Target Validation Information
TTD ID T63816
Target Name Histone deacetylase 4 (HDAC4)
Type of Target
Clinical trial
Drug Potency against Target Romidepsin Drug Info IC50 = 1 nM [19]
Drug Info IC50 = 3000 nM [18]
Drug Info IC50 = 2600 nM [4]
Drug Info IC50 = 1500 nM [8]
Drug Info IC50 = 568 nM [1]
Drug Info IC50 = 340 nM [8]
Drug Info IC50 = 2580 nM [6]
Drug Info IC50 = 2.2 nM [12]
Drug Info IC50 = 3.2 nM [12]
Drug Info IC50 = 1.8 nM [12]
Drug Info IC50 = 3600 nM [5]
(E)-8-Biphenyl-4-yl-1-oxazol-2-yl-oct-7-en-1-one Drug Info IC50 = 990 nM [3]
2,2-bis(3-fluorophenyl)-N-hydroxyacetamide Drug Info IC50 = 700 nM [17]
2,2-bis(4-chlorophenyl)-N-hydroxyacetamide Drug Info IC50 = 960 nM [17]
2,2-bis(4-fluorophenyl)-N-hydroxyacetamide Drug Info IC50 = 1100 nM [17]
2-(methylsulfonylthio)ethyl 2-propylpentanoate Drug Info IC50 = 9600 nM [14]
4-Benzoylamino-N-hydroxy-benzamide Drug Info IC50 = 210 nM [10]
4-Butyrylamino-N-hydroxy-benzamide Drug Info IC50 = 1500 nM [5]
4-Chloro-N-(5-hydroxycarbamoyl-pentyl)-benzamide Drug Info IC50 = 369 nM [4]
4-Dimethylamino-N-(6-mercapto-hexyl)-benzamide Drug Info IC50 = 610 nM [8]
4-Hydroxy-N-(5-hydroxycarbamoyl-pentyl)-benzamide Drug Info IC50 = 149 nM [1]
5-(4-hydroxyphenyl)-3H-1,2-dithiole-3-thione Drug Info IC50 = 450 nM [14]
5-Mercapto-pentanoic acid phenylamide Drug Info IC50 = 6200 nM [8]
6-benzenesulfinylhexanoic acid hydroxamide Drug Info IC50 = 60 nM [11]
6-benzenesulfonylhexanoic acid hydroxamide Drug Info IC50 = 40 nM [11]
6-Mercapto-hexanoic acid phenylamide Drug Info IC50 = 370 nM [8]
6-Phenoxy-hexane-1-thiol Drug Info IC50 = 11000 nM [8]
6-phenylsulfanylhexanoic acid hydroxamide Drug Info IC50 = 120 nM [11]
7-(Biphenyl-3-yloxy)-1-oxazol-2-yl-heptan-1-one Drug Info IC50 = 620 nM [3]
7-(Biphenyl-4-yloxy)-1-oxazol-2-yl-heptan-1-one Drug Info IC50 = 1100 nM [3]
7-(Naphthalen-2-yloxy)-1-oxazol-2-yl-heptan-1-one Drug Info IC50 = 520 nM [3]
7-Mercapto-heptanoic acid biphenyl-3-ylamide Drug Info IC50 = 75 nM [8]
7-Mercapto-heptanoic acid biphenyl-4-ylamide Drug Info IC50 = 1100 nM [8]
7-Mercapto-heptanoic acid pyridin-3-ylamide Drug Info IC50 = 110 nM [8]
7-Mercapto-heptanoic acid quinolin-3-ylamide Drug Info IC50 = 72 nM [8]
7-mercapto-N-(4-phenylthiazol-2-yl)heptanamide Drug Info IC50 = 32 nM [13]
8-(Biphenyl-4-yloxy)-1,1,1-trifluoro-octan-2-one Drug Info IC50 = 2900 nM [3]
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 [4]
AZUMAMIDE B Drug Info IC50 = 3660 nM [15]
AZUMAMIDE C Drug Info IC50 = 3160 nM [15]
AZUMAMIDE E Drug Info IC50 = 2280 nM [15]
Cyclo(-L-Am7(S2Py)-A2in-L-Ala-D-Pro-) Drug Info IC50 = 1.6 nM [12]
Cyclo(-L-Am7(S2Py)-Aib-L-Ala-D-Pro-) Drug Info IC50 = 5.2 nM [12]
Cyclo(-L-Am7(S2Py)-Aib-L-Ala-D-Tic-) Drug Info IC50 = 4.2 nM [12]
Cyclo(-L-Am7(S2Py)-Aib-L-Ph5-D-Pro-) Drug Info IC50 = 2.7 nM [12]
Cyclo(-L-Am7(S2Py)-Aib-L-Phg-D-Pro-) Drug Info IC50 = 56 nM [12]
Cyclo(-L-Am7(S2Py)-Aib-L-Ser(Bzl)-D-Pro-) Drug Info IC50 = 1.6 nM [12]
Cyclo(-L-Am7(S2Py)-Aib-L-Ser-D-Pro-) Drug Info IC50 = 4 nM [12]
Cyclo(-L-Am7(S2Py)-D-2MePhe-L-Ala-D-Pro-) Drug Info IC50 = 70 nM [12]
Cyclo(-L-Am7(S2Py)-D-A1in-L-Ala-D-Pro-) Drug Info IC50 = 2.4 nM [12]
Cyclo(-L-Am7(S2Py)-L-A1in-L-Ala-D-Pro-) Drug Info IC50 = 25 nM [12]
Cyclostellettamine derivative Drug Info IC50 = 17000 nM [7]
N-(2-Mercapto-ethyl)-N'-phenyl-oxalamide Drug Info IC50 = 2800 nM [9]
N-(2-Mercapto-ethyl)-N'-phenyl-succinamide Drug Info IC50 = 12500 nM [9]
N-(5-Hydroxycarbamoyl-pentyl)-4-nitro-benzamide Drug Info IC50 = 1566 nM [4]
N-(6-Mercapto-hexyl)-benzamide Drug Info IC50 = 360 nM [8]
N-hydroxy-2,2-diphenylacetamide Drug Info IC50 = 750 nM [17]
N-hydroxy-2,2-diphenylpropanamide Drug Info IC50 = 4500 nM [17]
N-Hydroxy-4-((R)-2-phenyl-butyrylamino)-benzamide Drug Info IC50 = 68 nM [10]
N-Hydroxy-4-((S)-2-phenyl-butyrylamino)-benzamide Drug Info IC50 = 34 nM [10]
N-Hydroxy-4-(2-phenyl-butyrylamino)-benzamide Drug Info IC50 = 54 nM [10]
N-Hydroxy-4-(3-phenyl-propionylamino)-benzamide Drug Info IC50 = 110 nM [10]
N-Hydroxy-4-(4-phenyl-butyrylamino)-benzamide Drug Info IC50 = 44 nM [10]
N-Hydroxy-4-(5-phenyl-pentanoylamino)-benzamide Drug Info IC50 = 250 nM [10]
N-Hydroxy-4-(phenylacetylamino-methyl)-benzamide Drug Info IC50 = 2500 nM [5]
N-Hydroxy-4-phenylacetylamino-benzamide Drug Info IC50 = 157 nM [10]
N-hydroxy-9,10-dihydroanthracene-9-carboxamide Drug Info IC50 = 2320 nM [17]
N-hydroxy-9H-xanthene-9-carboxamide Drug Info IC50 = 250 nM [17]
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 [4]
ST-2987 Drug Info IC50 = 2040 nM [16]
ST-3050 Drug Info IC50 = 16100 nM [16]
Action against Disease Model Romidepsin Drug Info Inhibitors of histone deacetylase (HDAC) de-repress genes that subsequently result in growth inhibition, differentiation and apoptosis of cancer cells. Vorinostat (SAHA), romidepsin (depsipeptide, FK-228), belinostat (PXD101) and LAQ824/LBH589 have demonstrated therapeutic benefit as monotherapy in cutaneous T-cell lymphoma (CTCL) and have also demonstrated some therapeutic benefit in other malignancies. [20]
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 Heterocyclic ketones as inhibitors of histone deacetylase. Bioorg Med Chem Lett. 2003 Nov 17;13(22):3909-13.
REF 4 Histone deacetylase inhibitors. J Med Chem. 2003 Nov 20;46(24):5097-116.
REF 5 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 6 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 7 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 8 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 9 Mercaptoamide-based non-hydroxamic acid type histone deacetylase inhibitors. Bioorg Med Chem Lett. 2005 Apr 15;15(8):1969-72.
REF 10 Structure-based optimization of phenylbutyrate-derived histone deacetylase inhibitors. J Med Chem. 2005 Aug 25;48(17):5530-5.
REF 11 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 12 Molecular design of histone deacetylase inhibitors by aromatic ring shifting in chlamydocin framework. Bioorg Med Chem. 2007 Dec 15;15(24):7830-9.
REF 13 Design, synthesis, structure--selectivity relationship, and effect on human cancer cells of a novel series of histone deacetylase 6-selective inhib... J Med Chem. 2007 Nov 1;50(22):5425-38.
REF 14 New sulfurated derivatives of valproic acid with enhanced histone deacetylase inhibitory activity. Bioorg Med Chem Lett. 2008 Mar 15;18(6):1893-7.
REF 15 Evaluation of antiangiogenic activity of azumamides by the in vitro vascular organization model using mouse induced pluripotent stem (iPS) cells. Bioorg Med Chem Lett. 2008 May 1;18(9):2982-4.
REF 16 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 17 Diphenylmethylene hydroxamic acids as selective class IIa histone deacetylase inhibitors. Bioorg Med Chem Lett. 2009 Oct 1;19(19):5684-8.
REF 18 Synthesis and biological characterization of the histone deacetylase inhibitor largazole and C7- modified analogues. J Med Chem. 2010 Jun 24;53(12):4654-67.
REF 19 Anticancer activities of histone deacetylase inhibitors. Nat Rev Drug Discov. 2006 Sep;5(9):769-84.
REF 20 HDAC inhibitors: clinical update and mechanism-based potential. Biochem Pharmacol. 2007 Sep 1;74(5):659-71.

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