Target Validation Information
TTD ID T28887
Target Name Histone deacetylase 8 (HDAC8)
Type of Target
Clinical trial
Drug Potency against Target (E)-8-Biphenyl-4-yl-1-oxazol-2-yl-oct-7-en-1-one Drug Info IC50 = 990 nM [2]
2-(methylsulfonylthio)ethyl 2-propylpentanoate Drug Info IC50 = 9600 nM [13]
4-Benzoylamino-N-hydroxy-benzamide Drug Info IC50 = 210 nM [9]
4-Butyrylamino-N-hydroxy-benzamide Drug Info IC50 = 1500 nM [4]
4-Chloro-N-(5-hydroxycarbamoyl-pentyl)-benzamide Drug Info IC50 = 369 nM [1]
4-Dimethylamino-N-(6-mercapto-hexyl)-benzamide Drug Info IC50 = 610 nM [7]
4-Hydroxy-N-(5-hydroxycarbamoyl-pentyl)-benzamide Drug Info IC50 = 149 nM [1]
4-Phenylbutyrohydroxamic acid Drug Info Ki = 1850 nM [16]
5-(4-Chloro-phenyl)-pentanoic acid hydroxyamide Drug Info IC50 = 2580 nM [5]
5-(4-hydroxyphenyl)-3H-1,2-dithiole-3-thione Drug Info IC50 = 450 nM [13]
5-Mercapto-pentanoic acid phenylamide Drug Info IC50 = 6200 nM [7]
6-(2-mercaptoacetamido)-N-phenylhexanamide Drug Info IC50 = 3890 nM [12]
6-benzenesulfinylhexanoic acid hydroxamide Drug Info IC50 = 7700 nM [10]
6-benzenesulfonylhexanoic acid hydroxamide Drug Info IC50 = 15500 nM [10]
6-Mercapto-hexanoic acid phenylamide Drug Info IC50 = 370 nM [7]
6-Phenoxy-hexane-1-thiol Drug Info IC50 = 11000 nM [7]
6-phenylsulfanylhexanoic acid hydroxamide Drug Info IC50 = 9400 nM [10]
7-(Biphenyl-3-yloxy)-1-oxazol-2-yl-heptan-1-one Drug Info IC50 = 620 nM [2]
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 [2]
7-(Naphthalen-2-yloxy)-1-oxazol-2-yl-heptan-1-one Drug Info IC50 = 520 nM [2]
7-Mercapto-heptanoic acid benzothiazol-2-ylamide Drug Info IC50 = 340 nM [7]
7-Mercapto-heptanoic acid biphenyl-3-ylamide Drug Info IC50 = 75 nM [7]
7-Mercapto-heptanoic acid biphenyl-4-ylamide Drug Info IC50 = 1100 nM [7]
7-Mercapto-heptanoic acid pyridin-3-ylamide Drug Info IC50 = 110 nM [7]
7-Mercapto-heptanoic acid quinolin-3-ylamide Drug Info IC50 = 72 nM [7]
8-(Biphenyl-4-yloxy)-1,1,1-trifluoro-octan-2-one Drug Info IC50 = 2900 nM [2]
8-Mercapto-octanoic acid phenylamide Drug Info IC50 = 1500 nM [7]
8-Oxo-8-phenyl-octanoic acid Drug Info IC50 = 270 nM [1]
9,9,9-Trifluoro-8-oxo-nonanoic acid phenylamide Drug Info IC50 = 6700 nM [3]
9-mercapto-8-oxo-N-phenylnonanamide Drug Info IC50 = 690 nM [12]
Azithromycin-N-benzyltriazolylhexahydroxamic Acid Drug Info IC50 = 4730 nM [14]
Azithromycin-N-benzyltriazolylnonahydroxamic Acid Drug Info IC50 = 11050 nM [14]
Azithromycin-N-benzyltriazolyloctahydroxamic Acid Drug Info IC50 = 7130 nM [14]
Azithromycinarylalkylhydroxamic Acid Drug Info IC50 = 6680 nM [14]
Cyclostellettamine derivative Drug Info IC50 = 17000 nM [6]
Desclasinose Azithromycinarylalkyl Hydroxamate Drug Info IC50 = 2320 nM [14]
N-(2-Mercapto-ethyl)-N'-phenyl-oxalamide Drug Info IC50 = 2800 nM [8]
N-(2-Mercapto-ethyl)-N'-phenyl-succinamide Drug Info IC50 = 12500 nM [8]
N-(5-Hydroxycarbamoyl-pentyl)-4-nitro-benzamide Drug Info IC50 = 1556 nM [1]
N-(6-Hydroxycarbamoyl-hexyl)-benzamide Drug Info IC50 = 568 nM [1]
N-(6-Mercapto-hexyl)-benzamide Drug Info IC50 = 360 nM [7]
N-hydroxy-1-naphthamide Drug Info IC50 = 14000 nM [11]
N-hydroxy-3-(naphthalen-1-yl)acrylamide Drug Info IC50 = 700 nM [11]
N-hydroxy-3-phenoxybenzamide Drug Info IC50 = 6600 nM [11]
N-Hydroxy-4-((R)-2-phenyl-butyrylamino)-benzamide Drug Info IC50 = 68 nM [9]
N-Hydroxy-4-((S)-2-phenyl-butyrylamino)-benzamide Drug Info IC50 = 34 nM [9]
N-Hydroxy-4-(2-phenyl-butyrylamino)-benzamide Drug Info IC50 = 54 nM [9]
N-Hydroxy-4-(3-phenyl-propionylamino)-benzamide Drug Info IC50 = 110 nM [9]
N-Hydroxy-4-(4-phenyl-butyrylamino)-benzamide Drug Info IC50 = 44 nM [9]
N-Hydroxy-4-(5-phenyl-pentanoylamino)-benzamide Drug Info IC50 = 250 nM [9]
N-hydroxy-4-(naphthalen-1-yl)benzamide Drug Info IC50 = 300 nM [11]
N-Hydroxy-4-(pentanoylamino-methyl)-benzamide Drug Info IC50 = 3600 nM [4]
N-Hydroxy-4-(phenylacetylamino-methyl)-benzamide Drug Info IC50 = 2500 nM [4]
N-Hydroxy-4-phenylacetylamino-benzamide Drug Info IC50 = 157 nM [9]
NILTUBACIN Drug Info Ki = 750 nM [16]
Octanedioic acid bis-hydroxyamide Drug Info Ki = 950 nM [16]
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 [3]
S-2,9-dioxo-9-(phenylamino)nonyl ethanethioate Drug Info IC50 = 190 nM [12]
ST-2986 Drug Info IC50 = 1290 nM [15]
ST-2987 Drug Info IC50 = 70 nM [15]
ST-3050 Drug Info IC50 = 235 nM [15]
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 Heterocyclic ketones as inhibitors of histone deacetylase. Bioorg Med Chem Lett. 2003 Nov 17;13(22):3909-13.
REF 3 Histone deacetylase inhibitors. J Med Chem. 2003 Nov 20;46(24):5097-116.
REF 4 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 5 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 6 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 7 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 8 Mercaptoamide-based non-hydroxamic acid type histone deacetylase inhibitors. Bioorg Med Chem Lett. 2005 Apr 15;15(8):1969-72.
REF 9 Structure-based optimization of phenylbutyrate-derived histone deacetylase inhibitors. J Med Chem. 2005 Aug 25;48(17):5530-5.
REF 10 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 11 Design and evaluation of 'Linkerless' hydroxamic acids as selective HDAC8 inhibitors. Bioorg Med Chem Lett. 2007 May 15;17(10):2874-8.
REF 12 Histone deacetylase inhibitors: from bench to clinic. J Med Chem. 2008 Mar 27;51(6):1505-29.
REF 13 New sulfurated derivatives of valproic acid with enhanced histone deacetylase inhibitory activity. Bioorg Med Chem Lett. 2008 Mar 15;18(6):1893-7.
REF 14 Non-peptide macrocyclic histone deacetylase inhibitors. J Med Chem. 2009 Jan 22;52(2):456-68.
REF 15 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 16 Chemical phylogenetics of histone deacetylases. Nat Chem Biol. 2010 Mar;6(3):238-243.

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