Target Validation Information
TTD ID T75498
Target Name Quinone reductase 2 (NQO2)
Type of Target
Successful
Drug Potency against Target 1,4-Dimethylquinolin-2(1H)-one Drug Info IC50 = 18200 nM [1]
2-iodo-melatonin Drug Info IC50 = 1100 nM [1]
3,4,5-Trimethoxy-4'-amino-trans-stilbene Drug Info IC50 = 270 nM
3,5-Dimethoxy-4'-amino-trans-stilbene Drug Info IC50 = 1700 nM
5,6,8-Trimethoxy-1,4-dimethylquinolin-2(1H)-one Drug Info IC50 = 10800 nM [1]
5,6,8-Trimethoxy-4-methylquinolin-2(1H)-one Drug Info IC50 = 6000 nM [1]
5,8-Dimethoxy-4-methylquinolin-2(1H)-one Drug Info IC50 = 10800 nM [1]
6,7,8-Trimethoxy-1,4-dimethylquinolin-2(1H)-one Drug Info IC50 = 7000 nM [1]
6,7,8-Trimethoxy-4-methylquinolin-2(1H)-one Drug Info IC50 = 10000 nM [1]
6,8-Dimethoxy-1,4-dimethylquinolin-2(1H)-one Drug Info IC50 = 1900 nM [1]
6,8-Dimethoxy-4-methylquinolin-2(1H)-one Drug Info IC50 = 8800 nM [1]
6-Methyl-[1,3]dioxolo[4,5-h]quinolin-8(9H)-one Drug Info IC50 = 10800 nM [1]
7,8-Dimethoxy-1,4-dimethylquinolin-2(1H)-one Drug Info IC50 = 9300 nM [1]
8-Methoxy-1,4-dimethylquinolin-2(1H)-one Drug Info IC50 = 5800 nM [1]
decynium 22 Drug Info IC50 = 2700 nM [3]
NSC-106080 Drug Info IC50 = 3900 nM [3]
NSC-115890 Drug Info IC50 = 3300 nM [3]
NSC-180969 Drug Info IC50 = 2000 nM [3]
NSC-204996 Drug Info IC50 = 2700 nM [3]
NSC-238146 Drug Info IC50 = 1900 nM [3]
NSC-300853 Drug Info IC50 = 5000 nM [3]
NSC-306843 Drug Info IC50 = 6200 nM [3]
NSC-356819 Drug Info IC50 = 1800 nM [3]
NSC-356820 Drug Info IC50 = 1400 nM [3]
NSC-359466 Drug Info IC50 = 6000 nM [3]
NSC-381864 Drug Info IC50 = 15000 nM [3]
NSC-637991 Drug Info IC50 = 50 nM [2]
NSC-637992 Drug Info IC50 = 16 nM [2]
NSC-637993 Drug Info IC50 = 9 nM [2]
NSC-637994 Drug Info IC50 = 597 nM [2]
NSC-640353 Drug Info IC50 = 3800 nM [3]
NSC-640556 Drug Info IC50 = 6000 nM [3]
NSC-640558 Drug Info IC50 = 5800 nM [3]
NSC-640559 Drug Info IC50 = 6500 nM [3]
NSC-640566 Drug Info IC50 = 5300 nM [3]
NSC-640583 Drug Info IC50 = 3200 nM [3]
NSC-640584 Drug Info IC50 = 4900 nM [3]
NSC-645808 Drug Info IC50 = 296 nM [2]
NSC-645809 Drug Info IC50 = 148 nM [2]
NSC-645811 Drug Info IC50 = 953 nM [2]
NSC-645812 Drug Info IC50 = 1000 nM [2]
NSC-645831 Drug Info IC50 = 427 nM [2]
NSC-645833 Drug Info IC50 = 830 nM [2]
NSC-645834 Drug Info IC50 = 323 nM [2]
NSC-645835 Drug Info IC50 = 693 nM [2]
NSC-645836 Drug Info IC50 = 172 nM [2]
NSC-649091 Drug Info IC50 = 3500 nM [3]
NSC-660838 Drug Info IC50 = 99 nM [2]
NSC-660839 Drug Info IC50 = 17 nM [2]
NSC-660840 Drug Info IC50 = 31 nM [2]
NSC-660841 Drug Info IC50 = 6 nM [2]
NSC-665126 Drug Info IC50 = 9600 nM [3]
NSC-669977 Drug Info IC50 = 2000 nM [3]
NSC-676468 Drug Info IC50 = 9700 nM [3]
NSC-677939 Drug Info IC50 = 2900 nM [3]
NSC-693571 Drug Info IC50 = 1700 nM [3]
NSC-720622 Drug Info IC50 = 5000 nM [3]
NSC-77833 Drug Info IC50 = 1800 nM [3]
NSC-78017 Drug Info IC50 = 2100 nM [3]
NSC-78021 Drug Info IC50 = 5500 nM [3]
NSC-86715 Drug Info IC50 = 2100 nM [3]
NSC-99495 Drug Info IC50 = 5100 nM [3]
NSC-99528 Drug Info IC50 = 6000 nM [3]
Action against Disease Model Prolarix Drug Info The prodrug CB1954 (5-(aziridin-1-yl)-2,4-dinitrobenzamide) is activated by Escherichia coli nitroreductase (NTR) to a potent DNA-crosslinking agent. Virus-mediated expression of NTR in t uMour cells sensitizes them to CB1954 in vitro and in vivo, providing the basis for a strategy of cancer gene therapy. An oncolytic (replication-competent) adenovirus vector allowed increased expression of NTR in vitro and in a mouse t uMour model, resulting in a greater reduction in t uMour growth when combined with CB1954 treatment [4]
References
REF 1 Synthesis of casimiroin and optimization of its quinone reductase 2 and aromatase inhibitory activities. J Med Chem. 2009 Apr 9;52(7):1873-84.
REF 2 Imidazoacridin-6-ones as novel inhibitors of the quinone oxidoreductase NQO2. Bioorg Med Chem Lett. 2010 May 1;20(9):2832-6.
REF 3 In silico identification and biochemical evaluation of novel inhibitors of NRH:quinone oxidoreductase 2 (NQO2). Bioorg Med Chem Lett. 2010 Dec 15;20(24):7331-6.
REF 4 Nitroreductase: a prodrug-activating enzyme for cancer gene therapy. Clin Exp Pharmacol Physiol. 2004 Nov;31(11):811-6.

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