| Target Validation Information | |||||
|---|---|---|---|---|---|
| Target ID | T24587 | ||||
| Target Name | Methylated-DNA--protein-cysteine methyltransferase | ||||
| Target Type | Clinical Trial |
||||
| Drug Potency against Target | 6-Allyloxy-9H-purin-2-ylamine | Drug Info | IC50 = 5100 nM | [525899] | |
| 6-Benzyloxy-5-nitroso-pyrimidine-2,4-diamine | Drug Info | IC50 = 130 nM | [534565] | ||
| 6-Benzyloxy-9H-purin-2-ylamine | Drug Info | IC50 = 2600 nM | [534565] | ||
| 6-Benzyloxy-5-nitro-pyrimidine-2,4-diamine | Drug Info | IC50 = 1300 nM | [534565] | ||
| References | |||||
| Ref 525899 | J Med Chem. 2000 Nov 2;43(22):4071-83.Resistance-modifying agents. 8. Inhibition of O(6)-alkylguanine-DNA alkyltransferase by O(6)-alkenyl-, O(6)-cycloalkenyl-, and O(6)-(2-oxoalkyl)guanines and potentiation of temozolomide cytotoxicity in vitro by O(6)-(1-cyclopentenylmethyl)guanine. | ||||
| Ref 534565 | J Med Chem. 1998 Feb 12;41(4):503-8.Inhibition of human O6-alkylguanine-DNA alkyltransferase and potentiation of the cytotoxicity of chloroethylnitrosourea by 4(6)-(benzyloxy)-2,6(4)-diamino-5-(nitroor nitroso)pyrimidine derivatives and analogues. | ||||
| Ref 534565 | J Med Chem. 1998 Feb 12;41(4):503-8.Inhibition of human O6-alkylguanine-DNA alkyltransferase and potentiation of the cytotoxicity of chloroethylnitrosourea by 4(6)-(benzyloxy)-2,6(4)-diamino-5-(nitroor nitroso)pyrimidine derivatives and analogues. | ||||
| Ref 534565 | J Med Chem. 1998 Feb 12;41(4):503-8.Inhibition of human O6-alkylguanine-DNA alkyltransferase and potentiation of the cytotoxicity of chloroethylnitrosourea by 4(6)-(benzyloxy)-2,6(4)-diamino-5-(nitroor nitroso)pyrimidine derivatives and analogues. | ||||
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