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]
Drug Info IC50 = 1600 nM [12]
Drug Info IC50 = 15700 nM [11]
Drug Info IC50 = 14000 nM [2]
Drug Info Ki = 1850 nM [8]
Drug Info IC50 = 1900 nM [13]
Drug Info IC50 = 2400 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-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]
ABT-751 Drug Info IC50 = 2200 nM [5]
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]
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.

If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.