Inhibitors | Comment | Organism | Structure |
---|---|---|---|
2,2,2-trifluoro-N-(8-(trifluoromethyl)benzo[f][1,2,3,4,5]pentathiepin-6-yl)acetamide | - |
Homo sapiens | |
2-(dibutylamino)-N-(8-(trifluoromethyl)benzo[f]-[1,2,3,4,5]pentathiepin-6-yl)acetamide | - |
Homo sapiens | |
2-(piperidin-1-yl)-N-(8-(trifluoromethyl)benzo[f]-[1,2,3,4,5]pentathiepin-6-yl)acetamide | - |
Homo sapiens | |
2-(pyrrolidin-1-yl)-N-(8-(trifluoromethyl)benzo[f]-[1,2,3,4,5]pentathiepin-6-yl)acetamide | - |
Homo sapiens | |
2-morpholino-N-(8-(trifluoromethyl)benzo[f]-[1,2,3,4,5]pentathiepin-6-yl)acetamide | - |
Homo sapiens | |
3-(piperidin-1-yl)-N-(8-(trifluoromethyl)benzo[f]-[1,2,3,4,5]pentathiepin-6-yl)propanamide | - |
Homo sapiens | |
3-(pyrrolidin-1-yl)-N-(8-(trifluoromethyl)benzo[f]-[1,2,3,4,5]pentathiepin-6-yl)propanamide | - |
Homo sapiens | |
3-morpholino-N-(8-(trifluoromethyl)benzo[f]-[1,2,3,4,5]pentathiepin-6-yl)propanamide | - |
Homo sapiens | |
aminobenzopentathiepine | - |
Homo sapiens | |
N-phenyl-2-(piperidin-1-yl)acetamide | - |
Homo sapiens | |
N-phenyl-2-(pyrrolidin-1-yl)acetamide | - |
Homo sapiens | |
NSC 88915 | - |
Homo sapiens |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
additional information | Homo sapiens | the enzyme cleaves the 3'-diester bond between tyrosine and DNA as well as removes other lesions, producing a 3'-phosphate that can be removed by polynucleotide kinase/phosphatase | ? | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | Q9NKW8 | - |
- |
Purification (Comment) | Organism |
---|---|
Ni-chelating resin column chromatography and phosphocellulose P11 column chromatography, and Superdex 200 gel filtration | Homo sapiens |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
5'-(5,6-FAM-aacgtcagggtcttcc-BHQ1)-3' + H2O | - |
Homo sapiens | ? | - |
? | |
additional information | the enzyme cleaves the 3'-diester bond between tyrosine and DNA as well as removes other lesions, producing a 3'-phosphate that can be removed by polynucleotide kinase/phosphatase | Homo sapiens | ? | - |
? |
Synonyms | Comment | Organism |
---|---|---|
TDP1 | - |
Homo sapiens |
tyrosyl-DNA phosphodiesterase 1 | - |
Homo sapiens |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.00022 | - |
at pH 8.0 and 26°C | Homo sapiens | 2-(dibutylamino)-N-(8-(trifluoromethyl)benzo[f]-[1,2,3,4,5]pentathiepin-6-yl)acetamide | |
0.00128 | - |
at pH 8.0 and 26°C | Homo sapiens | 2-(piperidin-1-yl)-N-(8-(trifluoromethyl)benzo[f]-[1,2,3,4,5]pentathiepin-6-yl)acetamide | |
0.0013 | - |
at pH 8.0 and 26°C | Homo sapiens | 3-morpholino-N-(8-(trifluoromethyl)benzo[f]-[1,2,3,4,5]pentathiepin-6-yl)propanamide | |
0.00162 | - |
at pH 8.0 and 26°C | Homo sapiens | 2-morpholino-N-(8-(trifluoromethyl)benzo[f]-[1,2,3,4,5]pentathiepin-6-yl)acetamide | |
0.00366 | - |
at pH 8.0 and 26°C | Homo sapiens | 3-(piperidin-1-yl)-N-(8-(trifluoromethyl)benzo[f]-[1,2,3,4,5]pentathiepin-6-yl)propanamide | |
0.0037 | - |
at pH 8.0 and 26°C | Homo sapiens | 2-(pyrrolidin-1-yl)-N-(8-(trifluoromethyl)benzo[f]-[1,2,3,4,5]pentathiepin-6-yl)acetamide | |
0.00603 | - |
at pH 8.0 and 26°C | Homo sapiens | 3-(pyrrolidin-1-yl)-N-(8-(trifluoromethyl)benzo[f]-[1,2,3,4,5]pentathiepin-6-yl)propanamide | |
0.01 | - |
IC50 above 0.01 mM, at pH 8.0 and 26°C | Homo sapiens | aminobenzopentathiepine | |
0.01 | - |
IC50 above 0.1 mM, at pH 8.0 and 26°C | Homo sapiens | 2,2,2-trifluoro-N-(8-(trifluoromethyl)benzo[f][1,2,3,4,5]pentathiepin-6-yl)acetamide | |
0.01 | - |
IC50 above 0.1 mM, at pH 8.0 and 26°C | Homo sapiens | N-phenyl-2-(piperidin-1-yl)acetamide | |
0.01 | - |
IC50 above 0.1 mM, at pH 8.0 and 26°C | Homo sapiens | N-phenyl-2-(pyrrolidin-1-yl)acetamide |