Found 309 hits of ic50 for UniProtKB: Q9H4B4 Target/Host
(Institution) | Ligand | Target/Host
Links | Ligand
Links | Trg + Lig
Links | Ki
nM | ΔG°
kcal/mole | IC50
nM | Kd
nM | EC50/IC50
nM | koff
s-1 | kon
M-1s-1 | pH | Temp
°C |
|---|
Serine/threonine-protein kinase PLK3
(Homo sapiens (Human)) | BDBM50323110
((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 |r| 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 | PDB
NCI pathway
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UniProtKB/SwissProt
antibodypedia
GoogleScholar
AffyNet 
| CHEMBL
PC cid
PC sid
UniChem
Similars
| Article
PubMed
| n/a | n/a | 5 | n/a | n/a | n/a | n/a | n/a | n/a |
GlaxoSmithKline
Curated by ChEMBL
| Assay Description
Inhibition of full lungth PLK3 by SPA assay |
Bioorg Med Chem Lett 20: 4587-92 (2010)
Article DOI: 10.1016/j.bmcl.2010.06.009
BindingDB Entry DOI: 10.7270/Q2MS3SZB |
More data for this
Ligand-Target Pair | |
Serine/threonine-protein kinase PLK3
(Homo sapiens (Human)) | BDBM50362985
(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) | PDB
NCI pathway
KEGG
UniProtKB/SwissProt
antibodypedia
GoogleScholar
AffyNet
| CHEMBL
PC cid
PC sid
UniChem
Similars
| Article
PubMed
| n/a | n/a | 5 | n/a | n/a | n/a | n/a | n/a | n/a |
Millennium Pharmaceuticals, Inc.
Curated by ChEMBL
| Assay Description
Inhibition of PLK3 |
J Med Chem 55: 197-208 (2012)
Article DOI: 10.1021/jm2011172
BindingDB Entry DOI: 10.7270/Q21C1XBR |
More data for this
Ligand-Target Pair | |
Serine/threonine-protein kinase PLK3
(Homo sapiens (Human)) | BDBM50362988
(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) | PDB
NCI pathway
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UniProtKB/SwissProt
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| CHEMBL
PC cid
PC sid
UniChem
Similars
| Article
PubMed
| n/a | n/a | 5 | n/a | n/a | n/a | n/a | n/a | n/a |
Millennium Pharmaceuticals, Inc.
Curated by ChEMBL
| Assay Description
Inhibition of PLK3 |
J Med Chem 55: 197-208 (2012)
Article DOI: 10.1021/jm2011172
BindingDB Entry DOI: 10.7270/Q21C1XBR |
More data for this
Ligand-Target Pair | |
Serine/threonine-protein kinase PLK3
(Homo sapiens (Human)) | BDBM28206
(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 |r| 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 | PDB
NCI pathway
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MMDB
PC cid
PC sid
PDB
UniChem
Similars
| Article
PubMed
| n/a | n/a | 6 | n/a | n/a | n/a | n/a | 7.2 | 22 |
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)
Article DOI: 10.1016/j.bmcl.2009.01.094
BindingDB Entry DOI: 10.7270/Q2319T6X |
More data for this
Ligand-Target Pair | |
Serine/threonine-protein kinase PLK3
(Homo sapiens (Human)) | BDBM50529099
(CHEMBL4592698)Show SMILES CC[C@H]1N(C2CCCC2)c2nc(Nc3ccc(cc3OC)C(=O)NC3CCCC3)ncc2N(C)C1=O |r| Show InChI InChI=1S/C27H36N6O3/c1-4-21-26(35)32(2)22-16-28-27(31-24(22)33(21)19-11-7-8-12-19)30-20-14-13-17(15-23(20)36-3)25(34)29-18-9-5-6-10-18/h13-16,18-19,21H,4-12H2,1-3H3,(H,29,34)(H,28,30,31)/t21-/m1/s1 | PDB
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| PC cid
PC sid
UniChem
| Article
PubMed
| n/a | n/a | 6 | n/a | n/a | n/a | n/a | n/a | n/a |
Hefei University of Technology
Curated by ChEMBL
| Assay Description
Inhibition of recombinant human GST-tagged PLK3 (58 to 340 residues) expressed in baculovirus expression system using ser/thr 16 as substrate incubat... |
Eur J Med Chem 184: (2019)
Article DOI: 10.1016/j.ejmech.2019.111769
BindingDB Entry DOI: 10.7270/Q290278N |
More data for this
Ligand-Target Pair | |
Serine/threonine-protein kinase PLK3
(Homo sapiens (Human)) | BDBM50318085
(1-Methyl-8-[(2-methylphenyl)amino]-4,5-dihydro-1H-...)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) | PDB
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| Article
PubMed
| n/a | n/a | 6 | n/a | n/a | n/a | n/a | n/a | n/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)
Article DOI: 10.1021/jm901713n
BindingDB Entry DOI: 10.7270/Q2RF5V5D |
More data for this
Ligand-Target Pair | |
Serine/threonine-protein kinase PLK3
(Homo sapiens (Human)) | BDBM50323109
((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 |r| 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 | PDB
NCI pathway
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| CHEMBL
PC cid
PC sid
UniChem
Patents
Similars
| Article
PubMed
| n/a | n/a | 6 | n/a | n/a | n/a | n/a | n/a | n/a |
GlaxoSmithKline
Curated by ChEMBL
| Assay Description
Inhibition of full lungth PLK3 by SPA assay |
Bioorg Med Chem Lett 20: 4587-92 (2010)
Article DOI: 10.1016/j.bmcl.2010.06.009
BindingDB Entry DOI: 10.7270/Q2MS3SZB |
More data for this
Ligand-Target Pair | |
Serine/threonine-protein kinase PLK3
(Homo sapiens (Human)) | BDBM50323122
((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 |r| 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 | PDB
NCI pathway
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| CHEMBL
PC cid
PC sid
UniChem
Similars
| Article
PubMed
| n/a | n/a | 6 | n/a | n/a | n/a | n/a | n/a | n/a |
GlaxoSmithKline
Curated by ChEMBL
| Assay Description
Inhibition of full lungth PLK3 by SPA assay |
Bioorg Med Chem Lett 20: 4587-92 (2010)
Article DOI: 10.1016/j.bmcl.2010.06.009
BindingDB Entry DOI: 10.7270/Q2MS3SZB |
More data for this
Ligand-Target Pair | |
Serine/threonine-protein kinase PLK3
(Homo sapiens (Human)) | BDBM26514
(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 |r| 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 | PDB
NCI pathway
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| PC cid
PC sid
UniChem
Similars
| Article
PubMed
| n/a | n/a | 6.70 | n/a | n/a | n/a | n/a | 7.5 | 22 |
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)
Article DOI: 10.1111/j.1747-0285.2007.00594.x
BindingDB Entry DOI: 10.7270/Q2T151Z8 |
More data for this
Ligand-Target Pair | |
Serine/threonine-protein kinase PLK3
(Homo sapiens (Human)) | BDBM50362986
(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) | PDB
NCI pathway
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UniChem
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| Article
PubMed
| n/a | n/a | 7 | n/a | n/a | n/a | n/a | n/a | n/a |
Millennium Pharmaceuticals, Inc.
Curated by ChEMBL
| Assay Description
Inhibition of PLK3 |
J Med Chem 55: 197-208 (2012)
Article DOI: 10.1021/jm2011172
BindingDB Entry DOI: 10.7270/Q21C1XBR |
More data for this
Ligand-Target Pair | |
Serine/threonine-protein kinase PLK3
(Homo sapiens (Human)) | BDBM50323113
((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 |r| 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 | PDB
NCI pathway
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PC sid
UniChem
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| Article
PubMed
| n/a | n/a | 8 | n/a | n/a | n/a | n/a | n/a | n/a |
GlaxoSmithKline
Curated by ChEMBL
| Assay Description
Inhibition of full lungth PLK3 by SPA assay |
Bioorg Med Chem Lett 20: 4587-92 (2010)
Article DOI: 10.1016/j.bmcl.2010.06.009
BindingDB Entry DOI: 10.7270/Q2MS3SZB |
More data for this
Ligand-Target Pair | |
Serine/threonine-protein kinase PLK3
(Homo sapiens (Human)) | BDBM50362984
(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) | PDB
NCI pathway
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| CHEMBL
PC cid
PC sid
UniChem
Similars
| Article
PubMed
| n/a | n/a | 9 | n/a | n/a | n/a | n/a | n/a | n/a |
Millennium Pharmaceuticals, Inc.
Curated by ChEMBL
| Assay Description
Inhibition of PLK3 |
J Med Chem 55: 197-208 (2012)
Article DOI: 10.1021/jm2011172
BindingDB Entry DOI: 10.7270/Q21C1XBR |
More data for this
Ligand-Target Pair | |
Serine/threonine-protein kinase PLK3
(Homo sapiens (Human)) | BDBM25120
(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) | PDB
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MCE
PC cid
PC sid
UniChem
Patents
Similars
| Article
PubMed
| n/a | n/a | 9 | n/a | n/a | n/a | n/a | 7.2 | 22 |
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)
Article DOI: 10.1016/j.bmcl.2008.11.041
BindingDB Entry DOI: 10.7270/Q26T0JZX |
More data for this
Ligand-Target Pair | |
Serine/threonine-protein kinase PLK3
(Homo sapiens (Human)) | BDBM28178
(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) | PDB
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| PC cid
PC sid
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Similars
| Article
PubMed
| n/a | n/a | 9 | n/a | n/a | n/a | n/a | 7.2 | 22 |
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)
Article DOI: 10.1016/j.bmcl.2009.01.094
BindingDB Entry DOI: 10.7270/Q2319T6X |
More data for this
Ligand-Target Pair | |
Serine/threonine-protein kinase PLK3
(Homo sapiens (Human)) | BDBM50323107
((R)-3-(1-(2-chlorophenyl)ethoxy)-5-(5-(pyridin-4-y...)Show SMILES C[C@@H](Oc1cc(sc1C(N)=O)-n1cnc2cc(ccc12)-c1ccncc1)c1ccccc1Cl |r| 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 | PDB
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| n/a | n/a | 10 | n/a | n/a | n/a | n/a | n/a | n/a |
GlaxoSmithKline
Curated by ChEMBL
| Assay Description
Inhibition of full lungth PLK3 by SPA assay |
Bioorg Med Chem Lett 20: 4587-92 (2010)
Article DOI: 10.1016/j.bmcl.2010.06.009
BindingDB Entry DOI: 10.7270/Q2MS3SZB |
More data for this
Ligand-Target Pair | |
Serine/threonine-protein kinase PLK3
(Homo sapiens (Human)) | BDBM50329197
(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 |r| 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 | PDB
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UniChem
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PubMed
| n/a | n/a | >10 | n/a | n/a | n/a | n/a | n/a | n/a |
Merck Research Laboratories
Curated by ChEMBL
| Assay Description
Inhibition of PLK3 |
Bioorg Med Chem Lett 20: 6739-43 (2010)
Article DOI: 10.1016/j.bmcl.2010.08.140
BindingDB Entry DOI: 10.7270/Q2K074HX |
More data for this
Ligand-Target Pair | |
Serine/threonine-protein kinase PLK3
(Homo sapiens (Human)) | BDBM50318061
(1-Methyl-8-{[2-(methylamino)phenyl]amino}-4,5-dihy...)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) | PDB
NCI pathway
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UniChem
Similars
| Article
PubMed
| n/a | n/a | 11 | n/a | n/a | n/a | n/a | n/a | n/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)
Article DOI: 10.1021/jm901713n
BindingDB Entry DOI: 10.7270/Q2RF5V5D |
More data for this
Ligand-Target Pair | |
Serine/threonine-protein kinase PLK3
(Homo sapiens (Human)) | BDBM50362982
(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) | PDB
NCI pathway
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UniChem
Similars
| Article
PubMed
| n/a | n/a | 12 | n/a | n/a | n/a | n/a | n/a | n/a |
Millennium Pharmaceuticals, Inc.
Curated by ChEMBL
| Assay Description
Inhibition of PLK3 |
J Med Chem 55: 197-208 (2012)
Article DOI: 10.1021/jm2011172
BindingDB Entry DOI: 10.7270/Q21C1XBR |
More data for this
Ligand-Target Pair | |
Serine/threonine-protein kinase PLK3
(Homo sapiens (Human)) | BDBM50318074
(8-[(2-Aminophenyl)amino]-1-methyl-4,5-dihydro-1H-p...)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) | PDB
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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)
Article DOI: 10.1021/jm901713n
BindingDB Entry DOI: 10.7270/Q2RF5V5D |
More data for this
Ligand-Target Pair | |
Serine/threonine-protein kinase PLK3
(Homo sapiens (Human)) | BDBM50318081
(8-[(2-Methoxyphenyl)amino]-1-methyl-4,5-dihydro-1H...)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) | PDB
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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)
Article DOI: 10.1021/jm901713n
BindingDB Entry DOI: 10.7270/Q2RF5V5D |
More data for this
Ligand-Target Pair | |
Serine/threonine-protein kinase PLK3
(Homo sapiens (Human)) | BDBM50323123
((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 |r| 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 | PDB
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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)
Article DOI: 10.1016/j.bmcl.2010.06.009
BindingDB Entry DOI: 10.7270/Q2MS3SZB |
More data for this
Ligand-Target Pair | |
Serine/threonine-protein kinase PLK3
(Homo sapiens (Human)) | BDBM25121
(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 |r| 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 | PDB
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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)
Article DOI: 10.1111/j.1747-0285.2007.00594.x
BindingDB Entry DOI: 10.7270/Q2T151Z8 |
More data for this
Ligand-Target Pair | |
Serine/threonine-protein kinase PLK3
(Homo sapiens (Human)) | BDBM31532
(pyrazolo[4,3-h]quinazoline-3-carboxamide, 1)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) | PDB
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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)
Article DOI: 10.1021/jm901713n
BindingDB Entry DOI: 10.7270/Q2RF5V5D |
More data for this
Ligand-Target Pair | |
Serine/threonine-protein kinase PLK3
(Homo sapiens (Human)) | BDBM50323114
((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 |r| 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 | PDB
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| n/a | n/a | 16 | n/a | n/a | n/a | n/a | n/a | n/a |
GlaxoSmithKline
Curated by ChEMBL
| Assay Description
Inhibition of full lungth PLK3 by SPA assay |
Bioorg Med Chem Lett 20: 4587-92 (2010)
Article DOI: 10.1016/j.bmcl.2010.06.009
BindingDB Entry DOI: 10.7270/Q2MS3SZB |
More data for this
Ligand-Target Pair | |
Serine/threonine-protein kinase PLK3
(Homo sapiens (Human)) | BDBM50323116
((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 |r| 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 | PDB
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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)
Article DOI: 10.1016/j.bmcl.2010.06.009
BindingDB Entry DOI: 10.7270/Q2MS3SZB |
More data for this
Ligand-Target Pair | |
Serine/threonine-protein kinase PLK3
(Homo sapiens (Human)) | BDBM50318076
(1-Methyl-8-{[2-(methylsulfanyl)phenyl]amino}-4,5-d...)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) | PDB
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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)
Article DOI: 10.1021/jm901713n
BindingDB Entry DOI: 10.7270/Q2RF5V5D |
More data for this
Ligand-Target Pair | |
Serine/threonine-protein kinase PLK3
(Homo sapiens (Human)) | BDBM50362981
(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) | PDB
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Millennium Pharmaceuticals, Inc.
Curated by ChEMBL
| Assay Description
Inhibition of PLK3 |
J Med Chem 55: 197-208 (2012)
Article DOI: 10.1021/jm2011172
BindingDB Entry DOI: 10.7270/Q21C1XBR |
More data for this
Ligand-Target Pair | |
Serine/threonine-protein kinase PLK3
(Homo sapiens (Human)) | BDBM50529109
(CHEMBL4454222)Show SMILES CC[C@H]1N(C2CCCC2)c2nc(Nc3ccc(cc3C)C(=O)NC3CCCC3)ncc2N(C)C1=O |r| Show InChI InChI=1S/C27H36N6O2/c1-4-22-26(35)32(3)23-16-28-27(31-24(23)33(22)20-11-7-8-12-20)30-21-14-13-18(15-17(21)2)25(34)29-19-9-5-6-10-19/h13-16,19-20,22H,4-12H2,1-3H3,(H,29,34)(H,28,30,31)/t22-/m1/s1 | PDB
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Hefei University of Technology
Curated by ChEMBL
| Assay Description
Inhibition of recombinant human GST-tagged PLK3 (58 to 340 residues) expressed in baculovirus expression system using ser/thr 16 as substrate incubat... |
Eur J Med Chem 184: (2019)
Article DOI: 10.1016/j.ejmech.2019.111769
BindingDB Entry DOI: 10.7270/Q290278N |
More data for this
Ligand-Target Pair | |
Serine/threonine-protein kinase PLK3
(Homo sapiens (Human)) | BDBM25121
(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 |r| 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 | PDB
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Hefei University of Technology
Curated by ChEMBL
| Assay Description
Inhibition of recombinant human GST-tagged PLK3 (58 to 340 residues) expressed in baculovirus expression system using ser/thr 16 as substrate incubat... |
Eur J Med Chem 184: (2019)
Article DOI: 10.1016/j.ejmech.2019.111769
BindingDB Entry DOI: 10.7270/Q290278N |
More data for this
Ligand-Target Pair | |
Serine/threonine-protein kinase PLK3
(Homo sapiens (Human)) | BDBM25121
(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 |r| 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 | PDB
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Hefei University of Technology
Curated by ChEMBL
| Assay Description
Inhibition human recombinant GST-tagged Plk3 catalytic domain (58 to 340 residues) expressed in baculovirus expression system after 1 hr by FRET-base... |
Eur J Med Chem 143: 724-731 (2018)
Article DOI: 10.1016/j.ejmech.2017.11.058
BindingDB Entry DOI: 10.7270/Q27D2XPT |
More data for this
Ligand-Target Pair | |
Serine/threonine-protein kinase PLK3
(Homo sapiens (Human)) | BDBM50529084
(CHEMBL4458460)Show SMILES CC[C@H]1N(C2CCCC2)c2nc(Nc3cc(F)c(cc3OCCO)C(=O)NC3CCCC3)ncc2N(C)C1=O |r| Show InChI InChI=1S/C28H37FN6O4/c1-3-22-27(38)34(2)23-16-30-28(33-25(23)35(22)18-10-6-7-11-18)32-21-15-20(29)19(14-24(21)39-13-12-36)26(37)31-17-8-4-5-9-17/h14-18,22,36H,3-13H2,1-2H3,(H,31,37)(H,30,32,33)/t22-/m1/s1 | PDB
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Hefei University of Technology
Curated by ChEMBL
| Assay Description
Inhibition of recombinant human GST-tagged PLK3 (58 to 340 residues) expressed in baculovirus expression system using ser/thr 16 as substrate incubat... |
Eur J Med Chem 184: (2019)
Article DOI: 10.1016/j.ejmech.2019.111769
BindingDB Entry DOI: 10.7270/Q290278N |
More data for this
Ligand-Target Pair | |
Serine/threonine-protein kinase PLK3
(Homo sapiens (Human)) | BDBM24933
(2-amino-isoxazolopyridine, 9 | 3-(2H-1,3-benzodiox...)Show SMILES C[C@H](Nc1cc2c(noc2cn1)-c1ccc2OCOc2c1)c1ccccc1 |r| 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 | PDB
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| n/a | n/a | 24 | n/a | n/a | n/a | n/a | 7.2 | 30 |
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)
Article DOI: 10.1016/j.bmcl.2008.08.091
BindingDB Entry DOI: 10.7270/Q22Z13T8 |
More data for this
Ligand-Target Pair | |
Serine/threonine-protein kinase PLK3
(Homo sapiens (Human)) | BDBM50323115
((R)-3-(1-(2-chlorophenyl)ethoxy)-5-(6-(pyridin-4-y...)Show SMILES C[C@@H](Oc1cc(sc1C(N)=O)-n1cnc2ccc(cc12)-c1ccncc1)c1ccccc1Cl |r| 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 | PDB
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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)
Article DOI: 10.1016/j.bmcl.2010.06.009
BindingDB Entry DOI: 10.7270/Q2MS3SZB |
More data for this
Ligand-Target Pair | |
Serine/threonine-protein kinase PLK3
(Homo sapiens (Human)) | BDBM50275752
(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) | PDB
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| n/a | n/a | 30 | n/a | n/a | n/a | n/a | n/a | n/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)
Article DOI: 10.1016/j.bmcl.2008.09.100
BindingDB Entry DOI: 10.7270/Q22Z15DQ |
More data for this
Ligand-Target Pair | |
Serine/threonine-protein kinase PLK3
(Homo sapiens (Human)) | BDBM50529100
(CHEMBL4548940)Show SMILES CC[C@H]1N(C2CCCC2)c2nc(Nc3ccc(cc3O)C(=O)NC3CCCC3)ncc2N(C)C1=O |r| Show InChI InChI=1S/C26H34N6O3/c1-3-20-25(35)31(2)21-15-27-26(30-23(21)32(20)18-10-6-7-11-18)29-19-13-12-16(14-22(19)33)24(34)28-17-8-4-5-9-17/h12-15,17-18,20,33H,3-11H2,1-2H3,(H,28,34)(H,27,29,30)/t20-/m1/s1 | PDB
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Hefei University of Technology
Curated by ChEMBL
| Assay Description
Inhibition of recombinant human GST-tagged PLK3 (58 to 340 residues) expressed in baculovirus expression system using ser/thr 16 as substrate incubat... |
Eur J Med Chem 184: (2019)
Article DOI: 10.1016/j.ejmech.2019.111769
BindingDB Entry DOI: 10.7270/Q290278N |
More data for this
Ligand-Target Pair | |
Serine/threonine-protein kinase PLK3
(Homo sapiens (Human)) | BDBM50362976
(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) | PDB
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Millennium Pharmaceuticals, Inc.
Curated by ChEMBL
| Assay Description
Inhibition of PLK3 |
J Med Chem 55: 197-208 (2012)
Article DOI: 10.1021/jm2011172
BindingDB Entry DOI: 10.7270/Q21C1XBR |
More data for this
Ligand-Target Pair | |
Serine/threonine-protein kinase PLK3
(Homo sapiens (Human)) | BDBM50329932
(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) | PDB
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| n/a | n/a | 32 | n/a | n/a | n/a | n/a | n/a | n/a |
Nerviano Medical Sciences srl
Curated by ChEMBL
| Assay Description
Inhibition of PLK3 |
Bioorg Med Chem Lett 20: 6489-94 (2010)
Article DOI: 10.1016/j.bmcl.2010.09.060
BindingDB Entry DOI: 10.7270/Q2VT1T39 |
More data for this
Ligand-Target Pair | |
Serine/threonine-protein kinase PLK3
(Homo sapiens (Human)) | BDBM28208
(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 |r| 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 | PDB
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| n/a | n/a | 35 | n/a | n/a | n/a | n/a | 7.2 | 22 |
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)
Article DOI: 10.1016/j.bmcl.2009.01.094
BindingDB Entry DOI: 10.7270/Q2319T6X |
More data for this
Ligand-Target Pair | |
Serine/threonine-protein kinase PLK3
(Homo sapiens (Human)) | BDBM50318062
(8-[(2-Fluorophenyl)amino]-1-methyl-4,5-dihydro-1H-...)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) | PDB
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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)
Article DOI: 10.1021/jm901713n
BindingDB Entry DOI: 10.7270/Q2RF5V5D |
More data for this
Ligand-Target Pair | |
Serine/threonine-protein kinase PLK3
(Homo sapiens (Human)) | BDBM50285537
(CHEMBL4166771)Show SMILES CC[C@H]1N(C2CCCC2)c2nc(Nc3ccc(cc3)S(=O)(=O)NC)ncc2N(C)C1=O |r| Show InChI InChI=1S/C21H28N6O3S/c1-4-17-20(28)26(3)18-13-23-21(25-19(18)27(17)15-7-5-6-8-15)24-14-9-11-16(12-10-14)31(29,30)22-2/h9-13,15,17,22H,4-8H2,1-3H3,(H,23,24,25)/t17-/m1/s1 | PDB
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Hefei University of Technology
Curated by ChEMBL
| Assay Description
Inhibition human recombinant GST-tagged Plk3 catalytic domain (58 to 340 residues) expressed in baculovirus expression system after 1 hr by FRET-base... |
Eur J Med Chem 143: 724-731 (2018)
Article DOI: 10.1016/j.ejmech.2017.11.058
BindingDB Entry DOI: 10.7270/Q27D2XPT |
More data for this
Ligand-Target Pair | |
Serine/threonine-protein kinase PLK3
(Homo sapiens (Human)) | BDBM50323117
((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 |r| 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 | PDB
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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)
Article DOI: 10.1016/j.bmcl.2010.06.009
BindingDB Entry DOI: 10.7270/Q2MS3SZB |
More data for this
Ligand-Target Pair | |
Serine/threonine-protein kinase PLK3
(Homo sapiens (Human)) | BDBM28209
(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 |r| 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 | PDB
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| n/a | n/a | 41 | n/a | n/a | n/a | n/a | 7.2 | 22 |
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)
Article DOI: 10.1016/j.bmcl.2009.01.094
BindingDB Entry DOI: 10.7270/Q2319T6X |
More data for this
Ligand-Target Pair | |
Serine/threonine-protein kinase PLK3
(Homo sapiens (Human)) | BDBM28207
(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 |r| 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 | PDB
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| n/a | n/a | 44 | n/a | n/a | n/a | n/a | 7.2 | 22 |
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)
Article DOI: 10.1016/j.bmcl.2009.01.094
BindingDB Entry DOI: 10.7270/Q2319T6X |
More data for this
Ligand-Target Pair | |
Serine/threonine-protein kinase PLK3
(Homo sapiens (Human)) | BDBM50529107
(CHEMBL4456400)Show SMILES CC[C@H]1N(C2CCCC2)c2nc(Nc3cc(F)c(cc3OCCO)C(=O)NC)ncc2N(C)C1=O |r| Show InChI InChI=1S/C24H31FN6O4/c1-4-18-23(34)30(3)19-13-27-24(29-21(19)31(18)14-7-5-6-8-14)28-17-12-16(25)15(22(33)26-2)11-20(17)35-10-9-32/h11-14,18,32H,4-10H2,1-3H3,(H,26,33)(H,27,28,29)/t18-/m1/s1 | PDB
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Hefei University of Technology
Curated by ChEMBL
| Assay Description
Inhibition of recombinant human GST-tagged PLK3 (58 to 340 residues) expressed in baculovirus expression system using ser/thr 16 as substrate incubat... |
Eur J Med Chem 184: (2019)
Article DOI: 10.1016/j.ejmech.2019.111769
BindingDB Entry DOI: 10.7270/Q290278N |
More data for this
Ligand-Target Pair | |
Serine/threonine-protein kinase PLK3
(Homo sapiens (Human)) | BDBM50529116
(CHEMBL4457656)Show SMILES CC[C@H]1N(C2CCCC2)c2nc(Nc3cc(F)c(cc3OCCO)C(=O)NC(C)C)ncc2N(C)C1=O |r| Show InChI InChI=1S/C26H35FN6O4/c1-5-20-25(36)32(4)21-14-28-26(31-23(21)33(20)16-8-6-7-9-16)30-19-13-18(27)17(24(35)29-15(2)3)12-22(19)37-11-10-34/h12-16,20,34H,5-11H2,1-4H3,(H,29,35)(H,28,30,31)/t20-/m1/s1 | PDB
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Hefei University of Technology
Curated by ChEMBL
| Assay Description
Inhibition of recombinant human GST-tagged PLK3 (58 to 340 residues) expressed in baculovirus expression system using ser/thr 16 as substrate incubat... |
Eur J Med Chem 184: (2019)
Article DOI: 10.1016/j.ejmech.2019.111769
BindingDB Entry DOI: 10.7270/Q290278N |
More data for this
Ligand-Target Pair | |
Serine/threonine-protein kinase PLK3
(Homo sapiens (Human)) | BDBM50529094
(CHEMBL4570557)Show SMILES CCNC(=O)c1cc(OCCO)c(Nc2ncc3N(C)C(=O)[C@@H](CC)N(C4CCCC4)c3n2)cc1F |r| Show InChI InChI=1S/C25H33FN6O4/c1-4-19-24(35)31(3)20-14-28-25(30-22(20)32(19)15-8-6-7-9-15)29-18-13-17(26)16(23(34)27-5-2)12-21(18)36-11-10-33/h12-15,19,33H,4-11H2,1-3H3,(H,27,34)(H,28,29,30)/t19-/m1/s1 | PDB
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Hefei University of Technology
Curated by ChEMBL
| Assay Description
Inhibition of recombinant human GST-tagged PLK3 (58 to 340 residues) expressed in baculovirus expression system using ser/thr 16 as substrate incubat... |
Eur J Med Chem 184: (2019)
Article DOI: 10.1016/j.ejmech.2019.111769
BindingDB Entry DOI: 10.7270/Q290278N |
More data for this
Ligand-Target Pair | |
Serine/threonine-protein kinase PLK3
(Homo sapiens (Human)) | BDBM15234
((1R,3R,5S,9R,18S)-18-(methoxymethyl)-1,5-dimethyl-...)Show SMILES [H][C@@]12CCC(=O)[C@@]1(C)C[C@@H](OC(C)=O)C1=C2C(=O)c2occ3c2[C@]1(C)[C@@H](COC)OC3=O |r,c:15| 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 | PDB
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| n/a | n/a | 48 | n/a | n/a | n/a | n/a | n/a | n/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)
Article DOI: 10.1074/jbc.M609603200
BindingDB Entry DOI: 10.7270/Q2QV3M8X |
More data for this
Ligand-Target Pair | |
Serine/threonine-protein kinase PLK3
(Homo sapiens (Human)) | BDBM50318064
(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) | PDB
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| n/a | n/a | 49 | n/a | n/a | n/a | n/a | n/a | n/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)
Article DOI: 10.1021/jm901713n
BindingDB Entry DOI: 10.7270/Q2RF5V5D |
More data for this
Ligand-Target Pair | |
Serine/threonine-protein kinase PLK3
(Homo sapiens (Human)) | BDBM15234
((1R,3R,5S,9R,18S)-18-(methoxymethyl)-1,5-dimethyl-...)Show SMILES [H][C@@]12CCC(=O)[C@@]1(C)C[C@@H](OC(C)=O)C1=C2C(=O)c2occ3c2[C@]1(C)[C@@H](COC)OC3=O |r,c:15| 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 | PDB
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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)
Article DOI: 10.1074/jbc.M609603200
BindingDB Entry DOI: 10.7270/Q2QV3M8X |
More data for this
Ligand-Target Pair | |
Serine/threonine-protein kinase PLK3
(Homo sapiens (Human)) | BDBM50323119
((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 |r| 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 | PDB
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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)
Article DOI: 10.1016/j.bmcl.2010.06.009
BindingDB Entry DOI: 10.7270/Q2MS3SZB |
More data for this
Ligand-Target Pair | |
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