Target Validation Information
Target ID T27325
Target Name DNA topoisomerase I
Target Type
Successful
Drug Potency against Target 4-hydroxysaprothoquinone Drug Info IC50 = 800 nM [526391]
CHO793076 Drug Info IC50 = 2300 nM [529993]
(5Z,9Z)-5,9-heptacosadienoic acid Drug Info IC50 = 900 nM [526463]
TOPOSTATIN Drug Info IC50 = 17000 nM [526096]
Topotecan Drug Info IC50 = 300 nM
References
Ref 526391J Nat Prod. 2002 Jul;65(7):1016-20.Bioactive abietane and seco-abietane diterpenoids from Salvia prionitis.
Ref 529993Bioorg Med Chem Lett. 2009 Apr 1;19(7):2018-21. Epub 2009 Feb 12.Synthesis of new camptothecin analogs with improved antitumor activities.
Ref 526463J Nat Prod. 2002 Nov;65(11):1715-8.Total synthesis and biological evaluation of (5Z,9Z)-5,9-hexadecadienoic acid, an inhibitor of human topoisomerase I.
Ref 526096J Nat Prod. 2001 Feb;64(2):204-7.Isoaurostatin, a novel topoisomerase inhibitor produced by Thermomonospora alba.

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