaxoSmithKline

Curated by ChEMBL


Assay Description
Inhibition of PLK3 (unknown origin) expressed in baculovirus infected Trichoplusia ni cells


Bioorg Med Chem Lett 18: 6214-7 (2008)

More data for this
Ligand-Target Pair
Serine/threonine-protein kinase PLK3


(Homo sapiens (human))
BDBM50362976
PNG
(CHEMBL1945803)
Show SMILES CN(C)CCCc1cncc(Nc2ncc3CC(=S)Nc4cc(Cl)ccc4-c3n2)c1
Show InChI InChI=1S/C22H23ClN6S/c1-29(2)7-3-4-14-8-17(13-24-11-14)26-22-25-12-15-9-20(30)27-19-10-16(23)5-6-18(19)21(15)28-22/h5-6,8,10-13H,3-4,7,9H2,1-2H3,(H,27,30)(H,25,26,28)
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n/an/a 31n/an/an/an/an/an/a



Millennium Pharmaceuticals, Inc.

Curated by ChEMBL


Assay Description
Inhibition of PLK3


J Med Chem 55: 197-208 (2012)

More data for this
Ligand-Target Pair
Serine/threonine-protein kinase PLK3


(Homo sapiens (human))
BDBM50329932
PNG
(1-methyl-8-(2-(trifluoromethoxy)phenylamino)-4,5-d...)
Show SMILES Cn1nc(C(N)=O)c2CCc3cnc(Nc4ccccc4OC(F)(F)F)nc3-c12
Show InChI InChI=1S/C18H15F3N6O2/c1-27-15-10(14(26-27)16(22)28)7-6-9-8-23-17(25-13(9)15)24-11-4-2-3-5-12(11)29-18(19,20)21/h2-5,8H,6-7H2,1H3,(H2,22,28)(H,23,24,25)
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n/an/a 32n/an/an/an/an/an/a



Nerviano Medical Sciences srl

Curated by ChEMBL


Assay Description
Inhibition of PLK3


Bioorg Med Chem Lett 20: 6489-94 (2010)

More data for this
Ligand-Target Pair
Serine/threonine-protein kinase PLK3


(Homo sapiens (human))
BDBM28208
PNG
(3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-(6-methoxy-1H-...)
Show SMILES COc1ccc2ncn(-c3cc(O[C@H](C)c4ccccc4Cl)c(s3)C(N)=O)c2c1
Show InChI InChI=1S/C21H18ClN3O3S/c1-12(14-5-3-4-6-15(14)22)28-18-10-19(29-20(18)21(23)26)25-11-24-16-8-7-13(27-2)9-17(16)25/h3-12H,1-2H3,(H2,23,26)/t12-/m1/s1
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n/an/a 35n/an/an/an/a7.222



GSK



Assay Description
The compound inhibitory activity was determined by incubation with purified PLK enzyme and biotinylated peptide substrate in the presence ATP/[gamma-...


Bioorg Med Chem Lett 19: 1694-7 (2009)

More data for this
Ligand-Target Pair
Serine/threonine-protein kinase PLK3


(Homo sapiens (human))
BDBM50318062
PNG
(8-[(2-Fluorophenyl)amino]-1-methyl-4,5-dihydro-1H-...)
Show SMILES Cn1nc(C(N)=O)c2CCc3cnc(Nc4ccccc4F)nc3-c12
Show InChI InChI=1S/C17H15FN6O/c1-24-15-10(14(23-24)16(19)25)7-6-9-8-20-17(22-13(9)15)21-12-5-3-2-4-11(12)18/h2-5,8H,6-7H2,1H3,(H2,19,25)(H,20,21,22)
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n/an/a 37n/an/an/an/an/an/a



Nerviano Medical Sciences Srl

Curated by ChEMBL


Assay Description
Inhibition of Plk3 assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting


J Med Chem 53: 3532-51 (2010)

More data for this
Ligand-Target Pair
Serine/threonine-protein kinase PLK3


(Homo sapiens (human))
BDBM50323117
PNG
((R)-5-(6-(pyridin-3-yl)-1H-benzo[d]imidazol-1-yl)-...)
Show SMILES C[C@@H](Oc1cc(sc1C(N)=O)-n1cnc2ccc(cc12)-c1cccnc1)c1ccccc1C(F)(F)F
Show InChI InChI=1S/C26H19F3N4O2S/c1-15(18-6-2-3-7-19(18)26(27,28)29)35-22-12-23(36-24(22)25(30)34)33-14-32-20-9-8-16(11-21(20)33)17-5-4-10-31-13-17/h2-15H,1H3,(H2,30,34)/t15-/m1/s1
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n/an/a 40n/an/an/an/an/an/a



GlaxoSmithKline

Curated by ChEMBL


Assay Description
Inhibition of full lungth PLK3 by SPA assay


Bioorg Med Chem Lett 20: 4587-92 (2010)

More data for this
Ligand-Target Pair
Serine/threonine-protein kinase PLK3


(Homo sapiens (human))
BDBM28209
PNG
(5-(6-methoxy-1H-1,3-benzodiazol-1-yl)-3-[(1R)-1-[2...)
Show SMILES COc1ccc2ncn(-c3cc(O[C@H](C)c4ccccc4C(F)(F)F)c(s3)C(N)=O)c2c1
Show InChI InChI=1S/C22H18F3N3O3S/c1-12(14-5-3-4-6-15(14)22(23,24)25)31-18-10-19(32-20(18)21(26)29)28-11-27-16-8-7-13(30-2)9-17(16)28/h3-12H,1-2H3,(H2,26,29)/t12-/m1/s1
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n/an/a 41n/an/an/an/a7.222



GSK



Assay Description
The compound inhibitory activity was determined by incubation with purified PLK enzyme and biotinylated peptide substrate in the presence ATP/[gamma-...


Bioorg Med Chem Lett 19: 1694-7 (2009)

More data for this
Ligand-Target Pair
Serine/threonine-protein kinase PLK3


(Homo sapiens (human))
BDBM28207
PNG
(3-[(1S)-1-(2-chlorophenyl)ethoxy]-5-(5,6-dimethoxy...)
Show SMILES COc1cc2ncn(-c3cc(O[C@@H](C)c4ccccc4Cl)c(s3)C(N)=O)c2cc1OC
Show InChI InChI=1S/C22H20ClN3O4S/c1-12(13-6-4-5-7-14(13)23)30-19-10-20(31-21(19)22(24)27)26-11-25-15-8-17(28-2)18(29-3)9-16(15)26/h4-12H,1-3H3,(H2,24,27)/t12-/m0/s1
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n/an/a 44n/an/an/an/a7.222



GSK



Assay Description
The compound inhibitory activity was determined by incubation with purified PLK enzyme and biotinylated peptide substrate in the presence ATP/[gamma-...


Bioorg Med Chem Lett 19: 1694-7 (2009)

More data for this
Ligand-Target Pair
Serine/threonine-protein kinase PLK3


(Homo sapiens (human))
BDBM15234
PNG
((1R,3R,5S,9R,18S)-18-(methoxymethyl)-1,5-dimethyl-...)
Show SMILES COC[C@H]1OC(=O)c2coc3c2[C@@]1(C)C1=C([C@@H]2CCC(=O)[C@@]2(C)C[C@H]1OC(C)=O)C3=O
Show InChI InChI=1S/C23H24O8/c1-10(24)30-13-7-22(2)12(5-6-14(22)25)16-18(13)23(3)15(9-28-4)31-21(27)11-8-29-20(17(11)23)19(16)26/h8,12-13,15H,5-7,9H2,1-4H3/t12-,13+,15+,22-,23-/m0/s1
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n/an/a 48n/an/an/an/an/an/a



ActivX Biosciences, Inc.

Curated by ChEMBL


Assay Description
Inhibition of recombinant Plk3 (unknown origin) assessed as casein substrate phosphorylation


J Biol Chem 282: 2505-11 (2007)

More data for this
Ligand-Target Pair
Serine/threonine-protein kinase PLK3


(Homo sapiens (human))
BDBM50318064
PNG
(8-{[2-(Acetylamino)phenyl]amino}-1-methyl-4,5-dihy...)
Show SMILES CC(=O)Nc1ccccc1Nc1ncc2CCc3c(nn(C)c3-c2n1)C(N)=O
Show InChI InChI=1S/C19H19N7O2/c1-10(27)22-13-5-3-4-6-14(13)23-19-21-9-11-7-8-12-16(18(20)28)25-26(2)17(12)15(11)24-19/h3-6,9H,7-8H2,1-2H3,(H2,20,28)(H,22,27)(H,21,23,24)
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n/an/a 49n/an/an/an/an/an/a



Nerviano Medical Sciences Srl

Curated by ChEMBL


Assay Description
Inhibition of Plk3 assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting


J Med Chem 53: 3532-51 (2010)

More data for this
Ligand-Target Pair
Serine/threonine-protein kinase PLK3


(Homo sapiens (human))
BDBM15234
PNG
((1R,3R,5S,9R,18S)-18-(methoxymethyl)-1,5-dimethyl-...)
Show SMILES COC[C@H]1OC(=O)c2coc3c2[C@@]1(C)C1=C([C@@H]2CCC(=O)[C@@]2(C)C[C@H]1OC(C)=O)C3=O
Show InChI InChI=1S/C23H24O8/c1-10(24)30-13-7-22(2)12(5-6-14(22)25)16-18(13)23(3)15(9-28-4)31-21(27)11-8-29-20(17(11)23)19(16)26/h8,12-13,15H,5-7,9H2,1-4H3/t12-,13+,15+,22-,23-/m0/s1
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n/an/a 49n/an/an/an/an/an/a



ActivX Biosciences, Inc.

Curated by ChEMBL


Assay Description
Inhibition of AX7503 binding to recombinant Plk3 (unknown origin) expressed in HeLa cells by Western blot


J Biol Chem 282: 2505-11 (2007)

More data for this
Ligand-Target Pair
Serine/threonine-protein kinase PLK3


(Homo sapiens (human))
BDBM50323119
PNG
((R)-5-(5-(thiophen-2-yl)-1H-benzo[d]imidazol-1-yl)...)
Show SMILES C[C@@H](Oc1cc(sc1C(N)=O)-n1cnc2cc(ccc12)-c1cccs1)c1ccccc1C(F)(F)F
Show InChI InChI=1S/C25H18F3N3O2S2/c1-14(16-5-2-3-6-17(16)25(26,27)28)33-20-12-22(35-23(20)24(29)32)31-13-30-18-11-15(8-9-19(18)31)21-7-4-10-34-21/h2-14H,1H3,(H2,29,32)/t14-/m1/s1
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n/an/a 50n/an/an/an/an/an/a



GlaxoSmithKline

Curated by ChEMBL


Assay Description
Inhibition of full lungth PLK3 by SPA assay


Bioorg Med Chem Lett 20: 4587-92 (2010)

More data for this
Ligand-Target Pair
Serine/threonine-protein kinase PLK3


(Homo sapiens (human))
BDBM50318065
PNG
(1-Methyl-8-[(2-phenoxyphenyl)amino]-4,5-dihydro-1H...)
Show SMILES Cn1nc(C(N)=O)c2CCc3cnc(Nc4ccccc4Oc4ccccc4)nc3-c12
Show InChI InChI=1S/C23H20N6O2/c1-29-21-16(20(28-29)22(24)30)12-11-14-13-25-23(27-19(14)21)26-17-9-5-6-10-18(17)31-15-7-3-2-4-8-15/h2-10,13H,11-12H2,1H3,(H2,24,30)(H,25,26,27)
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n/an/a 51n/an/an/an/an/an/a



Nerviano Medical Sciences Srl

Curated by ChEMBL


Assay Description
Inhibition of Plk3 assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting


J Med Chem 53: 3532-51 (2010)

More data for this
Ligand-Target Pair
Serine/threonine-protein kinase PLK3


(Homo sapiens (human))
BDBM28210
PNG
(3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-{6-[(2S)-2,3-d...)
Show SMILES C[C@@H](Oc1cc(sc1C(N)=O)-n1cnc2ccc(OC[C@@H](O)CO)cc12)c1ccccc1Cl
Show InChI InChI=1S/C23H22ClN3O5S/c1-13(16-4-2-3-5-17(16)24)32-20-9-21(33-22(20)23(25)30)27-12-26-18-7-6-15(8-19(18)27)31-11-14(29)10-28/h2-9,12-14,28-29H,10-11H2,1H3,(H2,25,30)/t13-,14+/m1/s1
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n/an/a 61n/an/an/an/a7.222



GSK



Assay Description
The compound inhibitory activity was determined by incubation with purified PLK enzyme and biotinylated peptide substrate in the presence ATP/[gamma-...


Bioorg Med Chem Lett 19: 1694-7 (2009)

More data for this
Ligand-Target Pair
Serine/threonine-protein kinase PLK3


(Homo sapiens (human))
BDBM50362983
PNG
(CHEMBL1945804)
Show SMILES CN(C)CCCc1cnc(C)c(Nc2ncc3CC(=S)Nc4cc(Cl)ccc4-c3n2)c1
Show InChI InChI=1S/C23H25ClN6S/c1-14-19(9-15(12-25-14)5-4-8-30(2)3)28-23-26-13-16-10-21(31)27-20-11-17(24)6-7-18(20)22(16)29-23/h6-7,9,11-13H,4-5,8,10H2,1-3H3,(H,27,31)(H,26,28,29)
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n/an/a 64n/an/an/an/an/an/a



Millennium Pharmaceuticals, Inc.

Curated by ChEMBL


Assay Description
Inhibition of PLK3


J Med Chem 55: 197-208 (2012)

More data for this
Ligand-Target Pair
Serine/threonine-protein kinase PLK3


(Homo sapiens (human))
BDBM50318063
PNG
(8-{[2-Methoxy-4-(4-methylpiperazin-1-yl)phenyl]ami...)
Show SMILES COc1cc(ccc1Nc1ncc2CCc3c(nn(C)c3-c2n1)C(N)=O)N1CCN(C)CC1
Show InChI InChI=1S/C23H28N8O2/c1-29-8-10-31(11-9-29)15-5-7-17(18(12-15)33-3)26-23-25-13-14-4-6-16-20(22(24)32)28-30(2)21(16)19(14)27-23/h5,7,12-13H,4,6,8-11H2,1-3H3,(H2,24,32)(H,25,26,27)
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n/an/a 66n/an/an/an/an/an/a



Nerviano Medical Sciences Srl

Curated by ChEMBL


Assay Description
Inhibition of Plk3 assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting


J Med Chem 53: 3532-51 (2010)

More data for this
Ligand-Target Pair
Serine/threonine-protein kinase PLK3


(Homo sapiens (human))
BDBM50362980
PNG
(CHEMBL1945172)
Show SMILES CN(C)CCCc1ccc(Cl)c(Nc2ncc3CC(=S)Nc4cc(Cl)ccc4-c3n2)c1
Show InChI InChI=1S/C23H23Cl2N5S/c1-30(2)9-3-4-14-5-8-18(25)20(10-14)28-23-26-13-15-11-21(31)27-19-12-16(24)6-7-17(19)22(15)29-23/h5-8,10,12-13H,3-4,9,11H2,1-2H3,(H,27,31)(H,26,28,29)
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n/an/a 73n/an/an/an/an/an/a



Millennium Pharmaceuticals, Inc.

Curated by ChEMBL


Assay Description
Inhibition of PLK3


J Med Chem 55: 197-208 (2012)

More data for this
Ligand-Target Pair
Serine/threonine-protein kinase PLK3


(Homo sapiens (human))
BDBM50323118
PNG
((R)-5-(5-(pyridin-2-yl)-1H-benzo[d]imidazol-1-yl)-...)
Show SMILES C[C@@H](Oc1cc(sc1C(N)=O)-n1cnc2cc(ccc12)-c1ccccn1)c1ccccc1C(F)(F)F
Show InChI InChI=1S/C26H19F3N4O2S/c1-15(17-6-2-3-7-18(17)26(27,28)29)35-22-13-23(36-24(22)25(30)34)33-14-32-20-12-16(9-10-21(20)33)19-8-4-5-11-31-19/h2-15H,1H3,(H2,30,34)/t15-/m1/s1
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n/an/a 79n/an/an/an/an/an/a



GlaxoSmithKline

Curated by ChEMBL


Assay Description
Inhibition of full lungth PLK3 by SPA assay


Bioorg Med Chem Lett 20: 4587-92 (2010)

More data for this
Ligand-Target Pair
Serine/threonine-protein kinase PLK3


(Homo sapiens (human))
BDBM50329933
PNG
(1-methyl-8-(5-(4-(piperazine-1-carbonyl)piperazin-...)
Show SMILES Cn1nc(C(N)=O)c2CCc3cnc(Nc4cc(ccc4OC(F)(F)F)N4CCN(CC4)C(=O)N4CCNCC4)nc3-c12
Show InChI InChI=1S/C27H31F3N10O3/c1-37-23-18(22(36-37)24(31)41)4-2-16-15-33-25(35-21(16)23)34-19-14-17(3-5-20(19)43-27(28,29)30)38-10-12-40(13-11-38)26(42)39-8-6-32-7-9-39/h3,5,14-15,32H,2,4,6-13H2,1H3,(H2,31,41)(H,33,34,35)
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n/an/a 83n/an/an/an/an/an/a



Nerviano Medical Sciences srl

Curated by ChEMBL


Assay Description
Inhibition of PLK3


Bioorg Med Chem Lett 20: 6489-94 (2010)

More data for this
Ligand-Target Pair
Serine/threonine-protein kinase PLK3


(Homo sapiens (human))
BDBM50275665
PNG
(5-methyl-7-phenyl-N-(3,4,5-trimethoxyphenyl)imidaz...)
Show SMILES COc1cc(Nc2ncc3c(C)nc(-c4ccccc4)n3n2)cc(OC)c1OC
Show InChI InChI=1S/C21H21N5O3/c1-13-16-12-22-21(25-26(16)20(23-13)14-8-6-5-7-9-14)24-15-10-17(27-2)19(29-4)18(11-15)28-3/h5-12H,1-4H3,(H,24,25)
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n/an/a 90n/an/an/an/an/an/a



GlaxoSmithKline

Curated by ChEMBL


Assay Description
Inhibition of PLK3 (unknown origin) expressed in baculovirus infected Trichoplusia ni cells


Bioorg Med Chem Lett 18: 6214-7 (2008)

More data for this
Ligand-Target Pair
Serine/threonine-protein kinase PLK3


(Homo sapiens (human))
BDBM25121
PNG
(4-{[(7R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,...)
Show SMILES CC[C@H]1N(C2CCCC2)c2nc(Nc3ccc(cc3OC)C(=O)NC3CCN(C)CC3)ncc2N(C)C1=O
Show InChI InChI=1S/C28H39N7O3/c1-5-22-27(37)34(3)23-17-29-28(32-25(23)35(22)20-8-6-7-9-20)31-21-11-10-18(16-24(21)38-4)26(36)30-19-12-14-33(2)15-13-19/h10-11,16-17,19-20,22H,5-9,12-15H2,1-4H3,(H,30,36)(H,29,31,32)/t22-/m1/s1
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US Patent
n/an/a 90n/an/an/an/a7.9n/a



Nerviano Medical Sciences S.r.l.

US Patent


Assay Description
The inhibitory activity of putative kinase inhibitors and the potency of selected compounds were determined using a trans-phosphorylation assay.


US Patent US8598172 (2013)

More data for this
Ligand-Target Pair
Serine/threonine-protein kinase PLK3


(Homo sapiens (human))
BDBM50318077
PNG
(1-Methyl-8-{[2-(trifluoromethyl)phenyl]amino}-4,5-...)
Show SMILES Cn1nc(C(N)=O)c2CCc3cnc(Nc4ccccc4C(F)(F)F)nc3-c12
Show InChI InChI=1S/C18H15F3N6O/c1-27-15-10(14(26-27)16(22)28)7-6-9-8-23-17(25-13(9)15)24-12-5-3-2-4-11(12)18(19,20)21/h2-5,8H,6-7H2,1H3,(H2,22,28)(H,23,24,25)
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n/an/a 95n/an/an/an/an/an/a



Nerviano Medical Sciences Srl

Curated by ChEMBL


Assay Description
Inhibition of Plk3 assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting


J Med Chem 53: 3532-51 (2010)

More data for this
Ligand-Target Pair
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