Target Validation Information
TTD ID T68547
Target Name Histone deacetylase 1 (HDAC1)
Type of Target
Successful
Drug Potency against Target Vorinostat Drug Info IC50 = 106 nM [41]
Romidepsin Drug Info IC50 = 36 nM [8]
(E)-8-Biphenyl-4-yl-1-oxazol-2-yl-oct-7-en-1-one Drug Info IC50 = 990 nM [7]
1,1,1-Trifluoro-8-(4-phenoxy-phenoxy)-octan-2-one Drug Info IC50 = 3400 nM [4]
1,1,1-Trifluoro-8-phenoxy-octan-2-one Drug Info IC50 = 8000 nM [4]
2-(methylsulfonylthio)ethyl 2-propylpentanoate Drug Info IC50 = 9600 nM [25]
4-Benzenesulfonylamino-N-hydroxy-benzamide Drug Info IC50 = 900 nM [1]
4-Benzoylamino-N-hydroxy-benzamide Drug Info IC50 = 210 nM [15]
4-Butyrylamino-N-hydroxy-benzamide Drug Info IC50 = 1500 nM [9]
4-Chloro-N-(5-hydroxycarbamoyl-pentyl)-benzamide Drug Info IC50 = 369 nM [8]
4-Dimethylamino-N-(6-mercapto-hexyl)-benzamide Drug Info IC50 = 610 nM [13]
4-Hydroxy-N-(5-hydroxycarbamoyl-pentyl)-benzamide Drug Info IC50 = 149 nM [2]
4-Phenylbutyrohydroxamic acid Drug Info Ki = 295 nM [35]
4-tert-butyl-N-hydroxybenzamide Drug Info IC50 = 715 nM [19]
5-(4-Chloro-phenyl)-pentanoic acid hydroxyamide Drug Info IC50 = 2580 nM [10]
5-(4-hydroxyphenyl)-3H-1,2-dithiole-3-thione Drug Info IC50 = 450 nM [25]
5-Mercapto-pentanoic acid phenylamide Drug Info IC50 = 6200 nM [13]
6-(3-Benzoyl-ureido)-hexanoic acid hydroxyamide Drug Info IC50 = 2210 nM [38]
6-(9H-carbazol-9-yl)-N-hydroxyhexanamide Drug Info IC50 = 3074 nM [40]
6-benzenesulfinylhexanoic acid hydroxamide Drug Info IC50 = 60 nM [16]
6-benzenesulfonylhexanoic acid hydroxamide Drug Info IC50 = 40 nM [16]
6-Mercapto-hexanoic acid phenylamide Drug Info IC50 = 370 nM [13]
6-Phenoxy-hexane-1-thiol Drug Info IC50 = 11000 nM [13]
6-phenylsulfanylhexanoic acid hydroxamide Drug Info IC50 = 120 nM [16]
7-(1H-indol-5-yloxy)-N-hydroxyheptanamide Drug Info IC50 = 3.6 nM [17]
7-(3-Benzoyl-ureido)-heptanoic acid hydroxyamide Drug Info IC50 = 2680 nM [38]
7-(4-(dimethylamino)phenoxy)-N-hydroxyheptanamide Drug Info IC50 = 18.8 nM [17]
7-(Biphenyl-3-yloxy)-1-oxazol-2-yl-heptan-1-one Drug Info IC50 = 620 nM [7]
7-(Biphenyl-4-yloxy)-1,1,1-trifluoro-heptan-2-one Drug Info IC50 = 2600 nM [4]
7-(Biphenyl-4-yloxy)-1-oxazol-2-yl-heptan-1-one Drug Info IC50 = 1100 nM [7]
7-(Naphthalen-2-yloxy)-1-oxazol-2-yl-heptan-1-one Drug Info IC50 = 520 nM [7]
7-Biphenyl-4-yl-heptanoic acid hydroxyamide Drug Info IC50 = 58 nM [6]
7-Mercapto-heptanoic acid benzothiazol-2-ylamide Drug Info IC50 = 340 nM [13]
7-Mercapto-heptanoic acid biphenyl-3-ylamide Drug Info IC50 = 75 nM [13]
7-Mercapto-heptanoic acid biphenyl-4-ylamide Drug Info IC50 = 1100 nM [13]
7-Mercapto-heptanoic acid pyridin-3-ylamide Drug Info IC50 = 110 nM [13]
7-Mercapto-heptanoic acid quinolin-3-ylamide Drug Info IC50 = 72 nM [13]
7-mercapto-N-(4-phenylthiazol-2-yl)heptanamide Drug Info IC50 = 48 nM [21]
7-Phenoxy-heptanoic acid hydroxyamide Drug Info IC50 = 330 nM [6]
8-(3-Benzoyl-ureido)-octanoic acid hydroxyamide Drug Info IC50 = 8280 nM [38]
8-(4-bromophenyl)-N-hydroxy-8-oxooctanamide Drug Info IC50 = 45 nM [31]
8-(Biphenyl-3-yloxy)-1,1,1-trifluoro-octan-2-one Drug Info IC50 = 2800 nM [4]
8-(biphenyl-4-yl)-N-hydroxy-8-oxooctanamide Drug Info IC50 = 5 nM [31]
8-(Biphenyl-4-yloxy)-1,1,1-trifluoro-octan-2-one Drug Info IC50 = 2900 nM [4]
8-(Biphenyl-4-yloxy)-2-oxo-octanoic acid Drug Info IC50 = 3.7 nM [5]
8-Mercapto-octanoic acid phenylamide Drug Info IC50 = 1500 nM [13]
8-Oxo-8-phenyl-octanoic acid Drug Info IC50 = 270 nM [2]
8-Phenyl-octanoic acid hydroxyamide Drug Info IC50 = 560 nM [6]
9,9,9-Trifluoro-8-oxo-nonanoic acid phenylamide Drug Info IC50 = 6700 nM [4]
ADS-100380 Drug Info IC50 = 750 nM [18]
ADS-102550 Drug Info IC50 = 29 nM [18]
Azithromycin-N-benzyltriazolyldecahydroxamic Acid Drug Info IC50 = 226.7 nM [30]
Azithromycin-N-benzyltriazolylhexahydroxamic Acid Drug Info IC50 = 91.6 nM [30]
Azithromycin-N-benzyltriazolylnonahydroxamic Acid Drug Info IC50 = 145.5 nM [30]
Azithromycin-N-benzyltriazolyloctahydroxamic Acid Drug Info IC50 = 58.9 nM [30]
Azithromycinarylalkylhydroxamic Acid Drug Info IC50 = 107.1 nM [30]
AZUMAMIDE B Drug Info IC50 = 1830 nM [26]
AZUMAMIDE C Drug Info IC50 = 1170 nM [26]
AZUMAMIDE E Drug Info IC50 = 1220 nM [26]
Cyclo(-L-Am7(S2Py)-A2in-L-Ala-D-Pro-) Drug Info IC50 = 2 nM [20]
Cyclo(-L-Am7(S2Py)-Aib-L-Ala-D-Pro-) Drug Info IC50 = 9.4 nM [20]
Cyclo(-L-Am7(S2Py)-Aib-L-Ala-D-Tic-) Drug Info IC50 = 4.7 nM [20]
Cyclo(-L-Am7(S2Py)-Aib-L-Ph4-D-Pro-) Drug Info IC50 = 6.2 nM [20]
Cyclo(-L-Am7(S2Py)-Aib-L-Ph5-D-Pro-) Drug Info IC50 = 5.3 nM [20]
Cyclo(-L-Am7(S2Py)-Aib-L-Phe-D-Pro-) Drug Info IC50 = 3.9 nM [20]
Cyclo(-L-Am7(S2Py)-Aib-L-Phg-D-Pro-) Drug Info IC50 = 88 nM [20]
Cyclo(-L-Am7(S2Py)-Aib-L-Ser(Bzl)-D-Pro-) Drug Info IC50 = 3.2 nM [20]
Cyclo(-L-Am7(S2Py)-Aib-L-Ser-D-Pro-) Drug Info IC50 = 6.4 nM [20]
Cyclo(-L-Am7(S2Py)-D-2MePhe-L-Ala-D-Pro-) Drug Info IC50 = 170 nM [20]
Cyclo(-L-Am7(S2Py)-D-A1in-L-Ala-D-Pro-) Drug Info IC50 = 2.7 nM [20]
Cyclo(-L-Am7(S2Py)-L-2MePhe-L-Ala-D-Pro-) Drug Info IC50 = 3.7 nM [20]
Cyclo(-L-Am7(S2Py)-L-A1in-L-Ala-D-Pro-) Drug Info IC50 = 36 nM [20]
Cyclostellettamine derivative Drug Info IC50 = 17000 nM [11]
Desclasinose Azithromycinarylalkyl Hydroxamate Drug Info IC50 = 109.8 nM [30]
Gymnochrome E Drug Info IC50 = 10900 nM [37]
LARGAZOLE Drug Info IC50 = 11.4 nM [39]
N,8-dihydroxy-8-(naphthalen-2-yl)octanamide Drug Info IC50 = 35 nM [31]
N-(2,3-Dimethylphenyl)-N'-hydroxyoctanediamide Drug Info IC50 = 1110 nM [36]
N-(2,4-Dimethylphenyl)-N'-hydroxyoctanediamide Drug Info IC50 = 638 nM [36]
N-(2,5-Dimethylphenyl)-N'-hydroxyoctanediamide Drug Info IC50 = 1142 nM [36]
N-(2,6-Dimethylphenyl)-N'-hydroxyoctanediamide Drug Info IC50 = 11614 nM [36]
N-(2-amino-5-(thiophen-2-yl)phenyl)nicotinamide Drug Info IC50 = 65 nM [27]
N-(2-aminophenyl)-4-(chroman-3-ylmethyl)benzamide Drug Info IC50 = 1000 nM [23]
N-(2-aminophenyl)-4-methoxybenzamide Drug Info IC50 = 2000 nM [22]
N-(2-aminophenyl)nicotinamide Drug Info IC50 = 2630 nM [27]
N-(2-aminophenyl)quinoxaline-6-carboxamide Drug Info IC50 = 2000 nM [22]
N-(2-Ethylphenyl)-N'-hydroxyoctanediamide Drug Info IC50 = 1101 nM [36]
N-(2-Mercapto-ethyl)-N'-phenyl-oxalamide Drug Info IC50 = 2800 nM [14]
N-(2-Mercapto-ethyl)-N'-phenyl-succinamide Drug Info IC50 = 12500 nM [14]
N-(3,4-Dimethylphenyl)-N'-hydroxyoctanediamide Drug Info IC50 = 30 nM [36]
N-(3,5-Dimethylphenyl)-N'-hydroxyoctanediamide Drug Info IC50 = 17 nM [36]
N-(3-Ethylphenyl)-N'-hydroxyoctanediamide Drug Info IC50 = 27 nM [36]
N-(4-aminobiphenyl-3-yl)nicotinamide Drug Info IC50 = 48 nM [27]
N-(4-Ethylphenyl)-N'-hydroxyoctanediamide Drug Info IC50 = 149 nM [36]
N-(4-hydroxybiphenyl-3-yl)benzamide Drug Info IC50 = 58 nM [27]
N-(5-Hydroxycarbamoyl-pentyl)-4-nitro-benzamide Drug Info IC50 = 1566 nM [8]
N-(6-Hydroxycarbamoyl-hexyl)-benzamide Drug Info IC50 = 568 nM [2]
N-(6-Mercapto-hexyl)-benzamide Drug Info IC50 = 360 nM [13]
N-hydroxy-2,2'-bithiophene-5-carboxamide Drug Info IC50 = 2500 nM [18]
N-Hydroxy-4-((R)-2-phenyl-butyrylamino)-benzamide Drug Info IC50 = 68 nM [15]
N-Hydroxy-4-((S)-2-phenyl-butyrylamino)-benzamide Drug Info IC50 = 34 nM [15]
N-Hydroxy-4-(2-phenyl-butyrylamino)-benzamide Drug Info IC50 = 54 nM [15]
N-Hydroxy-4-(3-phenyl-propionylamino)-benzamide Drug Info IC50 = 1100 nM [34]
N-Hydroxy-4-(4-phenyl-butyrylamino)-benzamide Drug Info IC50 = 44 nM [15]
N-Hydroxy-4-(5-phenyl-pentanoylamino)-benzamide Drug Info IC50 = 250 nM [15]
N-Hydroxy-4-(pentanoylamino-methyl)-benzamide Drug Info IC50 = 3600 nM [9]
N-Hydroxy-4-(phenylacetylamino-methyl)-benzamide Drug Info IC50 = 2500 nM [9]
N-Hydroxy-4-phenylacetylamino-benzamide Drug Info IC50 = 157 nM [15]
N-hydroxy-5-(pyridin-2-yl)thiophene-2-carboxamide Drug Info IC50 = 243 nM [18]
N-hydroxy-5-(pyridin-3-yl)thiophene-2-carboxamide Drug Info IC50 = 1130 nM [18]
N-hydroxy-5-(pyridin-4-yl)thiophene-2-carboxamide Drug Info IC50 = 1260 nM [18]
N-hydroxy-5-phenylthiophene-2-carboxamide Drug Info IC50 = 900 nM [18]
N-hydroxy-6-oxo-6-phenylhexanamide Drug Info IC50 = 1500 nM [31]
N-hydroxy-7-(4-methoxyphenyl)-7-oxoheptanamide Drug Info IC50 = 450 nM [31]
N-hydroxy-7-(naphthalen-2-yl)-7-oxoheptanamide Drug Info IC50 = 35 nM [31]
N-hydroxy-7-(naphthalen-2-yloxy)heptanamide Drug Info IC50 = 0.9 nM [17]
N-hydroxy-7-oxo-7-phenylheptanamide Drug Info IC50 = 500 nM [31]
N-hydroxy-8-(2-methoxyphenyl)-8-oxooctanamide Drug Info IC50 = 95 nM [31]
N-hydroxy-8-(4-methoxyphenyl)-8-oxooctanamide Drug Info IC50 = 15 nM [31]
N-hydroxy-8-(naphthalen-2-yl)non-8-enamide Drug Info IC50 = 8 nM [31]
N-hydroxy-8-(naphthalen-2-yl)oct-7-enamide Drug Info IC50 = 6 nM [31]
N-hydroxy-8-(naphthalen-2-yl)octanamide Drug Info IC50 = 25 nM [31]
N-hydroxy-8-oxo-8-(pyridin-3-yl)octanamide Drug Info IC50 = 153 nM [31]
N-hydroxy-9-oxo-9-phenylnonanamide Drug Info IC50 = 135 nM [31]
N-Hydroxy-N'-(2-methylphenyl)octanediamide Drug Info IC50 = 576 nM [36]
N-Hydroxy-N'-(3-methylphenyl)octanediamide Drug Info IC50 = 57 nM [36]
N-Hydroxy-N'-(4-methoxyphenyl)octanediamide Drug Info IC50 = 71 nM [36]
N-Hydroxy-N'-(4-methylphenyl)octanediamide Drug Info IC50 = 76 nM [36]
N-hydroxybenzo[b]thiophene-2-carboxamide Drug Info IC50 = 672 nM [24]
N1-(biphenyl-3-yl)-N8-hydroxyoctanediamide Drug Info IC50 = 9 nM [29]
N1-(biphenyl-4-yl)-N8-hydroxyoctanediamide Drug Info IC50 = 33 nM [33]
N1-hydroxy-N8-(4-phenylthiazol-2-yl)octanediamide Drug Info IC50 = 3 nM [33]
NSC-746457 Drug Info IC50 = 104 nM [28]
Octanedioic acid bis-hydroxyamide Drug Info IC50 = 1150 nM [3]
Octanedioic acid hydroxyamide pyridin-2-ylamide Drug Info IC50 = 248 nM [2]
Octanedioic acid hydroxyamide pyridin-4-ylamide Drug Info IC50 = 306 nM [2]
PSAMMAPLIN A Drug Info IC50 = 4 nM [8]
SK-683 Drug Info IC50 = 1 nM [12]
ST-2986 Drug Info IC50 = 5480 nM [32]
ST-2987 Drug Info IC50 = 790 nM [32]
ST-3050 Drug Info IC50 = 3060 nM [32]
Tacedinaline Drug Info Ki = 50 nM [35]
Action against Disease Model Vorinostat Drug Info IC50 on cutaneous T-cell lymphoma HH: about 800nM/L [42]
References
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REF 25 New sulfurated derivatives of valproic acid with enhanced histone deacetylase inhibitory activity. Bioorg Med Chem Lett. 2008 Mar 15;18(6):1893-7.
REF 26 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 27 Bioorg Med Chem Lett. 2008 Dec 1;18(23):6104-9. Epub 2008 Oct 14.SAR profiles of spirocyclic nicotinamide derived selective HDAC1/HDAC2 inhibitors (SHI-1:2).
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