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TargetSerine/threonine-protein kinase PLK1(Homo sapiens (Human))
University Of Maryland

Curated by ChEMBL
LigandPNGBDBM25121(4-{[(7R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,...)
Affinity DataKi:  0.220nMAssay Description:Binding affinity to PLK1 (unknown origin) expressed in HEK293 cells after 1 hr by proprietary competition assayMore data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase PLK1(Homo sapiens (Human))
University Of Maryland

Curated by ChEMBL
LigandPNGBDBM25121(4-{[(7R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,...)
Affinity DataKi: <1nM ΔG°: <-50.9kJ/molepH: 7.5 T: 2°CAssay Description:Kinase was assayed in 384-well polypropylene plate format. The compound was mixed with kinase and biotinylated peptide substrate and incubated. After...More data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase PLK1(Homo sapiens (Human))
University Of Maryland

Curated by ChEMBL
LigandPNGBDBM50355500(CHEMBL1908394 | US9695172, GSK461364)
Affinity DataKi:  2.20nMAssay Description:Inhibition of PLK1 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase PLK1(Homo sapiens (Human))
University Of Maryland

Curated by ChEMBL
LigandPNGBDBM50355500(CHEMBL1908394 | US9695172, GSK461364)
Affinity DataKi:  2.20nMAssay Description:Binding affinity to PLK1 (unknown origin) assessed as inhibition constantMore data for this Ligand-Target Pair
In DepthDetails PubMed
TargetSerine/threonine-protein kinase PLK1(Homo sapiens (Human))
University Of Maryland

Curated by ChEMBL
LigandPNGBDBM50355500(CHEMBL1908394 | US9695172, GSK461364)
Affinity DataKi:  2.20nMAssay Description:Inhibition of human recombinant His6-tagged PLK1 (1 to 603 residues) using casein as substrate preincubated for 60 mins followed by polo box peptide ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase PLK1(Homo sapiens (Human))
University Of Maryland

Curated by ChEMBL
LigandPNGBDBM25121(4-{[(7R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,...)
Affinity DataKi:  3nMAssay Description:Inhibition of recombinant GST-tagged PLK1 using biotin-ahx-AKMETTFYDDALNASFLPSEKKK-amide as substrate after 30 mins by scintillation counting analysi...More data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase PLK1(Homo sapiens (Human))
University Of Maryland

Curated by ChEMBL
LigandPNGBDBM2579((2S,3R,4R,6R)-3-methoxy-2-methyl-4-(methylamino)-2...)
Affinity DataKi:  790nM ΔG°:  -34.5kJ/molepH: 7.5 T: 2°CAssay Description:Kinase was assayed in 384-well polypropylene plate format. The compound was mixed with kinase and biotinylated peptide substrate and incubated. After...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase PLK1(Homo sapiens (Human))
University Of Maryland

Curated by ChEMBL
LigandPNGBDBM13534(CHEMBL572878 | N-[4-({4-[(3-methyl-1H-pyrazol-5-yl...)
Affinity DataKi: >2.00E+4nM ΔG°: >-26.6kJ/molepH: 7.5 T: 2°CAssay Description:Kinase was assayed in 384-well polypropylene plate format. The compound was mixed with kinase and biotinylated peptide substrate and incubated. After...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase PLK1(Homo sapiens (Human))
University Of Maryland

Curated by ChEMBL
LigandPNGBDBM13530(4-[(4-methylpiperazin-1-yl)methyl]-N-[4-methyl-3-[...)
Affinity DataKi: >2.00E+4nM ΔG°: >-26.6kJ/molepH: 7.5 T: 2°CAssay Description:Kinase was assayed in 384-well polypropylene plate format. The compound was mixed with kinase and biotinylated peptide substrate and incubated. After...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase PLK1(Homo sapiens (Human))
University Of Maryland

Curated by ChEMBL
LigandPNGBDBM15138(5-indazolyl pyridine 11g | 5-{5-[(2S)-2-amino-3-ph...)
Affinity DataKi: >2.00E+4nM ΔG°: >-26.6kJ/molepH: 7.5 T: 2°CAssay Description:Kinase was assayed in 384-well polypropylene plate format. The compound was mixed with kinase and biotinylated peptide substrate and incubated. After...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase PLK1(Homo sapiens (Human))
University Of Maryland

Curated by ChEMBL
LigandPNGBDBM25118((3Z)-4-amino-5-fluoro-3-[5-(4-methylpiperazino)-1,...)
Affinity DataKi: >2.00E+4nM ΔG°: >-26.6kJ/molepH: 7.5 T: 2°CAssay Description:Kinase was assayed in 384-well polypropylene plate format. The compound was mixed with kinase and biotinylated peptide substrate and incubated. After...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase PLK1(Homo sapiens (Human))
University Of Maryland

Curated by ChEMBL
LigandPNGBDBM4814(CHEMBL535 | N-[2-(diethylamino)ethyl]-5-[(Z)-(5-fl...)
Affinity DataKi: >2.00E+4nM ΔG°: >-26.6kJ/molepH: 7.5 T: 2°CAssay Description:Kinase was assayed in 384-well polypropylene plate format. The compound was mixed with kinase and biotinylated peptide substrate and incubated. After...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase PLK1(Homo sapiens (Human))
University Of Maryland

Curated by ChEMBL
LigandPNGBDBM25117(AG-013736 | AXITINIB | N-methyl-2-({3-[(E)-2-(pyri...)
Affinity DataKi: >2.00E+4nM ΔG°: >-26.6kJ/molepH: 7.5 T: 2°CAssay Description:Kinase was assayed in 384-well polypropylene plate format. The compound was mixed with kinase and biotinylated peptide substrate and incubated. After...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase PLK1(Homo sapiens (Human))
University Of Maryland

Curated by ChEMBL
LigandPNGBDBM16673(4-[4-({[4-chloro-3-(trifluoromethyl)phenyl]carbamo...)
Affinity DataKi: >2.00E+4nM ΔG°: >-26.6kJ/molepH: 7.5 T: 2°CAssay Description:Kinase was assayed in 384-well polypropylene plate format. The compound was mixed with kinase and biotinylated peptide substrate and incubated. After...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase PLK1(Homo sapiens (Human))
University Of Maryland

Curated by ChEMBL
LigandPNGBDBM25121(4-{[(7R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,...)
Affinity DataIC50:  0.0830nMAssay Description:Inhibition of PLK1 (unknown origin)More data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase PLK1(Homo sapiens (Human))
University Of Maryland

Curated by ChEMBL
LigandPNGBDBM25121(4-{[(7R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,...)
Affinity DataIC50:  0.800nMAssay Description:Inhibition of PLK1 (unknown origin)More data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase PLK1(Homo sapiens (Human))
University Of Maryland

Curated by ChEMBL
LigandPNGBDBM25121(4-{[(7R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,...)
Affinity DataIC50:  0.830nMAssay Description:Inhibition of PLK1 (unknown origin)More data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase PLK1(Homo sapiens (Human))
University Of Maryland

Curated by ChEMBL
LigandPNGBDBM25121(4-{[(7R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,...)
Affinity DataIC50:  0.830nMAssay Description:Inhibition of human recombinant GST-tagged PLK1 (1 to 603 residues) using casein as substrate incubated for 45 minsMore data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase PLK1(Homo sapiens (Human))
University Of Maryland

Curated by ChEMBL
LigandPNGBDBM25121(4-{[(7R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,...)
Affinity DataIC50:  0.830nMAssay Description:Inhibition of Plk1 in human A549 cells incubated for 2 hrs by microplate reader methodMore data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase PLK1(Homo sapiens (Human))
University Of Maryland

Curated by ChEMBL
LigandPNGBDBM25121(4-{[(7R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,...)
Affinity DataIC50:  0.830nMAssay Description:Inhibition of recombinant human N-terminal GST-tagged PLK1 (1 to 603 residues) expressed in baculovirus expression system using casein as substrate i...More data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase PLK1(Homo sapiens (Human))
University Of Maryland

Curated by ChEMBL
LigandPNGBDBM25121(4-{[(7R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,...)
Affinity DataIC50:  0.830nMAssay Description:Inhibition of N-terminal GST-tagged recombinant human PLK1 (1 to 603 residues) expressed in baculovirus expression system using bovine milk casein as...More data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase PLK1(Homo sapiens (Human))
University Of Maryland

Curated by ChEMBL
LigandPNGBDBM25121(4-{[(7R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,...)
Affinity DataIC50:  0.830nMAssay Description:Inhibition of recombinant human N-terminal GST-tagged PLK1 (1 to 603 residues) expressed in baculovirus expression system using casein as substrate a...More data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase PLK1(Homo sapiens (Human))
University Of Maryland

Curated by ChEMBL
LigandPNGBDBM25121(4-{[(7R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,...)
Affinity DataIC50:  0.830nMAssay Description:Inhibition of recombinant N-terminal GST-tagged human PLK1 (1 to 603 residues) expressed in baculovirus expression system incubated for 45 mins using...More data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase PLK1(Homo sapiens (Human))
University Of Maryland

Curated by ChEMBL
LigandPNGBDBM25121(4-{[(7R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,...)
Affinity DataIC50:  0.830nMAssay Description:Competitive inhibition of human PLK1 in presence of ATPMore data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase PLK1(Homo sapiens (Human))
University Of Maryland

Curated by ChEMBL
LigandPNGBDBM25121(4-{[(7R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,...)
Affinity DataIC50:  0.830nMAssay Description:Inhibition of human recombinant N-terminal GST-tagged PLK1 (1 to 603 residues) expressed in baculovirus expression system using casein as substrate a...More data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase PLK1(Homo sapiens (Human))
University Of Maryland

Curated by ChEMBL
LigandPNGBDBM25121(4-{[(7R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,...)
Affinity DataIC50: <2.60nMAssay Description:Inhibition of PLK1 (unknown origin) using Ser/Thr 16 as substrate after 60 mins by Z-LYTE activity assayMore data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase PLK1(Homo sapiens (Human))
University Of Maryland

Curated by ChEMBL
LigandPNGBDBM25121(4-{[(7R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,...)
Affinity DataIC50:  4nMAssay Description:Inhibition of human recombinant PLK1 by Z-Lyte assayMore data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase PLK1(Homo sapiens (Human))
University Of Maryland

Curated by ChEMBL
LigandPNGBDBM25121(4-{[(7R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,...)
Affinity DataIC50:  5.30nMAssay Description:Inhibition human recombinant full length His-tagged Plk1 expressed in baculovirus expression system after 1 hr by FRET-based Z'-Lyte assayMore data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase PLK1(Homo sapiens (Human))
University Of Maryland

Curated by ChEMBL
LigandPNGBDBM25121(4-{[(7R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,...)
Affinity DataIC50:  7.10nMAssay Description:Inhibition of recombinant full length human His-tagged PLK1 expressed in baculovirus expression system using ser/thr 16 as substrate incubated for 1 ...More data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase PLK1(Homo sapiens (Human))
University Of Maryland

Curated by ChEMBL
LigandPNGBDBM25121(4-{[(7R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,...)
Affinity DataIC50:  8nMpH: 7.9Assay Description:The inhibitory activity of putative kinase inhibitors and the potency of selected compounds were determined using a trans-phosphorylation assay.More data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase PLK1(Homo sapiens (Human))
University Of Maryland

Curated by ChEMBL
LigandPNGBDBM25121(4-{[(7R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,...)
Affinity DataIC50:  8nMpH: 7.5 T: 2°CAssay Description:Percent inhibition and IC50 values were determined with ATP concentrations at apparent Km using the Invitrogen SelectScreen Kinase Profiling Service ...More data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase PLK1(Homo sapiens (Human))
University Of Maryland

Curated by ChEMBL
LigandPNGBDBM25121(4-{[(7R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,...)
Affinity DataIC50:  8nMAssay Description:Inhibition of recombinant full length human PLK1 using casein as substrate incubated for 40 mins in the presence of [gamma33P]ATP at Km concentration...More data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase PLK1(Homo sapiens (Human))
University Of Maryland

Curated by ChEMBL
LigandPNGBDBM2579((2S,3R,4R,6R)-3-methoxy-2-methyl-4-(methylamino)-2...)
Affinity DataIC50:  76.9nMAssay Description:Inhibition of human PLK1 using casein as substrate by [gamma-33P]-ATP assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase PLK1(Homo sapiens (Human))
University Of Maryland

Curated by ChEMBL
LigandPNGBDBM25121(4-{[(7R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,...)
Affinity DataIC50: <100nMAssay Description:Inhibition of PLK1 in human MDA-MB-23 cells assessed as decrease in TCTP phosphorylation after 6 hrs by Western blot methodMore data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase PLK1(Homo sapiens (Human))
University Of Maryland

Curated by ChEMBL
LigandPNGBDBM50355500(CHEMBL1908394 | US9695172, GSK461364)
Affinity DataIC50: <100nMAssay Description:Inhibition of PLK1 in HEK293T cells assessed as decrease in TCTP phosphorylation after 6 hrs by Western blot methodMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase PLK1(Homo sapiens (Human))
University Of Maryland

Curated by ChEMBL
LigandPNGBDBM50355500(CHEMBL1908394 | US9695172, GSK461364)
Affinity DataIC50: <100nMAssay Description:Inhibition of PLK1 in human MDA-MB-23 cells assessed as decrease in TCTP phosphorylation after 6 hrs by Western blot methodMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase PLK1(Homo sapiens (Human))
University Of Maryland

Curated by ChEMBL
LigandPNGBDBM25121(4-{[(7R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,...)
Affinity DataIC50: <100nMAssay Description:Inhibition of PLK1 in HEK293T cells assessed as decrease in TCTP phosphorylation after 6 hrs by Western blot methodMore data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase PLK1(Homo sapiens (Human))
University Of Maryland

Curated by ChEMBL
LigandPNGBDBM25121(4-{[(7R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,...)
Affinity DataIC50:  106nMAssay Description:Inhibition of full length human PLK1 using casein as substrate incubated for 40 mins in presence of [gamma-33P]-ATP by radiometric assayMore data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase PLK1(Homo sapiens (Human))
University Of Maryland

Curated by ChEMBL
LigandPNGBDBM2579((2S,3R,4R,6R)-3-methoxy-2-methyl-4-(methylamino)-2...)
Affinity DataIC50:  192nMAssay Description:Inhibition of PLK1 (unknown origin) after 40 mins by scintillation counting analysisMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase PLK1(Homo sapiens (Human))
University Of Maryland

Curated by ChEMBL
LigandPNGBDBM2579((2S,3R,4R,6R)-3-methoxy-2-methyl-4-(methylamino)-2...)
Affinity DataIC50:  222nMAssay Description:Inhibition of human PLK1 using casein as substrate by [gamma-33P]-ATP assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase PLK1(Homo sapiens (Human))
University Of Maryland

Curated by ChEMBL
LigandPNGBDBM2579((2S,3R,4R,6R)-3-methoxy-2-methyl-4-(methylamino)-2...)
Affinity DataIC50:  318nMAssay Description:Inhibition of PLK1More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase PLK1(Homo sapiens (Human))
University Of Maryland

Curated by ChEMBL
LigandPNGBDBM2579((2S,3R,4R,6R)-3-methoxy-2-methyl-4-(methylamino)-2...)
Affinity DataIC50:  540nMAssay Description:Inhibition of PLK1 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase PLK1(Homo sapiens (Human))
University Of Maryland

Curated by ChEMBL
LigandPNGBDBM25121(4-{[(7R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,...)
Affinity DataIC50:  830nMAssay Description:Inhibition of recombinant human N-terminal GST-tagged PLK1 (1 to 603 residues) expressed in baculovirus expression system using casein as substrate m...More data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase PLK1(Homo sapiens (Human))
University Of Maryland

Curated by ChEMBL
LigandPNGBDBM2579((2S,3R,4R,6R)-3-methoxy-2-methyl-4-(methylamino)-2...)
Affinity DataIC50:  865nMAssay Description:Inhibition of recombinant full length human His-tagged PLK1 expressed in baculovirus expression system using ser/thr 16 as substrate incubated for 1 ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase PLK1(Homo sapiens (Human))
University Of Maryland

Curated by ChEMBL
LigandPNGBDBM2579((2S,3R,4R,6R)-3-methoxy-2-methyl-4-(methylamino)-2...)
Affinity DataIC50:  865nMAssay Description:Inhibition human recombinant full length His-tagged Plk1 expressed in baculovirus expression system after 1 hr by FRET-based Z'-Lyte assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase PLK1(Homo sapiens (Human))
University Of Maryland

Curated by ChEMBL
LigandPNGBDBM2579((2S,3R,4R,6R)-3-methoxy-2-methyl-4-(methylamino)-2...)
Affinity DataIC50:  1.97E+3nMAssay Description:Inhibition of PLK1More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase PLK1(Homo sapiens (Human))
University Of Maryland

Curated by ChEMBL
LigandPNGBDBM25117(AG-013736 | AXITINIB | N-methyl-2-({3-[(E)-2-(pyri...)
Affinity DataIC50: >1.00E+4nMAssay Description:Inhibition of PLK1 (unknown origin) by FRET-based homogeneous assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase PLK1(Homo sapiens (Human))
University Of Maryland

Curated by ChEMBL
LigandPNGBDBM13534(CHEMBL572878 | N-[4-({4-[(3-methyl-1H-pyrazol-5-yl...)
Affinity DataIC50: >1.00E+4nMAssay Description:In vitro kinase assay using human aurora kinase in a standard radiometric assay.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase PLK1(Homo sapiens (Human))
University Of Maryland

Curated by ChEMBL
LigandPNGBDBM50135286(CHEMBL3745885)
Affinity DataIC50: >1.00E+4nMAssay Description:Inhibition of human recombinant PLK1 using recombinant dephosphorylated bovine alpha- casein/synuclein as substrate after 30 mins by scintillation co...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase PLK1(Homo sapiens (Human))
University Of Maryland

Curated by ChEMBL
LigandPNGBDBM50135286(CHEMBL3745885)
Affinity DataIC50: >1.00E+4nMAssay Description:Inhibition of human PLK1 using casein as substrateMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
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