Compile Data Set for Download or QSAR
Report error Found 31 Enz. Inhib. hit(s) for PDB: 5GWK
TargetDNA topoisomerase 2-alpha/2-beta(Human)
Sterling Winthrop Pharmaceuticals Research Division

Curated by ChEMBL
LigandPNGBDBM50127140(4'-Demethylepipodophyllotoxin 9-(4,6-O-(R)-ethylid...)
Affinity DataEC50:  810nMAssay Description:Tested for inhibition of topoisomerase II isolated from HeLa cells by DNA-cleavage assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/6/2019
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetDNA topoisomerase 2-alpha/2-beta(Human)
Sterling Winthrop Pharmaceuticals Research Division

Curated by ChEMBL
LigandPNGBDBM50127140(4'-Demethylepipodophyllotoxin 9-(4,6-O-(R)-ethylid...)
Affinity DataEC50:  810nMAssay Description:Tested for inhibitory activity against Topoisomerase II isolated from HeLa cells by using SDS-K+ precipitation methodMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/20/2018
Entry Details
PDB3D3D Structure (crystal)
TargetDNA topoisomerase 2-alpha/2-beta(Human)
Sterling Winthrop Pharmaceuticals Research Division

Curated by ChEMBL
LigandPNGBDBM50127140(4'-Demethylepipodophyllotoxin 9-(4,6-O-(R)-ethylid...)
Affinity DataEC50:  810nMAssay Description:Compound was tested for topoisomerase II inhibition in purified HeLa cells by SDS/K+ precipitation methodMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/26/2012
Entry Details Article
PDB3D3D Structure (crystal)
TargetDNA topoisomerase 2-alpha/2-beta(Human)
Sterling Winthrop Pharmaceuticals Research Division

Curated by ChEMBL
LigandPNGBDBM50127140(4'-Demethylepipodophyllotoxin 9-(4,6-O-(R)-ethylid...)
Affinity DataEC50:  810nMAssay Description:Inhibitory activity against HeLa cell Topoisomerase IIMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/28/2018
Entry Details
PDB3D3D Structure (crystal)
TargetDNA topoisomerase 2-alpha/2-beta(Human)
Sterling Winthrop Pharmaceuticals Research Division

Curated by ChEMBL
LigandPNGBDBM50127140(4'-Demethylepipodophyllotoxin 9-(4,6-O-(R)-ethylid...)
Affinity DataEC50:  810nMAssay Description:Inhibitory activity in a cell-free assay of DNA cleavage mediated by purified HeLa cell topoisomerase II.More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/27/2018
Entry Details
PDB3D3D Structure (crystal)
TargetDNA topoisomerase 2-alpha(Human)
University of Ljubljana

Curated by ChEMBL
LigandPNGBDBM50127140(4'-Demethylepipodophyllotoxin 9-(4,6-O-(R)-ethylid...)
Affinity DataIC50: 4.70E+3nMAssay Description:Inhibition of human DNA topoisomerase 2 alpha assessed as ATP hydrolysis measured for 30 mins by absorbance based assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/17/2024
Entry Details
PubMedPDB3D3D Structure (crystal)
TargetDNA topoisomerase 2-alpha(Human)
University of Ljubljana

Curated by ChEMBL
LigandPNGBDBM50127140(4'-Demethylepipodophyllotoxin 9-(4,6-O-(R)-ethylid...)
Affinity DataIC50: 2.18E+4nMAssay Description:Inhibition of topoisomerase 2More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/7/2013
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetDNA topoisomerase 2-alpha/2-beta(Human)
Sterling Winthrop Pharmaceuticals Research Division

Curated by ChEMBL
LigandPNGBDBM50127140(4'-Demethylepipodophyllotoxin 9-(4,6-O-(R)-ethylid...)
Affinity DataIC50: 2.20E+4nMAssay Description:Inhibitory activity in a DNA cleavage assay using HeLa DNA topoisomerase II yielding its effective concentrationMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/22/2020
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetDNA topoisomerase 2-alpha(Human)
University of Ljubljana

Curated by ChEMBL
LigandPNGBDBM50127140(4'-Demethylepipodophyllotoxin 9-(4,6-O-(R)-ethylid...)
Affinity DataIC50: 2.82E+4nMAssay Description:Inhibition of human DNA topoisomerase-2alpha assessed as relaxation of supercoiled pBR322 DNA after 30 mins by agarose gel electrophoresisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/1/2020
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetDNA topoisomerase 2-alpha(Human)
University of Ljubljana

Curated by ChEMBL
LigandPNGBDBM50127140(4'-Demethylepipodophyllotoxin 9-(4,6-O-(R)-ethylid...)
Affinity DataIC50: 3.00E+4nMpH: 7.8 T: 2°CAssay Description:Supercoiled pHOT1 DNA (0.5 μg) was incubated with four units of human topoisomerase I in relaxation buffer (10mM Tris-HCl (pH 7.8), 1mM EDTA, 0.15...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/31/2017
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetDNA topoisomerase 2-alpha(Human)
University of Ljubljana

Curated by ChEMBL
LigandPNGBDBM50127140(4'-Demethylepipodophyllotoxin 9-(4,6-O-(R)-ethylid...)
Affinity DataIC50: 3.38E+4nMAssay Description:Inhibition of human DNA topoisomerase 2alpha using plasmid pNO1 substrate incubated at 37 degC for 30 mins by fluorimetryMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/15/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetDNA topoisomerase 2-alpha(Human)
University of Ljubljana

Curated by ChEMBL
LigandPNGBDBM50127140(4'-Demethylepipodophyllotoxin 9-(4,6-O-(R)-ethylid...)
Affinity DataIC50: 3.38E+4nMAssay Description:Inhibition of recombinant human topoisomerase 2alpha using supercoiled pNO1 plasmid as substrate after 30 mins by SYBR-GOLD staining based fluorimetr...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/23/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetDNA topoisomerase 2-alpha/2-beta(Human)
Sterling Winthrop Pharmaceuticals Research Division

Curated by ChEMBL
LigandPNGBDBM50127140(4'-Demethylepipodophyllotoxin 9-(4,6-O-(R)-ethylid...)
Affinity DataIC50: 3.80E+4nMAssay Description:In vitro activity against mammalian topoisomerase II measured as ATP-dependent unknotting of P4 DNA compared to enzyme and DNA controlMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/21/2020
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetDNA topoisomerase 2-alpha(Human)
University of Ljubljana

Curated by ChEMBL
LigandPNGBDBM50127140(4'-Demethylepipodophyllotoxin 9-(4,6-O-(R)-ethylid...)
Affinity DataIC50: 4.75E+4nMAssay Description:Inhibition of human topo2alpha incubated for 30 mins by SYBR safe DNA stain based decatenation assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/20/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetDNA topoisomerase 2-alpha(Human)
University of Ljubljana

Curated by ChEMBL
LigandPNGBDBM50127140(4'-Demethylepipodophyllotoxin 9-(4,6-O-(R)-ethylid...)
Affinity DataIC50: 5.00E+4nMAssay Description:Inhibition of human 1 unit topoisomerase 2alpha catalytic activity assessed as relaxation of 198 ng supercoiled pBR322 DNA by agarose gel electrophor...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/16/2012
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetDNA topoisomerase 2-alpha(Human)
University of Ljubljana

Curated by ChEMBL
LigandPNGBDBM50127140(4'-Demethylepipodophyllotoxin 9-(4,6-O-(R)-ethylid...)
Affinity DataIC50: 5.02E+4nMAssay Description:Inhibition of human placenta topoisomerase 2alpha assessed as reduction in pBR322 supercoiled DNA relaxation after 30 mins by ethidium bromide staini...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/17/2020
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetDNA topoisomerase 2-alpha/2-beta(Human)
Sterling Winthrop Pharmaceuticals Research Division

Curated by ChEMBL
LigandPNGBDBM50127140(4'-Demethylepipodophyllotoxin 9-(4,6-O-(R)-ethylid...)
Affinity DataIC50: 5.04E+4nMAssay Description:Inhibitory concentration against human DNA topoisomerase IIMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/23/2020
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetDNA topoisomerase 2-alpha(Human)
University of Ljubljana

Curated by ChEMBL
LigandPNGBDBM50127140(4'-Demethylepipodophyllotoxin 9-(4,6-O-(R)-ethylid...)
Affinity DataIC50: 5.60E+4nMAssay Description:Inhibition of recombinant human DNA topoisomerase-2alpha assessed as decrease in relaxation of supercoiled pBR322 DNA after 30 mins by ethidium bromi...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/3/2020
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetDNA topoisomerase 2-alpha/2-beta(Human)
Sterling Winthrop Pharmaceuticals Research Division

Curated by ChEMBL
LigandPNGBDBM50127140(4'-Demethylepipodophyllotoxin 9-(4,6-O-(R)-ethylid...)
Affinity DataEC50:  5.60E+4nMAssay Description:Concentration of compound at which inhibitory activity detected against DNA topoisomerase IIMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/22/2020
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetDNA topoisomerase 2-alpha(Human)
University of Ljubljana

Curated by ChEMBL
LigandPNGBDBM50127140(4'-Demethylepipodophyllotoxin 9-(4,6-O-(R)-ethylid...)
Affinity DataIC50: 5.60E+4nMAssay Description:Inhibition of human DNA topoisomerase 2alpha-mediated decatenation of kinetoplast plasmid DNA by fluorescent plate readerMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/28/2012
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetDNA topoisomerase 2-alpha(Human)
University of Ljubljana

Curated by ChEMBL
LigandPNGBDBM50127140(4'-Demethylepipodophyllotoxin 9-(4,6-O-(R)-ethylid...)
Affinity DataIC50: 5.95E+4nMpH: 7.9Assay Description:Relaxation of negatively supercoiled plasmid DNA by human topoisomerase IIα was assayed in 20 µL of reaction buffer (10 mM Tris-HCl, pH 7.9, 150...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/31/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetDNA topoisomerase 2-alpha(Human)
University of Ljubljana

Curated by ChEMBL
LigandPNGBDBM50127140(4'-Demethylepipodophyllotoxin 9-(4,6-O-(R)-ethylid...)
Affinity DataIC50: 6.03E+4nMAssay Description:Inhibition of human topoisomerase 2 alpha-mediated relaxation of supercoiled pBR322 DNA after 30 mins by agarose gel electrophoresisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/23/2012
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetDNA topoisomerase 2-alpha(Human)
University of Ljubljana

Curated by ChEMBL
LigandPNGBDBM50127140(4'-Demethylepipodophyllotoxin 9-(4,6-O-(R)-ethylid...)
Affinity DataIC50: 6.83E+4nMAssay Description:Inhibition of human DNA topoisomerase 2alpha assessed as suppression of decatenation using catenated kinetoplast DNA as substrate measured after 30 m...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/26/2022
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetDNA topoisomerase 2-alpha(Human)
University of Ljubljana

Curated by ChEMBL
LigandPNGBDBM50127140(4'-Demethylepipodophyllotoxin 9-(4,6-O-(R)-ethylid...)
Affinity DataIC50: 7.10E+4nMAssay Description:Inhibition of human topoisomerase 2alpha using supercoiled pNO1 plasmid DNA as substrate incubated for 30 mins by fluorescence based microplate reade...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/25/2022
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetDNA topoisomerase 2-alpha(Human)
University of Ljubljana

Curated by ChEMBL
LigandPNGBDBM50127140(4'-Demethylepipodophyllotoxin 9-(4,6-O-(R)-ethylid...)
Affinity DataIC50: 7.57E+4nMAssay Description:Inhibition of human DNA topoisomerase 2alphaMore data for this Ligand-Target Pair
In Depth
Date in BDB:
1/11/2010
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetDNA topoisomerase 2-alpha(Human)
University of Ljubljana

Curated by ChEMBL
LigandPNGBDBM50127140(4'-Demethylepipodophyllotoxin 9-(4,6-O-(R)-ethylid...)
Affinity DataIC50: 7.84E+4nMAssay Description:Inhibition of human topoisomerase-2alpha using kDNA as substrate assessed as inhibition of ATP-dependent kDNA decatenation after 30 mins by agarose g...More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/1/2020
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetDNA topoisomerase 2-alpha(Human)
University of Ljubljana

Curated by ChEMBL
LigandPNGBDBM50127140(4'-Demethylepipodophyllotoxin 9-(4,6-O-(R)-ethylid...)
Affinity DataIC50: 7.84E+4nMAssay Description:Inhibition of human topoisomerase-2 alpha assessed as reduction in enzyme-mediated kinetoplast DNA decatenation incubated for 30 mins by ethidium bro...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/17/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetDNA topoisomerase 2-alpha(Human)
University of Ljubljana

Curated by ChEMBL
LigandPNGBDBM50127140(4'-Demethylepipodophyllotoxin 9-(4,6-O-(R)-ethylid...)
Affinity DataIC50: 9.29E+4nMAssay Description:Inhibition of human recombinant topoisomerase 2 by decatenation assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/15/2012
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetDNA topoisomerase 2-alpha(Human)
University of Ljubljana

Curated by ChEMBL
LigandPNGBDBM50127140(4'-Demethylepipodophyllotoxin 9-(4,6-O-(R)-ethylid...)
Affinity DataIC50: 1.10E+5nMAssay Description:Inhibition of human topoisomerase 2-alpha assessed as reduction in relaxation of pBR322 DNA measured after 30 mins by agarose gel electrophoresis met...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/17/2024
Entry Details
PubMedPDB3D3D Structure (crystal)
TargetDNA topoisomerase 2-alpha(Human)
University of Ljubljana

Curated by ChEMBL
LigandPNGBDBM50127140(4'-Demethylepipodophyllotoxin 9-(4,6-O-(R)-ethylid...)
Affinity DataIC50: 1.20E+5nMAssay Description:Inhibition of recombinant human topoisomerase 2alpha using supercoiled pBR322 DNA as substrate incubated for 60 mins by ethidium bromide dye based ag...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/25/2022
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetDNA topoisomerase 2-alpha(Human)
University of Ljubljana

Curated by ChEMBL
LigandPNGBDBM50127140(4'-Demethylepipodophyllotoxin 9-(4,6-O-(R)-ethylid...)
Affinity DataIC50: 1.20E+5nMAssay Description:Inhibition of human topoisomerase 2alpha expressed in baculovirus-infected insect cells assessed as reduction in pBR322 supercoiled DNA relaxation af...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/29/2019
Entry Details Article
PubMedPDB3D3D Structure (crystal)