| Target Validation Information | |||||
|---|---|---|---|---|---|
| TTD ID | T68536 | ||||
| Target Name | Tubulin beta (TUBB) | ||||
| Type of Target |
Successful |
||||
| Drug Potency against Target | Vindesine | Drug Info | Ki = 0.110+/-0.007 microM | [16] | |
| 2'-amino-3,4,4',5-tetramethoxy-(Z)-stillbene | Drug Info | IC50 = 1600 nM | [12] | ||
| 2,3'-diamino-3,4,4',5-tetramethoxy-(Z)-stillbene | Drug Info | IC50 = 1800 nM | [12] | ||
| 2-(3-Chloro-phenyl)-1H-[1,8]naphthyridin-4-one | Drug Info | IC50 = 1500 nM | [13] | ||
| 2-(4-Methoxy-phenyl)-1H-indole-3-carbaldehyde | Drug Info | IC50 = 3300 nM | [14] | ||
| 2-amino-3,4',5-trimethoxy-(Z)-stillbene | Drug Info | IC50 = 2400 nM | [12] | ||
| 2-Furan-2-yl-7-methyl-1H-[1,8]naphthyridin-4-one | Drug Info | IC50 = 14000 nM | [2] | ||
| 2-m-Tolyl-1H-[1,8]naphthyridin-4-one | Drug Info | IC50 = 3300 nM | [13] | ||
| 2-Methoxy-5-(3,4,5-trimethoxy-benzyl)-phenol | Drug Info | IC50 = 7700 nM | [7] | ||
| 2-Methoxy-5-(3,4,5-trimethoxy-phenoxy)-phenol | Drug Info | IC50 = 16300 nM | [3] | ||
| 2-Methoxy-5-(5,6,7-trimethoxy-indan-1-yl)-phenol | Drug Info | IC50 = 10900 nM | [1] | ||
| 2-Naphthalen-1-yl-1H-[1,8]naphthyridin-4-one | Drug Info | IC50 = 1100 nM | [13] | ||
| 2-Naphthalen-2-yl-1H-[1,8]naphthyridin-4-one | Drug Info | IC50 = 14000 nM | [13] | ||
| 3,4',5-trimethoxy-(Z)-stilbene | Drug Info | IC50 = 3500 nM | [12] | ||
| 3,4,4',5-tetramethoxy-(Z)-stilbene | Drug Info | IC50 = 1500 nM | [12] | ||
| 3-bromo-4,4',5-trimethoxy-(Z)-stilbene | Drug Info | IC50 = 2100 nM | [12] | ||
| 5,7-Dimethyl-2-m-tolyl-1H-[1,8]naphthyridin-4-one | Drug Info | IC50 = 2300 nM | [13] | ||
| 5-Methyl-2-m-tolyl-1H-[1,8]naphthyridin-4-one | Drug Info | IC50 = 1800 nM | [13] | ||
| 6-ile-ustiloxin | Drug Info | IC50 = 4800 nM | [10] | ||
| 6-Methyl-2-m-tolyl-1H-[1,8]naphthyridin-4-one | Drug Info | IC50 = 1500 nM | [13] | ||
| 7-Methyl-2-m-tolyl-1H-[1,8]naphthyridin-4-one | Drug Info | IC50 = 1900 nM | [13] | ||
| ABT-751 | Drug Info | IC50 = 2200 nM | [5] | ||
| COLCHINOL | Drug Info | Ki = 1850 nM | [8] | ||
| COMBETASTATIN | Drug Info | IC50 = 4000 nM | [15] | ||
| DOLASTATIN-10 | Drug Info | IC50 = 0.5 nM | [10] | ||
| Isopropyl 3-(phenylthio)-1H-indole-2-carboxylate | Drug Info | IC50 = 18000 nM | [9] | ||
| MR-22388 | Drug Info | IC50 = 2400 nM | [6] | ||
| MYOSEVERIN | Drug Info | IC50 = 8000 nM | [4] | ||
| N-(4-(3-(pyridin-2-yl)acryloyl)phenyl)acetamide | Drug Info | IC50 = 15700 nM | [11] | ||
| NSC-679036 | Drug Info | IC50 = 720 nM | [13] | ||
| USTILOXIN A | Drug Info | IC50 = 1100 nM | [10] | ||
| Ustiloxin D | Drug Info | IC50 = 1500 nM | [10] | ||
| Ustiloxin F | Drug Info | IC50 = 8200 nM | [10] | ||
| References | |||||
| REF 1 | The synthesis and evaluation of temperature sensitive tubulin toxins. Bioorg Med Chem Lett. 1999 Feb 8;9(3):407-12. | ||||
| REF 2 | Antitumor agents. 196. Substituted 2-thienyl-1,8-naphthyridin-4-ones: their synthesis, cytotoxicity, and inhibition of tubulin polymerization. J Med Chem. 1999 Oct 7;42(20):4081-7. | ||||
| REF 3 | Antimitotic and cell growth inhibitory properties of combretastatin A-4-like ethers. Bioorg Med Chem Lett. 2001 Jan 8;11(1):51-4. | ||||
| REF 4 | Synthesis and biological evaluation of myoseverin derivatives: microtubule assembly inhibitors. J Med Chem. 2001 Dec 20;44(26):4497-500. | ||||
| REF 5 | Array-based structure and gene expression relationship study of antitumor sulfonamides including N-[2-[(4-hydroxyphenyl)amino]-3-pyridinyl]-4-metho... J Med Chem. 2002 Oct 24;45(22):4913-22. | ||||
| REF 6 | Design, synthesis, and evaluation of novel thienopyrrolizinones as antitubulin agents. J Med Chem. 2004 Mar 11;47(6):1448-64. | ||||
| REF 7 | Synthesis of alkoxy-substituted diaryl compounds and correlation of ring separation with inhibition of tubulin polymerization: differential enhance... J Med Chem. 1992 Mar 20;35(6):1058-67. | ||||
| REF 8 | Synthesis and structure-activity relationships of 1,2,4-triazoles as a novel class of potent tubulin polymerization inhibitors. Bioorg Med Chem Lett. 2005 Dec 1;15(23):5154-9. | ||||
| REF 9 | New arylthioindoles: potent inhibitors of tubulin polymerization. 2. Structure-activity relationships and molecular modeling studies. J Med Chem. 2006 Feb 9;49(3):947-54. | ||||
| REF 10 | Total synthesis and biological evaluation of ustiloxin natural products and two analogs. Bioorg Med Chem Lett. 2006 Sep 15;16(18):4804-7. | ||||
| REF 11 | 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 12 | 2-amino and 2'-aminocombretastatin derivatives as potent antimitotic agents. J Med Chem. 2006 Oct 19;49(21):6412-5. | ||||
| REF 13 | Antitumor agents. 178. Synthesis and biological evaluation of substituted 2-aryl-1,8-naphthyridin-4(1H)-ones as antitumor agents that inhibit tubul... J Med Chem. 1997 Sep 12;40(19):3049-56. | ||||
| REF 14 | Methoxy-substituted 3-formyl-2-phenylindoles inhibit tubulin polymerization. J Med Chem. 1998 Dec 3;41(25):4965-72. | ||||
| REF 15 | Asymmetric synthesis of antimitotic combretadioxolane with potent antitumor activity against multi-drug resistant cells. Bioorg Med Chem Lett. 1998 Aug 4;8(15):1997-2000. | ||||
| REF 16 | 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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