Inhibitors | Comment | Organism | Structure |
---|---|---|---|
2-(2,6-dimethylhept-5-en-1-yl)-5,7-dimethyl-1,3-diazatricyclo[3.3.1.1(3,7)]decan-6-one | - |
Homo sapiens | |
3,20-dioxopregn-4-en-21-yl 4-bromobenzene-1-sulfonate | - |
Homo sapiens | |
3-(((1R,5S)-6,6-dimethylbicyclo[3.1.1]hept-2-en-2-yl)methoxy)-7,8,9,10-tetrahydro-6H-benzo[c]chromen-6-one | - |
Homo sapiens | |
3-(((1S,5R)-6,6-dimethylbicyclo[3.1.1]hept-2-en-2-yl)methoxy)-7,8,9,10-tetrahydro-6H-benzo[c]chromen-6-one | - |
Homo sapiens | |
3-((3,4,5-trimethoxybenzyl)oxy)-7,8,9,10-tetrahydro-6H-benzo[c]chromen-6-one | - |
Homo sapiens | |
3-((3-methoxybenzyl)oxy)-7,8,9,10-tetrahydro-6Hbenzo[c]chromen-6-one | - |
Homo sapiens | |
3-(2-((1R,5S)-6,6-dimethylbicyclo[3.1.1]hept-2-en-2-yl)ethoxy)-7,8,9,10-tetrahydro-6H-benzo[c]chromen-6-one | - |
Homo sapiens | |
3-(benzyloxy)-7,8,9,10-tetrahydro-6H-benzo[c]chromen-6-one | - |
Homo sapiens | |
4,4'-(furan-2,5-diyl)di(benzene-1-carboximidamide) | - |
Homo sapiens | |
4-methyl-7-((3,4,5-trimethoxybenzyl)oxy)-2H-chromen-2-one | - |
Homo sapiens | |
6-(3-aminopropyl)-8-hydroxy-3-nitro-5H-indeno[1,2-c]isoquinoline-5,11(6H)-dione | - |
Homo sapiens | |
7-(((1R,5S)-6,6-dimethylbicyclo[3.1.1]hept-2-en-2-yl)methoxy)-2,3-dihydrocyclopenta[c]chromen-4(1H)-one | - |
Homo sapiens | |
7-(((1R,5S)-6,6-dimethylbicyclo[3.1.1]hept-2-en-2-yl)methoxy)-4-methyl-2H-chromen-2-one | - |
Homo sapiens | |
7-(((1S,5R)-6,6-dimethylbicyclo[3.1.1]hept-2-en-2-yl)methoxy)-2,3-dihydrocyclopenta[c]chromen-4(1H)-one | - |
Homo sapiens | |
7-(((1S,5R)-6,6-dimethylbicyclo[3.1.1]hept-2-en-2-yl)methoxy)-4-methyl-2H-chromen-2-one | - |
Homo sapiens | |
7-((3,4,5-trimethoxybenzyl)oxy)-2,3-dihydrocyclopenta[c]chromen-4(1H)-one | - |
Homo sapiens | |
7-((3-methoxybenzyl) oxy)-4-methyl-2H-chromen-2-one | - |
Homo sapiens | |
7-((3-methoxybenzyl)oxy)-2,3-dihydrocyclopenta[c]chromen-4(1H)-one | - |
Homo sapiens | |
7-(2-((1R,5S)-6,6-dimethylbicyclo[3.1.1]hept-2-en-2-yl)ethoxy)-2,3-dihydrocyclopenta[c]chromen-4(1H)-one | - |
Homo sapiens | |
7-(benzyloxy)-2,3-dihydrocyclopenta[c]chromen-4(1H)-one | - |
Homo sapiens | |
7-(benzyloxy)-4-methyl-2H-chromen-2-one | - |
Homo sapiens | |
N2,N2-dibutyl-N-[8-(trifluoromethyl)-1,2,3,4,5-benzopentathiepin-6-yl]glycinamide | - |
Homo sapiens |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
additional information | Homo sapiens | the enzyme hydrolyzes the phosphodiester bond between a catalytic tyrosine Tyr723 (human) of topoisomerase 1 and DNA 3'-phosphate | ? | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | Q9NUW8 | - |
- |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
MCF-7 cell | - |
Homo sapiens | - |
RPMI-8226 cell | - |
Homo sapiens | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
additional information | the enzyme hydrolyzes the phosphodiester bond between a catalytic tyrosine Tyr723 (human) of topoisomerase 1 and DNA 3'-phosphate | Homo sapiens | ? | - |
? |
Synonyms | Comment | Organism |
---|---|---|
Tdp 1 | - |
Homo sapiens |
tyrosyl-DNA phosphodiesterase I | - |
Homo sapiens |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.000675 | - |
pH and temperature not specified in the publication | Homo sapiens | 7-(((1S,5R)-6,6-dimethylbicyclo[3.1.1]hept-2-en-2-yl)methoxy)-2,3-dihydrocyclopenta[c]chromen-4(1H)-one | |
0.00109 | - |
pH and temperature not specified in the publication | Homo sapiens | 7-(2-((1R,5S)-6,6-dimethylbicyclo[3.1.1]hept-2-en-2-yl)ethoxy)-2,3-dihydrocyclopenta[c]chromen-4(1H)-one | |
0.0012 | - |
pH and temperature not specified in the publication | Homo sapiens | 3-(((1S,5R)-6,6-dimethylbicyclo[3.1.1]hept-2-en-2-yl)methoxy)-7,8,9,10-tetrahydro-6H-benzo[c]chromen-6-one | |
0.00123 | - |
pH and temperature not specified in the publication | Homo sapiens | 3-(((1R,5S)-6,6-dimethylbicyclo[3.1.1]hept-2-en-2-yl)methoxy)-7,8,9,10-tetrahydro-6H-benzo[c]chromen-6-one | |
0.00137 | - |
pH and temperature not specified in the publication | Homo sapiens | 7-(((1R,5S)-6,6-dimethylbicyclo[3.1.1]hept-2-en-2-yl)methoxy)-2,3-dihydrocyclopenta[c]chromen-4(1H)-one | |
0.00145 | - |
pH and temperature not specified in the publication | Homo sapiens | 3-(2-((1R,5S)-6,6-dimethylbicyclo[3.1.1]hept-2-en-2-yl)ethoxy)-7,8,9,10-tetrahydro-6H-benzo[c]chromen-6-one | |
0.00156 | - |
pH and temperature not specified in the publication | Homo sapiens | 7-(((1R,5S)-6,6-dimethylbicyclo[3.1.1]hept-2-en-2-yl)methoxy)-4-methyl-2H-chromen-2-one | |
0.00431 | - |
pH and temperature not specified in the publication | Homo sapiens | 7-(((1S,5R)-6,6-dimethylbicyclo[3.1.1]hept-2-en-2-yl)methoxy)-4-methyl-2H-chromen-2-one | |
0.00493 | - |
pH and temperature not specified in the publication | Homo sapiens | 3-((3-methoxybenzyl)oxy)-7,8,9,10-tetrahydro-6Hbenzo[c]chromen-6-one | |
0.00528 | - |
pH and temperature not specified in the publication | Homo sapiens | 7-(benzyloxy)-4-methyl-2H-chromen-2-one | |
0.00562 | - |
pH and temperature not specified in the publication | Homo sapiens | 3-(benzyloxy)-7,8,9,10-tetrahydro-6H-benzo[c]chromen-6-one | |
0.00917 | - |
pH and temperature not specified in the publication | Homo sapiens | 7-(benzyloxy)-2,3-dihydrocyclopenta[c]chromen-4(1H)-one | |
0.01 | - |
IC50 above 0.01 mM, pH and temperature not specified in the publication | Homo sapiens | 3-((3,4,5-trimethoxybenzyl)oxy)-7,8,9,10-tetrahydro-6H-benzo[c]chromen-6-one | |
0.01 | - |
IC50 above 0.01 mM, pH and temperature not specified in the publication | Homo sapiens | 4-methyl-7-((3,4,5-trimethoxybenzyl)oxy)-2H-chromen-2-one | |
0.01 | - |
IC50 above 0.01 mM, pH and temperature not specified in the publication | Homo sapiens | 7-((3,4,5-trimethoxybenzyl)oxy)-2,3-dihydrocyclopenta[c]chromen-4(1H)-one | |
0.01 | - |
IC50 above 0.01 mM, pH and temperature not specified in the publication | Homo sapiens | 7-((3-methoxybenzyl) oxy)-4-methyl-2H-chromen-2-one | |
0.01 | - |
IC50 above 0.01 mM, pH and temperature not specified in the publication | Homo sapiens | 7-((3-methoxybenzyl)oxy)-2,3-dihydrocyclopenta[c]chromen-4(1H)-one |
General Information | Comment | Organism |
---|---|---|
physiological function | the enzyme plays a key role in the removal of DNA damage resulting from Topo1 inhibition or caused by other anticancer drugs, e.g., temozolomide, bleomycin, etoposide, etc. | Homo sapiens |