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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