Therapeutic Targets Database
BIDD Pharmainformatics Databases


TTD Target ID: TTDR01156

Target Information
NameHistone deacetylase 2    
Type of targetResearch target    
DiseaseColon cancer
[ICD9: 153, 154   ICD10: C18-C21]
BioChemical ClassHydrolases acting on carbon-nitrogen bonds    
PathwayCell cycle
Chronic myeloid leukemia
Huntington's disease
Notch signaling pathway
Pathways in cancer
UniProt IDQ92769
PDB Structure3MAX.    
FunctionResponsible for the deacetylation of lysine residues on the n-terminal part of the core histones (h2a, h2b, h3 and h4). Histone deacetylation gives a tag for epigenetic repression and plays an important role in transcriptional regulation, cell cycle progression.    
Target ValidationClick to Find Target Validation Information.    
QSAR ModelClick to Find Target QSAR Model.    
Inhibitor (E)-8-Biphenyl-4-yl-1-oxazol-2-yl-oct-7-en-1-one[2]
1,1,1-Trifluoro-8- (4-phenoxy-phenoxy)-octan-2-one[3]
2- (allyloxy)-N8-hydroxy-N1-phenyloctanediamide[4]
2- (benzyloxy)-N7-hydroxy-N1-phenylheptanediamide[4]
2- (methylsulfonylthio)ethyl 2-propylpentanoate[5]
4-Chloro-N- (5-hydroxycarbamoyl-pentyl)-benzamide[8]
4-Dimethylamino-N- (6-mercapto-hexyl)-benzamide[9]
4-Hydroxy-N- (5-hydroxycarbamoyl-pentyl)-benzamide[10]
4-Phenylbutyrohydroxamic acid[11]
5- (4-Chloro-phenyl)-pentanoic acid hydroxyamide[12]
5- (4-hydroxyphenyl)-3H-1,2-dithiole-3-thione[5]
5- (Biphenyl-4-yl)-pentanoic acid N-hydroxyamide[13]
5-Mercapto-pentanoic acid phenylamide[9]
6- (2-Bromo-acetylamino)-hexanoic acid phenylamide[9]
6-Mercapto-hexanoic acid phenylamide[9]
6-benzenesulfinylhexanoic acid hydroxamide[14]
6-benzenesulfonylhexanoic acid hydroxamide[14]
6-phenylsulfanylhexanoic acid hydroxamide[14]
7- (Biphenyl-3-yloxy)-1-oxazol-2-yl-heptan-1-one[2]
7- (Biphenyl-4-yloxy)-1,1,1-trifluoro-heptan-2-one[3]
7- (Biphenyl-4-yloxy)-1-oxazol-2-yl-heptan-1-one[2]
7- (Biphenyl-4-yloxy)-heptanoic acid hydroxyamide[15]
7- (Naphthalen-2-yloxy)-1-oxazol-2-yl-heptan-1-one[2]
7-Biphenyl-4-yl-heptanoic acid hydroxyamide[16]
7-Mercapto-heptanoic acid benzothiazol-2-ylamide[9]
7-Mercapto-heptanoic acid biphenyl-3-ylamide[9]
7-Mercapto-heptanoic acid biphenyl-4-ylamide[9]
7-Mercapto-heptanoic acid phenylamide[9]
7-Mercapto-heptanoic acid pyridin-3-ylamide[9]
7-Mercapto-heptanoic acid quinolin-3-ylamide[9]
7-Phenoxy-heptanoic acid hydroxyamide[16]
8- (Biphenyl-3-yloxy)-1,1,1-trifluoro-octan-2-one[3]
8- (Biphenyl-4-yloxy)-1,1,1-trifluoro-octan-2-one[3]
8- (Biphenyl-4-yloxy)-2-oxo-octanoic acid[15]
8-Mercapto-octanoic acid phenylamide[9]
8-Oxo-8-phenyl-octanoic acid[10]
8-Oxo-8-phenyl-octanoic acid hydroxyamide[8]
8-Phenyl-octanoic acid hydroxyamide[16]
9,9,9-Trifluoro-8-oxo-nonanoic acid phenylamide[3]
9- (Biphenyl-4-yloxy)-1,1,1-trifluoro-nonan-2-one[3]
Cyclostellettamine derivative[17]
N- (2-Mercapto-ethyl)-N'-phenyl-oxalamide[18]
N- (2-Mercapto-ethyl)-N'-phenyl-succinamide[18]
N- (2-amino-5-[19]
N- (2-amino-5-[19]
N- (2-amino-5-[19]
N- (2-amino-5-[19]
N- (2-amino-5-[19]
N- (2-amino-5-[20]
N- (2-aminophenyl)-4-methoxybenzamide[21]
N- (2-aminophenyl)benzamide[19]
N- (2-aminophenyl)nicotinamide[20]
N- (2-aminophenyl)quinoxaline-6-carboxamide[21]
N- (3'-acetyl-4-aminobiphenyl-3-yl)benzamide[19]
N- (4'-acetyl-4-aminobiphenyl-3-yl)benzamide[19]
N- (4-amino-3'-methoxybiphenyl-3-yl)benzamide[19]
N- (4-amino-3'-methylbiphenyl-3-yl)benzamide[19]
N- (4-amino-4'-bromobiphenyl-3-yl)benzamide[19]
N- (4-amino-4'-fluorobiphenyl-3-yl)benzamide[19]
N- (4-amino-4'-methoxybiphenyl-3-yl)benzamide[19]
N- (4-amino-4'-vinylbiphenyl-3-yl)benzamide[19]
N- (4-aminobiphenyl-3-yl)benzamide[19]
N- (4-aminobiphenyl-3-yl)nicotinamide[20]
N- (4-hydroxybiphenyl-3-yl)benzamide[20]
N- (5-Hydroxycarbamoyl-pentyl)-4-nitro-benzamide[8]
N- (6-Hydroxycarbamoyl-hexyl)-benzamide[10]
N- (6-Mercapto-hexyl)-benzamide[9]
N-Hydroxy-4- ([6]
N-Hydroxy-4- ([6]
N-Hydroxy-4- (2-phenyl-butyrylamino)-benzamide[6]
N-Hydroxy-4- (4-phenyl-butyrylamino)-benzamide[6]
N-Hydroxy-4- (5-phenyl-pentanoylamino)-benzamide[6]
N-Hydroxy-4- (pentanoylamino-methyl)-benzamide[7]
N-Hydroxy-4- (phenylacetylamino-methyl)-benzamide[7]
N-Hydroxy-E-3- (4'-chlorobiphenyl-4-yl)-acrylamide[13]
N-Hydroxy-E-3- (4'-cyanobiphenyl-4-yl)-acrylamide[13]
N-Hydroxy-E-3- (biphenyl-4-yl)-acrylamide[13]
N-hydroxy-4- (3-phenylpropanamido)benzamide[22]
Octanedioic acid bis-hydroxyamide[23]
Octanedioic acid hydroxyamide pyridin-2-ylamide[10]
Octanedioic acid hydroxyamide pyridin-4-ylamide[10]
Thioacetic acid S- (6-phenylcarbamoyl-hexyl) ester[9]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Induction of HDAC2 expression upon loss of APC in colorectal tumorigenesis. Cancer Cell. 2004 May;5(5):455-63. To Reference
Ref 2Bioorg Med Chem Lett. 2003 Nov 17;13(22):3909-13.Heterocyclic ketones as inhibitors of histone deacetylase. To Reference
Ref 3Bioorg Med Chem Lett. 2002 Dec 2;12(23):3443-7.Trifluoromethyl ketones as inhibitors of histone deacetylase. To Reference
Ref 4Bioorg Med Chem Lett. 2007 Nov 15;17(22):6261-5. Epub 2007 Sep 8.Omega-alkoxy analogues of SAHA (vorinostat) as inhibitors of HDAC: a study of chain-length and stereochemical dependence. To Reference
Ref 5Bioorg Med Chem Lett. 2008 Mar 15;18(6):1893-7. Epub 2008 Feb 8.New sulfurated derivatives of valproic acid with enhanced histone deacetylase inhibitory activity. To Reference
Ref 6J Med Chem. 2005 Aug 25;48(17):5530-5.Structure-based optimization of phenylbutyrate-derived histone deacetylase inhibitors. To Reference
Ref 7J Med Chem. 2004 Jan 15;47(2):467-74.Zn2+-chelating motif-tethered short-chain fatty acids as a novel class of histone deacetylase inhibitors. To Reference
Ref 8J Med Chem. 2003 Nov 20;46(24):5097-116.Histone deacetylase inhibitors. To Reference
Ref 9J Med Chem. 2005 Feb 24;48(4):1019-32.Novel inhibitors of human histone deacetylases: design, synthesis, enzyme inhibition, and cancer cell growth inhibition of SAHA-based non-hydroxamates. To Reference
Ref 10J Med Chem. 2002 Feb 14;45(4):753-7.Inhibitors of human histone deacetylase: synthesis and enzyme and cellular activity of straight chain hydroxamates. To Reference
Ref 11Nat Chem Biol. 2010 Mar;6(3):238-243. Epub 2010 Feb 7.Chemical phylogenetics of histone deacetylases. To Reference
Ref 12Bioorg Med Chem Lett. 2004 May 17;14(10):2477-81.Stereodefined and polyunsaturated inhibitors of histone deacetylase based on (2E,4E)-5-arylpenta-2,4-dienoic acid hydroxyamides. To Reference
Ref 13Eur J Med Chem. 2009 May;44(5):1900-12. Epub 2008 Nov 19.Design, synthesis, and evaluation of biphenyl-4-yl-acrylohydroxamic acid derivatives as histone deacetylase (HDAC) inhibitors. To Reference
Ref 14J Med Chem. 2006 Jan 26;49(2):800-5.Aromatic sulfide inhibitors of histone deacetylase based on arylsulfinyl-2,4-hexadienoic acid hydroxyamides. To Reference
Ref 15Bioorg Med Chem Lett. 2003 Oct 6;13(19):3331-5.Alpha-keto amides as inhibitors of histone deacetylase. To Reference
Ref 16Bioorg Med Chem Lett. 2003 Nov 3;13(21):3817-20.A novel series of histone deacetylase inhibitors incorporating hetero aromatic ring systems as connection units. To Reference
Ref 17Bioorg Med Chem Lett. 2004 May 17;14(10):2617-20.Three new cyclostellettamines, which inhibit histone deacetylase, from a marine sponge of the genus Xestospongia. To Reference
Ref 18Bioorg Med Chem Lett. 2005 Apr 15;15(8):1969-72.Mercaptoamide-based non-hydroxamic acid type histone deacetylase inhibitors. To Reference
Ref 19Bioorg Med Chem Lett. 2010 May 15;20(10):3142-5. Epub 2010 Mar 30.Exploration of the HDAC2 foot pocket: Synthesis and SAR of substituted N-(2-aminophenyl)benzamides. To Reference
Ref 20Bioorg Med Chem Lett. 2008 Dec 1;18(23):6104-9. Epub 2008 Oct 14.SAR profiles of spirocyclic nicotinamide derived selective HDAC1/HDAC2 inhibitors (SHI-1:2). To Reference
Ref 21J Med Chem. 2007 Nov 15;50(23):5543-6. Epub 2007 Oct 17.Novel aminophenyl benzamide-type histone deacetylase inhibitors with enhanced potency and selectivity. To Reference
Ref 22Eur J Med Chem. 2009 Nov;44(11):4470-6. Epub 2009 Jun 17.Design, synthesis and preliminary biological evaluation of N-hydroxy-4-(3-phenylpropanamido)benzamide (HPPB) derivatives as novel histone deacetylase inhibitors. To Reference
Ref 23J Med Chem. 2002 Jul 18;45(15):3296-309.Structure-activity relationships on phenylalanine-containing inhibitors of histone deacetylase: in vitro enzyme inhibition, induction of differentiation, and inhibition of proliferation in Friend leukemic cells. To Reference
Ref 24Bioorg Med Chem Lett. 2009 Apr 15;19(8):2346-9. Epub 2009 Feb 12.N-Hydroxy-(4-oxime)-cinnamide: a versatile scaffold for the synthesis of novel histone deacetylase [correction of deacetilase] (HDAC) inhibitors. To Reference


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