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TargetDNA topoisomerase 1(Human)
Glaxo Research Institute

Curated by ChEMBL
LigandPNGBDBM50036132(15-chloromethyl-8-ethyl-8-hydroxy-(8S)-2,3,8,9,12,...)
Affinity DataIC50: 11nMAssay Description:Inhibition of topoisomerase I activity was determined in vitro by using the cleavable complex assay(calf thymus)More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetDNA topoisomerase 1(Human)
Glaxo Research Institute

Curated by ChEMBL
LigandPNGBDBM50036129(14-chloromethyl-7-ethyl-7-hydroxy-(7S)-7,8,11,13-t...)
Affinity DataIC50: 15nMAssay Description:Inhibition of topoisomerase I activity was determined in vitro by using the cleavable complex assay(calf thymus)More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetDNA topoisomerase 1(Human)
Glaxo Research Institute

Curated by ChEMBL
LigandPNGBDBM50008935(CHEMBL84 | 10-Dimethylaminomethyl-4-ethyl-4,9-dihy...)
Affinity DataIC50: 21nMAssay Description:Inhibition of recombinant human Top1 expressed in baculovirus infected sf9 insect cells using supercoiled pBS (SK+) DNA as substrate incubated for 30...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/30/2022
Entry Details Article
PubMed
TargetDNA topoisomerase 1(Human)
Glaxo Research Institute

Curated by ChEMBL
LigandPNGBDBM50008935(CHEMBL84 | 10-Dimethylaminomethyl-4-ethyl-4,9-dihy...)
Affinity DataIC50: 21nMAssay Description:Poison activity at recombinant human TOP1 expressed in baculovirus infected Sf9 insect cells assessed as decrease in relaxed supercoiled pBS(SK+) DNA...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/20/2021
Entry Details Article
PubMed
TargetDNA topoisomerase 1(Human)
Glaxo Research Institute

Curated by ChEMBL
LigandPNGBDBM50562433(CHEMBL4756086)
Affinity DataIC50: 21nMAssay Description:Inhibition of human topoisomerase-1 beta incubated for 2 hrs by ELISAMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/29/2022
Entry Details Article
PubMed
TargetDNA topoisomerase 1(Human)
Glaxo Research Institute

Curated by ChEMBL
LigandPNGBDBM50565242(CHEMBL4791048)
Affinity DataIC50: 24nMAssay Description:Inhibition of recombinant human Top1 expressed in baculovirus infected sf9 insect cells using supercoiled pBS (SK+) DNA as substrate incubated for 30...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/30/2022
Entry Details Article
PubMed
TargetDNA topoisomerase 1(Human)
Glaxo Research Institute

Curated by ChEMBL
LigandPNGBDBM50008923(4-Ethyl-4-hydroxy-1,12-dihydro-4H-2-oxa-6,12a-diaz...)
Affinity DataIC50: 25nMAssay Description:Poison activity at recombinant human TOP1 expressed in baculovirus infected Sf9 insect cells assessed as decrease in relaxed supercoiled pBS(SK+) DNA...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/20/2021
Entry Details Article
PubMed
TargetDNA topoisomerase 1(Human)
Glaxo Research Institute

Curated by ChEMBL
LigandPNGBDBM50008923(4-Ethyl-4-hydroxy-1,12-dihydro-4H-2-oxa-6,12a-diaz...)
Affinity DataIC50: 25nMAssay Description:Inhibition of recombinant human Top1 expressed in baculovirus infected sf9 insect cells using supercoiled pBS (SK+) DNA as substrate incubated for 30...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/30/2022
Entry Details Article
PubMed
TargetDNA topoisomerase 1(Human)
Glaxo Research Institute

Curated by ChEMBL
LigandPNGBDBM50036133(7-ethyl-7-hydroxy-(7S)-7,8,11,13-tetrahydro-10H-[1...)
Affinity DataIC50: 27nMAssay Description:Inhibition of Topoisomerase I by cleavage complex formation in intact human HL-60 cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/25/2012
Entry Details Article
PubMed
TargetDNA topoisomerase 1(Human)
Glaxo Research Institute

Curated by ChEMBL
LigandPNGBDBM50034013(9-Bromo-4-ethyl-4-hydroxy-11-methyl-1,12-dihydro-4...)
Affinity DataIC50: 28nMAssay Description:Inhibitory activity against DNA topoisomerase IMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/14/2012
Entry Details Article
PubMed
TargetDNA topoisomerase 1(Human)
Glaxo Research Institute

Curated by ChEMBL
LigandPNGBDBM50034013(9-Bromo-4-ethyl-4-hydroxy-11-methyl-1,12-dihydro-4...)
Affinity DataIC50: 28nMAssay Description:In vitro fragmentation of DNA in the presence of excess calf thymus topoisomerase.More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/31/2012
Entry Details Article
PubMed
TargetDNA topoisomerase 1(Human)
Glaxo Research Institute

Curated by ChEMBL
LigandPNGBDBM50510239(CHEMBL4454135)
Affinity DataIC50: 29nMAssay Description:Inhibition of recombinant human Top1 expressed in baculovirus infected sf9 insect cells using supercoiled pBS (SK+) DNA as substrate incubated for 30...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/30/2022
Entry Details Article
PubMed
TargetDNA topoisomerase 1(Human)
Glaxo Research Institute

Curated by ChEMBL
LigandPNGBDBM50510239(CHEMBL4454135)
Affinity DataIC50: 29nMAssay Description:Poison activity at recombinant human TOP1 expressed in baculovirus infected Sf9 insect cells assessed as decrease in relaxed supercoiled pBS(SK+) DNA...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/20/2021
Entry Details Article
PubMed
TargetDNA topoisomerase 1(Human)
Glaxo Research Institute

Curated by ChEMBL
LigandPNGBDBM50510239(CHEMBL4454135)
Affinity DataIC50: 29nMAssay Description:Inhibition of recombinant human Top1 derived from human MCF7 cell extract incubated for 30 minsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/20/2023
Entry Details
PubMed
TargetDNA topoisomerase 1(Human)
Glaxo Research Institute

Curated by ChEMBL
LigandPNGBDBM50036133(7-ethyl-7-hydroxy-(7S)-7,8,11,13-tetrahydro-10H-[1...)
Affinity DataIC50: 30nMAssay Description:Ability to inhibit calf thymus topoisomerase I when assayed in the cleavable complex formationMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/19/2010
Entry Details Article

TargetDNA topoisomerase 1(Human)
Glaxo Research Institute

Curated by ChEMBL
LigandPNGBDBM50073854(2,10-dihydroxy-12-(3,4,5-trihydroxy-6-hydroxymethy...)
Affinity DataIC50: 30nMAssay Description:Inhibition of topoisomerase I-DNA complex in trapping assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/4/2012
Entry Details Article
PubMed
TargetDNA topoisomerase 1(Human)
Glaxo Research Institute

Curated by ChEMBL
LigandPNGBDBM50562432(CHEMBL4786201)
Affinity DataIC50: 31nMAssay Description:Inhibition of human topoisomerase-1 beta incubated for 2 hrs by ELISAMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/29/2022
Entry Details Article
PubMed
TargetDNA topoisomerase 1(Human)
Glaxo Research Institute

Curated by ChEMBL
LigandPNGBDBM50034009((S)-4,11-Diethyl-4-hydroxy-3,13-dioxo-3,4,12,13-te...)
Affinity DataIC50: 33nMAssay Description:Minimum concentration that produced 50% fragmentation of DNA was measured in the presence of excess calf thymus topoisomerase.More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/31/2012
Entry Details Article
PubMed
TargetDNA topoisomerase 1(Human)
Glaxo Research Institute

Curated by ChEMBL
LigandPNGBDBM50045377((20S)-7-ethyl-7-hydroxy-7,8,11,13-tetrahydro-10H-[...)
Affinity DataIC50: 38nMAssay Description:Inhibition of Topoisomerase I by cleavage complex formation in intact human HL-60 cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/25/2012
Entry Details Article
PubMed
TargetDNA topoisomerase 1(Human)
Glaxo Research Institute

Curated by ChEMBL
LigandPNGBDBM50422003(CHEMBL10741)
Affinity DataIC50: 38nMAssay Description:Inhibition of Topoisomerase I by cleavage complex formation in intact human HL-60 cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/25/2012
Entry Details Article
PubMed
TargetDNA topoisomerase 1(Human)
Glaxo Research Institute

Curated by ChEMBL
LigandPNGBDBM50363804(CHEMBL1946917)
Affinity DataIC50: 39nMAssay Description:Inhibition of DNA topoisomerase 1 (unknown origin) at 50 uM measured by agar gel electrophoresisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/19/2024
Entry Details
PubMed
TargetDNA topoisomerase 1(Human)
Glaxo Research Institute

Curated by ChEMBL
LigandPNGBDBM50406999(CHEMBL2114243)
Affinity DataIC50: 48nMAssay Description:Inhibition of Topoisomerase I by cleavage complex formation in intact human HL-60 cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/25/2012
Entry Details Article
PubMed
TargetDNA topoisomerase 1(Human)
Glaxo Research Institute

Curated by ChEMBL
LigandPNGBDBM50250996(chebulanin | TANNIN | chebulagic acid | CHEMBL5252...)
Affinity DataIC50: 50nMAssay Description:Inhibition of human COLO201 cellular topoisomerase-1 mediated plasmid DNA cleavage by electrophoresis in presence of 14 units of enzymeMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/25/2010
Entry Details Article
PubMed
TargetDNA topoisomerase 1(Human)
Glaxo Research Institute

Curated by ChEMBL
LigandPNGBDBM50008935(CHEMBL84 | 10-Dimethylaminomethyl-4-ethyl-4,9-dihy...)
Affinity DataIC50: 50nMAssay Description:Inhibition of topoisomerase I-DNA complex in trapping assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/4/2012
Entry Details Article
PubMed
TargetDNA topoisomerase 1(Human)
Glaxo Research Institute

Curated by ChEMBL
LigandPNGBDBM50562431(CHEMBL4757169)
Affinity DataIC50: 59nMAssay Description:Inhibition of human topoisomerase-1 beta incubated for 2 hrs by ELISAMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/29/2022
Entry Details Article
PubMed
TargetDNA topoisomerase 1(Human)
Glaxo Research Institute

Curated by ChEMBL
LigandPNGBDBM50045368((20S)-15-chloro-7-ethyl-7-hydroxy-7,8,11,13-tetrah...)
Affinity DataIC50: 61nMAssay Description:Inhibition of Topoisomerase I by cleavage complex formation in intact human HL-60 cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/25/2012
Entry Details Article
PubMed
TargetDNA topoisomerase 1(Human)
Glaxo Research Institute

Curated by ChEMBL
LigandPNGBDBM50008923(4-Ethyl-4-hydroxy-1,12-dihydro-4H-2-oxa-6,12a-diaz...)
Affinity DataIC50: 62nMAssay Description:Inhibition of human topoisomerase-1 beta incubated for 2 hrs by ELISAMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/29/2022
Entry Details Article
PubMed
TargetDNA topoisomerase 1(Human)
Glaxo Research Institute

Curated by ChEMBL
LigandPNGBDBM50562430(CHEMBL4783134)
Affinity DataIC50: 64nMAssay Description:Inhibition of human topoisomerase-1 beta incubated for 2 hrs by ELISAMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/29/2022
Entry Details Article
PubMed
TargetDNA topoisomerase 1(Human)
Glaxo Research Institute

Curated by ChEMBL
LigandPNGBDBM50045377((20S)-7-ethyl-7-hydroxy-7,8,11,13-tetrahydro-10H-[...)
Affinity DataIC50: 67nMAssay Description:Inhibition of Topoisomerase I by cleavage complex formation in human HL-60 cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/25/2012
Entry Details Article
PubMed
TargetDNA topoisomerase 1(Human)
Glaxo Research Institute

Curated by ChEMBL
LigandPNGBDBM50045381((20S)-15-amino-7-ethyl-7-hydroxy-7,8,11,13-tetrahy...)
Affinity DataIC50: 69nMAssay Description:Inhibition of Topoisomerase I by cleavage complex formation in intact human HL-60 cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/25/2012
Entry Details Article
PubMed
TargetDNA topoisomerase 1(Human)
Glaxo Research Institute

Curated by ChEMBL
LigandPNGBDBM50034018((S)-4,11-Diethyl-4,N-dihydroxy-3,13-dioxo-3,4,12,1...)
Affinity DataIC50: 71nMAssay Description:Minimum concentration that produced 50% fragmentation of DNA was measured in the presence of excess calf thymus topoisomerase.More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/31/2012
Entry Details Article
PubMed
TargetDNA topoisomerase 1(Human)
Glaxo Research Institute

Curated by ChEMBL
LigandPNGBDBM50045381((20S)-15-amino-7-ethyl-7-hydroxy-7,8,11,13-tetrahy...)
Affinity DataIC50: 76nMAssay Description:Inhibition of Topoisomerase I by cleavage complex formation in intact human HL-60 cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/25/2012
Entry Details Article
PubMed
TargetDNA topoisomerase 1(Human)
Glaxo Research Institute

Curated by ChEMBL
LigandPNGBDBM50036133(7-ethyl-7-hydroxy-(7S)-7,8,11,13-tetrahydro-10H-[1...)
Affinity DataIC50: 78nMAssay Description:Inhibition of topoisomerase I activity was determined in vitro by using the cleavable complex assay(calf thymus)More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetDNA topoisomerase 1(Human)
Glaxo Research Institute

Curated by ChEMBL
LigandPNGBDBM50407001(CHEMBL2114244)
Affinity DataIC50: 86nMAssay Description:Inhibition of Topoisomerase I by cleavage complex formation in intact human HL-60 cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/25/2012
Entry Details Article
PubMed
TargetDNA topoisomerase 1(Human)
Glaxo Research Institute

Curated by ChEMBL
LigandPNGBDBM50049295(7-ethyl-7-hydroxy-14-(3-hydroxymethyl-1-pyridinium...)
Affinity DataIC50: 100nMAssay Description:Average concentration of compound to cause 50% inhibition of topoisomerase-1More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetDNA topoisomerase 1(Human)
Glaxo Research Institute

Curated by ChEMBL
LigandPNGBDBM50250996(chebulanin | TANNIN | chebulagic acid | CHEMBL5252...)
Affinity DataIC50: 100nMAssay Description:Inhibition of human COLO201 cellular topoisomerase-1 mediated plasmid DNA cleavage by electrophoresis in presence of 70 units of enzymeMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/25/2010
Entry Details Article
PubMed
TargetDNA topoisomerase 1(Human)
Glaxo Research Institute

Curated by ChEMBL
LigandPNGBDBM50045383((20S)-9,10-Dichloro-4-ethyl-4-hydroxy-1,12-dihydro...)
Affinity DataIC50: 110nMAssay Description:Inhibition of Topoisomerase I by cleavage complex formation in intact human HL-60 cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/25/2012
Entry Details Article
PubMed
TargetDNA topoisomerase 1(Human)
Glaxo Research Institute

Curated by ChEMBL
LigandPNGBDBM50008936(cid_72402 | 9-aminocamptothecan | CHEMBL274070 | 1...)
Affinity DataIC50: 110nMAssay Description:Inhibition of Topoisomerase I by cleavage complex formation in intact human HL-60 cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/25/2012
Entry Details Article
PubMed
TargetDNA topoisomerase 1(Human)
Glaxo Research Institute

Curated by ChEMBL
LigandPNGBDBM50008922(10-Hydroxycamptothecine | 4-Ethyl-4,10-dihydroxy-1...)
Affinity DataIC50: 110nMAssay Description:Inhibition of Topoisomerase I by cleavage complex formation in intact human HL-60 cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/25/2012
Entry Details Article
PubMed
TargetDNA topoisomerase 1(Human)
Glaxo Research Institute

Curated by ChEMBL
LigandPNGBDBM50562429(CHEMBL4758564)
Affinity DataIC50: 114nMAssay Description:Inhibition of human topoisomerase-1 beta incubated for 2 hrs by ELISAMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/29/2022
Entry Details Article
PubMed
TargetDNA topoisomerase 1(Human)
Glaxo Research Institute

Curated by ChEMBL
LigandPNGBDBM50034019((S)-9-Bromo-4,11-diethyl-4-hydroxy-1,12-dihydro-4H...)
Affinity DataIC50: 122nMAssay Description:In vitro fragmentation of DNA in the presence of excess calf thymus topoisomerase.More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/31/2012
Entry Details Article
PubMed
TargetDNA topoisomerase 1(Human)
Glaxo Research Institute

Curated by ChEMBL
LigandPNGBDBM50562434(CHEMBL4785034)
Affinity DataIC50: 123nMAssay Description:Inhibition of human topoisomerase-1 beta incubated for 2 hrs by ELISAMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/29/2022
Entry Details Article
PubMed
TargetDNA topoisomerase 1(Human)
Glaxo Research Institute

Curated by ChEMBL
LigandPNGBDBM50045398((20S)-9-Bromo-4-ethyl-4-hydroxy-1,12-dihydro-4H-2-...)
Affinity DataIC50: 130nMAssay Description:Inhibition of Topoisomerase I by cleavage complex formation in intact human HL-60 cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/25/2012
Entry Details Article
PubMed
TargetDNA topoisomerase 1(Human)
Glaxo Research Institute

Curated by ChEMBL
LigandPNGBDBM50406990(CHEMBL102252)
Affinity DataIC50: 140nMAssay Description:Inhibition of Topoisomerase I by cleavage complex formation in intact human HL-60 cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/25/2012
Entry Details Article
PubMed
TargetDNA topoisomerase 1(Human)
Glaxo Research Institute

Curated by ChEMBL
LigandPNGBDBM50406995(CHEMBL2115019)
Affinity DataIC50: 140nMAssay Description:Inhibition of Topoisomerase I by cleavage complex formation in intact human HL-60 cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/25/2012
Entry Details Article
PubMed
TargetDNA topoisomerase 1(Human)
Glaxo Research Institute

Curated by ChEMBL
LigandPNGBDBM50049303(7-ethyl-7-hydroxy-14-pyrazin-1-ium-1-ylmethyl-(7S)...)
Affinity DataIC50: 140nMAssay Description:Average concentration of compound to cause 50% inhibition of topoisomerase-1More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetDNA topoisomerase 1(Human)
Glaxo Research Institute

Curated by ChEMBL
LigandPNGBDBM50034014(4-Ethyl-4-hydroxy-11-methyl-3,13-dioxo-3,4,12,13-t...)
Affinity DataIC50: 143nMAssay Description:In vitro fragmentation of DNA in the presence of excess calf thymus topoisomerase.More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/31/2012
Entry Details Article
PubMed
TargetDNA topoisomerase 1(Human)
Glaxo Research Institute

Curated by ChEMBL
LigandPNGBDBM50034014(4-Ethyl-4-hydroxy-11-methyl-3,13-dioxo-3,4,12,13-t...)
Affinity DataIC50: 143nMAssay Description:Inhibitory activity against DNA topoisomerase IMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/14/2012
Entry Details Article
PubMed
TargetDNA topoisomerase 1(Human)
Glaxo Research Institute

Curated by ChEMBL
LigandPNGBDBM50562435(CHEMBL4755007)
Affinity DataIC50: 147nMAssay Description:Inhibition of human topoisomerase-1 beta incubated for 2 hrs by ELISAMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/29/2022
Entry Details Article
PubMed
TargetDNA topoisomerase 1(Human)
Glaxo Research Institute

Curated by ChEMBL
LigandPNGBDBM50406997(CHEMBL2114245)
Affinity DataIC50: 150nMAssay Description:Inhibition of Topoisomerase I by cleavage complex formation in intact human HL-60 cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/25/2012
Entry Details Article
PubMed
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