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Found 23 Enz. Inhib. hit(s) for PDB: 1T8I
TargetDNA topoisomerase 1(Homo sapiens (Human))
Decode Biostructures

Curated by ChEMBL
LigandPNGBDBM50008923((S)-4-ethyl-4-hydroxy-1,12-dihydro-4H-2-oxa-6,12a-...)
Affinity DataIC50:  300nMAssay Description:Inhibition of topoisomerase I-DNA complex in trapping assayMore data for this Ligand-Target Pair
TargetDNA topoisomerase 1(Homo sapiens (Human))
Decode Biostructures

Curated by ChEMBL
LigandPNGBDBM50008923((S)-4-ethyl-4-hydroxy-1,12-dihydro-4H-2-oxa-6,12a-...)
Affinity DataIC50:  679nMAssay 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
TargetDNA topoisomerase 1(Homo sapiens (Human))
Decode Biostructures

Curated by ChEMBL
LigandPNGBDBM50008923((S)-4-ethyl-4-hydroxy-1,12-dihydro-4H-2-oxa-6,12a-...)
Affinity DataIC50:  680nMAssay Description:Inhibition of Topoisomerase I by cleavage complex formation in human HL-60 cellsMore data for this Ligand-Target Pair
TargetDNA topoisomerase 1(Homo sapiens (Human))
Decode Biostructures

Curated by ChEMBL
LigandPNGBDBM50008923((S)-4-ethyl-4-hydroxy-1,12-dihydro-4H-2-oxa-6,12a-...)
Affinity DataIC50:  700nMAssay Description:Ability to inhibit calf thymus topoisomerase I when assayed in the cleavable complex formationMore data for this Ligand-Target Pair
TargetDNA topoisomerase 1(Homo sapiens (Human))
Decode Biostructures

Curated by ChEMBL
LigandPNGBDBM50008923((S)-4-ethyl-4-hydroxy-1,12-dihydro-4H-2-oxa-6,12a-...)
Affinity DataIC50:  700nMAssay Description:In vitro fragmentation of DNA in the presence of excess calf thymus topoisomerase.More data for this Ligand-Target Pair
TargetDNA topoisomerase 1(Homo sapiens (Human))
Decode Biostructures

Curated by ChEMBL
LigandPNGBDBM50008923((S)-4-ethyl-4-hydroxy-1,12-dihydro-4H-2-oxa-6,12a-...)
Affinity DataIC50:  700nMAssay Description:Inhibit supercoil relaxation property of topoisomerase I.More data for this Ligand-Target Pair
TargetDNA topoisomerase 1(Homo sapiens (Human))
Decode Biostructures

Curated by ChEMBL
LigandPNGBDBM50008923((S)-4-ethyl-4-hydroxy-1,12-dihydro-4H-2-oxa-6,12a-...)
Affinity DataIC50:  700nMAssay Description:Ability of the compound to satbilize DNA-topoisomerase (from calf) I-compound ternary complex was determinedMore data for this Ligand-Target Pair
TargetDNA topoisomerase 1(Homo sapiens (Human))
Decode Biostructures

Curated by ChEMBL
LigandPNGBDBM50045363((20R)-4-Ethyl-4-hydroxy-1,12-dihydro-4H-2-oxa-6,12...)
Affinity DataIC50:  1.40E+3nMAssay Description:Inhibition of Topoisomerase I by cleavage complex formation in human HL-60 cellsMore data for this Ligand-Target Pair
TargetDNA topoisomerase 1(Homo sapiens (Human))
Decode Biostructures

Curated by ChEMBL
LigandPNGBDBM50045363((20R)-4-Ethyl-4-hydroxy-1,12-dihydro-4H-2-oxa-6,12...)
Affinity DataIC50:  1.60E+3nMAssay Description:Inhibition of Topoisomerase I by cleavage complex formation in intact human HL-60 cellsMore data for this Ligand-Target Pair
TargetDNA topoisomerase 1(Homo sapiens (Human))
Decode Biostructures

Curated by ChEMBL
LigandPNGBDBM50008923((S)-4-ethyl-4-hydroxy-1,12-dihydro-4H-2-oxa-6,12a-...)
Affinity DataIC50:  2.20E+3nMAssay Description:Inhibition of human topoisomerase 1 assessed as decrease in pBR322 mobility on agarose gel by electrophoresisMore data for this Ligand-Target Pair
TargetDNA topoisomerase 1(Homo sapiens (Human))
Decode Biostructures

Curated by ChEMBL
LigandPNGBDBM50008923((S)-4-ethyl-4-hydroxy-1,12-dihydro-4H-2-oxa-6,12a-...)
Affinity DataIC50:  3.75E+3nMAssay Description:Inhibition of DNA topoisomerase 1 in Homo sapiens (human) SW480 cellsMore data for this Ligand-Target Pair
TargetDNA topoisomerase 1(Homo sapiens (Human))
Decode Biostructures

Curated by ChEMBL
LigandPNGBDBM50008923((S)-4-ethyl-4-hydroxy-1,12-dihydro-4H-2-oxa-6,12a-...)
Affinity DataIC50:  4.00E+3nMAssay Description:Inhibition topoisomerase 1 in human A549 cells assessed as conversion of supercoiled pBR322 DNA to relaxed formMore data for this Ligand-Target Pair
TargetDNA topoisomerase 1(Homo sapiens (Human))
Decode Biostructures

Curated by ChEMBL
LigandPNGBDBM50008923((S)-4-ethyl-4-hydroxy-1,12-dihydro-4H-2-oxa-6,12a-...)
Affinity DataIC50:  4.75E+3nMAssay Description:Inhibition of DNA topoisomerase 1 in Homo sapiens (human) HCT116 cellsMore data for this Ligand-Target Pair
TargetDNA topoisomerase 1(Homo sapiens (Human))
Decode Biostructures

Curated by ChEMBL
LigandPNGBDBM50008923((S)-4-ethyl-4-hydroxy-1,12-dihydro-4H-2-oxa-6,12a-...)
Affinity DataIC50:  4.95E+3nMAssay Description:Inhibition of DNA topoisomerase 1 in Homo sapiens (human) VACO 241 cellsMore data for this Ligand-Target Pair
TargetDNA topoisomerase 1(Homo sapiens (Human))
Decode Biostructures

Curated by ChEMBL
LigandPNGBDBM50008923((S)-4-ethyl-4-hydroxy-1,12-dihydro-4H-2-oxa-6,12a-...)
Affinity DataIC50:  9.00E+3nMAssay Description:Inhibition topoisomerase 1 in human HeLa cells assessed as conversion of supercoiled pBR322 DNA to relaxed formMore data for this Ligand-Target Pair
TargetDNA topoisomerase 1(Mus musculus)
Kumamoto University

Curated by ChEMBL
LigandPNGBDBM50008923((S)-4-ethyl-4-hydroxy-1,12-dihydro-4H-2-oxa-6,12a-...)
Affinity DataIC50:  1.20E+4nMAssay Description:Inhibition topoisomerase 1 in mouse NIH/3T3 cells assessed as conversion of supercoiled pBR322 DNA to relaxed formMore data for this Ligand-Target Pair
TargetDNA topoisomerase 1(Homo sapiens (Human))
Decode Biostructures

Curated by ChEMBL
LigandPNGBDBM50008923((S)-4-ethyl-4-hydroxy-1,12-dihydro-4H-2-oxa-6,12a-...)
Affinity DataIC50:  1.70E+4nMAssay Description:Inhibition topoisomerase 1 in human COLO201 cells assessed as conversion of supercoiled pBR322 DNA to relaxed formMore data for this Ligand-Target Pair
TargetDNA topoisomerase 1(Homo sapiens (Human))
Decode Biostructures

Curated by ChEMBL
LigandPNGBDBM50008923((S)-4-ethyl-4-hydroxy-1,12-dihydro-4H-2-oxa-6,12a-...)
Affinity DataIC50:  2.00E+4nMAssay Description:Inhibition of human recombinant DNA topoisomerase1More data for this Ligand-Target Pair
TargetDNA topoisomerase 1(Homo sapiens (Human))
Decode Biostructures

Curated by ChEMBL
LigandPNGBDBM50008923((S)-4-ethyl-4-hydroxy-1,12-dihydro-4H-2-oxa-6,12a-...)
Affinity DataIC50:  2.00E+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
TargetDNA topoisomerase 1(Cercopithecus aethiops)
Kumamoto University

Curated by ChEMBL
LigandPNGBDBM50008923((S)-4-ethyl-4-hydroxy-1,12-dihydro-4H-2-oxa-6,12a-...)
Affinity DataIC50:  2.70E+4nMAssay Description:Inhibition topoisomerase 1 in african green monkey Vero cells assessed as conversion of supercoiled pBR322 DNA to relaxed formMore data for this Ligand-Target Pair
TargetDNA topoisomerase 1(Mus musculus)
Kumamoto University

Curated by ChEMBL
LigandPNGBDBM50008923((S)-4-ethyl-4-hydroxy-1,12-dihydro-4H-2-oxa-6,12a-...)
Affinity DataIC50:  4.00E+4nMAssay Description:Average concentration to cause 50% inhibition of topo 1 using the cleavable complex assayMore data for this Ligand-Target Pair
TargetDNA topoisomerase 1(Homo sapiens (Human))
Decode Biostructures

Curated by ChEMBL
LigandPNGBDBM50008923((S)-4-ethyl-4-hydroxy-1,12-dihydro-4H-2-oxa-6,12a-...)
Affinity DataIC50:  1.27E+5nMAssay Description:Inhibitory activity against DNA topoisomerase-I obtained from Hela cellsMore data for this Ligand-Target Pair
TargetDNA topoisomerase 1(Homo sapiens (Human))
Decode Biostructures

Curated by ChEMBL
LigandPNGBDBM50008923((S)-4-ethyl-4-hydroxy-1,12-dihydro-4H-2-oxa-6,12a-...)
Affinity DataEC50:  350nMAssay Description:Effective concentration against DNA topoisomerase IMore data for this Ligand-Target Pair