Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T68547 Target Info
Target Name Histone deacetylase 1 (HDAC1)
Synonyms
RPD3L1; HD1
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Target Type Successful Target
Gene Name HDAC1
Biochemical Class Carbon-nitrogen hydrolase
UniProt ID
HDAC1_HUMAN
Co-Targets of This Target  Top
Co-Target Name Human immunodeficiency virus Tat protein (HIV tat) Successful Target
UniProt ID TAT_HV1H2
Gene Name HIV tat
Synonyms
Transactivating regulatory protein; TAT protein
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Representative Drug(s) Panobinostat Drug Info EC50 = 130 nM [1]
Co-Target Name Heat shock protein 90 alpha (HSP90A) Successful Target
UniProt ID HS90A_HUMAN
Gene Name HSP90AA1
Synonyms
Renal carcinoma antigen NY-REN-38; Lipopolysaccharide-associated protein 2; LPS-associated protein 2; LAP-2; Heat shock protein HSP 90-alpha; Heat shock 86 kDa; HSPCA; HSPC1; HSP90A; HSP86; HSP 86
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Representative Drug(s) Vorinostat Drug Info IC50 ~ 1000 nM [2]
Co-Target Name Histone deacetylase 2 (HDAC2) Clinical trial Target
UniProt ID HDAC2_HUMAN
Gene Name HDAC2
Synonyms
HD2
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Representative Drug(s) Romidepsin Drug Info Ki = 0.038 nM Click to Show More [3]
2 Panobinostat Drug Info Ki = 0.65 nM [5]
3 NVP-LAQ824 Drug Info Ki = 1.4 nM [5]
4 Vorinostat Drug Info Ki = 1.6 nM [5]
5 ITF2357 Drug Info Ki = 3 nM [5]
6 CHR-3996 Drug Info IC50 = 4 nM [11]
7 SNDX-275 Drug Info IC50 = 15 nM [14]
8 MGCD-0103 Drug Info IC50 = 22 nM [15]
9 SB-639 Drug Info Ki = 36 nM [7]
10 HBI-8000 Drug Info IC50 = 110 nM [18]
Co-Target Name Histone deacetylase 4 (HDAC4) Clinical trial Target
UniProt ID HDAC4_HUMAN
Gene Name HDAC4
Synonyms
KIAA0288; HD4
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Representative Drug(s) Vorinostat Drug Info IC50 = 0.047 ug.mL-1 Click to Show More [4]
2 Panobinostat Drug Info Ki = 0.6 nM [7]
3 NVP-LAQ824 Drug Info IC50 = 1 nM [6]
4 SB-639 Drug Info Ki = 8.5 nM [7]
5 Romidepsin Drug Info Ki = 20.5 nM [3]
6 SNDX-275 Drug Info IC50 = 510 nM [6]
Co-Target Name Histone deacetylase 3 (HDAC3) Clinical trial Target
UniProt ID HDAC3_HUMAN
Gene Name HDAC3
Synonyms
SMAP45; RPD32; RPD3-2; HD3
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Representative Drug(s) Romidepsin Drug Info Ki = 0.15 nM Click to Show More [5]
2 NVP-LAQ824 Drug Info IC50 = 0.4 nM [6]
3 Panobinostat Drug Info Ki = 1.1 nM [9]
4 Vorinostat Drug Info IC50 = 1.4 nM [10]
5 ITF2357 Drug Info Ki = 3 nM [5]
6 CHR-3996 Drug Info IC50 = 7 nM [11]
7 SB-639 Drug Info Ki = 12 nM [7]
8 RG-2833 Drug Info IC50 = 60 nM [16]
9 SNDX-275 Drug Info IC50 = 120 nM [14]
10 MGCD-0103 Drug Info Ki = 265 nM [5]
11 HBI-8000 Drug Info IC50 = 265 nM [19]
Co-Target Name Histone deacetylase 6 (HDAC6) Clinical trial Target
UniProt ID HDAC6_HUMAN
Gene Name HDAC6
Synonyms
KIAA0901; JM21; HD6
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Representative Drug(s) Panobinostat Drug Info Ki = 0.7 nM Click to Show More [7]
2 Vorinostat Drug Info Ki = 1 nM [8]
3 ITF2357 Drug Info Ki = 4.2 nM [9]
4 NVP-LAQ824 Drug Info IC50 = 5.93 nM [13]
5 Romidepsin Drug Info Ki = 9.5 nM [5]
6 SB-639 Drug Info Ki = 20 nM [7]
7 Resminostat Drug Info IC50 = 72 nM [17]
Co-Target Name Bromodomain-containing protein 4 (BRD4) Clinical trial Target
UniProt ID BRD4_HUMAN
Gene Name BRD4
Synonyms
Protein HUNK1; HUNK1
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Representative Drug(s) Panobinostat Drug Info IC50 = 5 nM Click to Show More [12]
2 Vorinostat Drug Info IC50 = 10 nM [12]
3 Romidepsin Drug Info IC50 = 36 nM [12]
Co-Target Name Albendazole monooxygenase (CYP3A4) Clinical trial Target
UniProt ID CP3A4_HUMAN
Gene Name CYP3A4
Synonyms
Taurochenodeoxycholate 6-alpha-hydroxylase; Quinine 3-monooxygenase; P450-PCN1; Nifedipine oxidase; NF-25; HLp; Cytochrome P450-PCN1; Cytochrome P450 NF-25; Cytochrome P450 HLp; Cytochrome P450 3A4; Cytochrome P450 3A3; CYPIIIA4; CYPIIIA3; CYP3A3; Albendazole sulfoxidase; Albendazole monooxygenase (sulfoxide-forming); 1,8-cineole 2-exo-monooxygenase
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Representative Drug(s) MGCD-0103 Drug Info IC50 = 570 nM Click to Show More [20]
2 SNDX-275 Drug Info IC50 = 730 nM [20]
Co-Target Name Histone deacetylase 8 (HDAC8) Patented-recorded Target
UniProt ID HDAC8_HUMAN
Gene Name HDAC8
Synonyms
Histone deacetylase-8; HDACL1; HD8; CDA07
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Representative Drug(s) Romidepsin Drug Info Ki = 0.15 nM Click to Show More [3]
2 Vorinostat Drug Info IC50 ~ 1 nM [22]
3 NVP-LAQ824 Drug Info IC50 = 3.84 nM [13]
4 Panobinostat Drug Info IC50 = 4.86 nM [24]
5 ITF2357 Drug Info Ki = 39 nM [5]
6 SB-639 Drug Info Ki = 82 nM [25]
7 SNDX-275 Drug Info IC50 = 181 nM [28]
8 HBI-8000 Drug Info IC50 = 833 nM [19]
Co-Target Name Histone deacetylase 11 (HDAC11) Patented-recorded Target
UniProt ID HDA11_HUMAN
Gene Name HDAC11
Synonyms
HD11
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Representative Drug(s) Romidepsin Drug Info IC50 = 0.3 nM Click to Show More [21]
2 Panobinostat Drug Info IC50 = 1.6 nM [23]
3 NVP-LAQ824 Drug Info IC50 = 5.58 nM [13]
4 SB-639 Drug Info Ki = 12.8 nM [25]
5 Vorinostat Drug Info Ki = 13 nM [3]
6 MGCD-0103 Drug Info IC50 = 590 nM [29]
7 HBI-8000 Drug Info IC50 = 760 nM [19]
8 SNDX-275 Drug Info IC50 = 900 nM [30]
Co-Target Name Histone deacetylase 5 (HDAC5) Patented-recorded Target
UniProt ID HDAC5_HUMAN
Gene Name HDAC5
Synonyms
KIAA0600; HD5; Antigen NY-CO-9
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Representative Drug(s) Panobinostat Drug Info Ki = 0.7 nM Click to Show More [7]
2 Vorinostat Drug Info IC50 ~ 1 nM [22]
3 NVP-LAQ824 Drug Info IC50 = 5.58 nM [13]
4 SB-639 Drug Info Ki = 17 nM [7]
5 CHR-3996 Drug Info IC50 = 200 nM [11]
6 Romidepsin Drug Info Ki = 550 nM [5]
7 ITF2357 Drug Info Ki = 600 nM [9]
8 SNDX-275 Drug Info IC50 ~ 1000 nM [31]
Co-Target Name Histone deacetylase 10 (HDAC10) Patented-recorded Target
UniProt ID HDA10_HUMAN
Gene Name HDAC10
Synonyms
Polyamine deacetylase HDAC10; HD10
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Representative Drug(s) Romidepsin Drug Info IC50 = 0.9 nM Click to Show More [21]
2 Panobinostat Drug Info IC50 = 2.1 nM [23]
3 NVP-LAQ824 Drug Info IC50 = 8.41 nM [13]
4 SB-639 Drug Info Ki = 18.9 nM [25]
5 Vorinostat Drug Info Ki = 40 nM [27]
6 HBI-8000 Drug Info IC50 = 235 nM [19]
7 SNDX-275 Drug Info IC50 ~ 1000 nM [31]
Co-Target Name Histone deacetylase 7 (HDAC7) Patented-recorded Target
UniProt ID HDAC7_HUMAN
Gene Name HDAC7
Synonyms
Histone deacetylase 7A; HDAC7A; HD7a; HD7
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Representative Drug(s) Vorinostat Drug Info IC50 ~ 1 nM Click to Show More [22]
2 Panobinostat Drug Info Ki = 2.3 nM [7]
3 NVP-LAQ824 Drug Info IC50 = 6.11 nM [13]
4 ITF2357 Drug Info Ki = 240 nM [9]
5 SNDX-275 Drug Info IC50 ~ 1000 nM [31]
Co-Target Name Histone deacetylase 9 (HDAC9) Patented-recorded Target
UniProt ID HDAC9_HUMAN
Gene Name HDAC9
Synonyms
MITR; MEF2-interacting transcription repressor MITR; KIAA0744; Histone deacetylase-related protein; Histone deacetylase 7B; HDRP; HDAC7B; HDAC7; HD9; HD7b
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Representative Drug(s) Panobinostat Drug Info Ki = 1.2 nM Click to Show More [7]
2 NVP-LAQ824 Drug Info IC50 = 8.24 nM [13]
3 SB-639 Drug Info Ki = 19 nM [7]
4 Vorinostat Drug Info IC50 = 20 nM [26]
5 ITF2357 Drug Info Ki = 390 nM [5]
6 SNDX-275 Drug Info IC50 ~ 1000 nM [31]
Co-Target Name Histone deacetylase 3-Nuclear receptor corepressor 1 complex (HDAC3-NCOR1) Co-Target
UniProt ID HDAC3_HUMAN-NCOR1_HUMAN
Gene Name HDAC3-NCOR1
Representative Drug(s) Romidepsin Drug Info Ki = 0.15 nM Click to Show More [3]
2 Vorinostat Drug Info IC50 = 9.8 nM [35]
3 MGCD-0103 Drug Info IC50 = 22 nM [15]
Co-Target Name Histone deacetylase 3-Nuclear receptor corepressor 2 complex (HDAC3-NCOR2) Co-Target
UniProt ID HDAC3_HUMAN-NCOR2_HUMAN
Gene Name HDAC3-NCOR2
Representative Drug(s) Panobinostat Drug Info IC50 = 1.673 nM Click to Show More [32]
2 Vorinostat Drug Info Ki = 2 nM [8]
3 Romidepsin Drug Info IC50 = 3 nM [33]
4 RG-2833 Drug Info Ki = 5 nM [34]
5 MGCD-0103 Drug Info IC50 = 45 nM [36]
6 SNDX-275 Drug Info IC50 = 77.18 nM [32]
7 HBI-8000 Drug Info IC50 = 330 nM [18]
References  Top
REF 1 Identification of 5-Substituted 2-Acylaminothiazoles That Activate Tat-Mediated Transcription in HIV-1 Latency Models. J Med Chem. 2019 May 23;62(10):5148-5175.
REF 2 1-Aroylindoline-hydroxamic acids as anticancer agents, inhibitors of HSP90 and HDAC. Eur J Med Chem. 2018 Apr 25;150:667-677.
REF 3 Total synthesis and full histone deacetylase inhibitory profiling of Azumamides A-E as well as beta?- epi-Azumamide E and beta?-epi-Azumamide E. J Med Chem. 2013 Aug 22;56(16):6512-20.
REF 4 Discovery of uracil-based histone deacetylase inhibitors able to reduce acquired antifungal resistance and trailing growth in Candida albicans. Bioorg Med Chem Lett. 2007 Mar 1;17(5):1221-5.
REF 5 Chemical phylogenetics of histone deacetylases. Nat Chem Biol. 2010 Mar;6(3):238-243.
REF 6 Unraveling the hidden catalytic activity of vertebrate class IIa histone deacetylases. Proc Natl Acad Sci U S A. 2007 Oct 30;104(44):17335-40.
REF 7 Discovery of (2E)-3-{2-butyl-1-[2-(diethylamino)ethyl]-1H-benzimidazol-5-yl}-N-hydroxyacrylamide (SB939), an orally active histone deacetylase inhibitor with a superior preclinical profile. J Med Chem. 2011 Jul 14;54(13):4694-720.
REF 8 Development of a fluorescence polarization based assay for histone deacetylase ligand discovery. Bioorg Med Chem Lett. 2008 May 1;18(9):2809-12.
REF 9 Evaluation of histone deacetylase inhibitors (HDACi) as therapeutic leads for human African trypanosomiasis (HAT). Bioorg Med Chem. 2015 Aug 15;23(16):5151-5.
REF 10 Design and Synthesis of Simplified Largazole Analogues as Isoform-Selective Human Lysine Deacetylase Inhibitors. J Med Chem. 2016 Feb 25;59(4):1613-33.
REF 11 Discovery of 2-(6-{[(6-fluoroquinolin-2-yl)methyl]amino}bicyclo[3.1.0]hex-3-yl)-N-hydroxypyrimidine-5-carboxamide (CHR-3996), a class I selective orally active histone deacetylase inhibitor. J Med Chem. 2010 Dec 23;53(24):8663-78.
REF 12 Structure-based design, synthesis and in vitro antiproliferative effects studies of novel dual BRD4/HDAC inhibitors. Bioorg Med Chem Lett. 2017 Sep 1;27(17):4051-5.
REF 13 Non-natural macrocyclic inhibitors of histone deacetylases: design, synthesis, and activity. J Med Chem. 2010 Dec 9;53(23):8387-99.
REF 14 On the inhibition of histone deacetylase 8. Bioorg Med Chem. 2010 Jun 1;18(11):4103-10.
REF 15 Discovery of potent, isoform-selective inhibitors of histone deacetylase containing chiral heterocyclic capping groups and a N-(2-aminophenyl)benzamide binding unit. J Med Chem. 2013 Aug 8;56(15):6156-74.
REF 16 HDAC3 is a potential validated target for cancer: An overview on the benzamide-based selective HDAC3 inhibitors through comparative SAR/QSAR/QAAR approaches. Eur J Med Chem. 2018 Sep 5;157:1127-42.
REF 17 Exploring Structural Determinants of Inhibitor Affinity and Selectivity in Complexes with Histone Deacetylase 6. J Med Chem. 2020 Jan 9;63(1):295-308.
REF 18 Nicotinamide Phosphoribosyltransferase (NAMPT) Is a New Target of Antitumor Agent Chidamide. ACS Med Chem Lett. 2019 Dec 13;11(1):40-44.
REF 19 Design, synthesis and biological evaluation of novel isoindolinone derivatives as potent histone deacetylase inhibitors. Eur J Med Chem. 2019 Apr 15;168:110-122.
REF 20 The design, synthesis and structure-activity relationships of novel isoindoline-based histone deacetylase inhibitors. Bioorg Med Chem Lett. 2011 Aug 15;21(16):4909-12.
REF 21 Modulation of Activity Profiles for Largazole-Based HDAC Inhibitors through Alteration of Prodrug Properties. ACS Med Chem Lett. 2014 Jul 7;5(8):905-10.
REF 22 Optimization of a series of potent and selective ketone histone deacetylase inhibitors. Bioorg Med Chem Lett. 2008 Oct 15;18(20):5528-32.
REF 23 Kinase and Histone Deacetylase Hybrid Inhibitors for Cancer Therapy. J Med Chem. 2019 Apr 11;62(7):3171-3183.
REF 24 Development of Purine-Based Hydroxamic Acid Derivatives: Potent Histone Deacetylase Inhibitors with Marked in Vitro and in Vivo Antitumor Activities. J Med Chem. 2016 Jun 9;59(11):5488-504.
REF 25 N-Hydroxy-1,2-disubstituted-1H-benzimidazol-5-yl acrylamides as novel histone deacetylase inhibitors: design, synthesis, SAR studies, and in vivo antitumor activity. Bioorg Med Chem Lett. 2009 Mar 1;19(5):1403-8.
REF 26 Oxime amides as a novel zinc binding group in histone deacetylase inhibitors: synthesis, biological activity, and computational evaluation. J Med Chem. 2011 Apr 14;54(7):2165-82.
REF 27 Methyl effect in azumamides provides insight into histone deacetylase inhibition by macrocycles. J Med Chem. 2014 Nov 26;57(22):9644-57.
REF 28 An efficient anticancer histone deacetylase inhibitor and its analogues for human HDAC8. Med Chem Res. 2011 Jan 28;21:568-77.
REF 29 Discovery of N-(2-aminophenyl)-4-[(4-pyridin-3-ylpyrimidin-2-ylamino)methyl]benzamide (MGCD0103), an orally active histone deacetylase inhibitor. J Med Chem. 2008 Jul 24;51(14):4072-5.
REF 30 Stabilizing HDAC11 with SAHA to assay slow-binding benzamide inhibitors. Bioorg Med Chem Lett. 2017 Jul 1;27(13):2943-5.
REF 31 Class I/IIb-Selective HDAC Inhibitor Exhibits Oral Bioavailability and Therapeutic Efficacy in Acute Myeloid Leukemia. ACS Med Chem Lett. 2019 Dec 13;11(1):56-64.
REF 32 Design of Hydrazide-Bearing HDACIs Based on Panobinostat and Their p53 and FLT3-ITD Dependency in Antileukemia Activity. J Med Chem. 2020 May 28;63(10):5501-5525.
REF 33 Discovery of HDAC Inhibitors That Lack an Active Site Zn(2+)-Binding Functional Group. ACS Med Chem Lett. 2012 Apr 26;3(6):505-8.
REF 34 Synthesis of Peptoid-Based Class I-Selective Histone Deacetylase Inhibitors with Chemosensitizing Properties. J Med Chem. 2019 Dec 26;62(24):11260-11279.
REF 35 Dual NAMPT/HDAC Inhibitors as a New Strategy for Multitargeting Antitumor Drug Discovery. ACS Med Chem Lett. 2017 Dec 14;9(1):34-38.
REF 36 Potent and Selective Inhibitors of Histone Deacetylase-3 Containing Chiral Oxazoline Capping Groups and a N-(2-Aminophenyl)-benzamide Binding Unit. J Med Chem. 2015 Sep 10;58(17):6803-18.

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