Target Validation Information
Target ID T68536
Target Name Tubulin beta
Target Type
Successful
Drug Potency against Target 5-Methyl-2-m-tolyl-1H-[1,8]naphthyridin-4-one Drug Info IC50 = 1800 nM [534469]
Vindesine Drug Info Ki = 0.110+/-0.007 microM [553149]
Ustiloxin D Drug Info IC50 = 1500 nM [528306]
USTILOXIN A Drug Info IC50 = 1100 nM [528306]
DOLASTATIN-10 Drug Info IC50 = 0.5 nM [528306]
3,4',5-trimethoxy-(Z)-stilbene Drug Info IC50 = 3500 nM [528474]
3,4,4',5-tetramethoxy-(Z)-stilbene Drug Info IC50 = 1500 nM [528474]
2'-amino-3,4,4',5-tetramethoxy-(Z)-stillbene Drug Info IC50 = 1600 nM [528474]
N-(4-(3-(pyridin-2-yl)acryloyl)phenyl)acetamide Drug Info IC50 = 15700 nM [528428]
2-Methoxy-5-(5,6,7-trimethoxy-indan-1-yl)-phenol Drug Info IC50 = 10900 nM [525450]
2-Naphthalen-2-yl-1H-[1,8]naphthyridin-4-one Drug Info IC50 = 14000 nM [534469]
NSC-679036 Drug Info IC50 = 720 nM [534469]
6-Methyl-2-m-tolyl-1H-[1,8]naphthyridin-4-one Drug Info IC50 = 1500 nM [534469]
2-Naphthalen-1-yl-1H-[1,8]naphthyridin-4-one Drug Info IC50 = 1100 nM [534469]
2-(3-Chloro-phenyl)-1H-[1,8]naphthyridin-4-one Drug Info IC50 = 1500 nM [534469]
MR-22388 Drug Info IC50 = 2400 nM [526982]
2-(4-Methoxy-phenyl)-1H-indole-3-carbaldehyde Drug Info IC50 = 3300 nM [534765]
MYOSEVERIN Drug Info IC50 = 8000 nM [526222]
2-Furan-2-yl-7-methyl-1H-[1,8]naphthyridin-4-one Drug Info IC50 = 14000 nM [525604]
COLCHINOL Drug Info Ki = 1850 nM [527777]
2-Methoxy-5-(3,4,5-trimethoxy-benzyl)-phenol Drug Info IC50 = 7700 nM [527276]
ABT-751 Drug Info IC50 = 2200 nM [526440]
COMBETASTATIN Drug Info IC50 = 4000 nM [534795]
Ustiloxin F Drug Info IC50 = 8200 nM [528306]
6-ile-ustiloxin Drug Info IC50 = 4800 nM [528306]
3-bromo-4,4',5-trimethoxy-(Z)-stilbene Drug Info IC50 = 2100 nM [528474]
2-Methoxy-5-(3,4,5-trimethoxy-phenoxy)-phenol Drug Info IC50 = 16300 nM [525946]
7-Methyl-2-m-tolyl-1H-[1,8]naphthyridin-4-one Drug Info IC50 = 1900 nM [534469]
2-amino-3,4',5-trimethoxy-(Z)-stillbene Drug Info IC50 = 2400 nM [528474]
2,3'-diamino-3,4,4',5-tetramethoxy-(Z)-stillbene Drug Info IC50 = 1800 nM [528474]
5,7-Dimethyl-2-m-tolyl-1H-[1,8]naphthyridin-4-one Drug Info IC50 = 2300 nM [534469]
2-m-Tolyl-1H-[1,8]naphthyridin-4-one Drug Info IC50 = 3300 nM [534469]
Isopropyl 3-(phenylthio)-1H-indole-2-carboxylate Drug Info IC50 = 18000 nM [527999]
References
Ref 534469J Med Chem. 1997 Sep 12;40(19):3049-56.Antitumor agents. 178. Synthesis and biological evaluation of substituted 2-aryl-1,8-naphthyridin-4(1H)-ones as antitumor agents that inhibit tubulin polymerization.
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 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 528474J Med Chem. 2006 Oct 19;49(21):6412-5.2-amino and 2'-aminocombretastatin derivatives as potent antimitotic agents.
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.
Ref 525450Bioorg Med Chem Lett. 1999 Feb 8;9(3):407-12.The synthesis and evaluation of temperature sensitive tubulin toxins.
Ref 534469J Med Chem. 1997 Sep 12;40(19):3049-56.Antitumor agents. 178. Synthesis and biological evaluation of substituted 2-aryl-1,8-naphthyridin-4(1H)-ones as antitumor agents that inhibit tubulin polymerization.
Ref 534469J Med Chem. 1997 Sep 12;40(19):3049-56.Antitumor agents. 178. Synthesis and biological evaluation of substituted 2-aryl-1,8-naphthyridin-4(1H)-ones as antitumor agents that inhibit tubulin polymerization.
Ref 534469J Med Chem. 1997 Sep 12;40(19):3049-56.Antitumor agents. 178. Synthesis and biological evaluation of substituted 2-aryl-1,8-naphthyridin-4(1H)-ones as antitumor agents that inhibit tubulin polymerization.
Ref 534469J Med Chem. 1997 Sep 12;40(19):3049-56.Antitumor agents. 178. Synthesis and biological evaluation of substituted 2-aryl-1,8-naphthyridin-4(1H)-ones as antitumor agents that inhibit tubulin polymerization.
Ref 534469J Med Chem. 1997 Sep 12;40(19):3049-56.Antitumor agents. 178. Synthesis and biological evaluation of substituted 2-aryl-1,8-naphthyridin-4(1H)-ones as antitumor agents that inhibit tubulin polymerization.
Ref 526982J Med Chem. 2004 Mar 11;47(6):1448-64.Design, synthesis, and evaluation of novel thienopyrrolizinones as antitubulin agents.
Ref 534765J Med Chem. 1998 Dec 3;41(25):4965-72.Methoxy-substituted 3-formyl-2-phenylindoles inhibit tubulin polymerization.
Ref 526222J Med Chem. 2001 Dec 20;44(26):4497-500.Synthesis and biological evaluation of myoseverin derivatives: microtubule assembly inhibitors.
Ref 525604J Med Chem. 1999 Oct 7;42(20):4081-7.Antitumor agents. 196. Substituted 2-thienyl-1,8-naphthyridin-4-ones: their synthesis, cytotoxicity, and inhibition of tubulin polymerization.
Ref 527777Bioorg Med Chem Lett. 2005 Dec 1;15(23):5154-9. Epub 2005 Sep 28.Synthesis and structure-activity relationships of 1,2,4-triazoles as a novel class of potent tubulin polymerization inhibitors.
Ref 527276J Med Chem. 1992 Mar 20;35(6):1058-67.Synthesis of alkoxy-substituted diaryl compounds and correlation of ring separation with inhibition of tubulin polymerization: differential enhancement of inhibitory effects under suboptimal polymerization reaction conditions.
Ref 526440J Med Chem. 2002 Oct 24;45(22):4913-22.Array-based structure and gene expression relationship study of antitumor sulfonamides including N-[2-[(4-hydroxyphenyl)amino]-3-pyridinyl]-4-methoxybenzenesulfonamide and N-(3-chloro-7-indolyl)-1,4-benzenedisulfonamide.
Ref 534795Bioorg Med Chem Lett. 1998 Aug 4;8(15):1997-2000.Asymmetric synthesis of antimitotic combretadioxolane with potent antitumor activity against multi-drug resistant cells.
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 525946Bioorg Med Chem Lett. 2001 Jan 8;11(1):51-4.Antimitotic and cell growth inhibitory properties of combretastatin A-4-like ethers.
Ref 534469J Med Chem. 1997 Sep 12;40(19):3049-56.Antitumor agents. 178. Synthesis and biological evaluation of substituted 2-aryl-1,8-naphthyridin-4(1H)-ones as antitumor agents that inhibit tubulin polymerization.
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 534469J Med Chem. 1997 Sep 12;40(19):3049-56.Antitumor agents. 178. Synthesis and biological evaluation of substituted 2-aryl-1,8-naphthyridin-4(1H)-ones as antitumor agents that inhibit tubulin polymerization.
Ref 534469J Med Chem. 1997 Sep 12;40(19):3049-56.Antitumor agents. 178. Synthesis and biological evaluation of substituted 2-aryl-1,8-naphthyridin-4(1H)-ones as antitumor agents that inhibit tubulin polymerization.
Ref 527999J Med Chem. 2006 Feb 9;49(3):947-54.New arylthioindoles: potent inhibitors of tubulin polymerization. 2. Structure-activity relationships and molecular modeling studies.

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