Target Validation Information
Target ID T28661
Target Name Tubulin beta-2 chain
Target Type
Successful
Drug Potency against Target 6-ile-ustiloxin Drug Info IC50 = 4800 nM [528306]
Ustiloxin F Drug Info IC50 = 8200 nM [528306]
DOLASTATIN-10 Drug Info IC50 = 0.5 nM [528306]
2,3'-diamino-3,4,4',5-tetramethoxy-(Z)-stillbene Drug Info IC50 = 1800 nM [528474]
3-bromo-4,4',5-trimethoxy-(Z)-stilbene Drug Info IC50 = 2100 nM [528474]
USTILOXIN A Drug Info IC50 = 1100 nM [528306]
Ustiloxin D Drug Info IC50 = 1500 nM [528306]
2-amino-3,4',5-trimethoxy-(Z)-stillbene Drug Info IC50 = 2400 nM [528474]
3,4',5-trimethoxy-(Z)-stilbene Drug Info IC50 = 3500 nM [528474]
2'-amino-3,4,4',5-tetramethoxy-(Z)-stillbene Drug Info IC50 = 1600 nM [528474]
3,4,4',5-tetramethoxy-(Z)-stilbene Drug Info IC50 = 1500 nM [528474]
Vinblastine Drug Info Ki = 0.178+/-0.025 microM [553149]
N-(4-(3-(pyridin-2-yl)acryloyl)phenyl)acetamide Drug Info IC50 = 15700 nM [528428]
References
Ref 528306Bioorg Med Chem Lett. 2006 Sep 15;16(18):4804-7. Epub 2006 Jul 11.Total synthesis and biological evaluation of ustiloxin natural products and two analogs.
Ref 528306Bioorg Med Chem Lett. 2006 Sep 15;16(18):4804-7. Epub 2006 Jul 11.Total synthesis and biological evaluation of ustiloxin natural products and two analogs.
Ref 528306Bioorg Med Chem Lett. 2006 Sep 15;16(18):4804-7. Epub 2006 Jul 11.Total synthesis and biological evaluation of ustiloxin natural products and two analogs.
Ref 528474J Med Chem. 2006 Oct 19;49(21):6412-5.2-amino and 2'-aminocombretastatin derivatives as potent antimitotic agents.
Ref 528474J Med Chem. 2006 Oct 19;49(21):6412-5.2-amino and 2'-aminocombretastatin derivatives as potent antimitotic agents.
Ref 528306Bioorg Med Chem Lett. 2006 Sep 15;16(18):4804-7. Epub 2006 Jul 11.Total synthesis and biological evaluation of ustiloxin natural products and two analogs.
Ref 528306Bioorg Med Chem Lett. 2006 Sep 15;16(18):4804-7. Epub 2006 Jul 11.Total synthesis and biological evaluation of ustiloxin natural products and two analogs.
Ref 528474J Med Chem. 2006 Oct 19;49(21):6412-5.2-amino and 2'-aminocombretastatin derivatives as potent antimitotic agents.
Ref 528474J Med Chem. 2006 Oct 19;49(21):6412-5.2-amino and 2'-aminocombretastatin derivatives as potent antimitotic agents.
Ref 528474J Med Chem. 2006 Oct 19;49(21):6412-5.2-amino and 2'-aminocombretastatin derivatives as potent antimitotic agents.
Ref 528474J Med Chem. 2006 Oct 19;49(21):6412-5.2-amino and 2'-aminocombretastatin derivatives as potent antimitotic agents.
Ref 553149Comparison of the effects of vinblastine, vincristine, vindesine, and vinepidine on microtubule dynamics and cell proliferation in vitro. Cancer Res. 1985 Jun;45(6):2741-7.
Ref 528428J Med Chem. 2006 Sep 21;49(19):5664-70.Design and biological evaluation of novel tubulin inhibitors as antimitotic agents using a pharmacophore binding model with tubulin.

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