Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary for 5.6.2.2 extracted from

  • Kim, J.S.; Rhee, H.K.; Park, H.J.; Lee, S.K.; Lee, C.O.; Park Choo, H.Y.
    Synthesis of 1-/2-substituted-[1,2,3]triazolo[4,5-g]phthalazine-4,9-diones and evaluation of their cytotoxicity and topoisomerase II inhibition (2008), Bioorg. Med. Chem., 16, 4545-4550.
    View publication on PubMed
Search for more literature for 5.6.2.2

Inhibitors

Inhibitors Comment Organism Structure
1-(4-methoxybenzyl)-1H-[1,2,3]triazolo[4,5-g]-phthalazine-4,9-dione
-
 Homo sapiens
1-ethyl-1H-[1,2,3]triazolo[4,5-g]phthalazine-4,9-dione
-
 Homo sapiens
1-iso-butyl-1H-[1,2,3]triazolo[4,5-g]phthalazine-4,9-dione
-
 Homo sapiens
1-iso-propyl-1H-[1,2,3]triazolo[4,5-g]phthalazine-4,9-dione
-
 Homo sapiens
1-methyl-1H-[1,2,3]triazolo[4,5-g]phthalazine-4,9-dione
-
 Homo sapiens
1-n-butyl-1H-[1,2,3]triazolo[4,5-g]phthalazine-4,9-dione
-
 Homo sapiens
1-n-propyl-1H-[1,2,3]triazolo[4,5-g]phthalazine-4,9-dione
-
 Homo sapiens
1H-[1,2,3]triazolo[4,5,-g]phthalazine-4,9-dione
-
 Homo sapiens
2-ethyl-2H-[1,2,3]triazolo[4,5-g]phthalazine-4,9-dione
-
 Homo sapiens
2-iso-butyl-2H-[1,2,3] triazolo[4,5-g]phthalazine-4,9-dione
-
 Homo sapiens
2-iso-propyl-2H-[1,2,3]triazolo[4,5-g]phthalazine-4,9-dione
-
 Homo sapiens
2-methyl-2H-[1,2,3]triazolo[4,5-g]phthalazine-4,9-dione
-
 Homo sapiens
2-n-butyl-2H-[1,2,3] triazolo[4,5-g]phthalazine-4,9-dione
-
 Homo sapiens
2-n-propyl-2H-[1,2,3] triazolo[4,5-g]phthalazine-4,9-dione
-
 Homo sapiens
doxorubicin
-
 Homo sapiens
etoposide
-
 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
A-549 cell
-
 Homo sapiens
-
HCT-15 cell
-
 Homo sapiens
-
HL-60 cell
-
 Homo sapiens
-
HT-1080 cell
-
 Homo sapiens
-
SK-MEL-2 cell
-
 Homo sapiens
-
SKOV-3 cell
-
 Homo sapiens
-
SNU-638 cell
-
 Homo sapiens
-
XF-498 cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
supercoiled DNA + ATP + H2O
-
 Homo sapiens catenated DNA networks + ADP + phosphate
-
 ?

Synonyms

Synonyms Comment Organism
topo II
-
 Homo sapiens
Topoisomerase II
-
 Homo sapiens

Cofactor

Cofactor Comment Organism Structure
ATP
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0194
-
 in 50 mM Tris-HCl, pH 8, 120 mM KCl, 10 mM MgCl2, 0.5 mM ATP, 0.5 mM dithiothreitol, 0.03 mg/ml bovine serum albumin, at 37°C Homo sapiens 2-iso-butyl-2H-[1,2,3] triazolo[4,5-g]phthalazine-4,9-dione
0.0286
-
 in 50 mM Tris-HCl, pH 8, 120 mM KCl, 10 mM MgCl2, 0.5 mM ATP, 0.5 mM dithiothreitol, 0.03 mg/ml bovine serum albumin, at 37°C Homo sapiens 1-(4-methoxybenzyl)-1H-[1,2,3]triazolo[4,5-g]-phthalazine-4,9-dione
0.0298
-
 in 50 mM Tris-HCl, pH 8, 120 mM KCl, 10 mM MgCl2, 0.5 mM ATP, 0.5 mM dithiothreitol, 0.03 mg/ml bovine serum albumin, at 37°C Homo sapiens 1-iso-butyl-1H-[1,2,3]triazolo[4,5-g]phthalazine-4,9-dione
0.0333
-
 in 50 mM Tris-HCl, pH 8, 120 mM KCl, 10 mM MgCl2, 0.5 mM ATP, 0.5 mM dithiothreitol, 0.03 mg/ml bovine serum albumin, at 37°C Homo sapiens 1-iso-propyl-1H-[1,2,3]triazolo[4,5-g]phthalazine-4,9-dione
0.039
-
 in 50 mM Tris-HCl, pH 8, 120 mM KCl, 10 mM MgCl2, 0.5 mM ATP, 0.5 mM dithiothreitol, 0.03 mg/ml bovine serum albumin, at 37°C Homo sapiens 1-methyl-1H-[1,2,3]triazolo[4,5-g]phthalazine-4,9-dione
0.0432
-
 in 50 mM Tris-HCl, pH 8, 120 mM KCl, 10 mM MgCl2, 0.5 mM ATP, 0.5 mM dithiothreitol, 0.03 mg/ml bovine serum albumin, at 37°C Homo sapiens 1-n-butyl-1H-[1,2,3]triazolo[4,5-g]phthalazine-4,9-dione
0.0444
-
 in 50 mM Tris-HCl, pH 8, 120 mM KCl, 10 mM MgCl2, 0.5 mM ATP, 0.5 mM dithiothreitol, 0.03 mg/ml bovine serum albumin, at 37°C Homo sapiens 2-n-propyl-2H-[1,2,3] triazolo[4,5-g]phthalazine-4,9-dione
0.049
-
 in 50 mM Tris-HCl, pH 8, 120 mM KCl, 10 mM MgCl2, 0.5 mM ATP, 0.5 mM dithiothreitol, 0.03 mg/ml bovine serum albumin, at 37°C Homo sapiens 1-n-propyl-1H-[1,2,3]triazolo[4,5-g]phthalazine-4,9-dione
0.0528
-
 in 50 mM Tris-HCl, pH 8, 120 mM KCl, 10 mM MgCl2, 0.5 mM ATP, 0.5 mM dithiothreitol, 0.03 mg/ml bovine serum albumin, at 37°C Homo sapiens 1H-[1,2,3]triazolo[4,5,-g]phthalazine-4,9-dione
0.0545
-
 in 50 mM Tris-HCl, pH 8, 120 mM KCl, 10 mM MgCl2, 0.5 mM ATP, 0.5 mM dithiothreitol, 0.03 mg/ml bovine serum albumin, at 37°C Homo sapiens 2-iso-propyl-2H-[1,2,3]triazolo[4,5-g]phthalazine-4,9-dione
0.0556
-
 in 50 mM Tris-HCl, pH 8, 120 mM KCl, 10 mM MgCl2, 0.5 mM ATP, 0.5 mM dithiothreitol, 0.03 mg/ml bovine serum albumin, at 37°C Homo sapiens 2-methyl-2H-[1,2,3]triazolo[4,5-g]phthalazine-4,9-dione
0.0556
-
 in 50 mM Tris-HCl, pH 8, 120 mM KCl, 10 mM MgCl2, 0.5 mM ATP, 0.5 mM dithiothreitol, 0.03 mg/ml bovine serum albumin, at 37°C Homo sapiens 1-ethyl-1H-[1,2,3]triazolo[4,5-g]phthalazine-4,9-dione
0.0615
-
 in 50 mM Tris-HCl, pH 8, 120 mM KCl, 10 mM MgCl2, 0.5 mM ATP, 0.5 mM dithiothreitol, 0.03 mg/ml bovine serum albumin, at 37°C Homo sapiens 2-ethyl-2H-[1,2,3]triazolo[4,5-g]phthalazine-4,9-dione
0.0648
-
 in 50 mM Tris-HCl, pH 8, 120 mM KCl, 10 mM MgCl2, 0.5 mM ATP, 0.5 mM dithiothreitol, 0.03 mg/ml bovine serum albumin, at 37°C Homo sapiens 2-n-butyl-2H-[1,2,3] triazolo[4,5-g]phthalazine-4,9-dione
0.0929
-
 in 50 mM Tris-HCl, pH 8, 120 mM KCl, 10 mM MgCl2, 0.5 mM ATP, 0.5 mM dithiothreitol, 0.03 mg/ml bovine serum albumin, at 37°C Homo sapiens etoposide