Target Validation Information
TTD ID T43189
Target Name Tubulin (TUB)
Type of Target
Successful
Drug Potency against Target 2-(3-Chloro-phenyl)-1H-[1,8]naphthyridin-4-one Drug Info IC50 = 1500 nM [11]
2-(4-Methoxy-phenyl)-1H-indole-3-carbaldehyde Drug Info IC50 = 3300 nM [13]
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 [11]
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 [11]
2-Naphthalen-2-yl-1H-[1,8]naphthyridin-4-one Drug Info IC50 = 14000 nM [11]
5,7-Dimethyl-2-m-tolyl-1H-[1,8]naphthyridin-4-one Drug Info IC50 = 2300 nM [11]
5-Methyl-2-m-tolyl-1H-[1,8]naphthyridin-4-one Drug Info IC50 = 1800 nM [11]
6-Methyl-2-m-tolyl-1H-[1,8]naphthyridin-4-one Drug Info IC50 = 1500 nM [11]
7-Methyl-2-m-tolyl-1H-[1,8]naphthyridin-4-one Drug Info IC50 = 1900 nM [11]
ABT-751 Drug Info IC50 = 2200 nM [5]
COLCHINOL Drug Info Ki = 1850 nM [8]
COMBETASTATIN Drug Info IC50 = 4000 nM [14]
DOLASTATIN-10 Drug Info IC50 = 2200 nM [12]
Fosbretabulin Drug Info IC50 = 1700 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 [11]
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 Synthesis and biological evaluation of 2-amino-3-(3',4',5'-trimethoxybenzoyl)-5-aryl thiophenes as a new class of potent antitubulin agents. J Med Chem. 2006 Jun 29;49(13):3906-15.
REF 11 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 12 Synthesis and biological activity of chimeric structures derived from the cytotoxic natural compounds dolastatin 10 and dolastatin 15. J Med Chem. 1998 Apr 23;41(9):1524-30.
REF 13 Methoxy-substituted 3-formyl-2-phenylindoles inhibit tubulin polymerization. J Med Chem. 1998 Dec 3;41(25):4965-72.
REF 14 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.

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