General Information of Drug Therapeutic Target (DTT) (ID: TTBH0VX)

DTT Name Histone deacetylase (HDAC)
Synonyms Human histone deacetylase
Gene Name HDAC
DTT Type
Successful target
[1]
UniProt ID
NOUNIPROTAC
TTD ID
T65755
Function
Responsible for the deacetylation of lysine residues on the n-terminal part of the core histones (H2a, H2b, H3 and H4). Histone deacetylation givesa tag for epigenetic repression and plays an important role in transcriptional regulation.

Molecular Interaction Atlas (MIA) of This DTT

Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This DTT
3 Approved Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
Sodium phenylbutyrate DMXLBCQ Spinal muscular atrophy 8B61 Approved [2]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [1]
HBI-8000 DMDWYUN Non-small-cell lung cancer 2C25.Y Registered [3]
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26 Clinical Trial Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
Abexinostat DM91LGU Follicular lymphoma 2A80 Phase 3 [4]
CMS-024-02 DMC4X7L Solid tumour/cancer 2A00-2F9Z Phase 3 [5]
ITF2357 DMFZBNE Duchenne dystrophy 8C70 Phase 3 [6]
NVP-LAQ824 DM8JWNA Mood disorder 6A60-6E23 Phase 3 [7]
Pracinostat DMTD7AB Acute myeloid leukaemia 2A60 Phase 3 [8]
SNDX-275 DMH7W9X Breast cancer 2C60-2C65 Phase 3 [3]
APH-0812 DM756GE Human immunodeficiency virus-1 infection 1C62 Phase 2 [9]
DAC-060 DMACTBM Keratosis ED56 Phase 2 [10]
JNJ-26481585 DMKIE9C Advanced stage follicular lymphoma 2A80 Phase 2 [11]
MGCD-0103 DM726HX Non-small-cell lung cancer 2C25.Y Phase 2 [3]
PDX-101 DM6OC53 Plasma cell myeloma 2A83.1 Phase 2 [12]
Remetinostat DMJIB89 Basal cell carcinoma 2C32 Phase 2 [3]
Rocilinostat DMSTH01 Multiple myeloma 2A83 Phase 2 [13]
SHAPE DMIQB13 Cutaneous T-cell lymphoma 2B01 Phase 2 [14]
CUDC-907 DMHIQDC Acute myelogenous leukaemia 2A41 Phase 1/2 [3]
EDO-S101 DMI71FN Solid tumour/cancer 2A00-2F9Z Phase 1/2 [3]
Tinostamustine DMA4DMQ Multiple myeloma 2A83 Phase 1/2 [15]
Tractinostat DM8D2LC Lymphoma 2A80-2A86 Phase 1/2 [3]
CG-200745 DM3U2VY Solid tumour/cancer 2A00-2F9Z Phase 1 [16]
CT-200 DMW16VR Solid tumour/cancer 2A00-2F9Z Phase 1 [17]
CXD-101 DMRD2B0 Solid tumour/cancer 2A00-2F9Z Phase 1 [18]
GSK311739 DM70DYV Rhinovirus infection CA07 Phase 1 [19]
GSK3117391 DMQZSXD Rheumatoid arthritis FA20 Phase 1 [20]
OBP-801 DMPLV9G Solid tumour/cancer 2A00-2F9Z Phase 1 [3]
OKI 179 DMSJWTE Solid tumour/cancer 2A00-2F9Z Phase 1 [21]
VTR-297 DM9W0B6 Hematologic tumour 2B33.Y Phase 1 [22]
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⏷ Show the Full List of 26 Clinical Trial Drug(s)
12 Patented Agent(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
Ampicidin analog 1 DM2V31C N. A. N. A. Patented [23]
Ampicidin analog 2 DMZH8S9 N. A. N. A. Patented [23]
Aniline derivative 1 DMDSUGF N. A. N. A. Patented [24]
Indole-based analog 11 DMVRX7S N. A. N. A. Patented [24]
Oxazolyl methylthiothiazole derivative 1 DMZM6FW N. A. N. A. Patented [24]
PMID27376512-Compound-PG-11047 DM5K4YF N. A. N. A. Patented [25]
PMID27376512-Compound-PG-11048 DM3U7RN N. A. N. A. Patented [25]
PMID28092474-Compound-32 DMC4TQL N. A. N. A. Patented [26]
PMID28092474-Compound-33 DMRE6GP N. A. N. A. Patented [26]
PMID28092474-Compound-34 DM6JRCW N. A. N. A. Patented [26]
PMID29671355-Compound-53 DMCRWV3 N. A. N. A. Patented [27]
PMID29671355-Compound-69 DMU61XP N. A. N. A. Patented [27]
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⏷ Show the Full List of 12 Patented Agent(s)
1 Preclinical Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
CS-00028 DMB4FWX Solid tumour/cancer 2A00-2F9Z Preclinical [28]
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1 Discontinued Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
MKC-1313 DMAITRL Solid tumour/cancer 2A00-2F9Z Terminated [29]
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93 Investigative Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
(E)-8-Biphenyl-4-yl-1-oxazol-2-yl-oct-7-en-1-one DM5LSY9 Discovery agent N.A. Investigative [30]
2,2-bis(3-fluorophenyl)-N-hydroxyacetamide DMTODR2 Discovery agent N.A. Investigative [31]
2,2-bis(4-chlorophenyl)-N-hydroxyacetamide DM2RKD6 Discovery agent N.A. Investigative [31]
2,2-bis(4-fluorophenyl)-N-hydroxyacetamide DM5PWQM Discovery agent N.A. Investigative [31]
2-(methylsulfonylthio)ethyl 2-propylpentanoate DMM52D3 Discovery agent N.A. Investigative [32]
4-Benzoylamino-N-hydroxy-benzamide DMYBPFS Discovery agent N.A. Investigative [33]
4-Butyrylamino-N-hydroxy-benzamide DMRY6B4 Discovery agent N.A. Investigative [34]
4-Chloro-N-(5-hydroxycarbamoyl-pentyl)-benzamide DM5AVG3 Discovery agent N.A. Investigative [35]
4-Dimethylamino-N-(6-mercapto-hexyl)-benzamide DM0M8G5 Discovery agent N.A. Investigative [36]
4-Hydroxy-N-(5-hydroxycarbamoyl-pentyl)-benzamide DMULOHZ Discovery agent N.A. Investigative [35]
4-Phenylbutyrohydroxamic acid DMCZKN7 Discovery agent N.A. Investigative [37]
5-(4-Chloro-phenyl)-pentanoic acid hydroxyamide DM6CRVS Discovery agent N.A. Investigative [38]
5-(4-hydroxyphenyl)-3H-1,2-dithiole-3-thione DM7KQXL Discovery agent N.A. Investigative [32]
5-Mercapto-pentanoic acid phenylamide DMET3OJ Discovery agent N.A. Investigative [36]
6-(2-Bromo-acetylamino)-hexanoic acid phenylamide DM9LKXD Discovery agent N.A. Investigative [36]
6-benzenesulfinylhexanoic acid hydroxamide DM2I95Z Discovery agent N.A. Investigative [39]
6-benzenesulfonylhexanoic acid hydroxamide DMY9IK8 Discovery agent N.A. Investigative [39]
6-Mercapto-hexanoic acid phenylamide DMD2FW9 Discovery agent N.A. Investigative [36]
6-Phenoxy-hexane-1-thiol DMVYIN2 Discovery agent N.A. Investigative [36]
6-phenylsulfanylhexanoic acid hydroxamide DM3OLM6 Discovery agent N.A. Investigative [39]
7-(Biphenyl-3-yloxy)-1-oxazol-2-yl-heptan-1-one DMLCGSY Discovery agent N.A. Investigative [30]
7-(Biphenyl-4-yloxy)-1,1,1-trifluoro-heptan-2-one DM28GZ7 Discovery agent N.A. Investigative [40]
7-(Biphenyl-4-yloxy)-1-oxazol-2-yl-heptan-1-one DMY027P Discovery agent N.A. Investigative [30]
7-(Naphthalen-2-yloxy)-1-oxazol-2-yl-heptan-1-one DM4VQN8 Discovery agent N.A. Investigative [30]
7-Mercapto-heptanoic acid benzothiazol-2-ylamide DMPYTHV Discovery agent N.A. Investigative [36]
7-Mercapto-heptanoic acid biphenyl-3-ylamide DMEQKPO Discovery agent N.A. Investigative [36]
7-Mercapto-heptanoic acid biphenyl-4-ylamide DMJMOUK Discovery agent N.A. Investigative [36]
7-Mercapto-heptanoic acid phenylamide DM4912P Discovery agent N.A. Investigative [36]
7-Mercapto-heptanoic acid pyridin-3-ylamide DMQ9PLA Discovery agent N.A. Investigative [36]
7-Mercapto-heptanoic acid quinolin-3-ylamide DMTAGJ1 Discovery agent N.A. Investigative [36]
8-(Biphenyl-4-yloxy)-1,1,1-trifluoro-octan-2-one DM23XGW Discovery agent N.A. Investigative [30]
8-Mercapto-octanoic acid phenylamide DMD3FWU Discovery agent N.A. Investigative [36]
8-Oxo-8-phenyl-octanoic acid DMXDQ25 Discovery agent N.A. Investigative [35]
8-Oxo-8-phenyl-octanoic acid hydroxyamide DMWM1UL Discovery agent N.A. Investigative [40]
9,9,9-Trifluoro-8-oxo-nonanoic acid phenylamide DMVBCID Discovery agent N.A. Investigative [40]
9-(Biphenyl-4-yloxy)-1,1,1-trifluoro-nonan-2-one DMIY3D6 Discovery agent N.A. Investigative [40]
Apicidin DM83WVF Solid tumour/cancer 2A00-2F9Z Investigative [41]
Azelaic bishydroxamic acid DMKSQY1 Discovery agent N.A. Investigative [42]
CG-1521 DMN3YEQ Solid tumour/cancer 2A00-2F9Z Investigative [42]
CHAP1 DMBZ0QY Solid tumour/cancer 2A00-2F9Z Investigative [41]
CHAP31 DMOXRID Solid tumour/cancer 2A00-2F9Z Investigative [41]
Cyclostellettamine derivative DMFTDPQ Discovery agent N.A. Investigative [43]
N-(2,3-Dimethylphenyl)-N'-hydroxyoctanediamide DM5R3ZG Discovery agent N.A. Investigative [44]
N-(2,4-Dimethylphenyl)-N'-hydroxyoctanediamide DMXA9MR Discovery agent N.A. Investigative [44]
N-(2,5-Dimethylphenyl)-N'-hydroxyoctanediamide DMOL79W Discovery agent N.A. Investigative [44]
N-(2,6-Dimethylphenyl)-N'-hydroxyoctanediamide DMTBAPH Discovery agent N.A. Investigative [44]
N-(2-amino-5-(thiophen-2-yl)phenyl)nicotinamide DMFYG79 Discovery agent N.A. Investigative [45]
N-(2-aminophenyl)-4-methoxybenzamide DMTKWUM Discovery agent N.A. Investigative [46]
N-(2-aminophenyl)nicotinamide DMRDQ1B Discovery agent N.A. Investigative [45]
N-(2-Ethylphenyl)-N'-hydroxyoctanediamide DMDM50P Discovery agent N.A. Investigative [44]
N-(2-Mercapto-ethyl)-N'-phenyl-oxalamide DM0GOPV Discovery agent N.A. Investigative [47]
N-(2-Mercapto-ethyl)-N'-phenyl-succinamide DMJLFOQ Discovery agent N.A. Investigative [47]
N-(3,4-Dimethylphenyl)-N'-hydroxyoctanediamide DMEP2VM Discovery agent N.A. Investigative [44]
N-(3,5-Dimethylphenyl)-N'-hydroxyoctanediamide DM1L3FM Discovery agent N.A. Investigative [44]
N-(3-Ethylphenyl)-N'-hydroxyoctanediamide DMC5G6Y Discovery agent N.A. Investigative [44]
N-(4-aminobiphenyl-3-yl)nicotinamide DMXVZIY Discovery agent N.A. Investigative [45]
N-(4-Ethylphenyl)-N'-hydroxyoctanediamide DMKN8U6 Discovery agent N.A. Investigative [44]
N-(5-Hydroxycarbamoyl-pentyl)-4-methoxy-benzamide DMUHKYW Discovery agent N.A. Investigative [48]
N-(5-Hydroxycarbamoyl-pentyl)-4-nitro-benzamide DMSUW7M Discovery agent N.A. Investigative [35]
N-(5-Hydroxycarbamoyl-pentyl)-benzamide DMZSGPB Discovery agent N.A. Investigative [48]
N-(6-Hydroxycarbamoyl-hexyl)-benzamide DMIZVMT Discovery agent N.A. Investigative [35]
N-(6-Mercapto-hexyl)-benzamide DM01Y37 Discovery agent N.A. Investigative [36]
N-hydroxy-2,2-diphenylacetamide DMX3KRQ Discovery agent N.A. Investigative [31]
N-hydroxy-2,2-diphenylpropanamide DM7I2TD Discovery agent N.A. Investigative [31]
N-Hydroxy-4-((R)-2-phenyl-butyrylamino)-benzamide DMCN91A Discovery agent N.A. Investigative [33]
N-Hydroxy-4-((S)-2-phenyl-butyrylamino)-benzamide DMVK2Y3 Discovery agent N.A. Investigative [33]
N-Hydroxy-4-(2-phenyl-butyrylamino)-benzamide DMHEQ41 Discovery agent N.A. Investigative [33]
N-Hydroxy-4-(3-phenyl-propionylamino)-benzamide DMUOCQB Discovery agent N.A. Investigative [33]
N-Hydroxy-4-(4-phenyl-butyrylamino)-benzamide DMVEOBY Discovery agent N.A. Investigative [33]
N-Hydroxy-4-(5-phenyl-pentanoylamino)-benzamide DMISRMT Discovery agent N.A. Investigative [33]
N-Hydroxy-4-(pentanoylamino-methyl)-benzamide DMGTNQY Discovery agent N.A. Investigative [34]
N-Hydroxy-4-(phenylacetylamino-methyl)-benzamide DMDUOH4 Discovery agent N.A. Investigative [34]
N-Hydroxy-4-phenylacetylamino-benzamide DMCRU17 Discovery agent N.A. Investigative [33]
N-hydroxy-9,10-dihydroanthracene-9-carboxamide DMID3BF Discovery agent N.A. Investigative [31]
N-hydroxy-9H-xanthene-9-carboxamide DM0DRHP Discovery agent N.A. Investigative [31]
N-Hydroxy-N'-(2-methylphenyl)octanediamide DM865Y2 Discovery agent N.A. Investigative [44]
N-Hydroxy-N'-(3-methylphenyl)octanediamide DMYRC2M Discovery agent N.A. Investigative [44]
N-Hydroxy-N'-(4-methoxyphenyl)octanediamide DMELB07 Discovery agent N.A. Investigative [44]
N-Hydroxy-N'-(4-methylphenyl)octanediamide DM3DPZ8 Discovery agent N.A. Investigative [44]
N1-(biphenyl-4-yl)-N8-hydroxyoctanediamide DMZA8NC Discovery agent N.A. Investigative [49]
Octanedioic acid bis-hydroxyamide DMJNQ9K Discovery agent N.A. Investigative [37]
Octanedioic acid hydroxyamide pyridin-2-ylamide DMHNWS1 Discovery agent N.A. Investigative [35]
Octanedioic acid hydroxyamide pyridin-4-ylamide DM945RK Discovery agent N.A. Investigative [35]
PSAMMAPLIN A DM6T0IQ Discovery agent N.A. Investigative [40]
ST-2986 DMNERM6 Discovery agent N.A. Investigative [50]
ST-2987 DMWXTM8 Solid tumour/cancer 2A00-2F9Z Investigative [50]
ST-3050 DM19K2D Discovery agent N.A. Investigative [50]
ST-5732 DM9FYPM Discovery agent N.A. Investigative [51]
Suberic bishydroxamic acid DM235XH Discovery agent N.A. Investigative [42]
Thioacetic acid S-(6-phenylcarbamoyl-hexyl) ester DMBOKSF Discovery agent N.A. Investigative [36]
Trapoxin DMXZAH6 Discovery agent N.A. Investigative [52]
Trichostatin A DM9C8NX Solid tumour/cancer 2A00-2F9Z Investigative [53]
Trifluoromethylketone DMEPFAB Discovery agent N.A. Investigative [42]
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⏷ Show the Full List of 93 Investigative Drug(s)

References

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45 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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50 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.
51 Exploring bis-(indolyl)methane moiety as an alternative and innovative CAP group in the design of histone deacetylase (HDAC) inhibitors. Bioorg Med Chem Lett. 2009 May 15;19(10):2840-3.
52 Histone deacetylase as a new target for cancer chemotherapy. Cancer Chemother Pharmacol. 2001 Aug;48 Suppl 1:S20-6.
53 Histone deacetylase inhibitors induce apoptosis, histone hyperacetylation and up-regulation of gene transcription in Schistosoma mansoni. Mol Biochem Parasitol. 2009 Nov;168(1):7-15.