Target Validation Information
TTD ID T51191
Target Name Histone deacetylase 2 (HDAC2)
Type of Target
Clinical trial
Drug Potency against Target Romidepsin Drug Info IC50 = 47 nM [7]
(E)-8-Biphenyl-4-yl-1-oxazol-2-yl-oct-7-en-1-one Drug Info IC50 = 990 nM [6]
1,1,1-Trifluoro-8-(4-phenoxy-phenoxy)-octan-2-one Drug Info IC50 = 3400 nM [3]
1,1,1-Trifluoro-8-phenoxy-octan-2-one Drug Info IC50 = 8000 nM [3]
2-(allyloxy)-N8-hydroxy-N1-phenyloctanediamide Drug Info IC50 = 500 nM [15]
2-(benzyloxy)-N7-hydroxy-N1-phenylheptanediamide Drug Info IC50 = 500 nM [15]
2-(methylsulfonylthio)ethyl 2-propylpentanoate Drug Info IC50 = 9600 nM [17]
4-Benzoylamino-N-hydroxy-benzamide Drug Info IC50 = 210 nM [13]
4-Butyrylamino-N-hydroxy-benzamide Drug Info IC50 = 1500 nM [8]
4-Chloro-N-(5-hydroxycarbamoyl-pentyl)-benzamide Drug Info IC50 = 369 nM [7]
4-Dimethylamino-N-(6-mercapto-hexyl)-benzamide Drug Info IC50 = 610 nM [11]
4-Hydroxy-N-(5-hydroxycarbamoyl-pentyl)-benzamide Drug Info IC50 = 149 nM [1]
4-Phenylbutyrohydroxamic acid Drug Info Ki = 430 nM [22]
5-(4-Chloro-phenyl)-pentanoic acid hydroxyamide Drug Info IC50 = 2580 nM [9]
5-(4-hydroxyphenyl)-3H-1,2-dithiole-3-thione Drug Info IC50 = 450 nM [17]
5-(Biphenyl-4-yl)-pentanoic acid N-hydroxyamide Drug Info IC50 = 720 nM [19]
5-Mercapto-pentanoic acid phenylamide Drug Info IC50 = 6200 nM [11]
6-benzenesulfinylhexanoic acid hydroxamide Drug Info IC50 = 60 nM [14]
6-benzenesulfonylhexanoic acid hydroxamide Drug Info IC50 = 40 nM [14]
6-Mercapto-hexanoic acid phenylamide Drug Info IC50 = 370 nM [11]
6-Phenoxy-hexane-1-thiol Drug Info IC50 = 11000 nM [11]
6-phenylsulfanylhexanoic acid hydroxamide Drug Info IC50 = 120 nM [14]
7-(Biphenyl-3-yloxy)-1-oxazol-2-yl-heptan-1-one Drug Info IC50 = 620 nM [6]
7-(Biphenyl-4-yloxy)-1,1,1-trifluoro-heptan-2-one Drug Info IC50 = 2600 nM [3]
7-(Biphenyl-4-yloxy)-1-oxazol-2-yl-heptan-1-one Drug Info IC50 = 1100 nM [6]
7-(Naphthalen-2-yloxy)-1-oxazol-2-yl-heptan-1-one Drug Info IC50 = 520 nM [6]
7-Biphenyl-4-yl-heptanoic acid hydroxyamide Drug Info IC50 = 58 nM [5]
7-Mercapto-heptanoic acid benzothiazol-2-ylamide Drug Info IC50 = 340 nM [11]
7-Mercapto-heptanoic acid biphenyl-3-ylamide Drug Info IC50 = 75 nM [11]
7-Mercapto-heptanoic acid biphenyl-4-ylamide Drug Info IC50 = 1100 nM [11]
7-Mercapto-heptanoic acid pyridin-3-ylamide Drug Info IC50 = 110 nM [11]
7-Mercapto-heptanoic acid quinolin-3-ylamide Drug Info IC50 = 72 nM [11]
7-Phenoxy-heptanoic acid hydroxyamide Drug Info IC50 = 330 nM [5]
8-(Biphenyl-3-yloxy)-1,1,1-trifluoro-octan-2-one Drug Info IC50 = 2800 nM [3]
8-(Biphenyl-4-yloxy)-1,1,1-trifluoro-octan-2-one Drug Info IC50 = 2900 nM [3]
8-(Biphenyl-4-yloxy)-2-oxo-octanoic acid Drug Info IC50 = 3.7 nM [4]
8-Mercapto-octanoic acid phenylamide Drug Info IC50 = 1500 nM [11]
8-Oxo-8-phenyl-octanoic acid Drug Info IC50 = 270 nM [1]
8-Phenyl-octanoic acid hydroxyamide Drug Info IC50 = 560 nM [5]
9,9,9-Trifluoro-8-oxo-nonanoic acid phenylamide Drug Info IC50 = 6700 nM [3]
Cyclostellettamine derivative Drug Info IC50 = 17000 nM [10]
N-(2-amino-5-(benzofuran-2-yl)phenyl)benzamide Drug Info IC50 = 10000 nM [23]
N-(2-amino-5-(furan-2-yl)phenyl)benzamide Drug Info IC50 = 1800 nM [23]
N-(2-amino-5-(furan-3-yl)phenyl)benzamide Drug Info IC50 = 810 nM [23]
N-(2-amino-5-(pyridin-4-yl)phenyl)benzamide Drug Info IC50 = 3900 nM [23]
N-(2-amino-5-(thiazol-2-yl)phenyl)benzamide Drug Info IC50 = 5800 nM [23]
N-(2-amino-5-(thiophen-2-yl)phenyl)nicotinamide Drug Info IC50 = 390 nM [18]
N-(2-aminophenyl)-4-methoxybenzamide Drug Info IC50 = 900 nM [16]
N-(2-aminophenyl)benzamide Drug Info IC50 = 10000 nM [23]
N-(2-aminophenyl)nicotinamide Drug Info IC50 = 6980 nM [18]
N-(2-aminophenyl)quinoxaline-6-carboxamide Drug Info IC50 = 2000 nM [16]
N-(2-Mercapto-ethyl)-N'-phenyl-oxalamide Drug Info IC50 = 2800 nM [12]
N-(2-Mercapto-ethyl)-N'-phenyl-succinamide Drug Info IC50 = 12500 nM [12]
N-(3'-acetyl-4-aminobiphenyl-3-yl)benzamide Drug Info IC50 = 13000 nM [23]
N-(4'-acetyl-4-aminobiphenyl-3-yl)benzamide Drug Info IC50 = 5000 nM [23]
N-(4-amino-3'-methoxybiphenyl-3-yl)benzamide Drug Info IC50 = 3400 nM [23]
N-(4-amino-3'-methylbiphenyl-3-yl)benzamide Drug Info IC50 = 7200 nM [23]
N-(4-amino-4'-bromobiphenyl-3-yl)benzamide Drug Info IC50 = 600 nM [23]
N-(4-amino-4'-fluorobiphenyl-3-yl)benzamide Drug Info IC50 = 1400 nM [23]
N-(4-amino-4'-methoxybiphenyl-3-yl)benzamide Drug Info IC50 = 860 nM [23]
N-(4-amino-4'-vinylbiphenyl-3-yl)benzamide Drug Info IC50 = 5000 nM [23]
N-(4-aminobiphenyl-3-yl)benzamide Drug Info IC50 = 900 nM [23]
N-(4-aminobiphenyl-3-yl)nicotinamide Drug Info IC50 = 900 nM [18]
N-(4-hydroxybiphenyl-3-yl)benzamide Drug Info IC50 = 200 nM [18]
N-(5-Hydroxycarbamoyl-pentyl)-4-nitro-benzamide Drug Info IC50 = 1566 nM [7]
N-(6-Hydroxycarbamoyl-hexyl)-benzamide Drug Info IC50 = 568 nM [1]
N-(6-Mercapto-hexyl)-benzamide Drug Info IC50 = 360 nM [11]
N-Hydroxy-4-((R)-2-phenyl-butyrylamino)-benzamide Drug Info IC50 = 68 nM [13]
N-Hydroxy-4-((S)-2-phenyl-butyrylamino)-benzamide Drug Info IC50 = 34 nM [13]
N-Hydroxy-4-(2-phenyl-butyrylamino)-benzamide Drug Info IC50 = 54 nM [13]
N-Hydroxy-4-(3-phenyl-propionylamino)-benzamide Drug Info IC50 = 1100 nM [21]
N-Hydroxy-4-(4-phenyl-butyrylamino)-benzamide Drug Info IC50 = 44 nM [13]
N-Hydroxy-4-(5-phenyl-pentanoylamino)-benzamide Drug Info IC50 = 250 nM [13]
N-Hydroxy-4-(pentanoylamino-methyl)-benzamide Drug Info IC50 = 3600 nM [8]
N-Hydroxy-4-(phenylacetylamino-methyl)-benzamide Drug Info IC50 = 2500 nM [8]
N-Hydroxy-4-phenylacetylamino-benzamide Drug Info IC50 = 157 nM [13]
N-Hydroxy-E-3-(4'-chlorobiphenyl-4-yl)-acrylamide Drug Info IC50 = 1860 nM [19]
N-Hydroxy-E-3-(4'-cyanobiphenyl-4-yl)-acrylamide Drug Info IC50 = 330 nM [19]
N-Hydroxy-E-3-(biphenyl-4-yl)-acrylamide Drug Info IC50 = 820 nM [19]
N7-hydroxy-2-methoxy-N1-phenylheptanediamide Drug Info IC50 = 500 nM [15]
N7-hydroxy-N1-phenyl-2-propoxyheptanediamide Drug Info IC50 = 500 nM [15]
N8,2-dihydroxy-N1-phenyloctanediamide Drug Info IC50 = 500 nM [15]
N8-hydroxy-2-methoxy-N1-phenyloctanediamide Drug Info IC50 = 500 nM [15]
Octanedioic acid bis-hydroxyamide Drug Info IC50 = 1150 nM [2]
Octanedioic acid hydroxyamide pyridin-2-ylamide Drug Info IC50 = 248 nM [1]
Octanedioic acid hydroxyamide pyridin-4-ylamide Drug Info IC50 = 306 nM [1]
PSAMMAPLIN A Drug Info IC50 = 4 nM [7]
ST-2986 Drug Info IC50 = 11000 nM [20]
ST-2987 Drug Info IC50 = 2670 nM [20]
Tacedinaline Drug Info Ki = 190 nM [22]
References
REF 1 Inhibitors of human histone deacetylase: synthesis and enzyme and cellular activity of straight chain hydroxamates. J Med Chem. 2002 Feb 14;45(4):753-7.
REF 2 Structure-activity relationships on phenylalanine-containing inhibitors of histone deacetylase: in vitro enzyme inhibition, induction of differenti... J Med Chem. 2002 Jul 18;45(15):3296-309.
REF 3 Trifluoromethyl ketones as inhibitors of histone deacetylase. Bioorg Med Chem Lett. 2002 Dec 2;12(23):3443-7.
REF 4 Alpha-keto amides as inhibitors of histone deacetylase. Bioorg Med Chem Lett. 2003 Oct 6;13(19):3331-5.
REF 5 A novel series of histone deacetylase inhibitors incorporating hetero aromatic ring systems as connection units. Bioorg Med Chem Lett. 2003 Nov 3;13(21):3817-20.
REF 6 Heterocyclic ketones as inhibitors of histone deacetylase. Bioorg Med Chem Lett. 2003 Nov 17;13(22):3909-13.
REF 7 Histone deacetylase inhibitors. J Med Chem. 2003 Nov 20;46(24):5097-116.
REF 8 Zn2+-chelating motif-tethered short-chain fatty acids as a novel class of histone deacetylase inhibitors. J Med Chem. 2004 Jan 15;47(2):467-74.
REF 9 Stereodefined and polyunsaturated inhibitors of histone deacetylase based on (2E,4E)-5-arylpenta-2,4-dienoic acid hydroxyamides. Bioorg Med Chem Lett. 2004 May 17;14(10):2477-81.
REF 10 Three new cyclostellettamines, which inhibit histone deacetylase, from a marine sponge of the genus Xestospongia. Bioorg Med Chem Lett. 2004 May 17;14(10):2617-20.
REF 11 Novel inhibitors of human histone deacetylases: design, synthesis, enzyme inhibition, and cancer cell growth inhibition of SAHA-based non-hydroxama... J Med Chem. 2005 Feb 24;48(4):1019-32.
REF 12 Mercaptoamide-based non-hydroxamic acid type histone deacetylase inhibitors. Bioorg Med Chem Lett. 2005 Apr 15;15(8):1969-72.
REF 13 Structure-based optimization of phenylbutyrate-derived histone deacetylase inhibitors. J Med Chem. 2005 Aug 25;48(17):5530-5.
REF 14 Aromatic sulfide inhibitors of histone deacetylase based on arylsulfinyl-2,4-hexadienoic acid hydroxyamides. J Med Chem. 2006 Jan 26;49(2):800-5.
REF 15 Omega-alkoxy analogues of SAHA (vorinostat) as inhibitors of HDAC: a study of chain-length and stereochemical dependence. Bioorg Med Chem Lett. 2007 Nov 15;17(22):6261-5.
REF 16 Novel aminophenyl benzamide-type histone deacetylase inhibitors with enhanced potency and selectivity. J Med Chem. 2007 Nov 15;50(23):5543-6.
REF 17 New sulfurated derivatives of valproic acid with enhanced histone deacetylase inhibitory activity. Bioorg Med Chem Lett. 2008 Mar 15;18(6):1893-7.
REF 18 Bioorg 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).
REF 19 Design, synthesis, and evaluation of biphenyl-4-yl-acrylohydroxamic acid derivatives as histone deacetylase (HDAC) inhibitors. Eur J Med Chem. 2009 May;44(5):1900-12.
REF 20 N-Hydroxy-(4-oxime)-cinnamide: a versatile scaffold for the synthesis of novel histone deacetylase [correction of deacetilase] (HDAC) inhibitors. Bioorg Med Chem Lett. 2009 Apr 15;19(8):2346-9.
REF 21 Design, synthesis and preliminary biological evaluation of N-hydroxy-4-(3-phenylpropanamido)benzamide (HPPB) derivatives as novel histone deacetyla... Eur J Med Chem. 2009 Nov;44(11):4470-6.
REF 22 Chemical phylogenetics of histone deacetylases. Nat Chem Biol. 2010 Mar;6(3):238-243.
REF 23 Exploration of the HDAC2 foot pocket: Synthesis and SAR of substituted N-(2-aminophenyl)benzamides. Bioorg Med Chem Lett. 2010 May 15;20(10):3142-5.

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