Target Validation Information | |||||
---|---|---|---|---|---|
TTD ID | T28661 | ||||
Target Name | Tubulin beta-2 chain (TUBB2) | ||||
Type of Target |
Successful |
||||
Drug Potency against Target | Vinblastine | Drug Info | Ki = 0.178+/-0.025 microM | [4] | |
2'-amino-3,4,4',5-tetramethoxy-(Z)-stillbene | Drug Info | IC50 = 1600 nM | [3] | ||
2,3'-diamino-3,4,4',5-tetramethoxy-(Z)-stillbene | Drug Info | IC50 = 1800 nM | [3] | ||
2-amino-3,4',5-trimethoxy-(Z)-stillbene | Drug Info | IC50 = 2400 nM | [3] | ||
3,4',5-trimethoxy-(Z)-stilbene | Drug Info | IC50 = 3500 nM | [3] | ||
3,4,4',5-tetramethoxy-(Z)-stilbene | Drug Info | IC50 = 1500 nM | [3] | ||
3-bromo-4,4',5-trimethoxy-(Z)-stilbene | Drug Info | IC50 = 2100 nM | [3] | ||
6-ile-ustiloxin | Drug Info | IC50 = 4800 nM | [1] | ||
DOLASTATIN-10 | Drug Info | IC50 = 0.5 nM | [1] | ||
N-(4-(3-(pyridin-2-yl)acryloyl)phenyl)acetamide | Drug Info | IC50 = 15700 nM | [2] | ||
USTILOXIN A | Drug Info | IC50 = 1100 nM | [1] | ||
Ustiloxin D | Drug Info | IC50 = 1500 nM | [1] | ||
Ustiloxin F | Drug Info | IC50 = 8200 nM | [1] | ||
References | |||||
REF 1 | Total synthesis and biological evaluation of ustiloxin natural products and two analogs. Bioorg Med Chem Lett. 2006 Sep 15;16(18):4804-7. | ||||
REF 2 | Design and biological evaluation of novel tubulin inhibitors as antimitotic agents using a pharmacophore binding model with tubulin. J Med Chem. 2006 Sep 21;49(19):5664-70. | ||||
REF 3 | 2-amino and 2'-aminocombretastatin derivatives as potent antimitotic agents. J Med Chem. 2006 Oct 19;49(21):6412-5. | ||||
REF 4 | Comparison 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. | ||||
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