Target Information
| Target General Information | Top | |||||
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| Target ID |
T68547
(Former ID: TTDS00095)
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| Target Name |
Histone deacetylase 1 (HDAC1)
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| Synonyms |
RPD3L1; HD1
Click to Show/Hide
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| Gene Name |
HDAC1
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| Target Type |
Successful target
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[1] | ||||
| Disease | [+] 2 Target-related Diseases | + | ||||
| 1 | Multiple myeloma [ICD-11: 2A83] | |||||
| 2 | Mycosis fungoides [ICD-11: 2B01] | |||||
| 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).
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| BioChemical Class |
Carbon-nitrogen hydrolase
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| UniProt ID | ||||||
| EC Number |
EC 3.5.1.98
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| Sequence |
MAQTQGTRRKVCYYYDGDVGNYYYGQGHPMKPHRIRMTHNLLLNYGLYRKMEIYRPHKAN
AEEMTKYHSDDYIKFLRSIRPDNMSEYSKQMQRFNVGEDCPVFDGLFEFCQLSTGGSVAS AVKLNKQQTDIAVNWAGGLHHAKKSEASGFCYVNDIVLAILELLKYHQRVLYIDIDIHHG DGVEEAFYTTDRVMTVSFHKYGEYFPGTGDLRDIGAGKGKYYAVNYPLRDGIDDESYEAI FKPVMSKVMEMFQPSAVVLQCGSDSLSGDRLGCFNLTIKGHAKCVEFVKSFNLPMLMLGG GGYTIRNVARCWTYETAVALDTEIPNELPYNDYFEYFGPDFKLHISPSNMTNQNTNEYLE KIKQRLFENLRMLPHAPGVQMQAIPEDAIPEESGDEDEDDPDKRISICSSDKRIACEEEF SDSEEEGEGGRKNSSNFKKAKRVKTEDEKEKDPEEKKEVTEEEKTKEEKPEAKGVKEEVK LA Click to Show/Hide
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| 3D Structure | Click to Show 3D Structure of This Target | PDB | ||||
| HIT2.0 ID | T42D4V | |||||
| Drugs and Modes of Action | Top | |||||
|---|---|---|---|---|---|---|
| Approved Drug(s) | [+] 4 Approved Drugs | + | ||||
| 1 | Panobinostat | Drug Info | Approved | Multiple myeloma | [2] | |
| 2 | Romidepsin | Drug Info | Approved | Cutaneous T-cell lymphoma | [3], [4] | |
| 3 | Vorinostat | Drug Info | Approved | Cutaneous T-cell lymphoma | [5], [6] | |
| 4 | HBI-8000 | Drug Info | Registered | Solid tumour/cancer | [7], [8] | |
| Clinical Trial Drug(s) | [+] 12 Clinical Trial Drugs | + | ||||
| 1 | ITF2357 | Drug Info | Phase 3 | Duchenne dystrophy | [9] | |
| 2 | NVP-LAQ824 | Drug Info | Phase 3 | Mood disorder | [10] | |
| 3 | SNDX-275 | Drug Info | Phase 3 | Breast cancer | [11] | |
| 4 | MGCD-0103 | Drug Info | Phase 2 | Solid tumour/cancer | [12], [13] | |
| 5 | Phenylbutyrate | Drug Info | Phase 2 | Urea cycle disorder | [14], [15] | |
| 6 | Resminostat | Drug Info | Phase 2 | Hepatocellular carcinoma | [16], [17] | |
| 7 | SB-623 | Drug Info | Phase 2 | Cerebrovascular ischaemia | [18] | |
| 8 | Sodium butyrate | Drug Info | Phase 2 | Refractory sickle cell ulcers | [19] | |
| 9 | CHR-3996 | Drug Info | Phase 1/2 | Lymphoma | [20] | |
| 10 | OBP-801 | Drug Info | Phase 1 | Solid tumour/cancer | [21] | |
| 11 | RG-2833 | Drug Info | Phase 1 | Friedreich's ataxia | [22], [23] | |
| 12 | SB-639 | Drug Info | Phase 1 | Solid tumour/cancer | [24] | |
| Discontinued Drug(s) | [+] 4 Discontinued Drugs | + | ||||
| 1 | AN-9 | Drug Info | Discontinued in Phase 2 | Melanoma | [25] | |
| 2 | Tacedinaline | Drug Info | Discontinued in Phase 2 | Solid tumour/cancer | [26], [27] | |
| 3 | Pyroxamide | Drug Info | Discontinued in Phase 1 | Solid tumour/cancer | [28] | |
| 4 | Oxamflatin | Drug Info | Terminated | Solid tumour/cancer | [35] | |
| Preclinical Drug(s) | [+] 8 Preclinical Drugs | + | ||||
| 1 | 4SC-202 | Drug Info | Preclinical | Solid tumour/cancer | [17] | |
| 2 | Chlamydocin | Drug Info | Preclinical | Solid tumour/cancer | [29] | |
| 3 | Depudecin | Drug Info | Preclinical | Solid tumour/cancer | [30] | |
| 4 | HC-Toxin | Drug Info | Preclinical | Solid tumour/cancer | [31] | |
| 5 | M-carboxycinnamic acid bishydroxamide | Drug Info | Preclinical | Solid tumour/cancer | [32] | |
| 6 | Scriptaid | Drug Info | Preclinical | Solid tumour/cancer | [15], [33] | |
| 7 | SK-7041 | Drug Info | Preclinical | Solid tumour/cancer | [34] | |
| 8 | SK-7068 | Drug Info | Preclinical | Solid tumour/cancer | [34] | |
| Mode of Action | [+] 2 Modes of Action | + | ||||
| Inhibitor | [+] 248 Inhibitor drugs | + | ||||
| 1 | Panobinostat | Drug Info | [1], [36], [37], [38] | |||
| 2 | Romidepsin | Drug Info | [4] | |||
| 3 | Vorinostat | Drug Info | [1], [39], [38] | |||
| 4 | ITF2357 | Drug Info | [41], [6] | |||
| 5 | NVP-LAQ824 | Drug Info | [42] | |||
| 6 | SNDX-275 | Drug Info | [6] | |||
| 7 | MGCD-0103 | Drug Info | [1], [37], [38] | |||
| 8 | Phenylbutyrate | Drug Info | [15] | |||
| 9 | Resminostat | Drug Info | [17] | |||
| 10 | SB-623 | Drug Info | [37] | |||
| 11 | Sodium butyrate | Drug Info | [38], [43] | |||
| 12 | CHR-3996 | Drug Info | [44] | |||
| 13 | OBP-801 | Drug Info | [45] | |||
| 14 | SB-639 | Drug Info | [37] | |||
| 15 | Diaryl amine derivative 2 | Drug Info | [46] | |||
| 16 | Diaryl amine derivative 3 | Drug Info | [46] | |||
| 17 | Isosteric imidazolyl pyrimidine derivative 1 | Drug Info | [47] | |||
| 18 | PMID28092474-Compound-32a | Drug Info | [46] | |||
| 19 | PMID28092474-Compound-32b | Drug Info | [46] | |||
| 20 | PMID28092474-Compound-32c | Drug Info | [46] | |||
| 21 | PMID28092474-Compound-32d | Drug Info | [46] | |||
| 22 | PMID28092474-Compound-32e | Drug Info | [46] | |||
| 23 | PMID28092474-Compound-32f | Drug Info | [46] | |||
| 24 | PMID28092474-Compound-32g | Drug Info | [46] | |||
| 25 | PMID28092474-Compound-32h | Drug Info | [46] | |||
| 26 | PMID28092474-Compound-32i | Drug Info | [46] | |||
| 27 | PMID28092474-Compound-32j | Drug Info | [46] | |||
| 28 | PMID28092474-Compound-32k | Drug Info | [46] | |||
| 29 | PMID28092474-Compound-32l | Drug Info | [46] | |||
| 30 | PMID28092474-Compound-32m | Drug Info | [46] | |||
| 31 | PMID28092474-Compound-32n | Drug Info | [46] | |||
| 32 | PMID28092474-Compound-32o | Drug Info | [46] | |||
| 33 | PMID28092474-Compound-32p | Drug Info | [46] | |||
| 34 | PMID28092474-Compound-32q | Drug Info | [46] | |||
| 35 | PMID28092474-Compound-32r | Drug Info | [46] | |||
| 36 | PMID28092474-Compound-32s | Drug Info | [46] | |||
| 37 | PMID28092474-Compound-32t | Drug Info | [46] | |||
| 38 | PMID28092474-Compound-32u | Drug Info | [46] | |||
| 39 | PMID28092474-Compound-32v | Drug Info | [46] | |||
| 40 | PMID28092474-Compound-32x | Drug Info | [46] | |||
| 41 | PMID28092474-Compound-32y | Drug Info | [46] | |||
| 42 | PMID28092474-Compound-32z | Drug Info | [46] | |||
| 43 | PMID28092474-Compound-33a | Drug Info | [46] | |||
| 44 | PMID28092474-Compound-33b | Drug Info | [46] | |||
| 45 | PMID28092474-Compound-33c | Drug Info | [46] | |||
| 46 | PMID28092474-Compound-33d | Drug Info | [46] | |||
| 47 | PMID28092474-Compound-33e | Drug Info | [46] | |||
| 48 | PMID28092474-Compound-33f | Drug Info | [46] | |||
| 49 | PMID28092474-Compound-33g | Drug Info | [46] | |||
| 50 | PMID28092474-Compound-33h | Drug Info | [46] | |||
| 51 | PMID28092474-Compound-33i | Drug Info | [46] | |||
| 52 | PMID28092474-Compound-33j | Drug Info | [46] | |||
| 53 | PMID28092474-Compound-33k | Drug Info | [46] | |||
| 54 | PMID28092474-Compound-33l | Drug Info | [46] | |||
| 55 | PMID28092474-Compound-33m | Drug Info | [46] | |||
| 56 | PMID28092474-Compound-33o | Drug Info | [46] | |||
| 57 | PMID28092474-Compound-33p | Drug Info | [46] | |||
| 58 | PMID28092474-Compound-34a | Drug Info | [46] | |||
| 59 | PMID28092474-Compound-34b | Drug Info | [46] | |||
| 60 | PMID28092474-Compound-34c | Drug Info | [46] | |||
| 61 | PMID29671355-Compound-11 | Drug Info | [48] | |||
| 62 | PMID29671355-Compound-13 | Drug Info | [48] | |||
| 63 | PMID29671355-Compound-18 | Drug Info | [48] | |||
| 64 | PMID29671355-Compound-19 | Drug Info | [48] | |||
| 65 | PMID29671355-Compound-21 | Drug Info | [48] | |||
| 66 | PMID29671355-Compound-22 | Drug Info | [48] | |||
| 67 | PMID29671355-Compound-23 | Drug Info | [48] | |||
| 68 | PMID29671355-Compound-24 | Drug Info | [48] | |||
| 69 | PMID29671355-Compound-25 | Drug Info | [48] | |||
| 70 | PMID29671355-Compound-26 | Drug Info | [48] | |||
| 71 | PMID29671355-Compound-27 | Drug Info | [48] | |||
| 72 | PMID29671355-Compound-28 | Drug Info | [48] | |||
| 73 | PMID29671355-Compound-31 | Drug Info | [48] | |||
| 74 | PMID29671355-Compound-38a | Drug Info | [48] | |||
| 75 | PMID29671355-Compound-38b | Drug Info | [48] | |||
| 76 | PMID29671355-Compound-39 | Drug Info | [48] | |||
| 77 | PMID29671355-Compound-42 | Drug Info | [48] | |||
| 78 | PMID29671355-Compound-43 | Drug Info | [48] | |||
| 79 | PMID29671355-Compound-44 | Drug Info | [48] | |||
| 80 | PMID29671355-Compound-55 | Drug Info | [48] | |||
| 81 | PMID29671355-Compound-56 | Drug Info | [48] | |||
| 82 | PMID29671355-Compound-57 | Drug Info | [48] | |||
| 83 | PMID29671355-Compound-59 | Drug Info | [48] | |||
| 84 | PMID29671355-Compound-61 | Drug Info | [48] | |||
| 85 | PMID29671355-Compound-62 | Drug Info | [48] | |||
| 86 | PMID29671355-Compound-65a | Drug Info | [48] | |||
| 87 | PMID29671355-Compound-67 | Drug Info | [48] | |||
| 88 | PMID29671355-Compound-73 | Drug Info | [48] | |||
| 89 | PMID29671355-Compound-8 | Drug Info | [48] | |||
| 90 | PMID29671355-Compound-9 | Drug Info | [48] | |||
| 91 | AN-9 | Drug Info | [38] | |||
| 92 | Tacedinaline | Drug Info | [37], [38] | |||
| 93 | Pyroxamide | Drug Info | [37], [38] | |||
| 94 | 4SC-202 | Drug Info | [17] | |||
| 95 | Chlamydocin | Drug Info | [37] | |||
| 96 | Depudecin | Drug Info | [37], [38] | |||
| 97 | HC-Toxin | Drug Info | [37] | |||
| 98 | M-carboxycinnamic acid bishydroxamide | Drug Info | [37], [38] | |||
| 99 | Scriptaid | Drug Info | [37], [15], [38] | |||
| 100 | SK-7041 | Drug Info | [37], [38] | |||
| 101 | SK-7068 | Drug Info | [37], [38] | |||
| 102 | Oxamflatin | Drug Info | [37], [38] | |||
| 103 | (E)-8-Biphenyl-4-yl-1-oxazol-2-yl-oct-7-en-1-one | Drug Info | [49] | |||
| 104 | 1,1,1-Trifluoro-8-(4-phenoxy-phenoxy)-octan-2-one | Drug Info | [50] | |||
| 105 | 1,1,1-Trifluoro-8-phenoxy-octan-2-one | Drug Info | [50] | |||
| 106 | 2-(methylsulfonylthio)ethyl 2-propylpentanoate | Drug Info | [51] | |||
| 107 | 4-Benzenesulfonylamino-N-hydroxy-benzamide | Drug Info | [52] | |||
| 108 | 4-Benzoylamino-N-hydroxy-benzamide | Drug Info | [53] | |||
| 109 | 4-Butyrylamino-N-hydroxy-benzamide | Drug Info | [54] | |||
| 110 | 4-Chloro-N-(5-hydroxycarbamoyl-pentyl)-benzamide | Drug Info | [55] | |||
| 111 | 4-Dimethylamino-N-(6-mercapto-hexyl)-benzamide | Drug Info | [56] | |||
| 112 | 4-Hydroxy-N-(5-hydroxycarbamoyl-pentyl)-benzamide | Drug Info | [57] | |||
| 113 | 4-Phenylbutyrohydroxamic acid | Drug Info | [58] | |||
| 114 | 4-tert-butyl-N-hydroxybenzamide | Drug Info | [59] | |||
| 115 | 5-(4-Chloro-phenyl)-pentanoic acid hydroxyamide | Drug Info | [60] | |||
| 116 | 5-(4-hydroxyphenyl)-3H-1,2-dithiole-3-thione | Drug Info | [51] | |||
| 117 | 5-Mercapto-pentanoic acid phenylamide | Drug Info | [56] | |||
| 118 | 6-(2-Bromo-acetylamino)-hexanoic acid phenylamide | Drug Info | [56] | |||
| 119 | 6-(3-Benzoyl-ureido)-hexanoic acid hydroxyamide | Drug Info | [61] | |||
| 120 | 6-(9H-carbazol-9-yl)-N-hydroxyhexanamide | Drug Info | [62] | |||
| 121 | 6-benzenesulfinylhexanoic acid hydroxamide | Drug Info | [63] | |||
| 122 | 6-benzenesulfonylhexanoic acid hydroxamide | Drug Info | [63] | |||
| 123 | 6-Mercapto-hexanoic acid phenylamide | Drug Info | [56] | |||
| 124 | 6-Phenoxy-hexane-1-thiol | Drug Info | [56] | |||
| 125 | 6-phenylsulfanylhexanoic acid hydroxamide | Drug Info | [63] | |||
| 126 | 7-(1H-indol-5-yloxy)-N-hydroxyheptanamide | Drug Info | [64] | |||
| 127 | 7-(3-Benzoyl-ureido)-heptanoic acid hydroxyamide | Drug Info | [61] | |||
| 128 | 7-(4-(dimethylamino)phenoxy)-N-hydroxyheptanamide | Drug Info | [64] | |||
| 129 | 7-(Biphenyl-3-yloxy)-1-oxazol-2-yl-heptan-1-one | Drug Info | [49] | |||
| 130 | 7-(Biphenyl-4-yloxy)-1,1,1-trifluoro-heptan-2-one | Drug Info | [50] | |||
| 131 | 7-(Biphenyl-4-yloxy)-1-oxazol-2-yl-heptan-1-one | Drug Info | [49] | |||
| 132 | 7-(Biphenyl-4-yloxy)-heptanoic acid hydroxyamide | Drug Info | [65] | |||
| 133 | 7-(Naphthalen-2-yloxy)-1-oxazol-2-yl-heptan-1-one | Drug Info | [49] | |||
| 134 | 7-Biphenyl-4-yl-heptanoic acid hydroxyamide | Drug Info | [66] | |||
| 135 | 7-Mercapto-heptanoic acid benzothiazol-2-ylamide | Drug Info | [56] | |||
| 136 | 7-Mercapto-heptanoic acid biphenyl-3-ylamide | Drug Info | [56] | |||
| 137 | 7-Mercapto-heptanoic acid biphenyl-4-ylamide | Drug Info | [56] | |||
| 138 | 7-Mercapto-heptanoic acid phenylamide | Drug Info | [56] | |||
| 139 | 7-Mercapto-heptanoic acid pyridin-3-ylamide | Drug Info | [56] | |||
| 140 | 7-Mercapto-heptanoic acid quinolin-3-ylamide | Drug Info | [56] | |||
| 141 | 7-mercapto-N-(4-phenylthiazol-2-yl)heptanamide | Drug Info | [67] | |||
| 142 | 7-Phenoxy-heptanoic acid hydroxyamide | Drug Info | [66] | |||
| 143 | 8-(3-Benzoyl-ureido)-octanoic acid hydroxyamide | Drug Info | [61] | |||
| 144 | 8-(4-bromophenyl)-N-hydroxy-8-oxooctanamide | Drug Info | [68] | |||
| 145 | 8-(Biphenyl-3-yloxy)-1,1,1-trifluoro-octan-2-one | Drug Info | [50] | |||
| 146 | 8-(biphenyl-4-yl)-N-hydroxy-8-oxooctanamide | Drug Info | [68] | |||
| 147 | 8-(Biphenyl-4-yloxy)-1,1,1-trifluoro-octan-2-one | Drug Info | [50] | |||
| 148 | 8-(Biphenyl-4-yloxy)-2-oxo-octanoic acid | Drug Info | [65] | |||
| 149 | 8-Mercapto-octanoic acid phenylamide | Drug Info | [56] | |||
| 150 | 8-Oxo-8-phenyl-octanoic acid | Drug Info | [57] | |||
| 151 | 8-Oxo-8-phenyl-octanoic acid hydroxyamide | Drug Info | [55] | |||
| 152 | 8-Phenyl-octanoic acid hydroxyamide | Drug Info | [66] | |||
| 153 | 9,9,9-Trifluoro-8-oxo-nonanoic acid phenylamide | Drug Info | [50] | |||
| 154 | 9-(Biphenyl-4-yloxy)-1,1,1-trifluoro-nonan-2-one | Drug Info | [50] | |||
| 155 | ADS-100380 | Drug Info | [69] | |||
| 156 | ADS-102550 | Drug Info | [69] | |||
| 157 | Azithromycin-N-benzyltriazolyldecahydroxamic Acid | Drug Info | [70] | |||
| 158 | Azithromycin-N-benzyltriazolylhexahydroxamic Acid | Drug Info | [70] | |||
| 159 | Azithromycin-N-benzyltriazolylnonahydroxamic Acid | Drug Info | [70] | |||
| 160 | Azithromycin-N-benzyltriazolyloctahydroxamic Acid | Drug Info | [70] | |||
| 161 | Azithromycinarylalkylhydroxamic Acid | Drug Info | [70] | |||
| 162 | AZUMAMIDE B | Drug Info | [71] | |||
| 163 | AZUMAMIDE C | Drug Info | [71] | |||
| 164 | AZUMAMIDE E | Drug Info | [71] | |||
| 165 | Cyclo(-L-Am7(S2Py)-A2in-L-Ala-D-Pro-) | Drug Info | [72] | |||
| 166 | Cyclo(-L-Am7(S2Py)-Aib-L-Ala-D-Pro-) | Drug Info | [72] | |||
| 167 | Cyclo(-L-Am7(S2Py)-Aib-L-Ala-D-Tic-) | Drug Info | [72] | |||
| 168 | Cyclo(-L-Am7(S2Py)-Aib-L-Ph4-D-Pro-) | Drug Info | [72] | |||
| 169 | Cyclo(-L-Am7(S2Py)-Aib-L-Ph5-D-Pro-) | Drug Info | [72] | |||
| 170 | Cyclo(-L-Am7(S2Py)-Aib-L-Phe-D-Pro-) | Drug Info | [72] | |||
| 171 | Cyclo(-L-Am7(S2Py)-Aib-L-Phg-D-Pro-) | Drug Info | [72] | |||
| 172 | Cyclo(-L-Am7(S2Py)-Aib-L-Ser(Bzl)-D-Pro-) | Drug Info | [72] | |||
| 173 | Cyclo(-L-Am7(S2Py)-Aib-L-Ser-D-Pro-) | Drug Info | [72] | |||
| 174 | Cyclo(-L-Am7(S2Py)-D-2MePhe-L-Ala-D-Pro-) | Drug Info | [72] | |||
| 175 | Cyclo(-L-Am7(S2Py)-D-A1in-L-Ala-D-Pro-) | Drug Info | [72] | |||
| 176 | Cyclo(-L-Am7(S2Py)-L-2MePhe-L-Ala-D-Pro-) | Drug Info | [72] | |||
| 177 | Cyclo(-L-Am7(S2Py)-L-A1in-L-Ala-D-Pro-) | Drug Info | [72] | |||
| 178 | Cyclostellettamine derivative | Drug Info | [73] | |||
| 179 | Desclasinose Azithromycinarylalkyl Hydroxamate | Drug Info | [70] | |||
| 180 | Gymnochrome E | Drug Info | [74] | |||
| 181 | LARGAZOLE | Drug Info | [75] | |||
| 182 | N,8-dihydroxy-8-(naphthalen-2-yl)octanamide | Drug Info | [68] | |||
| 183 | N-(2,3-Dimethylphenyl)-N'-hydroxyoctanediamide | Drug Info | [76] | |||
| 184 | N-(2,4-Dimethylphenyl)-N'-hydroxyoctanediamide | Drug Info | [76] | |||
| 185 | N-(2,5-Dimethylphenyl)-N'-hydroxyoctanediamide | Drug Info | [76] | |||
| 186 | N-(2,6-Dimethylphenyl)-N'-hydroxyoctanediamide | Drug Info | [76] | |||
| 187 | N-(2-amino-5-(thiophen-2-yl)phenyl)nicotinamide | Drug Info | [77] | |||
| 188 | N-(2-aminophenyl)-4-(chroman-3-ylmethyl)benzamide | Drug Info | [78] | |||
| 189 | N-(2-aminophenyl)-4-methoxybenzamide | Drug Info | [79] | |||
| 190 | N-(2-aminophenyl)nicotinamide | Drug Info | [77] | |||
| 191 | N-(2-aminophenyl)quinoxaline-6-carboxamide | Drug Info | [79] | |||
| 192 | N-(2-Ethylphenyl)-N'-hydroxyoctanediamide | Drug Info | [76] | |||
| 193 | N-(2-Mercapto-ethyl)-N'-phenyl-oxalamide | Drug Info | [80] | |||
| 194 | N-(2-Mercapto-ethyl)-N'-phenyl-succinamide | Drug Info | [80] | |||
| 195 | N-(3,4-Dimethylphenyl)-N'-hydroxyoctanediamide | Drug Info | [76] | |||
| 196 | N-(3,5-Dimethylphenyl)-N'-hydroxyoctanediamide | Drug Info | [76] | |||
| 197 | N-(3-Ethylphenyl)-N'-hydroxyoctanediamide | Drug Info | [76] | |||
| 198 | N-(4-aminobiphenyl-3-yl)nicotinamide | Drug Info | [77] | |||
| 199 | N-(4-Ethylphenyl)-N'-hydroxyoctanediamide | Drug Info | [76] | |||
| 200 | N-(4-hydroxybiphenyl-3-yl)benzamide | Drug Info | [77] | |||
| 201 | N-(5-Hydroxycarbamoyl-pentyl)-4-nitro-benzamide | Drug Info | [55] | |||
| 202 | N-(6-Hydroxycarbamoyl-hexyl)-benzamide | Drug Info | [57] | |||
| 203 | N-(6-Mercapto-hexyl)-benzamide | Drug Info | [56] | |||
| 204 | N-hydroxy-2,2'-bithiophene-5-carboxamide | Drug Info | [69] | |||
| 205 | N-Hydroxy-4-((R)-2-phenyl-butyrylamino)-benzamide | Drug Info | [53] | |||
| 206 | N-Hydroxy-4-((S)-2-phenyl-butyrylamino)-benzamide | Drug Info | [53] | |||
| 207 | N-Hydroxy-4-(2-phenyl-butyrylamino)-benzamide | Drug Info | [53] | |||
| 208 | N-Hydroxy-4-(3-phenyl-propionylamino)-benzamide | Drug Info | [81] | |||
| 209 | N-Hydroxy-4-(4-phenyl-butyrylamino)-benzamide | Drug Info | [53] | |||
| 210 | N-Hydroxy-4-(5-phenyl-pentanoylamino)-benzamide | Drug Info | [53] | |||
| 211 | N-Hydroxy-4-(pentanoylamino-methyl)-benzamide | Drug Info | [54] | |||
| 212 | N-Hydroxy-4-(phenylacetylamino-methyl)-benzamide | Drug Info | [54] | |||
| 213 | N-Hydroxy-4-phenylacetylamino-benzamide | Drug Info | [53] | |||
| 214 | N-hydroxy-5-(pyridin-2-yl)thiophene-2-carboxamide | Drug Info | [69] | |||
| 215 | N-hydroxy-5-(pyridin-3-yl)thiophene-2-carboxamide | Drug Info | [69] | |||
| 216 | N-hydroxy-5-(pyridin-4-yl)thiophene-2-carboxamide | Drug Info | [69] | |||
| 217 | N-hydroxy-5-phenylthiophene-2-carboxamide | Drug Info | [69] | |||
| 218 | N-hydroxy-6-oxo-6-phenylhexanamide | Drug Info | [68] | |||
| 219 | N-hydroxy-7-(4-methoxyphenyl)-7-oxoheptanamide | Drug Info | [68] | |||
| 220 | N-hydroxy-7-(naphthalen-2-yl)-7-oxoheptanamide | Drug Info | [68] | |||
| 221 | N-hydroxy-7-(naphthalen-2-yloxy)heptanamide | Drug Info | [64] | |||
| 222 | N-hydroxy-7-oxo-7-phenylheptanamide | Drug Info | [68] | |||
| 223 | N-hydroxy-8-(2-methoxyphenyl)-8-oxooctanamide | Drug Info | [68] | |||
| 224 | N-hydroxy-8-(4-methoxyphenyl)-8-oxooctanamide | Drug Info | [68] | |||
| 225 | N-hydroxy-8-(naphthalen-2-yl)non-8-enamide | Drug Info | [68] | |||
| 226 | N-hydroxy-8-(naphthalen-2-yl)oct-7-enamide | Drug Info | [68] | |||
| 227 | N-hydroxy-8-(naphthalen-2-yl)octanamide | Drug Info | [68] | |||
| 228 | N-hydroxy-8-oxo-8-(pyridin-3-yl)octanamide | Drug Info | [68] | |||
| 229 | N-hydroxy-9-oxo-9-phenylnonanamide | Drug Info | [68] | |||
| 230 | N-Hydroxy-N'-(2-methylphenyl)octanediamide | Drug Info | [76] | |||
| 231 | N-Hydroxy-N'-(3-methylphenyl)octanediamide | Drug Info | [76] | |||
| 232 | N-Hydroxy-N'-(4-methoxyphenyl)octanediamide | Drug Info | [76] | |||
| 233 | N-Hydroxy-N'-(4-methylphenyl)octanediamide | Drug Info | [76] | |||
| 234 | N-hydroxybenzo[b]thiophene-2-carboxamide | Drug Info | [82] | |||
| 235 | N1-(biphenyl-3-yl)-N8-hydroxyoctanediamide | Drug Info | [83] | |||
| 236 | N1-(biphenyl-4-yl)-N8-hydroxyoctanediamide | Drug Info | [84] | |||
| 237 | N1-hydroxy-N8-(4-phenylthiazol-2-yl)octanediamide | Drug Info | [84] | |||
| 238 | nexturastat A | Drug Info | [85] | |||
| 239 | NSC-746457 | Drug Info | [86] | |||
| 240 | Octanedioic acid bis-hydroxyamide | Drug Info | [87] | |||
| 241 | Octanedioic acid hydroxyamide pyridin-2-ylamide | Drug Info | [57] | |||
| 242 | Octanedioic acid hydroxyamide pyridin-4-ylamide | Drug Info | [57] | |||
| 243 | PSAMMAPLIN A | Drug Info | [55] | |||
| 244 | SK-683 | Drug Info | [88] | |||
| 245 | ST-2986 | Drug Info | [89] | |||
| 246 | ST-2987 | Drug Info | [89] | |||
| 247 | ST-3050 | Drug Info | [89] | |||
| 248 | Thioacetic acid S-(6-phenylcarbamoyl-hexyl) ester | Drug Info | [56] | |||
| Modulator | [+] 2 Modulator drugs | + | ||||
| 1 | HBI-8000 | Drug Info | [40] | |||
| 2 | RG-2833 | Drug Info | [40] | |||
| Cell-based Target Expression Variations | Top | |||||
|---|---|---|---|---|---|---|
| Cell-based Target Expression Variations | ||||||
| Drug Binding Sites of Target | Top | |||||
|---|---|---|---|---|---|---|
| Ligand Name: Myo-inositol hexaphosphate | Ligand Info | |||||
| Structure Description | HDAC1:MTA1 in complex with inositol-6-phosphate and a novel peptide inhibitor based on histone H4 | PDB:5ICN | ||||
| Method | X-ray diffraction | Resolution | 3.30 Å | Mutation | No | [90] |
| PDB Sequence |
RRKVCYYYDG
17 DVGNYYYGQG27 HPMKPHRIRM37 THNLLLNYGL47 YRKMEIYRPH57 KANAEEMTKY 67 HSDDYIKFLR77 SIRPDNMSEY87 SKQMQRFNVG97 EDCPVFDGLF107 EFCQLSTGGS 117 VASAVKLNKQ127 QTDIAVNWAG137 GLHHAKKSEA147 SGFCYVNDIV157 LAILELLKYH 167 QRVLYIDIDI177 HHGDGVEEAF187 YTTDRVMTVS197 FHKYGEYFPG207 TGDLRDIGAG 217 KGKYYAVNYP227 LRDGIDDESY237 EAIFKPVMSK247 VMEMFQPSAV257 VLQCGSDSLS 267 GDRLGCFNLT277 IKGHAKCVEF287 VKSFNLPMLM297 LGGGGYTIRN307 VARCWTYETA 317 VALDTEIPNE327 LPYNDYFEYF337 GPDFKLHISP347 SNMTNQNTNE357 YLEKIKQRLF 367 ENLRMLPHA
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| Click to View More Binding Site Information of This Target and Ligand Pair | ||||||
| Ligand Name: (2S)-2-amino-8-(hydroxyamino)-8-oxooctanoic acid | Ligand Info | |||||
| Structure Description | HDAC1:MTA1 in complex with inositol-6-phosphate and a novel peptide inhibitor based on histone H4 | PDB:5ICN | ||||
| Method | X-ray diffraction | Resolution | 3.30 Å | Mutation | No | [90] |
| PDB Sequence |
RRKVCYYYDG
17 DVGNYYYGQG27 HPMKPHRIRM37 THNLLLNYGL47 YRKMEIYRPH57 KANAEEMTKY 67 HSDDYIKFLR77 SIRPDNMSEY87 SKQMQRFNVG97 EDCPVFDGLF107 EFCQLSTGGS 117 VASAVKLNKQ127 QTDIAVNWAG137 GLHHAKKSEA147 SGFCYVNDIV157 LAILELLKYH 167 QRVLYIDIDI177 HHGDGVEEAF187 YTTDRVMTVS197 FHKYGEYFPG207 TGDLRDIGAG 217 KGKYYAVNYP227 LRDGIDDESY237 EAIFKPVMSK247 VMEMFQPSAV257 VLQCGSDSLS 267 GDRLGCFNLT277 IKGHAKCVEF287 VKSFNLPMLM297 LGGGGYTIRN307 VARCWTYETA 317 VALDTEIPNE327 LPYNDYFEYF337 GPDFKLHISP347 SNMTNQNTNE357 YLEKIKQRLF 367 ENLRMLPHA
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| Click to View More Binding Site Information of This Target with Different Ligands | ||||||
| Different Human System Profiles of Target | Top |
|---|---|
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Human Similarity Proteins
of target is determined by comparing the sequence similarity of all human proteins with the target based on BLAST. The similarity proteins for a target are defined as the proteins with E-value < 0.005 and outside the protein families of the target.
A target that has fewer human similarity proteins outside its family is commonly regarded to possess a greater capacity to avoid undesired interactions and thus increase the possibility of finding successful drugs
(Brief Bioinform, 21: 649-662, 2020).
Human Tissue Distribution
of target is determined from a proteomics study that quantified more than 12,000 genes across 32 normal human tissues. Tissue Specificity (TS) score was used to define the enrichment of target across tissues.
The distribution of targets among different tissues or organs need to be taken into consideration when assessing the target druggability, as it is generally accepted that the wider the target distribution, the greater the concern over potential adverse effects
(Nat Rev Drug Discov, 20: 64-81, 2021).
Human Pathway Affiliation
of target is determined by the life-essential pathways provided on KEGG database. The target-affiliated pathways were defined based on the following two criteria (a) the pathways of the studied target should be life-essential for both healthy individuals and patients, and (b) the studied target should occupy an upstream position in the pathways and therefore had the ability to regulate biological function.
Targets involved in a fewer pathways have greater likelihood to be successfully developed, while those associated with more human pathways increase the chance of undesirable interferences with other human processes
(Pharmacol Rev, 58: 259-279, 2006).
Biological Network Descriptors
of target is determined based on a human protein-protein interactions (PPI) network consisting of 9,309 proteins and 52,713 PPIs, which were with a high confidence score of ≥ 0.95 collected from STRING database.
The network properties of targets based on protein-protein interactions (PPIs) have been widely adopted for the assessment of target’s druggability. Proteins with high node degree tend to have a high impact on network function through multiple interactions, while proteins with high betweenness centrality are regarded to be central for communication in interaction networks and regulate the flow of signaling information
(Front Pharmacol, 9, 1245, 2018;
Curr Opin Struct Biol. 44:134-142, 2017).
Human Similarity Proteins
Human Tissue Distribution
Human Pathway Affiliation
Biological Network Descriptors
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There is no similarity protein (E value < 0.005) for this target
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Note:
If a protein has TS (tissue specficity) scores at least in one tissue >= 2.5, this protein is called tissue-enriched (including tissue-enriched-but-not-specific and tissue-specific). In the plots, the vertical lines are at thresholds 2.5 and 4.
|
| KEGG Pathway | Pathway ID | Affiliated Target | Pathway Map |
|---|---|---|---|
| Cell cycle | hsa04110 | Affiliated Target |
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| Class: Cellular Processes => Cell growth and death | Pathway Hierarchy | ||
| Longevity regulating pathway - multiple species | hsa04213 | Affiliated Target |
|
| Class: Organismal Systems => Aging | Pathway Hierarchy | ||
| Notch signaling pathway | hsa04330 | Affiliated Target |
|
| Class: Environmental Information Processing => Signal transduction | Pathway Hierarchy | ||
| Neutrophil extracellular trap formation | hsa04613 | Affiliated Target |
|
| Class: Organismal Systems => Immune system | Pathway Hierarchy | ||
| Thyroid hormone signaling pathway | hsa04919 | Affiliated Target |
|
| Class: Organismal Systems => Endocrine system | Pathway Hierarchy | ||
| Degree | 166 | Degree centrality | 1.78E-02 | Betweenness centrality | 2.19E-02 |
|---|---|---|---|---|---|
| Closeness centrality | 2.78E-01 | Radiality | 1.47E+01 | Clustering coefficient | 6.11E-02 |
| Neighborhood connectivity | 3.19E+01 | Topological coefficient | 1.82E-02 | Eccentricity | 11 |
| Download | Click to Download the Full PPI Network of This Target | ||||
| Chemical Structure based Activity Landscape of Target | Top |
|---|---|
| Drug Property Profile of Target | Top | |
|---|---|---|
| (1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
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| (3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
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| (5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
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| "RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five | ||
| Co-Targets | Top | |||||
|---|---|---|---|---|---|---|
| Co-Targets | ||||||
| Target Poor or Non Binders | Top | |||||
|---|---|---|---|---|---|---|
| Target Poor or Non Binders | ||||||
| Target Regulators | Top | |||||
|---|---|---|---|---|---|---|
| Target-regulating microRNAs | ||||||
| Target-interacting Proteins | ||||||
| Target Profiles in Patients | Top | |||||
|---|---|---|---|---|---|---|
| Target Expression Profile (TEP) | ||||||
| Target-Related Models and Studies | Top | |||||
|---|---|---|---|---|---|---|
| Target Validation | ||||||
| Target QSAR Model | ||||||
| References | Top | |||||
|---|---|---|---|---|---|---|
| REF 1 | Protein methyltransferases as a target class for drug discovery. Nat Rev Drug Discov. 2009 Sep;8(9):724-32. | |||||
| REF 2 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. | |||||
| REF 3 | 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. (Ligand id: 7006). | |||||
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| REF 5 | 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. (Ligand id: 6852). | |||||
| REF 6 | Emerging therapies for multiple myeloma. Expert Opin Emerg Drugs. 2009 Mar;14(1):99-127. | |||||
| REF 7 | 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. (Ligand id: 8305). | |||||
| REF 8 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800025931) | |||||
| REF 9 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
| REF 10 | Novel drugs and therapeutic targets for severe mood disorders. Neuropsychopharmacology. 2008 Aug;33(9):2080-92. | |||||
| REF 11 | ClinicalTrials.gov (NCT03538171) Ph3 Study of Exemestane With or Without Entinostat in Chinese Patients With Hormone Receptor-Positive, Locally Advanced or Metastatic Breast Cancer. U.S. National Institutes of Health. | |||||
| REF 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. (Ligand id: 7008). | |||||
| REF 13 | MGCD0103, a novel isotype-selective histone deacetylase inhibitor, has broad spectrum antitumor activity in vitro and in vivo. Mol Cancer Ther. 2008 Apr;7(4):759-68. | |||||
| REF 14 | 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. (Ligand id: 8480). | |||||
| REF 15 | Emerging disease-modifying therapies for the treatment of motor neuron disease/amyotropic lateral sclerosis. Expert Opin Emerg Drugs. 2007 May;12(2):229-52. | |||||
| REF 16 | 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. (Ligand id: 7502). | |||||
| REF 17 | 2011 Pipeline of 4SC AG. | |||||
| REF 18 | ClinicalTrials.gov (NCT02448641) Study of Modified Stem Cells (SB623) in Patients With Chronic Motor Deficit From Ischemic Stroke. U.S. National Institutes of Health. | |||||
| REF 19 | The enhancement of phase 2 enzyme activities by sodium butyrate in normal intestinal epithelial cells is associated with Nrf2 and p53. Mol Cell Biochem. 2012 Nov;370(1-2):7-14. | |||||
| REF 20 | ClinicalTrials.gov (NCT03397706) Dose Escalation & Expansion Study of Oral VRx-3996 & Valganciclovir in Subjects With EBV-Associated Lymphoid Malignancies. U.S. National Institutes of Health. | |||||
| REF 21 | ClinicalTrials.gov (NCT02414516) A Dose-Escalation Study of OBP-801 in Patients With Advanced Solid Tumors. U.S. National Institutes of Health. | |||||
| REF 22 | 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. (Ligand id: 7501). | |||||
| REF 23 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800035788) | |||||
| REF 24 | Epigenetics in vascular disease - therapeutic potential of new agents. Curr Vasc Pharmacol. 2014 Jan;12(1):77-86. | |||||
| REF 25 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004320) | |||||
| REF 26 | 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. (Ligand id: 8367). | |||||
| REF 27 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002525) | |||||
| REF 28 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800018698) | |||||
| REF 29 | Preclinical and clinical studies of clindamycin-2-phosphate (author's transl). Jpn J Antibiot. 1977 Jan;30(1):42-50. | |||||
| REF 30 | HDAC inhibitors repress the polycomb protein BMI1. Cell Cycle. 2010 Jul 15; 9(14): 2722-2730. | |||||
| REF 31 | Inhibition of maize histone deacetylases by HC toxin, the host-selective toxin of Cochliobolus carbonum. Plant Cell. 1995 Nov;7(11):1941-50. | |||||
| REF 32 | Selective extraction of an intrinsic fat-cell plasma-membrane glycoprotein by Triton X-100. Correlation with [3H]cytochalasin B binding activity. FEBS Lett. 1977 Nov 1;83(1):71-5. | |||||
| REF 33 | 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. (Ligand id: 7505). | |||||
| REF 34 | Class I histone deacetylase-selective novel synthetic inhibitors potently inhibit human tumor proliferation. Clin Cancer Res. 2004 Aug 1;10(15):5271-81. | |||||
| REF 35 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007547) | |||||
| REF 36 | Emerging drugs in cutaneous T cell lymphoma. Expert Opin Emerg Drugs. 2008 Jun;13(2):345-61. | |||||
| REF 37 | Histone deacetylase inhibitors in cancer therapy: latest developments, trends and medicinal chemistry perspective. Anticancer Agents Med Chem. 2007 Sep;7(5):576-92. | |||||
| REF 38 | Anticancer activities of histone deacetylase inhibitors. Nat Rev Drug Discov. 2006 Sep;5(9):769-84. | |||||
| REF 39 | Discovery of a potent class I selective ketone histone deacetylase inhibitor with antitumor activity in vivo and optimized pharmacokinetic properties. J Med Chem. 2009 Jun 11;52(11):3453-6. | |||||
| REF 40 | Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41. | |||||
| REF 41 | 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. | |||||
| REF 42 | NVP-LAQ824 is a potent novel histone deacetylase inhibitor with significant activity against multiple myeloma. Blood. 2003 Oct 1;102(7):2615-22. | |||||
| REF 43 | Two histone deacetylase inhibitors, trichostatin A and sodium butyrate, suppress differentiation into osteoclasts but not into macrophages. Blood. 2003 May 1;101(9):3451-9. | |||||
| REF 44 | 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. | |||||
| REF 45 | 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). | |||||
| REF 46 | Novel histone deacetylase 6 (HDAC6) selective inhibitors: a patent evaluation (WO2014181137).Expert Opin Ther Pat. 2017 Mar;27(3):229-236. | |||||
| REF 47 | Cyclin-dependent kinase inhibitors for cancer therapy: a patent review (2009 - 2014).Expert Opin Ther Pat. 2015;25(9):953-70. | |||||
| REF 48 | HDAC inhibitors: a 2013-2017 patent survey.Expert Opin Ther Pat. 2018 Apr 19:1-17. | |||||
| REF 49 | Heterocyclic ketones as inhibitors of histone deacetylase. Bioorg Med Chem Lett. 2003 Nov 17;13(22):3909-13. | |||||
| REF 50 | Trifluoromethyl ketones as inhibitors of histone deacetylase. Bioorg Med Chem Lett. 2002 Dec 2;12(23):3443-7. | |||||
| REF 51 | New sulfurated derivatives of valproic acid with enhanced histone deacetylase inhibitory activity. Bioorg Med Chem Lett. 2008 Mar 15;18(6):1893-7. | |||||
| REF 52 | Design and synthesis of a novel class of histone deacetylase inhibitors. Bioorg Med Chem Lett. 2001 Nov 5;11(21):2847-50. | |||||
| REF 53 | Structure-based optimization of phenylbutyrate-derived histone deacetylase inhibitors. J Med Chem. 2005 Aug 25;48(17):5530-5. | |||||
| REF 54 | 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 55 | Histone deacetylase inhibitors. J Med Chem. 2003 Nov 20;46(24):5097-116. | |||||
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| REF 57 | 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 58 | Chemical phylogenetics of histone deacetylases. Nat Chem Biol. 2010 Mar;6(3):238-243. | |||||
| REF 59 | Design of novel histone deacetylase inhibitors. Bioorg Med Chem Lett. 2007 Aug 15;17(16):4619-24. | |||||
| REF 60 | 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 61 | 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. | |||||
| REF 62 | Inhibitors selective for HDAC6 in enzymes and cells. Bioorg Med Chem Lett. 2010 Dec 1;20(23):7067-70. | |||||
| REF 63 | 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 64 | Structure-activity relationships of aryloxyalkanoic acid hydroxyamides as potent inhibitors of histone deacetylase. Bioorg Med Chem Lett. 2007 Jan 1;17(1):136-41. | |||||
| REF 65 | Alpha-keto amides as inhibitors of histone deacetylase. Bioorg Med Chem Lett. 2003 Oct 6;13(19):3331-5. | |||||
| REF 66 | 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. | |||||
| REF 67 | 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 68 | 3D-QSAR studies of HDACs inhibitors using pharmacophore-based alignment. Eur J Med Chem. 2009 Jul;44(7):2868-76. | |||||
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| REF 70 | Non-peptide macrocyclic histone deacetylase inhibitors. J Med Chem. 2009 Jan 22;52(2):456-68. | |||||
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| REF 72 | Molecular design of histone deacetylase inhibitors by aromatic ring shifting in chlamydocin framework. Bioorg Med Chem. 2007 Dec 15;15(24):7830-9. | |||||
| REF 73 | 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 74 | Gymnochromes E and F, cytotoxic phenanthroperylenequinones from a deep-water crinoid, Holopus rangii. J Nat Prod. 2010 Apr 23;73(4):712-5. | |||||
| REF 75 | Synthesis and biological characterization of the histone deacetylase inhibitor largazole and C7- modified analogues. J Med Chem. 2010 Jun 24;53(12):4654-67. | |||||
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| REF 77 | 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). | |||||
| REF 78 | N-(2-Amino-phenyl)-4-(heteroarylmethyl)-benzamides as new histone deacetylase inhibitors. Bioorg Med Chem Lett. 2007 Dec 15;17(24):6729-33. | |||||
| REF 79 | Novel aminophenyl benzamide-type histone deacetylase inhibitors with enhanced potency and selectivity. J Med Chem. 2007 Nov 15;50(23):5543-6. | |||||
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