Target Validation Information | |||||
---|---|---|---|---|---|
TTD ID | T24587 | ||||
Target Name | O-6-methylguanine-DNA-alkyltransferase (MGMT) | ||||
Type of Target |
Clinical trial |
||||
Drug Potency against Target | 6-Allyloxy-9H-purin-2-ylamine | Drug Info | IC50 = 5100 nM | [1] | |
6-Benzyloxy-5-nitro-pyrimidine-2,4-diamine | Drug Info | IC50 = 1300 nM | [2] | ||
6-Benzyloxy-5-nitroso-pyrimidine-2,4-diamine | Drug Info | IC50 = 130 nM | [2] | ||
6-Benzyloxy-9H-purin-2-ylamine | Drug Info | IC50 = 2600 nM | [2] | ||
References | |||||
REF 1 | Resistance-modifying agents. 8. Inhibition of O(6)-alkylguanine-DNA alkyltransferase by O(6)-alkenyl-, O(6)-cycloalkenyl-, and O(6)-(2-oxoalkyl)gua... J Med Chem. 2000 Nov 2;43(22):4071-83. | ||||
REF 2 | Inhibition of human O6-alkylguanine-DNA alkyltransferase and potentiation of the cytotoxicity of chloroethylnitrosourea by 4(6)-(benzyloxy)-2,6(4)-... J Med Chem. 1998 Feb 12;41(4):503-8. | ||||
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