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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