Therapeutic Targets Database
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Target Validation Information
TTD IDTTDR01167
Target NameHistone deacetylase 6    
Type of TargetResearch target    
Drug Potency against Target7-Mercapto-heptanoic acid pyridin-3-ylamideIC50 = 110 nM[1]
N-Hydroxy-4-(3-phenyl-propionylamino)-benzamideIC50 = 110 nM[2]
7-(Biphenyl-4-yloxy)-1-oxazol-2-yl-heptan-1-oneIC50 = 1100 nM[3]
7-Mercapto-heptanoic acid biphenyl-4-ylamideIC50 = 1100 nM[1]
N-(biphenyl-3-yl)-6-(sulfamoylamino)hexanamideIC50 = 1100 nM[4]
6-Phenoxy-hexane-1-thiolIC50 = 11000 nM[1]
Octanedioic acid bis-hydroxyamideIC50 = 1150 nM[5]
cyclo(-L-Am7(S2Py)-D-A1in-L-Ala-D-Pro-)IC50 = 12 nM[6]
6-phenylsulfanylhexanoic acid hydroxamideIC50 = 120 nM[7]
ST-2987IC50 = 124 nM[8]
N-(2-Mercapto-ethyl)-N'-phenyl-succinamideIC50 = 12500 nM[9]
4-Hydroxy-N-(5-hydroxycarbamoyl-pentyl)-benzamideIC50 = 149 nM[10]
4-Butyrylamino-N-hydroxy-benzamideIC50 = 1500 nM[11]
8-Mercapto-octanoic acid phenylamideIC50 = 1500 nM[1]
N-phenyl-6-(sulfamoylamino)hexanamideIC50 = 1500 nM[4]
N-(5-Hydroxycarbamoyl-pentyl)-4-nitro-benzamideIC50 = 1566 nM[12]
N-Hydroxy-4-phenylacetylamino-benzamideIC50 = 157 nM[2]
Cyclostellettamine derivativeIC50 = 17000 nM[13]
4-Benzoylamino-N-hydroxy-benzamideIC50 = 210 nM[2]
cyclo(-L-Am7(S2Py)-Aib-L-Ser(Bzl)-D-Pro-)IC50 = 24 nM[6]
Octanedioic acid hydroxyamide pyridin-2-ylamideIC50 = 248 nM[10]
N-Hydroxy-4-(5-phenyl-pentanoylamino)-benzamideIC50 = 250 nM[2]
N-Hydroxy-4-(phenylacetylamino-methyl)-benzamideIC50 = 2500 nM[11]
5-(4-Chloro-phenyl)-pentanoic acid hydroxyamideIC50 = 2580 nM[14]
cyclo(-L-Am7(S2Py)-Aib-L-Ser-D-Pro-)IC50 = 26 nM[6]
7-(Biphenyl-4-yloxy)-1,1,1-trifluoro-heptan-2-oneIC50 = 2600 nM[12]
8-Oxo-8-phenyl-octanoic acidIC50 = 270 nM[10]
8-Oxo-8-phenyl-octanoic acid hydroxyamideIC50 = 270 nM[12]
N-(2-Mercapto-ethyl)-N'-phenyl-oxalamideIC50 = 2800 nM[9]
cyclo(-L-Am7(S2Py)-Aib-L-Ala-D-Tic-)IC50 = 29 nM[6]
8-(Biphenyl-4-yloxy)-1,1,1-trifluoro-octan-2-oneIC50 = 2900 nM[3]
N1-hydroxy-N8-(4-phenylthiazol-2-yl)octanediamideIC50 = 3 nM[15]
ST-3050IC50 = 303 nM[8]
Octanedioic acid hydroxyamide pyridin-4-ylamideIC50 = 306 nM[10]
cyclo(-L-Am7(S2Py)-L-A1in-L-Ala-D-Pro-)IC50 = 33 nM[6]
N-Hydroxy-4-((S)-2-phenyl-butyrylamino)-benzamideIC50 = 34 nM[2]
7-Mercapto-heptanoic acid benzothiazol-2-ylamideIC50 = 340 nM[1]
cyclo(-L-Am7(S2Py)-Aib-L-Ph4-D-Pro-)IC50 = 36 nM[6]
N-(6-Mercapto-hexyl)-benzamideIC50 = 360 nM[1]
N-Hydroxy-4-(pentanoylamino-methyl)-benzamideIC50 = 3600 nM[11]
4-Chloro-N-(5-hydroxycarbamoyl-pentyl)-benzamideIC50 = 369 nM[12]
6-Mercapto-hexanoic acid phenylamideIC50 = 370 nM[1]
(S)-2-Amino-N-cyclopentyl-7-mercaptoheptanamideIC50 = 3860 nM[16]
N-(quinolin-8-yl)-6-(sulfamoylamino)hexanamideIC50 = 390 nM[4]
PSAMMAPLIN AIC50 = 4 nM[12]
6-benzenesulfonylhexanoic acid hydroxamideIC50 = 40 nM[7]
cyclo(-L-Am7(S2Py)-Aib-L-Phe-D-Pro-)IC50 = 40 nM[6]
6-(9H-carbazol-9-yl)-N-hydroxyhexanamideIC50 = 41 nM[17]
7-mercapto-N-(4-phenylthiazol-2-yl)heptanamideIC50 = 41 nM[16]
cyclo(-L-Am7(S2Py)-Aib-L-Ala-D-Pro-)IC50 = 43 nM[6]
cyclo(-L-Am7(S2Py)-Aib-L-Ph5-D-Pro-)IC50 = 43 nM[6]
N-[5-(Formyl-hydroxy-amino)-pentyl]-benzamideIC50 = 4300 nM[18]
N-Hydroxy-4-(4-phenyl-butyrylamino)-benzamideIC50 = 44 nM[2]
5-(4-hydroxyphenyl)-3H-1,2-dithiole-3-thioneIC50 = 450 nM[19]
N-(quinolin-6-yl)-6-(sulfamoylamino)hexanamideIC50 = 490 nM[4]
N1-(biphenyl-4-yl)-N8-hydroxyoctanediamideIC50 = 5 nM[15]
7-(Naphthalen-2-yloxy)-1-oxazol-2-yl-heptan-1-oneIC50 = 520 nM[3]
N-Hydroxy-4-(2-phenyl-butyrylamino)-benzamideIC50 = 54 nM[2]
cyclo(-L-Am7(S2Py)-L-2MePhe-L-Ala-D-Pro-)IC50 = 56 nM[6]
N-(6-Hydroxycarbamoyl-hexyl)-benzamideIC50 = 568 nM[10]
6-benzenesulfinylhexanoic acid hydroxamideIC50 = 60 nM[7]
ST-2741IC50 = 6000 nM[20]
4-Dimethylamino-N-(6-mercapto-hexyl)-benzamideIC50 = 610 nM[1]
7-(Biphenyl-3-yloxy)-1-oxazol-2-yl-heptan-1-oneIC50 = 620 nM[3]
5-Mercapto-pentanoic acid phenylamideIC50 = 6200 nM[1]
ST-2986IC50 = 661 nM[8]
9,9,9-Trifluoro-8-oxo-nonanoic acid phenylamideIC50 = 6700 nM[12]
N-Hydroxy-4-((R)-2-phenyl-butyrylamino)-benzamideIC50 = 68 nM[2]
cyclo(-L-Am7(S2Py)-D-2MePhe-L-Ala-D-Pro-)IC50 = 71 nM[6]
N-(quinolin-3-yl)-6-(sulfamoylamino)hexanamideIC50 = 710 nM[4]
7-Mercapto-heptanoic acid quinolin-3-ylamideIC50 = 72 nM[1]
7-Mercapto-heptanoic acid biphenyl-3-ylamideIC50 = 75 nM[1]
cyclo(-L-Am7(S2Py)-A2in-L-Ala-D-Pro-)IC50 = 8.8 nM[6]
cyclo(-L-Am7(S2Py)-Aib-L-Phg-D-Pro-)IC50 = 86 nM[6]
N1-(biphenyl-3-yl)-N8-hydroxyoctanediamideIC50 = 9 nM[4]
2-(methylsulfonylthio)ethyl 2-propylpentanoateIC50 = 9600 nM[19]
(E)-8-Biphenyl-4-yl-1-oxazol-2-yl-oct-7-en-1-oneIC50 = 990 nM[3]
4-Phenylbutyrohydroxamic acidKi = 150 nM[21]
NILTUBACINKi = 2200 nM[21]
Ref 1J 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 2J Med Chem. 2005 Aug 25;48(17):5530-5.Structure-based optimization of phenylbutyrate-derived histone deacetylase inhibitors. To Reference
Ref 3Bioorg Med Chem Lett. 2003 Nov 17;13(22):3909-13.Heterocyclic ketones as inhibitors of histone deacetylase. To Reference
Ref 4Bioorg Med Chem Lett. 2009 Jan 15;19(2):336-40. Epub 2008 Nov 27.Sulfamides as novel histone deacetylase inhibitors. To Reference
Ref 5J 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 6Bioorg Med Chem. 2007 Dec 15;15(24):7830-9. Epub 2007 Aug 26.Molecular design of histone deacetylase inhibitors by aromatic ring shifting in chlamydocin framework. To Reference
Ref 7J 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 8Bioorg 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
Ref 9Bioorg Med Chem Lett. 2005 Apr 15;15(8):1969-72.Mercaptoamide-based non-hydroxamic acid type histone deacetylase inhibitors. 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 11J 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 12J Med Chem. 2003 Nov 20;46(24):5097-116.Histone deacetylase inhibitors. To Reference
Ref 13Bioorg 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 14Bioorg 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 15Bioorg Med Chem Lett. 2009 Jun 1;19(11):3023-6. Epub 2009 Apr 20.Isoxazole moiety in the linker region of HDAC inhibitors adjacent to the Zn-chelating group: effects on HDAC biology and antiproliferative activity. To Reference
Ref 16J Med Chem. 2007 Nov 1;50(22):5425-38. Epub 2007 Oct 11.Design, synthesis, structure--selectivity relationship, and effect on human cancer cells of a novel series of histone deacetylase 6-selective inhibitors. To Reference
Ref 17Bioorg Med Chem Lett. 2010 Dec 1;20(23):7067-70. Epub 2010 Oct 12.Inhibitors selective for HDAC6 in enzymes and cells. To Reference
Ref 18Bioorg Med Chem Lett. 2004 Jan 19;14(2):449-53.Design, synthesis, and activity of HDAC inhibitors with a N-formyl hydroxylamine head group. To Reference
Ref 19Bioorg 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 20Bioorg Med Chem Lett. 2009 May 15;19(10):2840-3. Epub 2009 Mar 26.Exploring bis-(indolyl)methane moiety as an alternative and innovative CAP group in the design of histone deacetylase (HDAC) inhibitors. To Reference
Ref 21Nat Chem Biol. 2010 Mar;6(3):238-243. Epub 2010 Feb 7.Chemical phylogenetics of histone deacetylases. To Reference



 

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Professor in Department of Pharmacy
National University of Singapore, Singapore


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