Target Validation Information
Target ID T68547
Target Name Histone deacetylase 1
Target Type
Successful
Drug Potency against Target Octanedioic acid bis-hydroxyamide Drug Info IC50 = 1150 nM [526376]
7-(3-Benzoyl-ureido)-heptanoic acid hydroxyamide Drug Info IC50 = 2680 nM [530898]
6-(3-Benzoyl-ureido)-hexanoic acid hydroxyamide Drug Info IC50 = 2210 nM [530898]
N-Hydroxy-4-(phenylacetylamino-methyl)-benzamide Drug Info IC50 = 2500 nM [526922]
Azithromycinarylalkylhydroxamic Acid Drug Info IC50 = 107.1 nM [529875]
Azithromycin-N-benzyltriazolylnonahydroxamic Acid Drug Info IC50 = 145.5 nM [529875]
4-Phenylbutyrohydroxamic acid Drug Info Ki = 295 nM [530700]
Cyclostellettamine derivative Drug Info IC50 = 17000 nM [527058]
N-Hydroxy-4-(pentanoylamino-methyl)-benzamide Drug Info IC50 = 3600 nM [526922]
Desclasinose Azithromycinarylalkyl Hydroxamate Drug Info IC50 = 109.8 nM [529875]
4-Dimethylamino-N-(6-mercapto-hexyl)-benzamide Drug Info IC50 = 610 nM [527439]
Octanedioic acid hydroxyamide pyridin-2-ylamide Drug Info IC50 = 248 nM [526266]
5-(4-hydroxyphenyl)-3H-1,2-dithiole-3-thione Drug Info IC50 = 450 nM [529333]
Octanedioic acid hydroxyamide pyridin-4-ylamide Drug Info IC50 = 306 nM [526266]
7-(Biphenyl-4-yloxy)-1-oxazol-2-yl-heptan-1-one Drug Info IC50 = 1100 nM [526871]
N-Hydroxy-4-(2-phenyl-butyrylamino)-benzamide Drug Info IC50 = 54 nM [527691]
Azithromycin-N-benzyltriazolyldecahydroxamic Acid Drug Info IC50 = 226.7 nM [529875]
Azithromycin-N-benzyltriazolyloctahydroxamic Acid Drug Info IC50 = 58.9 nM [529875]
NSC-746457 Drug Info IC50 = 104 nM [529805]
N-(5-Hydroxycarbamoyl-pentyl)-4-nitro-benzamide Drug Info IC50 = 1566 nM [526878]
Vorinostat Drug Info IC50 = 106 nM [536272]
N-(2-Ethylphenyl)-N'-hydroxyoctanediamide Drug Info IC50 = 1101 nM [530704]
7-Mercapto-heptanoic acid biphenyl-4-ylamide Drug Info IC50 = 1100 nM [527439]
N-(2-aminophenyl)nicotinamide Drug Info IC50 = 2630 nM [529767]
4-Hydroxy-N-(5-hydroxycarbamoyl-pentyl)-benzamide Drug Info IC50 = 149 nM [526266]
N-(3,4-Dimethylphenyl)-N'-hydroxyoctanediamide Drug Info IC50 = 30 nM [530704]
N-(3,5-Dimethylphenyl)-N'-hydroxyoctanediamide Drug Info IC50 = 17 nM [530704]
N-Hydroxy-N'-(4-methoxyphenyl)octanediamide Drug Info IC50 = 71 nM [530704]
N-(4-Ethylphenyl)-N'-hydroxyoctanediamide Drug Info IC50 = 149 nM [530704]
N-(4-hydroxybiphenyl-3-yl)benzamide Drug Info IC50 = 58 nM [529767]
N-Hydroxy-4-(5-phenyl-pentanoylamino)-benzamide Drug Info IC50 = 250 nM [527691]
7-(1H-indol-5-yloxy)-N-hydroxyheptanamide Drug Info IC50 = 3.6 nM [528478]
N-hydroxy-7-(naphthalen-2-yloxy)heptanamide Drug Info IC50 = 0.9 nM [528478]
7-(4-(dimethylamino)phenoxy)-N-hydroxyheptanamide Drug Info IC50 = 18.8 nM [528478]
N-(2-aminophenyl)-4-(chroman-3-ylmethyl)benzamide Drug Info IC50 = 1000 nM [529129]
8-(3-Benzoyl-ureido)-octanoic acid hydroxyamide Drug Info IC50 = 8280 nM [530898]
6-benzenesulfinylhexanoic acid hydroxamide Drug Info IC50 = 60 nM [527980]
N-hydroxybenzo[b]thiophene-2-carboxamide Drug Info IC50 = 672 nM [529285]
N-Hydroxy-4-(3-phenyl-propionylamino)-benzamide Drug Info IC50 = 1100 nM [530261]
N1-hydroxy-N8-(4-phenylthiazol-2-yl)octanediamide Drug Info IC50 = 3 nM [530106]
ST-3050 Drug Info IC50 = 3060 nM [530016]
6-Phenoxy-hexane-1-thiol Drug Info IC50 = 11000 nM [527439]
6-Mercapto-hexanoic acid phenylamide Drug Info IC50 = 370 nM [527439]
7-Mercapto-heptanoic acid pyridin-3-ylamide Drug Info IC50 = 110 nM [527439]
7-Biphenyl-4-yl-heptanoic acid hydroxyamide Drug Info IC50 = 58 nM [526847]
ST-2986 Drug Info IC50 = 5480 nM [530016]
6-(9H-carbazol-9-yl)-N-hydroxyhexanamide Drug Info IC50 = 3074 nM [531216]
N-(2-aminophenyl)quinoxaline-6-carboxamide Drug Info IC50 = 2000 nM [529104]
4-tert-butyl-N-hydroxybenzamide Drug Info IC50 = 715 nM [528882]
4-Benzenesulfonylamino-N-hydroxy-benzamide Drug Info IC50 = 900 nM [526165]
N-Hydroxy-4-((S)-2-phenyl-butyrylamino)-benzamide Drug Info IC50 = 34 nM [527691]
1,1,1-Trifluoro-8-(4-phenoxy-phenoxy)-octan-2-one Drug Info IC50 = 3400 nM [526450]
8-Oxo-8-phenyl-octanoic acid Drug Info IC50 = 270 nM [526266]
7-(Naphthalen-2-yloxy)-1-oxazol-2-yl-heptan-1-one Drug Info IC50 = 520 nM [526871]
ADS-100380 Drug Info IC50 = 750 nM [528523]
8-(Biphenyl-3-yloxy)-1,1,1-trifluoro-octan-2-one Drug Info IC50 = 2800 nM [526450]
N-hydroxy-2,2'-bithiophene-5-carboxamide Drug Info IC50 = 2500 nM [528523]
8-(Biphenyl-4-yloxy)-1,1,1-trifluoro-octan-2-one Drug Info IC50 = 2900 nM [526450]
Gymnochrome E Drug Info IC50 = 10900 nM [530729]
8-Mercapto-octanoic acid phenylamide Drug Info IC50 = 1500 nM [527439]
8-Phenyl-octanoic acid hydroxyamide Drug Info IC50 = 560 nM [526847]
N-(2-aminophenyl)-4-methoxybenzamide Drug Info IC50 = 2000 nM [529104]
N-(6-Mercapto-hexyl)-benzamide Drug Info IC50 = 360 nM [527439]
N-(6-Hydroxycarbamoyl-hexyl)-benzamide Drug Info IC50 = 568 nM [526266]
4-Benzoylamino-N-hydroxy-benzamide Drug Info IC50 = 210 nM [527691]
5-(4-Chloro-phenyl)-pentanoic acid hydroxyamide Drug Info IC50 = 2580 nM [527056]
AZUMAMIDE C Drug Info IC50 = 1170 nM [529411]
Cyclo(-L-Am7(S2Py)-L-A1in-L-Ala-D-Pro-) Drug Info IC50 = 36 nM [529054]
Cyclo(-L-Am7(S2Py)-Aib-L-Ala-D-Tic-) Drug Info IC50 = 4.7 nM [529054]
Cyclo(-L-Am7(S2Py)-Aib-L-Phg-D-Pro-) Drug Info IC50 = 88 nM [529054]
Cyclo(-L-Am7(S2Py)-Aib-L-Ph5-D-Pro-) Drug Info IC50 = 5.3 nM [529054]
5-Mercapto-pentanoic acid phenylamide Drug Info IC50 = 6200 nM [527439]
Cyclo(-L-Am7(S2Py)-D-A1in-L-Ala-D-Pro-) Drug Info IC50 = 2.7 nM [529054]
N-(2-Mercapto-ethyl)-N'-phenyl-oxalamide Drug Info IC50 = 2800 nM [527500]
6-phenylsulfanylhexanoic acid hydroxamide Drug Info IC50 = 120 nM [527980]
N-(2-Mercapto-ethyl)-N'-phenyl-succinamide Drug Info IC50 = 12500 nM [527500]
7-mercapto-N-(4-phenylthiazol-2-yl)heptanamide Drug Info IC50 = 48 nM [529093]
7-Mercapto-heptanoic acid quinolin-3-ylamide Drug Info IC50 = 72 nM [527439]
7-(Biphenyl-3-yloxy)-1-oxazol-2-yl-heptan-1-one Drug Info IC50 = 620 nM [526871]
N1-(biphenyl-3-yl)-N8-hydroxyoctanediamide Drug Info IC50 = 9 nM [529866]
N-Hydroxy-4-phenylacetylamino-benzamide Drug Info IC50 = 157 nM [527691]
(E)-8-Biphenyl-4-yl-1-oxazol-2-yl-oct-7-en-1-one Drug Info IC50 = 990 nM [526871]
9,9,9-Trifluoro-8-oxo-nonanoic acid phenylamide Drug Info IC50 = 6700 nM [526450]
1,1,1-Trifluoro-8-phenoxy-octan-2-one Drug Info IC50 = 8000 nM [526450]
N-Hydroxy-4-((R)-2-phenyl-butyrylamino)-benzamide Drug Info IC50 = 68 nM [527691]
N-Hydroxy-4-(4-phenyl-butyrylamino)-benzamide Drug Info IC50 = 44 nM [527691]
Cyclo(-L-Am7(S2Py)-Aib-L-Ser(Bzl)-D-Pro-) Drug Info IC50 = 3.2 nM [529054]
7-Mercapto-heptanoic acid biphenyl-3-ylamide Drug Info IC50 = 75 nM [527439]
ST-2987 Drug Info IC50 = 790 nM [530016]
N-(2,4-Dimethylphenyl)-N'-hydroxyoctanediamide Drug Info IC50 = 638 nM [530704]
Cyclo(-L-Am7(S2Py)-A2in-L-Ala-D-Pro-) Drug Info IC50 = 2 nM [529054]
Cyclo(-L-Am7(S2Py)-D-2MePhe-L-Ala-D-Pro-) Drug Info IC50 = 170 nM [529054]
Cyclo(-L-Am7(S2Py)-Aib-L-Ser-D-Pro-) Drug Info IC50 = 6.4 nM [529054]
Cyclo(-L-Am7(S2Py)-L-2MePhe-L-Ala-D-Pro-) Drug Info IC50 = 3.7 nM [529054]
Cyclo(-L-Am7(S2Py)-Aib-L-Phe-D-Pro-) Drug Info IC50 = 3.9 nM [529054]
Cyclo(-L-Am7(S2Py)-Aib-L-Ala-D-Pro-) Drug Info IC50 = 9.4 nM [529054]
6-benzenesulfonylhexanoic acid hydroxamide Drug Info IC50 = 40 nM [527980]
N1-(biphenyl-4-yl)-N8-hydroxyoctanediamide Drug Info IC50 = 33 nM [530106]
LARGAZOLE Drug Info IC50 = 11.4 nM [530933]
7-Mercapto-heptanoic acid benzothiazol-2-ylamide Drug Info IC50 = 340 nM [527439]
2-(methylsulfonylthio)ethyl 2-propylpentanoate Drug Info IC50 = 9600 nM [529333]
4-Butyrylamino-N-hydroxy-benzamide Drug Info IC50 = 1500 nM [526922]
PSAMMAPLIN A Drug Info IC50 = 4 nM [526878]
N-hydroxy-9-oxo-9-phenylnonanamide Drug Info IC50 = 135 nM [529911]
4-Chloro-N-(5-hydroxycarbamoyl-pentyl)-benzamide Drug Info IC50 = 369 nM [526878]
8-(biphenyl-4-yl)-N-hydroxy-8-oxooctanamide Drug Info IC50 = 5 nM [529911]
N,8-dihydroxy-8-(naphthalen-2-yl)octanamide Drug Info IC50 = 35 nM [529911]
ADS-102550 Drug Info IC50 = 29 nM [528523]
N-hydroxy-5-(pyridin-2-yl)thiophene-2-carboxamide Drug Info IC50 = 243 nM [528523]
Romidepsin Drug Info IC50 = 36 nM [526878]
Tacedinaline Drug Info Ki = 50 nM [530700]
N-hydroxy-5-(pyridin-4-yl)thiophene-2-carboxamide Drug Info IC50 = 1260 nM [528523]
N-hydroxy-5-phenylthiophene-2-carboxamide Drug Info IC50 = 900 nM [528523]
AZUMAMIDE E Drug Info IC50 = 1220 nM [529411]
N-(4-aminobiphenyl-3-yl)nicotinamide Drug Info IC50 = 48 nM [529767]
N-hydroxy-7-(naphthalen-2-yl)-7-oxoheptanamide Drug Info IC50 = 35 nM [529911]
N-hydroxy-8-(naphthalen-2-yl)oct-7-enamide Drug Info IC50 = 6 nM [529911]
N-(2-amino-5-(thiophen-2-yl)phenyl)nicotinamide Drug Info IC50 = 65 nM [529767]
N-hydroxy-7-(4-methoxyphenyl)-7-oxoheptanamide Drug Info IC50 = 450 nM [529911]
N-(2,5-Dimethylphenyl)-N'-hydroxyoctanediamide Drug Info IC50 = 1142 nM [530704]
Cyclo(-L-Am7(S2Py)-Aib-L-Ph4-D-Pro-) Drug Info IC50 = 6.2 nM [529054]
N-(3-Ethylphenyl)-N'-hydroxyoctanediamide Drug Info IC50 = 27 nM [530704]
N-hydroxy-8-oxo-8-(pyridin-3-yl)octanamide Drug Info IC50 = 153 nM [529911]
N-(2,3-Dimethylphenyl)-N'-hydroxyoctanediamide Drug Info IC50 = 1110 nM [530704]
N-hydroxy-8-(naphthalen-2-yl)octanamide Drug Info IC50 = 25 nM [529911]
N-(2,6-Dimethylphenyl)-N'-hydroxyoctanediamide Drug Info IC50 = 11614 nM [530704]
N-hydroxy-8-(naphthalen-2-yl)non-8-enamide Drug Info IC50 = 8 nM [529911]
N-hydroxy-6-oxo-6-phenylhexanamide Drug Info IC50 = 1500 nM [529911]
7-Phenoxy-heptanoic acid hydroxyamide Drug Info IC50 = 330 nM [526847]
N-hydroxy-8-(4-methoxyphenyl)-8-oxooctanamide Drug Info IC50 = 15 nM [529911]
N-hydroxy-7-oxo-7-phenylheptanamide Drug Info IC50 = 500 nM [529911]
8-(4-bromophenyl)-N-hydroxy-8-oxooctanamide Drug Info IC50 = 45 nM [529911]
N-Hydroxy-N'-(2-methylphenyl)octanediamide Drug Info IC50 = 576 nM [530704]
N-Hydroxy-N'-(3-methylphenyl)octanediamide Drug Info IC50 = 57 nM [530704]
N-hydroxy-8-(2-methoxyphenyl)-8-oxooctanamide Drug Info IC50 = 95 nM [529911]
N-Hydroxy-N'-(4-methylphenyl)octanediamide Drug Info IC50 = 76 nM [530704]
Azithromycin-N-benzyltriazolylhexahydroxamic Acid Drug Info IC50 = 91.6 nM [529875]
AZUMAMIDE B Drug Info IC50 = 1830 nM [529411]
N-hydroxy-5-(pyridin-3-yl)thiophene-2-carboxamide Drug Info IC50 = 1130 nM [528523]
SK-683 Drug Info IC50 = 1 nM [527104]
7-(Biphenyl-4-yloxy)-1,1,1-trifluoro-heptan-2-one Drug Info IC50 = 2600 nM [526450]
8-(Biphenyl-4-yloxy)-2-oxo-octanoic acid Drug Info IC50 = 3.7 nM [526708]
Action against Disease Model Vorinostat IC50 on cutaneous T-cell lymphoma HH: about 800nM/L [552818] Drug Info
References
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Ref 529054Bioorg 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.
Ref 529054Bioorg 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.
Ref 529054Bioorg 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.
Ref 529054Bioorg 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.
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Ref 530704J Med Chem. 2010 Mar 11;53(5):1937-50.Biological and biophysical properties of the histone deacetylase inhibitor suberoylanilide hydroxamic acid are affected by the presence of short alkyl groups on the phenyl ring.
Ref 529054Bioorg 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.
Ref 530704J Med Chem. 2010 Mar 11;53(5):1937-50.Biological and biophysical properties of the histone deacetylase inhibitor suberoylanilide hydroxamic acid are affected by the presence of short alkyl groups on the phenyl ring.
Ref 529911Eur J Med Chem. 2009 Jul;44(7):2868-76. Epub 2008 Dec 16.3D-QSAR studies of HDACs inhibitors using pharmacophore-based alignment.
Ref 530704J Med Chem. 2010 Mar 11;53(5):1937-50.Biological and biophysical properties of the histone deacetylase inhibitor suberoylanilide hydroxamic acid are affected by the presence of short alkyl groups on the phenyl ring.
Ref 529911Eur J Med Chem. 2009 Jul;44(7):2868-76. Epub 2008 Dec 16.3D-QSAR studies of HDACs inhibitors using pharmacophore-based alignment.
Ref 530704J Med Chem. 2010 Mar 11;53(5):1937-50.Biological and biophysical properties of the histone deacetylase inhibitor suberoylanilide hydroxamic acid are affected by the presence of short alkyl groups on the phenyl ring.
Ref 529911Eur J Med Chem. 2009 Jul;44(7):2868-76. Epub 2008 Dec 16.3D-QSAR studies of HDACs inhibitors using pharmacophore-based alignment.
Ref 529911Eur J Med Chem. 2009 Jul;44(7):2868-76. Epub 2008 Dec 16.3D-QSAR studies of HDACs inhibitors using pharmacophore-based alignment.
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Ref 529911Eur J Med Chem. 2009 Jul;44(7):2868-76. Epub 2008 Dec 16.3D-QSAR studies of HDACs inhibitors using pharmacophore-based alignment.
Ref 529911Eur J Med Chem. 2009 Jul;44(7):2868-76. Epub 2008 Dec 16.3D-QSAR studies of HDACs inhibitors using pharmacophore-based alignment.
Ref 530704J Med Chem. 2010 Mar 11;53(5):1937-50.Biological and biophysical properties of the histone deacetylase inhibitor suberoylanilide hydroxamic acid are affected by the presence of short alkyl groups on the phenyl ring.
Ref 530704J Med Chem. 2010 Mar 11;53(5):1937-50.Biological and biophysical properties of the histone deacetylase inhibitor suberoylanilide hydroxamic acid are affected by the presence of short alkyl groups on the phenyl ring.
Ref 529911Eur J Med Chem. 2009 Jul;44(7):2868-76. Epub 2008 Dec 16.3D-QSAR studies of HDACs inhibitors using pharmacophore-based alignment.
Ref 530704J Med Chem. 2010 Mar 11;53(5):1937-50.Biological and biophysical properties of the histone deacetylase inhibitor suberoylanilide hydroxamic acid are affected by the presence of short alkyl groups on the phenyl ring.
Ref 529875J Med Chem. 2009 Jan 22;52(2):456-68.Non-peptide macrocyclic histone deacetylase inhibitors.
Ref 529411Bioorg Med Chem Lett. 2008 May 1;18(9):2982-4. Epub 2008 Mar 21.Evaluation of antiangiogenic activity of azumamides by the in vitro vascular organization model using mouse induced pluripotent stem (iPS) cells.
Ref 528523Bioorg Med Chem Lett. 2007 Jan 15;17(2):363-9. Epub 2006 Oct 24.Identification and optimisation of a series of substituted 5-pyridin-2-yl-thiophene-2-hydroxamic acids as potent histone deacetylase (HDAC) inhibitors.
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Ref 526450Bioorg Med Chem Lett. 2002 Dec 2;12(23):3443-7.Trifluoromethyl ketones as inhibitors of histone deacetylase.
Ref 526708Bioorg Med Chem Lett. 2003 Oct 6;13(19):3331-5.Alpha-keto amides as inhibitors of histone deacetylase.

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