General Information of Drug Therapeutic Target (DTT) (ID: TT6R7JZ)

DTT Name Histone deacetylase 1 (HDAC1)
Synonyms RPD3L1; HD1
Gene Name HDAC1
DTT Type
Successful target
[1]
BioChemical Class
Carbon-nitrogen hydrolase
UniProt ID
HDAC1_HUMAN
TTD ID
T68547
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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EC Number
EC 3.5.1.98
Sequence
MAQTQGTRRKVCYYYDGDVGNYYYGQGHPMKPHRIRMTHNLLLNYGLYRKMEIYRPHKAN
AEEMTKYHSDDYIKFLRSIRPDNMSEYSKQMQRFNVGEDCPVFDGLFEFCQLSTGGSVAS
AVKLNKQQTDIAVNWAGGLHHAKKSEASGFCYVNDIVLAILELLKYHQRVLYIDIDIHHG
DGVEEAFYTTDRVMTVSFHKYGEYFPGTGDLRDIGAGKGKYYAVNYPLRDGIDDESYEAI
FKPVMSKVMEMFQPSAVVLQCGSDSLSGDRLGCFNLTIKGHAKCVEFVKSFNLPMLMLGG
GGYTIRNVARCWTYETAVALDTEIPNELPYNDYFEYFGPDFKLHISPSNMTNQNTNEYLE
KIKQRLFENLRMLPHAPGVQMQAIPEDAIPEESGDEDEDDPDKRISICSSDKRIACEEEF
SDSEEEGEGGRKNSSNFKKAKRVKTEDEKEKDPEEKKEVTEEEKTKEEKPEAKGVKEEVK
LA
Function
Gives a tag for epigenetic repression and plays an important role in transcriptional regulation, cell cycle progression and developmental events. Histone deacetylases act via the formation of large multiprotein complexes. Deacetylates SP proteins, SP1 and SP3, and regulates their function. Component of the BRG1-RB1-HDAC1 complex, which negatively regulates the CREST-mediated transcription in resting neurons. Upon calcium stimulation, HDAC1 is released from the complex and CREBBP is recruited, which facilitates transcriptional activation. Deacetylates TSHZ3 and regulates its transcriptional repressor activity. Deacetylates 'Lys-310' in RELA and thereby inhibits the transcriptional activity of NF-kappa-B. Deacetylates NR1D2 and abrogates the effect of KAT5-mediated relieving of NR1D2 transcription repression activity. Component of a RCOR/GFI/KDM1A/HDAC complex that suppresses, via histone deacetylase (HDAC) recruitment, a number of genes implicated in multilineage blood cell development. Involved in CIART-mediated transcriptional repression of the circadian transcriptional activator: CLOCK-ARNTL/BMAL1 heterodimer. Required for the transcriptional repression of circadian target genes, such as PER1, mediated by the large PER complex or CRY1 through histone deacetylation. Responsible for the deacetylation of lysine residues on the N-terminal part of the core histones (H2A, H2B, H3 and H4).
KEGG Pathway
Cell cycle (hsa04110 )
Notch signaling pathway (hsa04330 )
Thyroid hormone signaling pathway (hsa04919 )
Huntington's disease (hsa05016 )
Amphetamine addiction (hsa05031 )
Alcoholism (hsa05034 )
Epstein-Barr virus infection (hsa05169 )
Pathways in cancer (hsa05200 )
Transcriptional misregulation in cancer (hsa05202 )
Viral carcinogenesis (hsa05203 )
MicroRNAs in cancer (hsa05206 )
Chronic myeloid leukemia (hsa05220 )
Reactome Pathway
p75NTR negatively regulates cell cycle via SC1 (R-HSA-193670 )
Formation of the beta-catenin (R-HSA-201722 )
NOTCH1 Intracellular Domain Regulates Transcription (R-HSA-2122947 )
SMAD2/SMAD3 (R-HSA-2173796 )
Constitutive Signaling by NOTCH1 PEST Domain Mutants (R-HSA-2644606 )
Constitutive Signaling by NOTCH1 HD+PEST Domain Mutants (R-HSA-2894862 )
HDACs deacetylate histones (R-HSA-3214815 )
Deactivation of the beta-catenin transactivating complex (R-HSA-3769402 )
NoRC negatively regulates rRNA expression (R-HSA-427413 )
RNA Polymerase I Transcription Initiation (R-HSA-73762 )
Factors involved in megakaryocyte development and platelet production (R-HSA-983231 )
G0 and Early G1 (R-HSA-1538133 )

Molecular Interaction Atlas (MIA) of This DTT

Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This DTT
4 Approved Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
Panobinostat DM58WKG Chronic graft versus host disease Approved [1]
Romidepsin DMT5GNL Cutaneous T-cell lymphoma 2B01 Approved [2]
Vorinostat DMWMPD4 Adult acute monocytic leukemia Approved [1]
HBI-8000 DMDWYUN Non-small-cell lung cancer 2C25.Y Registered [3]
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12 Clinical Trial Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
ITF2357 DMFZBNE Duchenne dystrophy 8C70 Phase 3 [4]
NVP-LAQ824 DM8JWNA Mood disorder 6A60-6E23 Phase 3 [5]
SNDX-275 DMH7W9X Breast cancer 2C60-2C65 Phase 3 [6]
MGCD-0103 DM726HX Non-small-cell lung cancer 2C25.Y Phase 2 [1]
Phenylbutyrate DMBHPDW Urea cycle disorder 5C50.A Phase 2 [7]
Resminostat DMNE1FR Hepatocellular carcinoma 2C12.02 Phase 2 [8]
SB-623 DM4NY58 Cerebrovascular ischaemia 8B1Z Phase 2 [9]
Sodium butyrate DMKNIVG Acute myeloid leukaemia 2A60 Phase 2 [10]
CHR-3996 DMIXPNG Lymphoma 2A80-2A86 Phase 1/2 [11]
OBP-801 DMPLV9G Solid tumour/cancer 2A00-2F9Z Phase 1 [12]
RG-2833 DM7B650 Friedreich's ataxia 8A03.10 Phase 1 [3]
SB-639 DMSZIP5 Solid tumour/cancer 2A00-2F9Z Phase 1 [9]
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⏷ Show the Full List of 12 Clinical Trial Drug(s)
76 Patented Agent(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
Diaryl amine derivative 2 DMRBYAV N. A. N. A. Patented [13]
Diaryl amine derivative 3 DMLBN1T N. A. N. A. Patented [13]
Isosteric imidazolyl pyrimidine derivative 1 DMP2QDM N. A. N. A. Patented [14]
PMID28092474-Compound-32a DMGZ61E N. A. N. A. Patented [13]
PMID28092474-Compound-32b DMT2B5A N. A. N. A. Patented [13]
PMID28092474-Compound-32c DMGA3XL N. A. N. A. Patented [13]
PMID28092474-Compound-32d DMW21U4 N. A. N. A. Patented [13]
PMID28092474-Compound-32e DM8NHQS N. A. N. A. Patented [13]
PMID28092474-Compound-32f DMEIZ6Y N. A. N. A. Patented [13]
PMID28092474-Compound-32g DMTKLEP N. A. N. A. Patented [13]
PMID28092474-Compound-32h DME1WHT N. A. N. A. Patented [13]
PMID28092474-Compound-32i DMN3ZEF N. A. N. A. Patented [13]
PMID28092474-Compound-32j DMSGWTX N. A. N. A. Patented [13]
PMID28092474-Compound-32k DMHSJ65 N. A. N. A. Patented [13]
PMID28092474-Compound-32l DMSP5IA N. A. N. A. Patented [13]
PMID28092474-Compound-32m DMADMWB N. A. N. A. Patented [13]
PMID28092474-Compound-32n DMJO3RW N. A. N. A. Patented [13]
PMID28092474-Compound-32o DMV9BQN N. A. N. A. Patented [13]
PMID28092474-Compound-32p DM4ZO21 N. A. N. A. Patented [13]
PMID28092474-Compound-32q DMEASZY N. A. N. A. Patented [13]
PMID28092474-Compound-32r DMLTKMS N. A. N. A. Patented [13]
PMID28092474-Compound-32s DMS103B N. A. N. A. Patented [13]
PMID28092474-Compound-32t DM2JF0T N. A. N. A. Patented [13]
PMID28092474-Compound-32u DM805ZN N. A. N. A. Patented [13]
PMID28092474-Compound-32v DMHV3ES N. A. N. A. Patented [13]
PMID28092474-Compound-32x DML79XQ N. A. N. A. Patented [13]
PMID28092474-Compound-32y DMLR03U N. A. N. A. Patented [13]
PMID28092474-Compound-32z DMEPWGH N. A. N. A. Patented [13]
PMID28092474-Compound-33a DM7GH4Y N. A. N. A. Patented [13]
PMID28092474-Compound-33b DMIJQZV N. A. N. A. Patented [13]
PMID28092474-Compound-33c DM51JP6 N. A. N. A. Patented [13]
PMID28092474-Compound-33d DMW38MK N. A. N. A. Patented [13]
PMID28092474-Compound-33e DMGTSXL N. A. N. A. Patented [13]
PMID28092474-Compound-33f DMA360M N. A. N. A. Patented [13]
PMID28092474-Compound-33g DM18DY6 N. A. N. A. Patented [13]
PMID28092474-Compound-33h DM1DN6V N. A. N. A. Patented [13]
PMID28092474-Compound-33i DM16E95 N. A. N. A. Patented [13]
PMID28092474-Compound-33j DMNTRIZ N. A. N. A. Patented [13]
PMID28092474-Compound-33k DMF2ZNT N. A. N. A. Patented [13]
PMID28092474-Compound-33l DMPJSB2 N. A. N. A. Patented [13]
PMID28092474-Compound-33m DMXSPT9 N. A. N. A. Patented [13]
PMID28092474-Compound-33o DM6DJZ7 N. A. N. A. Patented [13]
PMID28092474-Compound-33p DMI8ZBK N. A. N. A. Patented [13]
PMID28092474-Compound-34a DMXQE7C N. A. N. A. Patented [13]
PMID28092474-Compound-34b DM6X2CO N. A. N. A. Patented [13]
PMID28092474-Compound-34c DMMI7DY N. A. N. A. Patented [13]
PMID29671355-Compound-11 DMNKABH N. A. N. A. Patented [15]
PMID29671355-Compound-13 DMALXYR N. A. N. A. Patented [15]
PMID29671355-Compound-18 DMUY53P N. A. N. A. Patented [15]
PMID29671355-Compound-19 DM9LMNB N. A. N. A. Patented [15]
PMID29671355-Compound-21 DMPJN0M N. A. N. A. Patented [15]
PMID29671355-Compound-22 DMRGV83 N. A. N. A. Patented [15]
PMID29671355-Compound-23 DMUBOEX N. A. N. A. Patented [15]
PMID29671355-Compound-24 DMCIGJ1 N. A. N. A. Patented [15]
PMID29671355-Compound-25 DMPV0KZ N. A. N. A. Patented [15]
PMID29671355-Compound-26 DM5K6MG N. A. N. A. Patented [15]
PMID29671355-Compound-27 DMP7S9E N. A. N. A. Patented [15]
PMID29671355-Compound-28 DMLXSHW N. A. N. A. Patented [15]
PMID29671355-Compound-31 DM3H78D N. A. N. A. Patented [15]
PMID29671355-Compound-38a DMYATB5 N. A. N. A. Patented [15]
PMID29671355-Compound-38b DMYXE4J N. A. N. A. Patented [15]
PMID29671355-Compound-39 DM6EJ93 N. A. N. A. Patented [15]
PMID29671355-Compound-42 DMXY103 N. A. N. A. Patented [15]
PMID29671355-Compound-43 DMVPMWJ N. A. N. A. Patented [15]
PMID29671355-Compound-44 DM80A3V N. A. N. A. Patented [15]
PMID29671355-Compound-55 DMJV1SY N. A. N. A. Patented [15]
PMID29671355-Compound-56 DM0VBMI N. A. N. A. Patented [15]
PMID29671355-Compound-57 DM57N3Y N. A. N. A. Patented [15]
PMID29671355-Compound-59 DM2F0CQ N. A. N. A. Patented [15]
PMID29671355-Compound-61 DMXH1G3 N. A. N. A. Patented [15]
PMID29671355-Compound-62 DMWRS34 N. A. N. A. Patented [15]
PMID29671355-Compound-65a DMY3Q58 N. A. N. A. Patented [15]
PMID29671355-Compound-67 DM1RPL4 N. A. N. A. Patented [15]
PMID29671355-Compound-73 DMCNF36 N. A. N. A. Patented [15]
PMID29671355-Compound-8 DM7YQJK N. A. N. A. Patented [15]
PMID29671355-Compound-9 DMXL96M N. A. N. A. Patented [15]
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⏷ Show the Full List of 76 Patented Agent(s)
4 Discontinued Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
AN-9 DMGL0Q2 Melanoma 2C30 Discontinued in Phase 2 [10]
Tacedinaline DM1Z74X Solid tumour/cancer 2A00-2F9Z Discontinued in Phase 2 [9]
Pyroxamide DM4LNBQ Solid tumour/cancer 2A00-2F9Z Discontinued in Phase 1 [9]
Oxamflatin DM1TG3C Solid tumour/cancer 2A00-2F9Z Terminated [9]
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8 Preclinical Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
4SC-202 DMXFC3W Solid tumour/cancer 2A00-2F9Z Preclinical [8]
Chlamydocin DM89DQP Solid tumour/cancer 2A00-2F9Z Preclinical [9]
Depudecin DMD0T1U Solid tumour/cancer 2A00-2F9Z Preclinical [9]
HC-Toxin DMPLZ7E Solid tumour/cancer 2A00-2F9Z Preclinical [9]
M-carboxycinnamic acid bishydroxamide DMHJLPS Solid tumour/cancer 2A00-2F9Z Preclinical [9]
Scriptaid DM9JZ21 Solid tumour/cancer 2A00-2F9Z Preclinical [9]
SK-7041 DM7DNOG Solid tumour/cancer 2A00-2F9Z Preclinical [9]
SK-7068 DMCI371 Solid tumour/cancer 2A00-2F9Z Preclinical [9]
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⏷ Show the Full List of 8 Preclinical Drug(s)
146 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 [16]
1,1,1-Trifluoro-8-(4-phenoxy-phenoxy)-octan-2-one DM6GI4Z Discovery agent N.A. Investigative [17]
1,1,1-Trifluoro-8-phenoxy-octan-2-one DM41R2O Discovery agent N.A. Investigative [17]
2-(methylsulfonylthio)ethyl 2-propylpentanoate DMM52D3 Discovery agent N.A. Investigative [18]
4-Benzenesulfonylamino-N-hydroxy-benzamide DMM6UPD Discovery agent N.A. Investigative [19]
4-Benzoylamino-N-hydroxy-benzamide DMYBPFS Discovery agent N.A. Investigative [20]
4-Butyrylamino-N-hydroxy-benzamide DMRY6B4 Discovery agent N.A. Investigative [21]
4-Chloro-N-(5-hydroxycarbamoyl-pentyl)-benzamide DM5AVG3 Discovery agent N.A. Investigative [22]
4-Dimethylamino-N-(6-mercapto-hexyl)-benzamide DM0M8G5 Discovery agent N.A. Investigative [23]
4-Hydroxy-N-(5-hydroxycarbamoyl-pentyl)-benzamide DMULOHZ Discovery agent N.A. Investigative [24]
4-Phenylbutyrohydroxamic acid DMCZKN7 Discovery agent N.A. Investigative [25]
4-tert-butyl-N-hydroxybenzamide DMUWTPX Discovery agent N.A. Investigative [26]
5-(4-Chloro-phenyl)-pentanoic acid hydroxyamide DM6CRVS Discovery agent N.A. Investigative [27]
5-(4-hydroxyphenyl)-3H-1,2-dithiole-3-thione DM7KQXL Discovery agent N.A. Investigative [18]
5-Mercapto-pentanoic acid phenylamide DMET3OJ Discovery agent N.A. Investigative [23]
6-(2-Bromo-acetylamino)-hexanoic acid phenylamide DM9LKXD Discovery agent N.A. Investigative [23]
6-(3-Benzoyl-ureido)-hexanoic acid hydroxyamide DMQZTS3 Discovery agent N.A. Investigative [28]
6-(9H-carbazol-9-yl)-N-hydroxyhexanamide DMVMDJ3 Discovery agent N.A. Investigative [29]
6-benzenesulfinylhexanoic acid hydroxamide DM2I95Z Discovery agent N.A. Investigative [30]
6-benzenesulfonylhexanoic acid hydroxamide DMY9IK8 Discovery agent N.A. Investigative [30]
6-Mercapto-hexanoic acid phenylamide DMD2FW9 Discovery agent N.A. Investigative [23]
6-Phenoxy-hexane-1-thiol DMVYIN2 Discovery agent N.A. Investigative [23]
6-phenylsulfanylhexanoic acid hydroxamide DM3OLM6 Discovery agent N.A. Investigative [30]
7-(1H-indol-5-yloxy)-N-hydroxyheptanamide DMOZV9W Discovery agent N.A. Investigative [31]
7-(3-Benzoyl-ureido)-heptanoic acid hydroxyamide DMCFV0X Discovery agent N.A. Investigative [28]
7-(4-(dimethylamino)phenoxy)-N-hydroxyheptanamide DM2TNCK Discovery agent N.A. Investigative [31]
7-(Biphenyl-3-yloxy)-1-oxazol-2-yl-heptan-1-one DMLCGSY Discovery agent N.A. Investigative [16]
7-(Biphenyl-4-yloxy)-1,1,1-trifluoro-heptan-2-one DM28GZ7 Discovery agent N.A. Investigative [17]
7-(Biphenyl-4-yloxy)-1-oxazol-2-yl-heptan-1-one DMY027P Discovery agent N.A. Investigative [16]
7-(Biphenyl-4-yloxy)-heptanoic acid hydroxyamide DMO4YLA Discovery agent N.A. Investigative [32]
7-(Naphthalen-2-yloxy)-1-oxazol-2-yl-heptan-1-one DM4VQN8 Discovery agent N.A. Investigative [16]
7-Biphenyl-4-yl-heptanoic acid hydroxyamide DMV54MT Discovery agent N.A. Investigative [33]
7-Mercapto-heptanoic acid benzothiazol-2-ylamide DMPYTHV Discovery agent N.A. Investigative [23]
7-Mercapto-heptanoic acid biphenyl-3-ylamide DMEQKPO Discovery agent N.A. Investigative [23]
7-Mercapto-heptanoic acid biphenyl-4-ylamide DMJMOUK Discovery agent N.A. Investigative [23]
7-Mercapto-heptanoic acid phenylamide DM4912P Discovery agent N.A. Investigative [23]
7-Mercapto-heptanoic acid pyridin-3-ylamide DMQ9PLA Discovery agent N.A. Investigative [23]
7-Mercapto-heptanoic acid quinolin-3-ylamide DMTAGJ1 Discovery agent N.A. Investigative [23]
7-mercapto-N-(4-phenylthiazol-2-yl)heptanamide DM03XYF Discovery agent N.A. Investigative [34]
7-Phenoxy-heptanoic acid hydroxyamide DM1FL5G Discovery agent N.A. Investigative [33]
8-(3-Benzoyl-ureido)-octanoic acid hydroxyamide DMW2NJR Discovery agent N.A. Investigative [28]
8-(4-bromophenyl)-N-hydroxy-8-oxooctanamide DMVOCWY Discovery agent N.A. Investigative [35]
8-(Biphenyl-3-yloxy)-1,1,1-trifluoro-octan-2-one DMH3SDO Discovery agent N.A. Investigative [17]
8-(biphenyl-4-yl)-N-hydroxy-8-oxooctanamide DMD6VSY Discovery agent N.A. Investigative [35]
8-(Biphenyl-4-yloxy)-1,1,1-trifluoro-octan-2-one DM23XGW Discovery agent N.A. Investigative [17]
8-(Biphenyl-4-yloxy)-2-oxo-octanoic acid DMDIGPW Discovery agent N.A. Investigative [32]
8-Mercapto-octanoic acid phenylamide DMD3FWU Discovery agent N.A. Investigative [23]
8-Oxo-8-phenyl-octanoic acid DMXDQ25 Discovery agent N.A. Investigative [24]
8-Oxo-8-phenyl-octanoic acid hydroxyamide DMWM1UL Discovery agent N.A. Investigative [22]
8-Phenyl-octanoic acid hydroxyamide DM516NE Discovery agent N.A. Investigative [33]
9,9,9-Trifluoro-8-oxo-nonanoic acid phenylamide DMVBCID Discovery agent N.A. Investigative [17]
9-(Biphenyl-4-yloxy)-1,1,1-trifluoro-nonan-2-one DMIY3D6 Discovery agent N.A. Investigative [17]
ADS-100380 DM7U4OT Discovery agent N.A. Investigative [36]
ADS-102550 DMEU6MH Discovery agent N.A. Investigative [36]
Azithromycin-N-benzyltriazolyldecahydroxamic Acid DMDQ2VN Discovery agent N.A. Investigative [37]
Azithromycin-N-benzyltriazolylhexahydroxamic Acid DM7KD5Y Discovery agent N.A. Investigative [37]
Azithromycin-N-benzyltriazolylnonahydroxamic Acid DMW0HXO Discovery agent N.A. Investigative [37]
Azithromycin-N-benzyltriazolyloctahydroxamic Acid DMAJ4LI Discovery agent N.A. Investigative [37]
Azithromycinarylalkylhydroxamic Acid DM8ZQG3 Discovery agent N.A. Investigative [37]
AZUMAMIDE B DMXOGE8 Discovery agent N.A. Investigative [38]
AZUMAMIDE C DMEBA61 Discovery agent N.A. Investigative [38]
AZUMAMIDE E DMAX06G Discovery agent N.A. Investigative [38]
Cyclo(-L-Am7(S2Py)-A2in-L-Ala-D-Pro-) DMZF35W Discovery agent N.A. Investigative [39]
Cyclo(-L-Am7(S2Py)-Aib-L-Ala-D-Pro-) DMIVREK Discovery agent N.A. Investigative [39]
Cyclo(-L-Am7(S2Py)-Aib-L-Ala-D-Tic-) DMLBECR Discovery agent N.A. Investigative [39]
Cyclo(-L-Am7(S2Py)-Aib-L-Ph4-D-Pro-) DMA76KW Discovery agent N.A. Investigative [39]
Cyclo(-L-Am7(S2Py)-Aib-L-Ph5-D-Pro-) DMLNJ0O Discovery agent N.A. Investigative [39]
Cyclo(-L-Am7(S2Py)-Aib-L-Phe-D-Pro-) DMTVMWA Discovery agent N.A. Investigative [39]
Cyclo(-L-Am7(S2Py)-Aib-L-Phg-D-Pro-) DMUSEDF Discovery agent N.A. Investigative [39]
Cyclo(-L-Am7(S2Py)-Aib-L-Ser(Bzl)-D-Pro-) DMSEQ0W Discovery agent N.A. Investigative [39]
Cyclo(-L-Am7(S2Py)-Aib-L-Ser-D-Pro-) DMBKP48 Discovery agent N.A. Investigative [39]
Cyclo(-L-Am7(S2Py)-D-2MePhe-L-Ala-D-Pro-) DMVY89X Discovery agent N.A. Investigative [39]
Cyclo(-L-Am7(S2Py)-D-A1in-L-Ala-D-Pro-) DMTDIM9 Discovery agent N.A. Investigative [39]
Cyclo(-L-Am7(S2Py)-L-2MePhe-L-Ala-D-Pro-) DMV23XD Discovery agent N.A. Investigative [39]
Cyclo(-L-Am7(S2Py)-L-A1in-L-Ala-D-Pro-) DM0VIH4 Discovery agent N.A. Investigative [39]
Cyclostellettamine derivative DMFTDPQ Discovery agent N.A. Investigative [40]
Desclasinose Azithromycinarylalkyl Hydroxamate DMAB9KG Discovery agent N.A. Investigative [37]
Gymnochrome E DM7SLAM Discovery agent N.A. Investigative [41]
LARGAZOLE DMSYLIJ Discovery agent N.A. Investigative [42]
N,8-dihydroxy-8-(naphthalen-2-yl)octanamide DM8G0WX Discovery agent N.A. Investigative [35]
N-(2,3-Dimethylphenyl)-N'-hydroxyoctanediamide DM5R3ZG Discovery agent N.A. Investigative [43]
N-(2,4-Dimethylphenyl)-N'-hydroxyoctanediamide DMXA9MR Discovery agent N.A. Investigative [43]
N-(2,5-Dimethylphenyl)-N'-hydroxyoctanediamide DMOL79W Discovery agent N.A. Investigative [43]
N-(2,6-Dimethylphenyl)-N'-hydroxyoctanediamide DMTBAPH Discovery agent N.A. Investigative [43]
N-(2-amino-5-(thiophen-2-yl)phenyl)nicotinamide DMFYG79 Discovery agent N.A. Investigative [44]
N-(2-aminophenyl)-4-(chroman-3-ylmethyl)benzamide DMT7JUC 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 [44]
N-(2-aminophenyl)quinoxaline-6-carboxamide DMJXV7C Discovery agent N.A. Investigative [46]
N-(2-Ethylphenyl)-N'-hydroxyoctanediamide DMDM50P Discovery agent N.A. Investigative [43]
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 [43]
N-(3,5-Dimethylphenyl)-N'-hydroxyoctanediamide DM1L3FM Discovery agent N.A. Investigative [43]
N-(3-Ethylphenyl)-N'-hydroxyoctanediamide DMC5G6Y Discovery agent N.A. Investigative [43]
N-(4-aminobiphenyl-3-yl)nicotinamide DMXVZIY Discovery agent N.A. Investigative [44]
N-(4-Ethylphenyl)-N'-hydroxyoctanediamide DMKN8U6 Discovery agent N.A. Investigative [43]
N-(4-hydroxybiphenyl-3-yl)benzamide DMC5H8G Discovery agent N.A. Investigative [44]
N-(5-Hydroxycarbamoyl-pentyl)-4-nitro-benzamide DMSUW7M Discovery agent N.A. Investigative [22]
N-(6-Hydroxycarbamoyl-hexyl)-benzamide DMIZVMT Discovery agent N.A. Investigative [24]
N-(6-Mercapto-hexyl)-benzamide DM01Y37 Discovery agent N.A. Investigative [23]
N-hydroxy-2,2'-bithiophene-5-carboxamide DMWIMR4 Discovery agent N.A. Investigative [36]
N-Hydroxy-4-((R)-2-phenyl-butyrylamino)-benzamide DMCN91A Discovery agent N.A. Investigative [20]
N-Hydroxy-4-((S)-2-phenyl-butyrylamino)-benzamide DMVK2Y3 Discovery agent N.A. Investigative [20]
N-Hydroxy-4-(2-phenyl-butyrylamino)-benzamide DMHEQ41 Discovery agent N.A. Investigative [20]
N-Hydroxy-4-(3-phenyl-propionylamino)-benzamide DMUOCQB Discovery agent N.A. Investigative [48]
N-Hydroxy-4-(4-phenyl-butyrylamino)-benzamide DMVEOBY Discovery agent N.A. Investigative [20]
N-Hydroxy-4-(5-phenyl-pentanoylamino)-benzamide DMISRMT Discovery agent N.A. Investigative [20]
N-Hydroxy-4-(pentanoylamino-methyl)-benzamide DMGTNQY Discovery agent N.A. Investigative [21]
N-Hydroxy-4-(phenylacetylamino-methyl)-benzamide DMDUOH4 Discovery agent N.A. Investigative [21]
N-Hydroxy-4-phenylacetylamino-benzamide DMCRU17 Discovery agent N.A. Investigative [20]
N-hydroxy-5-(pyridin-2-yl)thiophene-2-carboxamide DMYKJZ2 Discovery agent N.A. Investigative [36]
N-hydroxy-5-(pyridin-3-yl)thiophene-2-carboxamide DMK98LE Discovery agent N.A. Investigative [36]
N-hydroxy-5-(pyridin-4-yl)thiophene-2-carboxamide DM653RM Discovery agent N.A. Investigative [36]
N-hydroxy-5-phenylthiophene-2-carboxamide DMA2WUQ Discovery agent N.A. Investigative [36]
N-hydroxy-6-oxo-6-phenylhexanamide DM0JNO2 Discovery agent N.A. Investigative [35]
N-hydroxy-7-(4-methoxyphenyl)-7-oxoheptanamide DMUXZL1 Discovery agent N.A. Investigative [35]
N-hydroxy-7-(naphthalen-2-yl)-7-oxoheptanamide DM8Z4L0 Discovery agent N.A. Investigative [35]
N-hydroxy-7-(naphthalen-2-yloxy)heptanamide DMBUNAP Discovery agent N.A. Investigative [31]
N-hydroxy-7-oxo-7-phenylheptanamide DMQW7JZ Discovery agent N.A. Investigative [35]
N-hydroxy-8-(2-methoxyphenyl)-8-oxooctanamide DMSIMNR Discovery agent N.A. Investigative [35]
N-hydroxy-8-(4-methoxyphenyl)-8-oxooctanamide DMD2K4T Discovery agent N.A. Investigative [35]
N-hydroxy-8-(naphthalen-2-yl)non-8-enamide DMRN1C6 Discovery agent N.A. Investigative [35]
N-hydroxy-8-(naphthalen-2-yl)oct-7-enamide DMGZY1Q Discovery agent N.A. Investigative [35]
N-hydroxy-8-(naphthalen-2-yl)octanamide DMXQICK Discovery agent N.A. Investigative [35]
N-hydroxy-8-oxo-8-(pyridin-3-yl)octanamide DMO4CR7 Discovery agent N.A. Investigative [35]
N-hydroxy-9-oxo-9-phenylnonanamide DMIC2A8 Discovery agent N.A. Investigative [35]
N-Hydroxy-N'-(2-methylphenyl)octanediamide DM865Y2 Discovery agent N.A. Investigative [43]
N-Hydroxy-N'-(3-methylphenyl)octanediamide DMYRC2M Discovery agent N.A. Investigative [43]
N-Hydroxy-N'-(4-methoxyphenyl)octanediamide DMELB07 Discovery agent N.A. Investigative [43]
N-Hydroxy-N'-(4-methylphenyl)octanediamide DM3DPZ8 Discovery agent N.A. Investigative [43]
N-hydroxybenzo[b]thiophene-2-carboxamide DMR4J8G Discovery agent N.A. Investigative [49]
N1-(biphenyl-3-yl)-N8-hydroxyoctanediamide DMMQXON Discovery agent N.A. Investigative [50]
N1-(biphenyl-4-yl)-N8-hydroxyoctanediamide DMZA8NC Discovery agent N.A. Investigative [51]
N1-hydroxy-N8-(4-phenylthiazol-2-yl)octanediamide DMOZARM Discovery agent N.A. Investigative [51]
nexturastat A DM6NS7H Discovery agent N.A. Investigative [52]
NSC-746457 DM2GO7N Discovery agent N.A. Investigative [53]
Octanedioic acid bis-hydroxyamide DMJNQ9K Discovery agent N.A. Investigative [54]
Octanedioic acid hydroxyamide pyridin-2-ylamide DMHNWS1 Discovery agent N.A. Investigative [24]
Octanedioic acid hydroxyamide pyridin-4-ylamide DM945RK Discovery agent N.A. Investigative [24]
PSAMMAPLIN A DM6T0IQ Discovery agent N.A. Investigative [22]
SK-683 DMM32CF Discovery agent N.A. Investigative [55]
ST-2986 DMNERM6 Discovery agent N.A. Investigative [56]
ST-2987 DMWXTM8 Solid tumour/cancer 2A00-2F9Z Investigative [56]
ST-3050 DM19K2D Discovery agent N.A. Investigative [56]
Thioacetic acid S-(6-phenylcarbamoyl-hexyl) ester DMBOKSF Discovery agent N.A. Investigative [23]
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⏷ Show the Full List of 146 Investigative Drug(s)

Molecular Expression Atlas (MEA) of This DTT

Molecular Expression Atlas (MEA) Jump to Detail Molecular Expression Atlas of This DTT
Disease Name ICD 11 Studied Tissue p-value Fold-Change Z-score
Renal cancer 2C82 Kidney 5.21E-01 0.1 0.23
Prostate cancer 2C82 Prostate 6.73E-02 0.24 0.59
Multiple myeloma 2C82 Bone marrow 1.54E-06 0.66 4.44
Type 2 diabetes 5A11 Liver tissue 6.27E-01 0.11 0.33
Polycythemia vera 2C82 Whole blood 3.55E-11 -0.48 -1.91
Liver cancer 2C82 Liver tissue 1.91E-11 0.44 1.3
Melanoma 2C82 Skin 7.87E-02 0.06 0.18
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⏷ Show the Full List of DTT Expression Under 7 Diseases

References

1 Protein methyltransferases as a target class for drug discovery. Nat Rev Drug Discov. 2009 Sep;8(9):724-32.
2 Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92.
3 Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
4 Emerging drugs for the therapy of primary and post essential thrombocythemia, post polycythemia vera myelofibrosis. Expert Opin Emerg Drugs. 2009 Sep;14(3):471-9.
5 NVP-LAQ824 is a potent novel histone deacetylase inhibitor with significant activity against multiple myeloma. Blood. 2003 Oct 1;102(7):2615-22.
6 Emerging therapies for multiple myeloma. Expert Opin Emerg Drugs. 2009 Mar;14(1):99-127.
7 Emerging disease-modifying therapies for the treatment of motor neuron disease/amyotropic lateral sclerosis. Expert Opin Emerg Drugs. 2007 May;12(2):229-52.
8 2011 Pipeline of 4SC AG.
9 Histone deacetylase inhibitors in cancer therapy: latest developments, trends and medicinal chemistry perspective. Anticancer Agents Med Chem. 2007 Sep;7(5):576-92.
10 Anticancer activities of histone deacetylase inhibitors. Nat Rev Drug Discov. 2006 Sep;5(9):769-84.
11 A phase I pharmacokinetic and pharmacodynamic study of CHR-3996, an oral class I selective histone deacetylase inhibitor in refractory solid tumors. Clin Cancer Res. 2012 May 1;18(9):2687-94.
12 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 2658).
13 Novel histone deacetylase 6 (HDAC6) selective inhibitors: a patent evaluation (WO2014181137).Expert Opin Ther Pat. 2017 Mar;27(3):229-236.
14 Cyclin-dependent kinase inhibitors for cancer therapy: a patent review (2009 - 2014).Expert Opin Ther Pat. 2015;25(9):953-70.
15 HDAC inhibitors: a 2013-2017 patent survey.Expert Opin Ther Pat. 2018 Apr 19:1-17.
16 Heterocyclic ketones as inhibitors of histone deacetylase. Bioorg Med Chem Lett. 2003 Nov 17;13(22):3909-13.
17 Trifluoromethyl ketones as inhibitors of histone deacetylase. Bioorg Med Chem Lett. 2002 Dec 2;12(23):3443-7.
18 New sulfurated derivatives of valproic acid with enhanced histone deacetylase inhibitory activity. Bioorg Med Chem Lett. 2008 Mar 15;18(6):1893-7.
19 Design and synthesis of a novel class of histone deacetylase inhibitors. Bioorg Med Chem Lett. 2001 Nov 5;11(21):2847-50.
20 Structure-based optimization of phenylbutyrate-derived histone deacetylase inhibitors. J Med Chem. 2005 Aug 25;48(17):5530-5.
21 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.
22 Histone deacetylase inhibitors. J Med Chem. 2003 Nov 20;46(24):5097-116.
23 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.
24 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.
25 Chemical phylogenetics of histone deacetylases. Nat Chem Biol. 2010 Mar;6(3):238-243.
26 Design of novel histone deacetylase inhibitors. Bioorg Med Chem Lett. 2007 Aug 15;17(16):4619-24.
27 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.
28 Acylurea connected straight chain hydroxamates as novel histone deacetylase inhibitors: Synthesis, SAR, and in vivo antitumor activity. Bioorg Med Chem Lett. 2010 Jun 1;20(11):3314-21.
29 Inhibitors selective for HDAC6 in enzymes and cells. Bioorg Med Chem Lett. 2010 Dec 1;20(23):7067-70.
30 Aromatic sulfide inhibitors of histone deacetylase based on arylsulfinyl-2,4-hexadienoic acid hydroxyamides. J Med Chem. 2006 Jan 26;49(2):800-5.
31 Structure-activity relationships of aryloxyalkanoic acid hydroxyamides as potent inhibitors of histone deacetylase. Bioorg Med Chem Lett. 2007 Jan 1;17(1):136-41.
32 Alpha-keto amides as inhibitors of histone deacetylase. Bioorg Med Chem Lett. 2003 Oct 6;13(19):3331-5.
33 A novel series of histone deacetylase inhibitors incorporating hetero aromatic ring systems as connection units. Bioorg Med Chem Lett. 2003 Nov 3;13(21):3817-20.
34 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.
35 3D-QSAR studies of HDACs inhibitors using pharmacophore-based alignment. Eur J Med Chem. 2009 Jul;44(7):2868-76.
36 Identification and optimisation of a series of substituted 5-pyridin-2-yl-thiophene-2-hydroxamic acids as potent histone deacetylase (HDAC) inhibit... Bioorg Med Chem Lett. 2007 Jan 15;17(2):363-9.
37 Non-peptide macrocyclic histone deacetylase inhibitors. J Med Chem. 2009 Jan 22;52(2):456-68.
38 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.
39 Molecular design of histone deacetylase inhibitors by aromatic ring shifting in chlamydocin framework. Bioorg Med Chem. 2007 Dec 15;15(24):7830-9.
40 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.
41 Gymnochromes E and F, cytotoxic phenanthroperylenequinones from a deep-water crinoid, Holopus rangii. J Nat Prod. 2010 Apr 23;73(4):712-5.
42 Synthesis and biological characterization of the histone deacetylase inhibitor largazole and C7- modified analogues. J Med Chem. 2010 Jun 24;53(12):4654-67.
43 Biological and biophysical properties of the histone deacetylase inhibitor suberoylanilide hydroxamic acid are affected by the presence of short al... J Med Chem. 2010 Mar 11;53(5):1937-50.
44 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).
45 N-(2-Amino-phenyl)-4-(heteroarylmethyl)-benzamides as new histone deacetylase inhibitors. Bioorg Med Chem Lett. 2007 Dec 15;17(24):6729-33.
46 Novel aminophenyl benzamide-type histone deacetylase inhibitors with enhanced potency and selectivity. J Med Chem. 2007 Nov 15;50(23):5543-6.
47 Mercaptoamide-based non-hydroxamic acid type histone deacetylase inhibitors. Bioorg Med Chem Lett. 2005 Apr 15;15(8):1969-72.
48 Design, synthesis and preliminary biological evaluation of N-hydroxy-4-(3-phenylpropanamido)benzamide (HPPB) derivatives as novel histone deacetyla... Eur J Med Chem. 2009 Nov;44(11):4470-6.
49 Histone deacetylase inhibitors: from bench to clinic. J Med Chem. 2008 Mar 27;51(6):1505-29.
50 Sulfamides as novel histone deacetylase inhibitors. Bioorg Med Chem Lett. 2009 Jan 15;19(2):336-40.
51 Isoxazole moiety in the linker region of HDAC inhibitors adjacent to the Zn-chelating group: effects on HDAC biology and antiproliferative activity. Bioorg Med Chem Lett. 2009 Jun 1;19(11):3023-6.
52 Selective histone deacetylase 6 inhibitors bearing substituted urea linkers inhibit melanoma cell growth. J Med Chem. 2012 Nov 26;55(22):9891-9.
53 Histone deacetylase inhibitors through click chemistry. J Med Chem. 2008 Dec 11;51(23):7417-27.
54 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.
55 On the function of the 14 A long internal cavity of histone deacetylase-like protein: implications for the design of histone deacetylase inhibitors. J Med Chem. 2004 Jun 17;47(13):3409-17.
56 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.