Target Validation Information
Target ID T43189
Target Name Tubulin
Target Type
Successful
Drug Potency against Target MYOSEVERIN Drug Info IC50 = 8000 nM [526222]
ABT-751 Drug Info IC50 = 2200 nM [526440]
2-Naphthalen-1-yl-1H-[1,8]naphthyridin-4-one Drug Info IC50 = 1100 nM [534469]
2-Methoxy-5-(5,6,7-trimethoxy-indan-1-yl)-phenol Drug Info IC50 = 10900 nM [525450]
DOLASTATIN-10 Drug Info IC50 = 2200 nM [534612]
Fosbretabulin Drug Info IC50 = 1700 nM [528267]
NSC-679036 Drug Info IC50 = 720 nM [534469]
2-(3-Chloro-phenyl)-1H-[1,8]naphthyridin-4-one Drug Info IC50 = 1500 nM [534469]
2-m-Tolyl-1H-[1,8]naphthyridin-4-one Drug Info IC50 = 3300 nM [534469]
6-Methyl-2-m-tolyl-1H-[1,8]naphthyridin-4-one Drug Info IC50 = 1500 nM [534469]
MR-22388 Drug Info IC50 = 2400 nM [526982]
COMBETASTATIN Drug Info IC50 = 4000 nM [534795]
2-(4-Methoxy-phenyl)-1H-indole-3-carbaldehyde Drug Info IC50 = 3300 nM [534765]
2-Furan-2-yl-7-methyl-1H-[1,8]naphthyridin-4-one Drug Info IC50 = 14000 nM [525604]
7-Methyl-2-m-tolyl-1H-[1,8]naphthyridin-4-one Drug Info IC50 = 1900 nM [534469]
Isopropyl 3-(phenylthio)-1H-indole-2-carboxylate Drug Info IC50 = 18000 nM [527999]
COLCHINOL Drug Info Ki = 1850 nM [527777]
2-Methoxy-5-(3,4,5-trimethoxy-benzyl)-phenol Drug Info IC50 = 7700 nM [527276]
5,7-Dimethyl-2-m-tolyl-1H-[1,8]naphthyridin-4-one Drug Info IC50 = 2300 nM [534469]
2-Naphthalen-2-yl-1H-[1,8]naphthyridin-4-one Drug Info IC50 = 14000 nM [534469]
5-Methyl-2-m-tolyl-1H-[1,8]naphthyridin-4-one Drug Info IC50 = 1800 nM [534469]
2-Methoxy-5-(3,4,5-trimethoxy-phenoxy)-phenol Drug Info IC50 = 16300 nM [525946]
References
Ref 526222J Med Chem. 2001 Dec 20;44(26):4497-500.Synthesis and biological evaluation of myoseverin derivatives: microtubule assembly inhibitors.
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 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 525450Bioorg Med Chem Lett. 1999 Feb 8;9(3):407-12.The synthesis and evaluation of temperature sensitive tubulin toxins.
Ref 534612J Med Chem. 1998 Apr 23;41(9):1524-30.Synthesis and biological activity of chimeric structures derived from the cytotoxic natural compounds dolastatin 10 and dolastatin 15.
Ref 528267J Med Chem. 2006 Jun 29;49(13):3906-15.Synthesis and biological evaluation of 2-amino-3-(3',4',5'-trimethoxybenzoyl)-5-aryl thiophenes as a new class of potent antitubulin 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 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 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 534765J Med Chem. 1998 Dec 3;41(25):4965-72.Methoxy-substituted 3-formyl-2-phenylindoles inhibit tubulin polymerization.
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 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.
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 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 525946Bioorg Med Chem Lett. 2001 Jan 8;11(1):51-4.Antimitotic and cell growth inhibitory properties of combretastatin A-4-like ethers.

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