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Compile Data Set for Download or QSAR

Found 282 hits of ic50 for UniProtKB: Q9NYY3   
Target/Host
(Institution)
LigandTarget/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
pHTemp
°C
Serine/threonine-protein kinase PLK2


(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 2n/an/an/an/an/an/a



Nerviano Medical Sciences Srl

Curated by ChEMBL


Assay Description
Inhibition of Plk2 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 PLK2


(Homo sapiens (Human))
BDBM50285537
PNG
(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
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n/an/a 3.40n/an/an/an/an/an/a



Hefei University of Technology

Curated by ChEMBL


Assay Description
Inhibition human recombinant full length GST-tagged Plk2 expressed in baculovirus expression system after 1 hr by FRET-based Z'-Lyte assay


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 PLK2


(Homo sapiens (Human))
BDBM24933
PNG
(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
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n/an/a 4n/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)


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 PLK2


(Homo sapiens (Human))
BDBM50529099
PNG
(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
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n/an/a 4n/an/an/an/an/an/a



Hefei University of Technology

Curated by ChEMBL


Assay Description
Inhibition of recombinant full length human GST-tagged PLK2 expressed in baculovirus expression system using ser/thr 16 as substrate incubated for 1 ...


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 PLK2


(Homo sapiens (Human))
BDBM50529109
PNG
(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
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n/an/a 4.70n/an/an/an/an/an/a



Hefei University of Technology

Curated by ChEMBL


Assay Description
Inhibition of recombinant full length human GST-tagged PLK2 expressed in baculovirus expression system using ser/thr 16 as substrate incubated for 1 ...


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 PLK2


(Homo sapiens (Human))
BDBM50285547
PNG
(CHEMBL4171770)
Show SMILES CCNC(=O)c1ccc2n(ccc2c1)-c1ncc2N(C)C(=O)[C@@H](CC)N(C3CCCC3)c2n1 |r|
Show InChI InChI=1S/C25H30N6O2/c1-4-19-24(33)29(3)21-15-27-25(28-22(21)31(19)18-8-6-7-9-18)30-13-12-16-14-17(10-11-20(16)30)23(32)26-5-2/h10-15,18-19H,4-9H2,1-3H3,(H,26,32)/t19-/m1/s1
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n/an/a 4.90n/an/an/an/an/an/a



Hefei University of Technology

Curated by ChEMBL


Assay Description
Inhibition human recombinant full length GST-tagged Plk2 expressed in baculovirus expression system after 1 hr by FRET-based Z'-Lyte assay


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 PLK2


(Homo sapiens (Human))
CHEMBL5276995
PNG
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n/an/a 5n/an/an/an/an/an/a


TBA



Citation and Details
More data for this
Ligand-Target Pair
Serine/threonine-protein kinase PLK2


(Homo sapiens (Human))
BDBM50436720
PNG
(CHEMBL2401963)
Show SMILES CC[C@H]1N(C2CCCC2)c2nc(ncc2N(C)C1=O)-n1ccnc1-c1ccccc1 |r|
Show InChI InChI=1S/C23H26N6O/c1-3-18-22(30)27(2)19-15-25-23(26-21(19)29(18)17-11-7-8-12-17)28-14-13-24-20(28)16-9-5-4-6-10-16/h4-6,9-10,13-15,17-18H,3,7-8,11-12H2,1-2H3/t18-/m1/s1
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n/an/a 5n/an/an/an/an/an/a



Elan Pharmaceuticals

Curated by ChEMBL


Assay Description
Inhibition of GST-tagged Plk2 (unknown origin) assessed as inhibition of DEKTDDED phosphorylation at Thr1342 after 60 mins by TR-FRET assay


Bioorg Med Chem Lett 23: 2743-9 (2013)


Article DOI: 10.1016/j.bmcl.2013.02.065
BindingDB Entry DOI: 10.7270/Q28G8N4M
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Serine/threonine-protein kinase PLK2


(Homo sapiens (Human))
BDBM50436742
PNG
(CHEMBL2402081)
Show SMILES CC[C@H]1N(c2ccn(C)n2)c2nc(ncc2N(C)C1=O)-n1ccnc1-c1ccc(F)cc1 |r|
Show InChI InChI=1S/C22H21FN8O/c1-4-16-21(32)29(3)17-13-25-22(26-20(17)31(16)18-9-11-28(2)27-18)30-12-10-24-19(30)14-5-7-15(23)8-6-14/h5-13,16H,4H2,1-3H3/t16-/m1/s1
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n/an/a 7n/an/an/an/an/an/a



Elan Pharmaceuticals

Curated by ChEMBL


Assay Description
Inhibition of GST-tagged Plk2 (unknown origin) assessed as inhibition of DEKTDDED phosphorylation at Thr1342 after 60 mins by TR-FRET assay


Bioorg Med Chem Lett 23: 2743-9 (2013)


Article DOI: 10.1016/j.bmcl.2013.02.065
BindingDB Entry DOI: 10.7270/Q28G8N4M
More data for this
Ligand-Target Pair
Serine/threonine-protein kinase PLK2


(Homo sapiens (Human))
BDBM50285531
PNG
(CHEMBL4175722)
Show SMILES CC[C@H]1N(C2CCCC2)c2nc(ncc2N(C)C1=O)-n1ccc2cc(ccc12)C(=O)NC1CCCC1 |r|
Show InChI InChI=1S/C28H34N6O2/c1-3-22-27(36)32(2)24-17-29-28(31-25(24)34(22)21-10-6-7-11-21)33-15-14-18-16-19(12-13-23(18)33)26(35)30-20-8-4-5-9-20/h12-17,20-22H,3-11H2,1-2H3,(H,30,35)/t22-/m1/s1
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n/an/a 7.10n/an/an/an/an/an/a



Hefei University of Technology

Curated by ChEMBL


Assay Description
Inhibition human recombinant full length GST-tagged Plk2 expressed in baculovirus expression system after 1 hr by FRET-based Z'-Lyte assay


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 PLK2


(Homo sapiens (Human))
BDBM50285587
PNG
(CHEMBL4176983)
Show SMILES CC[C@H]1N(C2CCCC2)c2nc(Nc3ccc(cc3)S(=O)(=O)NCCO)ncc2N(C)C1=O |r|
Show InChI InChI=1S/C22H30N6O4S/c1-3-18-21(30)27(2)19-14-23-22(26-20(19)28(18)16-6-4-5-7-16)25-15-8-10-17(11-9-15)33(31,32)24-12-13-29/h8-11,14,16,18,24,29H,3-7,12-13H2,1-2H3,(H,23,25,26)/t18-/m1/s1
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n/an/a 7.90n/an/an/an/an/an/a



Hefei University of Technology

Curated by ChEMBL


Assay Description
Inhibition human recombinant full length GST-tagged Plk2 expressed in baculovirus expression system after 1 hr by FRET-based Z'-Lyte assay


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 PLK2


(Homo sapiens (Human))
BDBM50436746
PNG
(CHEMBL2401971)
Show SMILES CC[C@H]1N([C@H]2CCOC2)c2nc(ncc2N(C)C1=O)-n1ccnc1-c1ccccc1 |r|
Show InChI InChI=1S/C22H24N6O2/c1-3-17-21(29)26(2)18-13-24-22(25-20(18)28(17)16-9-12-30-14-16)27-11-10-23-19(27)15-7-5-4-6-8-15/h4-8,10-11,13,16-17H,3,9,12,14H2,1-2H3/t16-,17+/m0/s1
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n/an/a 8n/an/an/an/an/an/a



Elan Pharmaceuticals

Curated by ChEMBL


Assay Description
Inhibition of GST-tagged Plk2 (unknown origin) assessed as inhibition of DEKTDDED phosphorylation at Thr1342 after 60 mins by TR-FRET assay


Bioorg Med Chem Lett 23: 2743-9 (2013)


Article DOI: 10.1016/j.bmcl.2013.02.065
BindingDB Entry DOI: 10.7270/Q28G8N4M
More data for this
Ligand-Target Pair
Serine/threonine-protein kinase PLK2


(Homo sapiens (Human))
BDBM50529100
PNG
(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
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n/an/a 8n/an/an/an/an/an/a



Hefei University of Technology

Curated by ChEMBL


Assay Description
Inhibition of recombinant full length human GST-tagged PLK2 expressed in baculovirus expression system using ser/thr 16 as substrate incubated for 1 ...


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 PLK2


(Homo sapiens (Human))
BDBM50285526
PNG
(CHEMBL4169129)
Show SMILES CC[C@H]1N(C2CCCC2)c2nc(Nc3ccc(cc3)S(=O)(=O)NCCCO)ncc2N(C)C1=O |r|
Show InChI InChI=1S/C23H32N6O4S/c1-3-19-22(31)28(2)20-15-24-23(27-21(20)29(19)17-7-4-5-8-17)26-16-9-11-18(12-10-16)34(32,33)25-13-6-14-30/h9-12,15,17,19,25,30H,3-8,13-14H2,1-2H3,(H,24,26,27)/t19-/m1/s1
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n/an/a 8.20n/an/an/an/an/an/a



Hefei University of Technology

Curated by ChEMBL


Assay Description
Inhibition human recombinant full length GST-tagged Plk2 expressed in baculovirus expression system after 1 hr by FRET-based Z'-Lyte assay


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 PLK2


(Homo sapiens (Human))
BDBM50285580
PNG
(CHEMBL4163892)
Show SMILES CC[C@H]1N(C2CCCC2)c2nc(ncc2N(C)C1=O)-n1ccc2cc(ccc12)C(=O)NC |r|
Show InChI InChI=1S/C24H28N6O2/c1-4-18-23(32)28(3)20-14-26-24(27-21(20)30(18)17-7-5-6-8-17)29-12-11-15-13-16(22(31)25-2)9-10-19(15)29/h9-14,17-18H,4-8H2,1-3H3,(H,25,31)/t18-/m1/s1
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n/an/a 8.60n/an/an/an/an/an/a



Hefei University of Technology

Curated by ChEMBL


Assay Description
Inhibition human recombinant full length GST-tagged Plk2 expressed in baculovirus expression system after 1 hr by FRET-based Z'-Lyte assay


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 PLK2


(Homo sapiens (Human))
BDBM50436749
PNG
(CHEMBL2401966)
Show SMILES CC[C@H]1N(CCC(F)(F)F)c2nc(ncc2N(C)C1=O)-n1ccnc1-c1ccccc1 |r|
Show InChI InChI=1S/C21H21F3N6O/c1-3-15-19(31)28(2)16-13-26-20(27-18(16)29(15)11-9-21(22,23)24)30-12-10-25-17(30)14-7-5-4-6-8-14/h4-8,10,12-13,15H,3,9,11H2,1-2H3/t15-/m1/s1
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n/an/a 9n/an/an/an/an/an/a



Elan Pharmaceuticals

Curated by ChEMBL


Assay Description
Inhibition of GST-tagged Plk2 (unknown origin) assessed as inhibition of DEKTDDED phosphorylation at Thr1342 after 60 mins by TR-FRET assay


Bioorg Med Chem Lett 23: 2743-9 (2013)


Article DOI: 10.1016/j.bmcl.2013.02.065
BindingDB Entry DOI: 10.7270/Q28G8N4M
More data for this
Ligand-Target Pair
Serine/threonine-protein kinase PLK2


(Homo sapiens (Human))
BDBM50436734
PNG
(CHEMBL2402079)
Show SMILES CCC1N(c2ccn[nH]2)c2nc(ncc2N(C)C1=O)-n1ccnc1-c1ccc(F)cc1
Show InChI InChI=1S/C21H19FN8O/c1-3-15-20(31)28(2)16-12-24-21(26-19(16)30(15)17-8-9-25-27-17)29-11-10-23-18(29)13-4-6-14(22)7-5-13/h4-12,15H,3H2,1-2H3,(H,25,27)
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n/an/a 9n/an/an/an/an/an/a



Elan Pharmaceuticals

Curated by ChEMBL


Assay Description
Inhibition of GST-tagged Plk2 (unknown origin) assessed as inhibition of DEKTDDED phosphorylation at Thr1342 after 60 mins by TR-FRET assay


Bioorg Med Chem Lett 23: 2743-9 (2013)


Article DOI: 10.1016/j.bmcl.2013.02.065
BindingDB Entry DOI: 10.7270/Q28G8N4M
More data for this
Ligand-Target Pair
Serine/threonine-protein kinase PLK2


(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 9n/an/an/an/an/an/a



Nerviano Medical Sciences Srl

Curated by ChEMBL


Assay Description
Inhibition of Plk2 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 PLK2


(Homo sapiens (Human))
BDBM50285583
PNG
(CHEMBL4168155)
Show SMILES CC[C@H]1N(C2CCCC2)c2nc(Nc3ccc(cc3)S(N)(=O)=O)ncc2N(C)C1=O |r|
Show InChI InChI=1S/C20H26N6O3S/c1-3-16-19(27)25(2)17-12-22-20(24-18(17)26(16)14-6-4-5-7-14)23-13-8-10-15(11-9-13)30(21,28)29/h8-12,14,16H,3-7H2,1-2H3,(H2,21,28,29)(H,22,23,24)/t16-/m1/s1
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n/an/a 10n/an/an/an/an/an/a



Hefei University of Technology

Curated by ChEMBL


Assay Description
Inhibition human recombinant full length GST-tagged Plk2 expressed in baculovirus expression system after 1 hr by FRET-based Z'-Lyte assay


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 PLK2


(Homo sapiens (Human))
BDBM50285586
PNG
(CHEMBL4164012)
Show SMILES CCCNC(=O)c1ccc2n(ccc2c1)-c1ncc2N(C)C(=O)[C@@H](CC)N(C3CCCC3)c2n1 |r|
Show InChI InChI=1S/C26H32N6O2/c1-4-13-27-24(33)18-10-11-21-17(15-18)12-14-31(21)26-28-16-22-23(29-26)32(19-8-6-7-9-19)20(5-2)25(34)30(22)3/h10-12,14-16,19-20H,4-9,13H2,1-3H3,(H,27,33)/t20-/m1/s1
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n/an/a 11n/an/an/an/an/an/a



Hefei University of Technology

Curated by ChEMBL


Assay Description
Inhibition human recombinant full length GST-tagged Plk2 expressed in baculovirus expression system after 1 hr by FRET-based Z'-Lyte assay


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 PLK2


(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 |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
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n/an/a 11.5n/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)


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 PLK2


(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 12n/an/an/an/an/an/a



Nerviano Medical Sciences Srl

Curated by ChEMBL


Assay Description
Inhibition of Plk2 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 PLK2


(Homo sapiens (Human))
BDBM50436726
PNG
(CHEMBL2401969)
Show SMILES CC[C@H]1N(C2CC(F)(F)C2)c2nc(ncc2N(C)C1=O)-n1ccnc1-c1ccc(F)cc1 |r|
Show InChI InChI=1S/C22H21F3N6O/c1-3-16-20(32)29(2)17-12-27-21(28-19(17)31(16)15-10-22(24,25)11-15)30-9-8-26-18(30)13-4-6-14(23)7-5-13/h4-9,12,15-16H,3,10-11H2,1-2H3/t16-/m1/s1
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n/an/a 12n/an/an/an/an/an/a



Elan Pharmaceuticals

Curated by ChEMBL


Assay Description
Inhibition of GST-tagged Plk2 (unknown origin) assessed as inhibition of DEKTDDED phosphorylation at Thr1342 after 60 mins by TR-FRET assay


Bioorg Med Chem Lett 23: 2743-9 (2013)


Article DOI: 10.1016/j.bmcl.2013.02.065
BindingDB Entry DOI: 10.7270/Q28G8N4M
More data for this
Ligand-Target Pair
Serine/threonine-protein kinase PLK2


(Homo sapiens (Human))
BDBM50436727
PNG
(CHEMBL2402078)
Show SMILES CC[C@H]1N(c2cn[nH]c2)c2nc(ncc2N(C)C1=O)-n1ccnc1-c1ccc(F)cc1 |r|
Show InChI InChI=1S/C21H19FN8O/c1-3-16-20(31)28(2)17-12-24-21(27-19(17)30(16)15-10-25-26-11-15)29-9-8-23-18(29)13-4-6-14(22)7-5-13/h4-12,16H,3H2,1-2H3,(H,25,26)/t16-/m1/s1
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Elan Pharmaceuticals

Curated by ChEMBL


Assay Description
Inhibition of GST-tagged Plk2 (unknown origin) assessed as inhibition of DEKTDDED phosphorylation at Thr1342 after 60 mins by TR-FRET assay


Bioorg Med Chem Lett 23: 2743-9 (2013)


Article DOI: 10.1016/j.bmcl.2013.02.065
BindingDB Entry DOI: 10.7270/Q28G8N4M
More data for this
Ligand-Target Pair
Serine/threonine-protein kinase PLK2


(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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Nerviano Medical Sciences Srl

Curated by ChEMBL


Assay Description
Inhibition of Plk2 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 PLK2


(Homo sapiens (Human))
BDBM50436747
PNG
(CHEMBL2401968)
Show SMILES CCC1N(C2CCC(F)(F)C2)c2nc(ncc2N(C)C1=O)-n1ccnc1-c1ccc(F)cc1
Show InChI InChI=1S/C23H23F3N6O/c1-3-17-21(33)30(2)18-13-28-22(29-20(18)32(17)16-8-9-23(25,26)12-16)31-11-10-27-19(31)14-4-6-15(24)7-5-14/h4-7,10-11,13,16-17H,3,8-9,12H2,1-2H3
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n/an/a 13n/an/an/an/an/an/a



Elan Pharmaceuticals

Curated by ChEMBL


Assay Description
Inhibition of GST-tagged Plk2 (unknown origin) assessed as inhibition of DEKTDDED phosphorylation at Thr1342 after 60 mins by TR-FRET assay


Bioorg Med Chem Lett 23: 2743-9 (2013)


Article DOI: 10.1016/j.bmcl.2013.02.065
BindingDB Entry DOI: 10.7270/Q28G8N4M
More data for this
Ligand-Target Pair
Serine/threonine-protein kinase PLK2


(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 |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
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n/an/a 14n/an/an/an/an/an/a



Hefei University of Technology

Curated by ChEMBL


Assay Description
Inhibition of recombinant full length human GST-tagged PLK2 expressed in baculovirus expression system using ser/thr 16 as substrate incubated for 1 ...


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
3D
3D Structure (crystal)
Serine/threonine-protein kinase PLK2


(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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Nerviano Medical Sciences Srl

Curated by ChEMBL


Assay Description
Inhibition of Plk2 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 PLK2


(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 |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
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n/an/a 14n/an/an/an/an/an/a



Hefei University of Technology

Curated by ChEMBL


Assay Description
Inhibition human recombinant full length GST-tagged Plk2 expressed in baculovirus expression system after 1 hr by FRET-based Z'-Lyte assay


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
3D
3D Structure (crystal)
Serine/threonine-protein kinase PLK2


(Homo sapiens (Human))
BDBM50436738
PNG
(CHEMBL2401975)
Show SMILES CCC1N(c2ccc(F)cc2)c2nc(ncc2N(C)C1=O)-n1ccnc1-c1ccc(F)cc1
Show InChI InChI=1S/C24H20F2N6O/c1-3-19-23(33)30(2)20-14-28-24(29-22(20)32(19)18-10-8-17(26)9-11-18)31-13-12-27-21(31)15-4-6-16(25)7-5-15/h4-14,19H,3H2,1-2H3
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n/an/a 15n/an/an/an/an/an/a



Elan Pharmaceuticals

Curated by ChEMBL


Assay Description
Inhibition of GST-tagged Plk2 (unknown origin) assessed as inhibition of DEKTDDED phosphorylation at Thr1342 after 60 mins by TR-FRET assay


Bioorg Med Chem Lett 23: 2743-9 (2013)


Article DOI: 10.1016/j.bmcl.2013.02.065
BindingDB Entry DOI: 10.7270/Q28G8N4M
More data for this
Ligand-Target Pair
Serine/threonine-protein kinase PLK2


(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 |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
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n/an/a 16.8n/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)


Article DOI: 10.1111/j.1747-0285.2007.00594.x
BindingDB Entry DOI: 10.7270/Q2T151Z8
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Serine/threonine-protein kinase PLK2


(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 |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
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n/an/a 17n/an/an/an/an/an/a


TBA



Citation and Details

Article DOI: 10.1021/acs.jmedchem.2c00614
BindingDB Entry DOI: 10.7270/Q2Z89HD2
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Serine/threonine-protein kinase PLK2


(Homo sapiens (Human))
BDBM50436737
PNG
(CHEMBL2401974)
Show SMILES CCC1N(c2ccccc2)c2nc(ncc2N(C)C1=O)-n1ccnc1-c1ccccc1
Show InChI InChI=1S/C24H22N6O/c1-3-19-23(31)28(2)20-16-26-24(27-22(20)30(19)18-12-8-5-9-13-18)29-15-14-25-21(29)17-10-6-4-7-11-17/h4-16,19H,3H2,1-2H3
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Elan Pharmaceuticals

Curated by ChEMBL


Assay Description
Inhibition of GST-tagged Plk2 (unknown origin) assessed as inhibition of DEKTDDED phosphorylation at Thr1342 after 60 mins by TR-FRET assay


Bioorg Med Chem Lett 23: 2743-9 (2013)


Article DOI: 10.1016/j.bmcl.2013.02.065
BindingDB Entry DOI: 10.7270/Q28G8N4M
More data for this
Ligand-Target Pair
Serine/threonine-protein kinase PLK2


(Homo sapiens (Human))
BDBM50285539
PNG
(CHEMBL4174667)
Show SMILES CC[C@H]1N(C2CCCC2)c2nc(ncc2N(C)C1=O)-n1ccc2cc(ccc12)C(=O)NC(C)C |r|
Show InChI InChI=1S/C26H32N6O2/c1-5-20-25(34)30(4)22-15-27-26(29-23(22)32(20)19-8-6-7-9-19)31-13-12-17-14-18(10-11-21(17)31)24(33)28-16(2)3/h10-16,19-20H,5-9H2,1-4H3,(H,28,33)/t20-/m1/s1
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Hefei University of Technology

Curated by ChEMBL


Assay Description
Inhibition human recombinant full length GST-tagged Plk2 expressed in baculovirus expression system after 1 hr by FRET-based Z'-Lyte assay


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 PLK2


(Homo sapiens (Human))
BDBM50285528
PNG
(CHEMBL4160611)
Show SMILES CCCCNC(=O)c1ccc2n(ccc2c1)-c1ncc2N(C)C(=O)[C@@H](CC)N(C3CCCC3)c2n1 |r|
Show InChI InChI=1S/C27H34N6O2/c1-4-6-14-28-25(34)19-11-12-22-18(16-19)13-15-32(22)27-29-17-23-24(30-27)33(20-9-7-8-10-20)21(5-2)26(35)31(23)3/h11-13,15-17,20-21H,4-10,14H2,1-3H3,(H,28,34)/t21-/m1/s1
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Hefei University of Technology

Curated by ChEMBL


Assay Description
Inhibition human recombinant full length GST-tagged Plk2 expressed in baculovirus expression system after 1 hr by FRET-based Z'-Lyte assay


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 PLK2


(Homo sapiens (Human))
BDBM50285529
PNG
(CHEMBL4177399)
Show SMILES CCCNS(=O)(=O)c1ccc(Nc2ncc3N(C)C(=O)[C@@H](CC)N(C4CCCC4)c3n2)cc1 |r|
Show InChI InChI=1S/C23H32N6O3S/c1-4-14-25-33(31,32)18-12-10-16(11-13-18)26-23-24-15-20-21(27-23)29(17-8-6-7-9-17)19(5-2)22(30)28(20)3/h10-13,15,17,19,25H,4-9,14H2,1-3H3,(H,24,26,27)/t19-/m1/s1
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n/an/a 18n/an/an/an/an/an/a



Hefei University of Technology

Curated by ChEMBL


Assay Description
Inhibition human recombinant full length GST-tagged Plk2 expressed in baculovirus expression system after 1 hr by FRET-based Z'-Lyte assay


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 PLK2


(Homo sapiens (Human))
BDBM50285588
PNG
(CHEMBL4171224)
Show SMILES CC[C@H]1N(C2CCCC2)c2nc(ncc2N(C)C1=O)-n1ccc2cc(ccc12)C(=O)NCC(C)C |r|
Show InChI InChI=1S/C27H34N6O2/c1-5-21-26(35)31(4)23-16-29-27(30-24(23)33(21)20-8-6-7-9-20)32-13-12-18-14-19(10-11-22(18)32)25(34)28-15-17(2)3/h10-14,16-17,20-21H,5-9,15H2,1-4H3,(H,28,34)/t21-/m1/s1
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n/an/a 19n/an/an/an/an/an/a



Hefei University of Technology

Curated by ChEMBL


Assay Description
Inhibition human recombinant full length GST-tagged Plk2 expressed in baculovirus expression system after 1 hr by FRET-based Z'-Lyte assay


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 PLK2


(Homo sapiens (Human))
BDBM50285582
PNG
(CHEMBL4170176)
Show SMILES CCCCNS(=O)(=O)c1ccc(Nc2ncc3N(C)C(=O)[C@@H](CC)N(C4CCCC4)c3n2)cc1 |r|
Show InChI InChI=1S/C24H34N6O3S/c1-4-6-15-26-34(32,33)19-13-11-17(12-14-19)27-24-25-16-21-22(28-24)30(18-9-7-8-10-18)20(5-2)23(31)29(21)3/h11-14,16,18,20,26H,4-10,15H2,1-3H3,(H,25,27,28)/t20-/m1/s1
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n/an/a 20n/an/an/an/an/an/a



Hefei University of Technology

Curated by ChEMBL


Assay Description
Inhibition human recombinant full length GST-tagged Plk2 expressed in baculovirus expression system after 1 hr by FRET-based Z'-Lyte assay


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 PLK2


(Homo sapiens (Human))
BDBM50297985
PNG
((R)-3-(1-(4-((tert-butylamino)methyl)-2-(difluorom...)
Show SMILES C[C@@H](Oc1cc(sc1C(N)=O)-c1cnc2ccccn12)c1ccc(CNC(C)(C)C)cc1OC(F)F |r|
Show InChI InChI=1S/C26H28F2N4O3S/c1-15(17-9-8-16(13-31-26(2,3)4)11-19(17)35-25(27)28)34-20-12-21(36-23(20)24(29)33)18-14-30-22-7-5-6-10-32(18)22/h5-12,14-15,25,31H,13H2,1-4H3,(H2,29,33)/t15-/m1/s1
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n/an/a 21n/an/an/an/an/an/a



Banyu Tsukuba Research Institute

Curated by ChEMBL


Assay Description
Inhibition of PLK2


Bioorg Med Chem Lett 19: 4673-8 (2009)


Article DOI: 10.1016/j.bmcl.2009.06.084
BindingDB Entry DOI: 10.7270/Q22R3RQG
More data for this
Ligand-Target Pair
Serine/threonine-protein kinase PLK2


(Homo sapiens (Human))
BDBM50436745
PNG
(CHEMBL2401972)
Show SMILES CC[C@H]1N([C@@H]2CCOC2)c2nc(ncc2N(C)C1=O)-n1ccnc1-c1ccccc1 |r|
Show InChI InChI=1S/C22H24N6O2/c1-3-17-21(29)26(2)18-13-24-22(25-20(18)28(17)16-9-12-30-14-16)27-11-10-23-19(27)15-7-5-4-6-8-15/h4-8,10-11,13,16-17H,3,9,12,14H2,1-2H3/t16-,17-/m1/s1
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n/an/a 21n/an/an/an/an/an/a



Elan Pharmaceuticals

Curated by ChEMBL


Assay Description
Inhibition of GST-tagged Plk2 (unknown origin) assessed as inhibition of DEKTDDED phosphorylation at Thr1342 after 60 mins by TR-FRET assay


Bioorg Med Chem Lett 23: 2743-9 (2013)


Article DOI: 10.1016/j.bmcl.2013.02.065
BindingDB Entry DOI: 10.7270/Q28G8N4M
More data for this
Ligand-Target Pair
Serine/threonine-protein kinase PLK2


(Homo sapiens (Human))
BDBM50436735
PNG
(CHEMBL2402080)
Show SMILES CC[C@H]1N(c2cnn(C)c2)c2nc(ncc2N(C)C1=O)-n1ccnc1-c1ccc(F)cc1 |r|
Show InChI InChI=1S/C22H21FN8O/c1-4-17-21(32)29(3)18-12-25-22(27-20(18)31(17)16-11-26-28(2)13-16)30-10-9-24-19(30)14-5-7-15(23)8-6-14/h5-13,17H,4H2,1-3H3/t17-/m1/s1
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n/an/a 21n/an/an/an/an/an/a



Elan Pharmaceuticals

Curated by ChEMBL


Assay Description
Inhibition of GST-tagged Plk2 (unknown origin) assessed as inhibition of DEKTDDED phosphorylation at Thr1342 after 60 mins by TR-FRET assay


Bioorg Med Chem Lett 23: 2743-9 (2013)


Article DOI: 10.1016/j.bmcl.2013.02.065
BindingDB Entry DOI: 10.7270/Q28G8N4M
More data for this
Ligand-Target Pair
Serine/threonine-protein kinase PLK2


(Homo sapiens (Human))
BDBM50285545
PNG
(CHEMBL4162262)
Show SMILES CC[C@H]1N(C2CCCC2)c2nc(Nc3ccc(cc3)S(=O)(=O)NCC(C)C)ncc2N(C)C1=O |r|
Show InChI InChI=1S/C24H34N6O3S/c1-5-20-23(31)29(4)21-15-25-24(28-22(21)30(20)18-8-6-7-9-18)27-17-10-12-19(13-11-17)34(32,33)26-14-16(2)3/h10-13,15-16,18,20,26H,5-9,14H2,1-4H3,(H,25,27,28)/t20-/m1/s1
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n/an/a 22n/an/an/an/an/an/a



Hefei University of Technology

Curated by ChEMBL


Assay Description
Inhibition human recombinant full length GST-tagged Plk2 expressed in baculovirus expression system after 1 hr by FRET-based Z'-Lyte assay


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 PLK2


(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 24n/an/an/an/an/an/a



Nerviano Medical Sciences Srl

Curated by ChEMBL


Assay Description
Inhibition of Plk2 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 PLK2


(Homo sapiens (Human))
BDBM50285581
PNG
(CHEMBL4173620)
Show SMILES CC[C@H]1N(C2CCCC2)c2nc(Nc3ccc(cc3)S(=O)(=O)NC3CCCC3)ncc2N(C)C1=O |r|
Show InChI InChI=1S/C25H34N6O3S/c1-3-21-24(32)30(2)22-16-26-25(28-23(22)31(21)19-10-6-7-11-19)27-17-12-14-20(15-13-17)35(33,34)29-18-8-4-5-9-18/h12-16,18-19,21,29H,3-11H2,1-2H3,(H,26,27,28)/t21-/m1/s1
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n/an/a 24n/an/an/an/an/an/a



Hefei University of Technology

Curated by ChEMBL


Assay Description
Inhibition human recombinant full length GST-tagged Plk2 expressed in baculovirus expression system after 1 hr by FRET-based Z'-Lyte assay


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 PLK2


(Homo sapiens (Human))
BDBM50436744
PNG
(CHEMBL2401965)
Show SMILES CC[C@H]1N(C(C)C)c2nc(ncc2N(C)C1=O)-n1ccnc1-c1ccccc1 |r|
Show InChI InChI=1S/C21H24N6O/c1-5-16-20(28)25(4)17-13-23-21(24-19(17)27(16)14(2)3)26-12-11-22-18(26)15-9-7-6-8-10-15/h6-14,16H,5H2,1-4H3/t16-/m1/s1
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n/an/a 25n/an/an/an/an/an/a



Elan Pharmaceuticals

Curated by ChEMBL


Assay Description
Inhibition of GST-tagged Plk2 (unknown origin) assessed as inhibition of DEKTDDED phosphorylation at Thr1342 after 60 mins by TR-FRET assay


Bioorg Med Chem Lett 23: 2743-9 (2013)


Article DOI: 10.1016/j.bmcl.2013.02.065
BindingDB Entry DOI: 10.7270/Q28G8N4M
More data for this
Ligand-Target Pair
Serine/threonine-protein kinase PLK2


(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 27n/an/an/an/an/an/a



Nerviano Medical Sciences Srl

Curated by ChEMBL


Assay Description
Inhibition of Plk2 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 PLK2


(Homo sapiens (Human))
BDBM50285525
PNG
(CHEMBL4161572)
Show SMILES CC[C@H]1N(C2CCCC2)c2nc(ncc2N(C)C1=O)-n1ccc2cc(ccc12)C(N)=O |r|
Show InChI InChI=1S/C23H26N6O2/c1-3-17-22(31)27(2)19-13-25-23(26-21(19)29(17)16-6-4-5-7-16)28-11-10-14-12-15(20(24)30)8-9-18(14)28/h8-13,16-17H,3-7H2,1-2H3,(H2,24,30)/t17-/m1/s1
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n/an/a 29n/an/an/an/an/an/a



Hefei University of Technology

Curated by ChEMBL


Assay Description
Inhibition human recombinant full length GST-tagged Plk2 expressed in baculovirus expression system after 1 hr by FRET-based Z'-Lyte assay


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 PLK2


(Homo sapiens (Human))
BDBM50436730
PNG
(CHEMBL2401959)
Show SMILES CCC1(C)N(CCC(F)(F)F)c2nc(ncc2N(C)C1=O)-n1ccnc1-c1ccc(F)cc1
Show InChI InChI=1S/C22H22F4N6O/c1-4-21(2)19(33)30(3)16-13-28-20(29-18(16)32(21)11-9-22(24,25)26)31-12-10-27-17(31)14-5-7-15(23)8-6-14/h5-8,10,12-13H,4,9,11H2,1-3H3
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n/an/a 30n/an/an/an/an/an/a



Elan Pharmaceuticals

Curated by ChEMBL


Assay Description
Inhibition of GST-tagged Plk2 (unknown origin) assessed as inhibition of DEKTDDED phosphorylation at Thr1342 after 60 mins by TR-FRET assay


Bioorg Med Chem Lett 23: 2743-9 (2013)


Article DOI: 10.1016/j.bmcl.2013.02.065
BindingDB Entry DOI: 10.7270/Q28G8N4M
More data for this
Ligand-Target Pair
Serine/threonine-protein kinase PLK2


(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 |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
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US Patent
n/an/a 30n/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)


BindingDB Entry DOI: 10.7270/Q2SJ1J7D
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Serine/threonine-protein kinase PLK2


(Homo sapiens (Human))
BDBM50436731
PNG
(CHEMBL2402076)
Show SMILES CCC1N(c2ccc(cc2)C#N)c2nc(ncc2N(C)C1=O)-n1ccnc1-c1ccc(F)cc1
Show InChI InChI=1S/C25H20FN7O/c1-3-20-24(34)31(2)21-15-29-25(30-23(21)33(20)19-10-4-16(14-27)5-11-19)32-13-12-28-22(32)17-6-8-18(26)9-7-17/h4-13,15,20H,3H2,1-2H3
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n/an/a 31n/an/an/an/an/an/a



Elan Pharmaceuticals

Curated by ChEMBL


Assay Description
Inhibition of GST-tagged Plk2 (unknown origin) assessed as inhibition of DEKTDDED phosphorylation at Thr1342 after 60 mins by TR-FRET assay


Bioorg Med Chem Lett 23: 2743-9 (2013)


Article DOI: 10.1016/j.bmcl.2013.02.065
BindingDB Entry DOI: 10.7270/Q28G8N4M
More data for this
Ligand-Target Pair
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