Page last updated: 2024-12-05

entinostat

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Entinostat, also known as SNDX-5613, is a potent and selective inhibitor of histone deacetylase (HDAC) enzymes. It is currently being investigated in clinical trials for the treatment of various cancers, including hematologic malignancies, solid tumors, and myelodysplastic syndromes. Entinostat has demonstrated promising preclinical activity, inhibiting the growth and proliferation of cancer cells by inducing cell cycle arrest and apoptosis. Its mechanism of action involves the inhibition of HDACs, which are enzymes that remove acetyl groups from histone proteins. This deacetylation process can silence genes involved in cell growth and differentiation. By inhibiting HDACs, entinostat increases histone acetylation, leading to the reactivation of these genes and promoting cancer cell death. Entinostat's importance lies in its potential to be a novel and effective treatment for cancers that are currently difficult to treat. The study of entinostat aims to determine its safety and efficacy in humans and to identify the optimal dosing and treatment strategies for different cancer types. '

Cross-References

ID SourceID
PubMed CID4261
CHEMBL ID27759
CHEBI ID132082
SCHEMBL ID148309
MeSH IDM0540391

Synonyms (111)

Synonym
HY-12163
bay86-5274
n-[[4-[(2-aminoanilino)-oxomethyl]phenyl]methyl]carbamic acid 3-pyridinylmethyl ester
pyridin-3-ylmethyl 4-(2-aminophenylcarbamoyl)benzylcarbamate
sndx 275
CHEBI:132082
entinostatum
bay 86-5274
nsc706995
n-(2-aminophenyl)-4-[n-(pyridin-3-yl-methoxycarbonyl)aminomethyl]benzamide
NCI60_038022
ms-27-275
NCGC00165833-02
NCGC00165833-01
entinostat ,
ms-275
sndx-275
nsc-706995
209783-80-2
carbamic acid, 3-pyridinylmethyl ester
ms 275
carbamic acid, ((4-(((2-aminophenyl)amino)carbonyl)phenyl)methyl)-, 3-pyridinylmethyl ester
ms 27-275
3-pyridinylmethyl ((4-(((2-aminophenyl)amino)carbonyl)phenyl)methyl)carbamate
n-(2-aminophenyl)-4-(n-(pyridin-3-ylmethoxycarbonyl)aminomethyl)benzamide
ms275
pyridin-3-ylmethyl {4-[(2-aminophenyl)carbamoyl]benzyl}carbamate
carbamic acid, n-((4-(((2-aminophenyl)amino)carbonyl)phenyl)methyl)-, 3- pyridinylmethyl ester
pyridin-3-ylmethyl n-({4-[(2-aminophenyl)carbamoyl]phenyl}methyl)carbamate
benzamide-type inhibitor, 3
chembl27759 ,
bdbm19410
3-pyridylmethyl n-[[4-[(2-aminophenyl)carbamoyl]phenyl]methyl]carbamate
carbamic acid, [[4-[[(2-aminophenyl)carbaonyl]phenyl]methyl]-, 3-pyridinylmethyl ester
ms-275-27
BRD-K77908580-001-02-1
EC-000.2117
entinostat (jan/usan/inn)
D09338
442532-99-2
FT-0667871
pyridin-3-ylmethyl n-[[4-[(2-aminophenyl)carbamoyl]phenyl]methyl]carbamate
NCGC00165833-03
1zny4fkk9h ,
unii-1zny4fkk9h
entinostat [usan:inn]
nsc 706995
MS-275 - ENTINOSTAT
sndx 275;3-pyridylmethyl n-[[4-[(2-aminophenyl)carbamoyl]phenyl]methyl]carbamate
A815057
entinostat (ms-275,sndx-275)
BCP9000967
BCPP000155
ms-275,entinostat, sndx-275, ms-27-275
NCGC00165833-04
CS-0511
S1053
entinostat [jan]
entinostat [inn]
entinostat [who-dd]
entinostat [usan]
pyridin-3-ylmethyl ({4-[(2-aminophenyl)carbamoyl]phenyl}methyl)carbamate
gtpl7007
zk 244894
CCG-208680
MLS006010183
smr004458705
SCHEMBL148309
n-(2-aminophenyl)-4-[n-(pyridin-3-ylmethoxycarbonyl)aminomethyl]benzamide
AKOS024262667
pyridin-3-ylmethyl 4-((2-aminophenyl)carbamoyl)benzylcarbamate
W-201831
n-[[4-[[(2-aminophenyl)amino]carbonyl]phenyl]methyl]-3-pyridinylmethyl ester, carbamic acid
HB3983
HMS3648K12
DTXSID0041068
EX-A038
AC-8968
ms-275, a hdac1 and hdac3 inhibitor
HMS3654O11
mfcd08272435
(pyridin-3-yl)methyl 4-(2-aminophenylcarbamoyl)benzylcarbamate
(pyridin-3-yl)methyl n-({4-[(2-aminophenyl)carbamoyl]phenyl}methyl)carbamate
EN300-6488260
NCGC00165833-13
entinostat (ms-275)
SW219667-1
DB11841
E1454
pyridin-3-ylmethyl 4-((2-aminophenyl)carbamoyl)benzylcarbamate.
n-[[4-[[(2-aminophenyl)amino]carbonyl]phenyl]methyl]carbamic acid 3-pyridinylmethyl ester
Z2037280922
entinostat (ms-275, sndx-275) ,
AS-17906
SR-01000946382-1
sr-01000946382
BCP01824
Q1281020
BRD-K77908580-001-04-7
entinostat (ms-275;sndx-275)
SB16665
HMS3426G07
AMY31163
HMS3744O17
carbamic acid, n-[[4-[[(2-aminophenyl)amino]carbonyl]phenyl]methyl]-, 3-pyridinylmethyl ester
NCGC00165833-11
BP-25653
nsc-756642
nsc756642
entinostat, free base
pyridin-3-ylmethyl4-((2-aminophenyl)carbamoyl)benzylcarbamate

Research Excerpts

Overview

Entinostat is an oral inhibitor of class I histone deacetylases intended for endocrine therapy-resistant patients with hormone receptor-positive (HR+) advanced or metastatic breast cancer (BC) It has shown anti-neoplastic activity and tolerability in hematologic and solid tumors.

ExcerptReferenceRelevance
"Entinostat is an oral inhibitor of class I histone deacetylases intended for endocrine therapy-resistant patients with hormone receptor-positive (HR+) advanced or metastatic breast cancer (BC). "( Phase 1 trial of entinostat as monotherapy and combined with exemestane in Japanese patients with hormone receptor-positive advanced breast cancer.
Iwata, H; Kimura, R; Lee, MJ; Masuda, N; Nishimura, Y; Saji, S; Sawaki, M; Shimomura, A; Tamura, K; Trepel, J; Yasojima, H; Yuno, A, 2021
)
2.4
"Entinostat is a synthetic benzamide derivative histone deacetylase (HDAC) inhibitor, which potently and selectively inhibits class I and IV HDAC enzymes. "( Entinostat: a promising treatment option for patients with advanced breast cancer.
Connolly, RM; Piekarz, R; Rudek, MA, 2017
)
3.34
"Entinostat is an oral isoform selective histone deacetylase inhibitor that targets resistance to hormonal therapies in estrogen receptor-positive (ER+) breast cancer. "( Randomized phase II, double-blind, placebo-controlled study of exemestane with or without entinostat in postmenopausal women with locally recurrent or metastatic estrogen receptor-positive breast cancer progressing on treatment with a nonsteroidal aromata
Cruickshank, S; Ismail-Khan, RR; Klein, PM; Lee, MJ; Lichinitser, M; Melichar, B; Miller, KD; Munster, PN; Trepel, JB; Yardley, DA, 2013
)
2.05
"Entinostat is a histone deacetylase inhibitor that has been combined with AZA with significant clinical activity in a previous phase I dose finding study."( Prolonged administration of azacitidine with or without entinostat for myelodysplastic syndrome and acute myeloid leukemia with myelodysplasia-related changes: results of the US Leukemia Intergroup trial E1905.
Czader, M; Erba, HP; Figueroa, ME; Gabrilove, J; Gore, SD; Greenberg, PL; Herman, J; Juckett, M; Ketterling, R; Litzow, M; Malick, L; Melnick, A; Paietta, E; Prebet, T; Smith, MR; Sun, Z; Tallman, MS, 2014
)
1.37
"Entinostat is an orally bioavailable class I HDAC inhibitor with a long half-life, which is under evaluation in haematological and solid tumour malignancies."( Entinostat, a novel histone deacetylase inhibitor is active in B-cell lymphoma and enhances the anti-tumour activity of rituximab and chemotherapy agents.
Barth, MJ; Czuczman, MS; Frys, S; Gu, JJ; Hernandez-Ilizaliturri, FJ; Hu, Q; Mavis, C; Simons, Z; Skitzki, J; Song, L, 2015
)
2.58
"Entinostat is a selective HDAC inhibitor that has shown anti-neoplastic activity and tolerability in hematologic and solid tumors, including lung cancer."( Entinostat (SNDX-275) for the treatment of non-small cell lung cancer.
Raez, LE; Rolfo, C; Ruiz, R, 2015
)
2.58
"Entinostat is an emerging HDACi that has shown promise in multiple preclinical studies."( Entinostat for treatment of solid tumors and hematologic malignancies.
Gore, L; Knipstein, J, 2011
)
2.53
"Entinostat is a well-tolerated HDACi that demonstrates promising therapeutic potential in both solid and hematologic malignancies. "( Entinostat for treatment of solid tumors and hematologic malignancies.
Gore, L; Knipstein, J, 2011
)
3.25

Treatment

Entinostat treatment significantly reduced the number of degenerating neurons and TUNEL-positive cells after ICH in comparison to vehicle-treated controls. Entinost at pretreatment of colon carcinoma and sarcoma cells, NK cells, or both led to enhanced overall cytotoxicity in vitro.

ExcerptReferenceRelevance
"Entinostat treatment changed the expression of genes involved in 22 pathways, including downregulation of DNA damage response. "( Class I HDAC inhibition reduces DNA damage repair capacity of MYC-amplified medulloblastoma cells.
Ecker, J; Hielscher, T; Jamaladdin, N; Milde, T; Oehme, I; Peterziel, H; Ridinger, J; Valinciute, G; van Tilburg, CM; Vollmer, J; Witt, O, 2023
)
2.35
"Entinostat treatment significantly reduced the number of degenerating neurons and TUNEL-positive cells after ICH in comparison to vehicle-treated controls."( Entinostat improves acute neurological outcomes and attenuates hematoma volume after Intracerebral Hemorrhage.
Bonsack, F; Sukumari-Ramesh, S, 2021
)
2.79
"Entinostat treatment decreased the growth of both subcutaneously and omental ID8 tumors and prolonged survival in immunocompetent C57BL/6 mice. "( The antitumor effects of entinostat in ovarian cancer require adaptive immunity.
Arend, RC; Buchsbaum, DJ; Forero, A; Katre, AA; Londono, AI; McCaw, TR; Meza-Perez, S; Norian, LA; Randall, TD; Smith, HJ; Straughn, JM; Yang, ES, 2018
)
2.23
"Entinostat treatment partially restored KCNH2 and Cav1.3 gene expressions in failing hearts, and inhibited the development of cardiac fibrosis in vivo."( Histone deacetylase inhibition by Entinostat for the prevention of electrical and structural remodeling in heart failure.
Eckardt, L; Freundt, JK; Frommeyer, G; Grotthoff, JS; Hempel, G; Jacobs, AH; Lange, PS; Schäfers, M; Spieker, T; Stypmann, J; Wötzel, F, 2019
)
1.51
"Entinostat treatment reduced the association of the Her-2 protein with HSP-90, possibly by reducing the stability of Her-2 protein."( HDAC inhibitor entinostat restores responsiveness of letrozole-resistant MCF-7Ca xenografts to aromatase inhibitors through modulation of Her-2.
Brodie, AH; Goloubeva, OG; Kazi, AA; Sabnis, GJ; Shah, P, 2013
)
1.46
"Entinostat pretreatment of colon carcinoma and sarcoma cells, NK cells, or both led to enhanced overall cytotoxicity in vitro, which was reversed by NKG2D blockade, and inhibited growth of tumor xenografts."( The narrow-spectrum HDAC inhibitor entinostat enhances NKG2D expression without NK cell toxicity, leading to enhanced recognition of cancer cells.
Cobanoglu, ZS; Denman, CJ; Gottschalk, SM; Hughes, DP; Kiany, S; Kleinerman, ES; Lau, CC; Lee, DA; Zhu, S, 2015
)
1.42
"Entinostat treatment was able to reduce the CD44(high)/CD24(low) cell population, ALDH-1 activity, as well as protein and mRNA expression of known TIC markers such as Bmi-1, Nanog, and Oct-4."( Histone Deacetylase Inhibitor Entinostat Inhibits Tumor-Initiating Cells in Triple-Negative Breast Cancer Cells.
Kazi, A; Sabnis, G; Schech, A; Shah, P; Yu, S, 2015
)
1.43
"Entinostat treatment altered cell cycle progression, resulting in a significant increase in the fraction of cells present in the G0/G1 phase at low micromolar concentrations."( The histone deacetylase inhibitor Entinostat enhances polymer-mediated transgene expression in cancer cell lines.
Barua, S; Christensen, MD; Elmer, JJ; Haynes, KA; Lehrman, J; Rege, K, 2016
)
1.43
"Entinostat treatment leads to upregulation of Cathepsin L1, and the HLA-DR peptidome of the Entinostat treated cells is consistent with increased Cathepsin L1 mediated proteolysis."( Regulation of HLA-DR peptide occupancy by histone deacetylase inhibitors.
Blanck, G; Cronin, K; Delgado, JC; Escobar, H; Lloyd, MC; Reyes-Vargas, E; Rockwood, AL; Szekeres, K, 2013
)
1.11
"Treatment with entinostat and azacytidine of ID8 cells in vitro increased mRNA levels of Cd74, Ciita, and H2-Aa, H2-Eb1."( Epigenetic modifiers upregulate MHC II and impede ovarian cancer tumor growth.
Arend, RC; Buchsbaum, DJ; Forero, A; Katre, A; Londoño, A; Meza-Perez, S; Norian, LA; Peabody, JE; Randall, TD; Smith, HJ; Straughn, JM; Turner, TB, 2017
)
0.79
"Treatment with entinostat had no effect on erbB2/erbB3 mRNA, suggesting a transcription-independent mechanism."( Functional cooperation of miR-125a, miR-125b, and miR-205 in entinostat-induced downregulation of erbB2/erbB3 and apoptosis in breast cancer cells.
Huang, J; Lee, CK; Liu, B; Lyu, H; Tan, J; Wang, J; Wang, S, 2013
)
0.97
"Treatment with entinostat significantly reduced tumor formation at the primary site as well as lung metastasis."( Histone Deacetylase Inhibitor Entinostat Inhibits Tumor-Initiating Cells in Triple-Negative Breast Cancer Cells.
Kazi, A; Sabnis, G; Schech, A; Shah, P; Yu, S, 2015
)
1.05

Toxicity

ExcerptReferenceRelevance
" Histone deacetylase inhibitors (HDACi) at high concentrations inhibit tumor growth and can increase NKG2D ligand expression on tumor targets, but are widely regarded as toxic to NK cells."( The narrow-spectrum HDAC inhibitor entinostat enhances NKG2D expression without NK cell toxicity, leading to enhanced recognition of cancer cells.
Cobanoglu, ZS; Denman, CJ; Gottschalk, SM; Hughes, DP; Kiany, S; Kleinerman, ES; Lau, CC; Lee, DA; Zhu, S, 2015
)
0.69
"These results suggest that epigenetic changes at the striatal Drd2 promoter drive age-related increases in antipsychotic side effect susceptibility, and HDAC inhibitors may be an effective adjunct treatment strategy to reduce side effects in aged populations."( Histone deacetylase inhibitors reverse age-related increases in side effects of haloperidol in mice.
Csernansky, JG; Dong, H; Fang, D; Fisher, DW; Montalvo-Ortiz, JL; Rodríguez, G, 2017
)
0.46

Pharmacokinetics

ExcerptReferenceRelevance
"The objective of this study was to define the maximum-tolerated dose (MTD), the recommended phase II dose, the dose-limiting toxicity, and determine the pharmacokinetic (PK) and pharmacodynamic profiles of MS-275."( Phase I and pharmacokinetic study of MS-275, a histone deacetylase inhibitor, in patients with advanced and refractory solid tumors or lymphoma.
Acharya, M; Chung, EJ; Elsayed, Y; Figg, WD; Headlee, D; Hwang, K; Kalnitskiy, M; Melillo, G; Monga, M; Murgo, A; Ryan, QC; Sausville, EA; Sparreboom, A; Trepel, JB; Ye, J; Zwiebel, J, 2005
)
0.33
" Preliminary PK analysis suggested the half-life of MS-275 in humans was 39 to 80 hours, substantially longer than predicted by preclinical studies."( Phase I and pharmacokinetic study of MS-275, a histone deacetylase inhibitor, in patients with advanced and refractory solid tumors or lymphoma.
Acharya, M; Chung, EJ; Elsayed, Y; Figg, WD; Headlee, D; Hwang, K; Kalnitskiy, M; Melillo, G; Monga, M; Murgo, A; Ryan, QC; Sausville, EA; Sparreboom, A; Trepel, JB; Ye, J; Zwiebel, J, 2005
)
0.33
" The aim of this study was to develop a versatile and sensitive technique for the pharmacodynamic (PD) assessment of HDAC inhibitor activity as monotherapy and in combination therapy."( Histone deacetylase inhibitor pharmacodynamic analysis by multiparameter flow cytometry.
Chung, EJ; Gojo, I; Karp, JE; Kong, HS; Lee, MJ; Lee, S; Ryan, Q; Sausville, EA; Telford, WG; Trepel, JB, 2005
)
0.33
" In vivo pharmacokinetic data were obtained from 64 adult patients (36 male/28 female; median age, 57 years) receiving MS-275 orally (dose range, 2 to 12 mg/m2)."( Factors affecting the pharmacokinetic profile of MS-275, a novel histone deacetylase inhibitor, in patients with cancer.
Acharya, MR; Figg, WD; Gojo, I; Hwang, K; Karp, JE; Ryan, Q; Sausville, EA; Sparreboom, A; Venitz, J, 2006
)
0.33
" Pharmacokinetic variables revealed dose-dependent and dose-proportional increases."( A phase I and pharmacokinetic study of the oral histone deacetylase inhibitor, MS-275, in patients with refractory solid tumors and lymphomas.
Coffin, D; Eckhardt, SG; Gore, L; McCoy, C; O'Bryant, CL; Rothenberg, ML; Sandler, AB; Scholz, C; Schott, A; Schultz, MK, 2008
)
0.35
" It possesses optimized pharmacokinetic properties in preclinical species, has a clean off-target profile, and is negative in a microbial mutagenicity (Ames) test."( Discovery of a potent class I selective ketone histone deacetylase inhibitor with antitumor activity in vivo and optimized pharmacokinetic properties.
Fiore, F; Fonsi, M; Gonzalez Paz, O; Jones, P; Kinzel, O; Llauger-Bufi, L; Monteagudo, E; Pescatore, G; Rowley, M; Schultz-Fademrecht, C; Steinkühler, C, 2009
)
0.35
"Herein, we describe the pharmacokinetic optimization of a series of class-selective histone deacetylase (HDAC) inhibitors and the subsequent identification of candidate predictive biomarkers of hepatocellular carcinoma (HCC) tumor response for our clinical lead using patient-derived HCC tumor xenograft models."( Pharmacokinetic optimization of class-selective histone deacetylase inhibitors and identification of associated candidate predictive biomarkers of hepatocellular carcinoma tumor response.
Cai, J; Chen, D; Chen, J; Chen, L; Chen, T; Feng, L; Guo, L; He, Y; Ji, Y; Jin, TG; Li, S; Liang, C; Lin, X; Liu, Y; Lu, X; Mei, J; Ning, Z; Pan, D; Pan, S; Peng, Z; Ren, S; Ren, Y; Rong, Y; Shan, S; She, J; Tang, G; Wang, Z; Wong, JC; Wu, X; Xu, C; Zhang, C; Zhang, M; Zhang, N; Zhang, W; Zhang, X; Zhang, Z; Zhao, R; Zhao, W; Zhou, M, 2012
)
0.38
" This study examined whether oral administration of MS-275 to the rats with lapatinib led to any pharmacokinetic interactions."( Pharmacokinetic interaction of entinostat and lapatinib following single and co-oral administration in rats.
Chen, M; Hu, L; Yang, X; Zhang, Q, 2014
)
0.69

Compound-Compound Interactions

Entinostat (HDAC1 inhibitor) combination with Fludarabine significantly induced apoptosis in TP53 mutations CLL cells.

ExcerptReferenceRelevance
"To investigate the antiproliferative effect of the histone deacetylase (HDAC) inhibitor MS-275 on cholangiocarcinoma cells alone and in combination with conventional cytostatic drugs (gemcitabine or doxorubicin) or the novel anticancer agents sorafenib or bortezomib."( Histone deacetylase inhibitor MS-275 alone or combined with bortezomib or sorafenib exhibits strong antiproliferative action in human cholangiocarcinoma cells.
Baradari, V; Höpfner, M; Huether, A; Scherübl, H; Schuppan, D, 2007
)
0.34
" Furthermore, additive anti-neoplastic effects were observed when MS-275 treatment was combined with gemcitabine or doxorubicin, while combination with the multi-kinase inhibitor sorafenib or the proteasome inhibitor bortezomib resulted in overadditive anti-neoplastic effects."( Histone deacetylase inhibitor MS-275 alone or combined with bortezomib or sorafenib exhibits strong antiproliferative action in human cholangiocarcinoma cells.
Baradari, V; Höpfner, M; Huether, A; Scherübl, H; Schuppan, D, 2007
)
0.34
"The growth of human cholangiocarcinoma cells can be potently inhibited by MS-275 alone or in combination with conventional cytostatic drugs or new, targeted anticancer agents."( Histone deacetylase inhibitor MS-275 alone or combined with bortezomib or sorafenib exhibits strong antiproliferative action in human cholangiocarcinoma cells.
Baradari, V; Höpfner, M; Huether, A; Scherübl, H; Schuppan, D, 2007
)
0.34
" These results demonstrate that compound 2 and its combination with SAHA are potentially useful agents that warrant further preclinical development for treatment of prostate cancer."( Improved synthesis of histone deacetylase inhibitors (HDIs) (MS-275 and CI-994) and inhibitory effects of HDIs alone or in combination with RAMBAs or retinoids on growth of human LNCaP prostate cancer cells and tumor xenografts.
Belosay, A; Gediya, LK; Khandelwal, A; Njar, VC; Purushottamachar, P, 2008
)
0.35
" The objective of this study was to determine the safety, tolerability, and the pharmacokinetic (PK)/pharmacodynamic (PD) profiles of the HDAC inhibitor entinostat in combination with 13-cis retinoic acid (CRA) in patients with solid tumours."( Phase I study of the histone deacetylase inhibitor entinostat in combination with 13-cis retinoic acid in patients with solid tumours.
Altiok, S; Carducci, MA; Pili, R; Qian, D; Rudek, MA; Salumbides, B; Zhao, M; Zwiebel, J, 2012
)
0.83
" Entinostat 10 mg orally once every 2 weeks in combination with sorafenib 400 mg orally twice daily, representing full single agent doses of each drug was identified as the recommended phase 2 dose (RP2D)."( A phase I study of the histone deacetylase (HDAC) inhibitor entinostat, in combination with sorafenib in patients with advanced solid tumors.
Adjei, AA; Brady, W; DePaolo, D; Ding, Y; Dy, GK; Fetterly, G; Ma, WW; Ngamphaiboon, N; Reungwetwattana, T; Zhao, Y, 2015
)
1.57
" Subsequently, we demonstrated Entinostat (HDAC1 inhibitor) combination with Fludarabine significantly induced apoptosis in TP53 mutations CLL cells."( Entinostat combined with Fludarabine synergistically enhances the induction of apoptosis in TP53 mutated CLL cells via the HDAC1/HO-1 pathway.
Chen, B; Fang, Q; He, Z; Li, P; Ma, D; Ren, M; Wang, J; Zhe, N; Zhong, Q; Zhou, Z, 2019
)
2.24
" This study aimed to evaluate the anticancer effects of MS-275 combined with DDP on ESCC cell line EC9706 both in vitro and in vivo, and to investigate the possible mechanisms that mediate these effects."( MS-275 combined with cisplatin exerts synergistic antitumor effects in human esophageal squamous cell carcinoma cells.
Cui, Y; Guan, F; Li, Y; Li, Z; Liu, H; Liu, T; Ma, S; Wang, Y; Zhang, Y; Zhang, Z, 2020
)
0.56
"Entinostat at the selected dose levels in combination with a standard dose of enzalutamide showed a promising safety profile in this small phase I study BACKGROUND: Entinostat inhibits prostate cancer (PCa) growth and suppresses Treg cell function in vitro and in vivo."( Phase I Study of Entinostat in Combination with Enzalutamide for Treatment of Patients with Metastatic Castration-Resistant Prostate Cancer.
Burgess, B; Elkon, J; Lin, J; Ma, Y; Noonepalle, S; Palmer, E; Ricart, B; Siegel, R; Villagra, A; Zevallos-Delgado, C, 2021
)
2.4
"This was a phase I study to explore the safety and preliminary efficacy of entinostat (3 and 5 mg orally per week) in combination with enzalutamide in castration resistant PCa (CRPC)."( Phase I Study of Entinostat in Combination with Enzalutamide for Treatment of Patients with Metastatic Castration-Resistant Prostate Cancer.
Burgess, B; Elkon, J; Lin, J; Ma, Y; Noonepalle, S; Palmer, E; Ricart, B; Siegel, R; Villagra, A; Zevallos-Delgado, C, 2021
)
1.19
"Entinostat 5 mg weekly in combination with enzalutamide showed an acceptable safety profile in this small phase I study."( Phase I Study of Entinostat in Combination with Enzalutamide for Treatment of Patients with Metastatic Castration-Resistant Prostate Cancer.
Burgess, B; Elkon, J; Lin, J; Ma, Y; Noonepalle, S; Palmer, E; Ricart, B; Siegel, R; Villagra, A; Zevallos-Delgado, C, 2021
)
2.4

Bioavailability

ExcerptReferenceRelevance
"New orally bioavailable 5-(thiophen-2-yl)-substituted 2-aminobenzamide-series histone deacetylase inhibitors were synthesized."( Anti-tumor activity of new orally bioavailable 2-amino-5-(thiophen-2-yl)benzamide-series histone deacetylase inhibitors, possessing an aqueous soluble functional group as a surface recognition domain.
Baba, K; Hirata, M; Hirata, Y; Kawaratani, Y; Nagaoka, Y; Ohmomo, Y; Shibano, M; Taniguchi, M; Uesato, S; Yasuda, M, 2012
)
0.38
" Through a combination of conformational constraint and scaffold hopping, we lowered the in vivo clearance (CL) and significantly improved the bioavailability (F) and exposure (AUC) of our HDAC inhibitors while maintaining selectivity toward the class I HDAC family with particular potency against HDAC1, resulting in clinical lead 5 (HDAC1 IC₅₀ = 60 nM, mouse CL = 39 mL/min/kg, mouse F = 100%, mouse AUC after single oral dose at 10 mg/kg = 6316 h·ng/mL)."( Pharmacokinetic optimization of class-selective histone deacetylase inhibitors and identification of associated candidate predictive biomarkers of hepatocellular carcinoma tumor response.
Cai, J; Chen, D; Chen, J; Chen, L; Chen, T; Feng, L; Guo, L; He, Y; Ji, Y; Jin, TG; Li, S; Liang, C; Lin, X; Liu, Y; Lu, X; Mei, J; Ning, Z; Pan, D; Pan, S; Peng, Z; Ren, S; Ren, Y; Rong, Y; Shan, S; She, J; Tang, G; Wang, Z; Wong, JC; Wu, X; Xu, C; Zhang, C; Zhang, M; Zhang, N; Zhang, W; Zhang, X; Zhang, Z; Zhao, R; Zhao, W; Zhou, M, 2012
)
0.38
" The subcutaneous dosing route for consecutive days and reduced bioavailability of 5-azacytidine because of inactivation by cytidine deaminase may limit the expansion of epigenetic therapy into Phase III trials."( Aerosolised 5-azacytidine suppresses tumour growth and reprogrammes the epigenome in an orthotopic lung cancer model.
Belinsky, SA; Cheng, YS; Grimes, MJ; Kuehl, PJ; March, TH; Picchi, MA; Reed, MD; Tellez, CS; Tessema, M, 2013
)
0.39
" Entinostat is an orally bioavailable class I HDAC inhibitor with a long half-life, which is under evaluation in haematological and solid tumour malignancies."( Entinostat, a novel histone deacetylase inhibitor is active in B-cell lymphoma and enhances the anti-tumour activity of rituximab and chemotherapy agents.
Barth, MJ; Czuczman, MS; Frys, S; Gu, JJ; Hernandez-Ilizaliturri, FJ; Hu, Q; Mavis, C; Simons, Z; Skitzki, J; Song, L, 2015
)
2.77
" What's more, 6d possessed desirable pharmacokinetic profiles with the oral bioavailability of 72% in SD rats and considerable in vivo antitumor efficacy in a human colorectal adenocarcinoma (HT-29) xenograft model."( Discovery of Novel Pazopanib-Based HDAC and VEGFR Dual Inhibitors Targeting Cancer Epigenetics and Angiogenesis Simultaneously.
Chou, CJ; Huang, Y; Jia, Y; Li, X; Liang, X; Xu, W; Zang, J; Zhang, Y, 2018
)
0.48
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51
" Importantly, in vivo preclinical studies showed that 009P1 and 009P2 dramatically suppressed KSHV+ lymphoma progression with oral bioavailability and minimal visible toxicity."( Oncolytic strategy using new bifunctional HDACs/BRD4 inhibitors against virus-associated lymphomas.
Chen, J; Chen, Z; Dai, L; Kendrick, S; Li, HY; Lin, Z; Phuc, T; Qin, Z; Wang, Z; Xu, Z; Yang, D, 2023
)
0.91

Dosage Studied

ExcerptRelevanceReference
" Based on PK data from the q14-day schedule, a more frequent dosing schedule, weekly x 4, repeated every 6 weeks is presently being evaluated."( Phase I and pharmacokinetic study of MS-275, a histone deacetylase inhibitor, in patients with advanced and refractory solid tumors or lymphoma.
Acharya, M; Chung, EJ; Elsayed, Y; Figg, WD; Headlee, D; Hwang, K; Kalnitskiy, M; Melillo, G; Monga, M; Murgo, A; Ryan, QC; Sausville, EA; Sparreboom, A; Trepel, JB; Ye, J; Zwiebel, J, 2005
)
0.33
" Furthermore, MS-275 can be added to the list of cancer drugs where BSA-based dosing is not more accurate than fixed dosing."( Factors affecting the pharmacokinetic profile of MS-275, a novel histone deacetylase inhibitor, in patients with cancer.
Acharya, MR; Figg, WD; Gojo, I; Hwang, K; Karp, JE; Ryan, Q; Sausville, EA; Sparreboom, A; Venitz, J, 2006
)
0.33
" A dose-response relationship was observed between the parameter k2 in this formula and the concentration of the cytotoxic agent etoposide, in high-grade glioma cells was independent of incubation time."( Measuring cytotoxicity: a new perspective on LC50.
Aguilera, D; Das, C; Gopalakrishnan, V; Vasquez, H; Wolff, J; Zage, P; Zhang, M,
)
0.13
"To evaluate the toxicity profile, pharmacologic, and biological properties of 3-pyridylmethyl N-{4-[(2-aminophenyl)carbamoyl]benzyl}carbamate (MS-275), a histone deacetylase inhibitor, when administered orally on three different dosing schedules."( A phase I and pharmacokinetic study of the oral histone deacetylase inhibitor, MS-275, in patients with refractory solid tumors and lymphomas.
Coffin, D; Eckhardt, SG; Gore, L; McCoy, C; O'Bryant, CL; Rothenberg, ML; Sandler, AB; Scholz, C; Schott, A; Schultz, MK, 2008
)
0.35
" Hypophosphatemia and asthenia were dose limiting on the weekly and twice-weekly dosing schedules; there was no dose-limiting toxicity on the every other week schedule."( A phase I and pharmacokinetic study of the oral histone deacetylase inhibitor, MS-275, in patients with refractory solid tumors and lymphomas.
Coffin, D; Eckhardt, SG; Gore, L; McCoy, C; O'Bryant, CL; Rothenberg, ML; Sandler, AB; Scholz, C; Schott, A; Schultz, MK, 2008
)
0.35
" Twice-weekly dosing was not tolerable due to asthenia, and further evaluation of this schedule was halted."( A phase I and pharmacokinetic study of the oral histone deacetylase inhibitor, MS-275, in patients with refractory solid tumors and lymphomas.
Coffin, D; Eckhardt, SG; Gore, L; McCoy, C; O'Bryant, CL; Rothenberg, ML; Sandler, AB; Scholz, C; Schott, A; Schultz, MK, 2008
)
0.35
" The subcutaneous dosing route for consecutive days and reduced bioavailability of 5-azacytidine because of inactivation by cytidine deaminase may limit the expansion of epigenetic therapy into Phase III trials."( Aerosolised 5-azacytidine suppresses tumour growth and reprogrammes the epigenome in an orthotopic lung cancer model.
Belinsky, SA; Cheng, YS; Grimes, MJ; Kuehl, PJ; March, TH; Picchi, MA; Reed, MD; Tellez, CS; Tessema, M, 2013
)
0.39
" Delayed dosing did not reduce adhesions."( Histone deacetylase inhibitors decrease intra-abdominal adhesions with one intraoperative dose by reducing peritoneal fibrin deposition pathways.
Cassidy, MR; Gainsbury, ML; Heydrick, S; Sheldon, HK; Sherburne, AC; Stucchi, AF, 2014
)
0.4
" A single, intraoperative intervention provides an ideal dosing strategy and indicates an exciting new role for HDACIs in adhesion prevention."( Histone deacetylase inhibitors decrease intra-abdominal adhesions with one intraoperative dose by reducing peritoneal fibrin deposition pathways.
Cassidy, MR; Gainsbury, ML; Heydrick, S; Sheldon, HK; Sherburne, AC; Stucchi, AF, 2014
)
0.4
" However, the prolonged administration of AZA by itself seems to increase HN rate compared with standard dosing and warrants additional investigation."( Prolonged administration of azacitidine with or without entinostat for myelodysplastic syndrome and acute myeloid leukemia with myelodysplasia-related changes: results of the US Leukemia Intergroup trial E1905.
Czader, M; Erba, HP; Figueroa, ME; Gabrilove, J; Gore, SD; Greenberg, PL; Herman, J; Juckett, M; Ketterling, R; Litzow, M; Malick, L; Melnick, A; Paietta, E; Prebet, T; Smith, MR; Sun, Z; Tallman, MS, 2014
)
0.65
" Additionally, the dose-response curve test indicated that MS-275 has a U-shape effect on ethanol self-administration with the dose of 500 µM as the most efficient dose."( The Class I-Specific HDAC Inhibitor MS-275 Decreases Motivation to Consume Alcohol and Relapse in Heavy Drinking Rats.
Alaux-Cantin, S; Jeanblanc, J; Jeanblanc, V; Lemoine, S; Naassila, M, 2015
)
0.42
" The N-hydroxyl group of this motif is highly subject to sulfation/glucoronidation-based inactivation in humans; compounds containing this motif require much higher dosing in clinic to achieve therapeutic concentrations."( Development of Allosteric Hydrazide-Containing Class I Histone Deacetylase Inhibitors for Use in Acute Myeloid Leukemia.
Chou, CJ; Inks, ES; Li, J; McClure, JJ; Peterson, YK; Zhang, C, 2016
)
0.43
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (3)

RoleDescription
EC 3.5.1.98 (histone deacetylase) inhibitorAn EC 3.5.1.* (non-peptide linear amide C-N hydrolase) inhibitor that interferes with the function of histone deacetylase (EC 3.5.1.98).
antineoplastic agentA substance that inhibits or prevents the proliferation of neoplasms.
apoptosis inducerAny substance that induces the process of apoptosis (programmed cell death) in multi-celled organisms.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (5)

ClassDescription
benzamides
pyridinesAny organonitrogen heterocyclic compound based on a pyridine skeleton and its substituted derivatives.
carbamate esterAny ester of carbamic acid or its N-substituted derivatives.
substituted aniline
primary amino compoundA compound formally derived from ammonia by replacing one hydrogen atom by an organyl group.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (29)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
ATAD5 protein, partialHomo sapiens (human)Potency9.31690.004110.890331.5287AID624247; AID624252; AID686934; AID720565
PPM1D proteinHomo sapiens (human)Potency5.23000.00529.466132.9993AID1347411
EWS/FLI fusion proteinHomo sapiens (human)Potency3.92730.001310.157742.8575AID1259252; AID1259253; AID1259255; AID1259256
heat shock 70kDa protein 5 (glucose-regulated protein, 78kDa)Homo sapiens (human)Potency1.99530.016525.307841.3999AID602332
tyrosine-protein kinase YesHomo sapiens (human)Potency15.41030.00005.018279.2586AID686947
Interferon betaHomo sapiens (human)Potency5.23000.00339.158239.8107AID1347411
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Histone deacetylase 8Schistosoma mansoniIC50 (µMol)30.00000.30341.33503.6200AID1446915
Histone deacetylase 3Homo sapiens (human)IC50 (µMol)3.48380.00040.619610.0000AID1263144; AID1280295; AID1293874; AID1293875; AID1294943; AID1340801; AID1380938; AID1380954; AID1403456; AID1408543; AID1453365; AID1525779; AID1541444; AID1548728; AID1556401; AID1596080; AID1691039; AID1732165; AID1737648; AID1740014; AID1797850; AID1798524; AID1798526; AID1802398; AID1846973; AID1864216; AID1865258; AID1881855; AID1882461; AID1901146; AID1901148; AID1917928; AID292436; AID294382; AID313731; AID316888; AID316931; AID324949; AID328795; AID364648; AID374818; AID421212; AID488275; AID525002; AID551597; AID622254; AID664380; AID717827; AID748112; AID90208; AID90211; AID90529
Histone deacetylase 3Homo sapiens (human)Ki0.73000.00020.42378.1900AID1873437; AID1873440; AID1873449; AID1873480; AID496803
Bromodomain-containing protein 4Homo sapiens (human)IC50 (µMol)10.00000.00040.40329.0500AID1727731; AID1727732
Cytochrome P450 3A4Homo sapiens (human)IC50 (µMol)0.73000.00011.753610.0000AID609494
Leukotriene A-4 hydrolaseHomo sapiens (human)IC50 (µMol)10.00000.00051.28547.6500AID1441630; AID1441631
Androgen receptorHomo sapiens (human)IC50 (µMol)10.00000.00000.875310.0000AID1888465
Tissue factorHomo sapiens (human)IC50 (µMol)8.00000.00010.734410.0000AID360094; AID360095
Cytochrome P450 2C19Homo sapiens (human)IC50 (µMol)3.93000.00002.398310.0000AID1401904
Histone deacetylase 4Homo sapiens (human)IC50 (µMol)11.49800.00061.052610.0000AID1293874; AID1293875; AID1294943; AID1340801; AID1380938; AID1466062; AID1548733; AID1578487; AID1596080; AID1737649; AID1740016; AID1798524; AID1798526; AID1802398; AID1864216; AID1865258; AID1901148; AID1901156; AID292436; AID294382; AID313732; AID316888; AID328796; AID328797; AID329915; AID364648; AID385685; AID385686; AID421212; AID525000; AID622254; AID664382; AID717827; AID764213; AID90208; AID90211; AID90529
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)IC50 (µMol)30.00000.00091.901410.0000AID609493; AID613341
Histone deacetylase 1Homo sapiens (human)IC50 (µMol)2.50190.00010.55439.9000AID1203889; AID1231807; AID1235132; AID1280294; AID1293874; AID1293875; AID1294943; AID1308513; AID1340801; AID1380938; AID1380952; AID1401902; AID1403454; AID1453363; AID1466061; AID1474461; AID1486677; AID1525777; AID1541446; AID1548244; AID1548726; AID1556399; AID1578485; AID1586077; AID1596049; AID1596080; AID1691037; AID1727729; AID1732163; AID1737644; AID1740012; AID1797850; AID1798524; AID1798526; AID1802398; AID1846972; AID1864216; AID1865258; AID1879890; AID1881853; AID1882460; AID1888466; AID1901147; AID1901148; AID1915537; AID1915555; AID1917926; AID274110; AID292436; AID294382; AID303014; AID313729; AID316888; AID316892; AID316896; AID324948; AID328793; AID329914; AID364648; AID374811; AID420324; AID421212; AID488273; AID488358; AID525003; AID538408; AID551595; AID609489; AID622254; AID650229; AID664039; AID664379; AID670719; AID717827; AID748114; AID764214; AID90208; AID90211; AID90347; AID90348; AID90529; AID90666
Histone deacetylase 1Homo sapiens (human)Ki0.30600.00000.49888.1900AID1873442; AID496801
Histone deacetylase-like amidohydrolaseAlcaligenaceae bacterium FB188IC50 (µMol)118.00001.00001.10001.2000AID420319
Histone deacetylase-like amidohydrolaseAlcaligenaceae bacterium FB188Ki100.00000.70003.05009.2000AID420317
Histone deacetylase 7Homo sapiens (human)IC50 (µMol)9.54170.00071.02609.9000AID1293874; AID1293875; AID1294943; AID1340801; AID1380938; AID1548735; AID1578489; AID1596080; AID1737651; AID1740017; AID1798524; AID1802398; AID1846975; AID1864216; AID1865258; AID1901148; AID292436; AID294382; AID313735; AID316888; AID328800; AID364648; AID374821; AID421212; AID524997; AID622254; AID717827; AID90208; AID90211; AID90529
Histone deacetylase 2Homo sapiens (human)IC50 (µMol)3.37690.00010.72219.9700AID1203890; AID1231808; AID1293874; AID1293875; AID1294943; AID1340801; AID1380938; AID1380953; AID1401903; AID1403455; AID1453364; AID1466055; AID1486678; AID1541445; AID1548244; AID1548727; AID1556400; AID1578486; AID1586078; AID1596050; AID1596080; AID1691038; AID1732164; AID1737645; AID1740013; AID1797850; AID1798524; AID1802398; AID1864216; AID1865258; AID1881854; AID1901148; AID1917927; AID292436; AID294382; AID303015; AID313730; AID316888; AID328794; AID364648; AID374817; AID421212; AID488274; AID525001; AID551596; AID622254; AID650228; AID670720; AID717827; AID748113; AID90208; AID90211; AID90347; AID90529
Histone deacetylase 2Homo sapiens (human)Ki0.18350.00000.47098.1900AID1873438; AID1873441; AID1873450; AID496802
Polyamine deacetylase HDAC10Homo sapiens (human)IC50 (µMol)6.71890.00050.72459.9000AID1293874; AID1293875; AID1294943; AID1340801; AID1380938; AID1578491; AID1596080; AID1732167; AID1737653; AID1802398; AID1864216; AID1865258; AID1901148; AID292436; AID294382; AID316888; AID364648; AID421212; AID524995; AID622254; AID664384; AID717827; AID90208; AID90211; AID90529
Histone deacetylase 11 Homo sapiens (human)IC50 (µMol)4.18650.00030.92989.9000AID1293874; AID1293875; AID1294943; AID1340801; AID1380938; AID1467234; AID1467241; AID1596080; AID1864216; AID1865258; AID1901148; AID292436; AID294382; AID316888; AID364648; AID421212; AID622254; AID717827; AID90208; AID90211; AID90529
NAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)IC50 (µMol)100.00000.00601.62509.0000AID664385
Histone deacetylase 8Homo sapiens (human)IC50 (µMol)9.06400.00070.99479.9000AID1203891; AID1231809; AID1280297; AID1293874; AID1293875; AID1294943; AID1340801; AID1380938; AID1466064; AID1548732; AID1586083; AID1596080; AID1691040; AID1732166; AID1737647; AID1740015; AID1797850; AID1798524; AID1802398; AID1846976; AID1864216; AID1865258; AID1879896; AID1901148; AID1901154; AID292436; AID294382; AID313736; AID316888; AID316893; AID328801; AID364648; AID374822; AID421212; AID488277; AID524996; AID622254; AID664381; AID717827; AID90208; AID90211; AID90529
Histone deacetylase 6Homo sapiens (human)IC50 (µMol)16.43990.00000.53769.9000AID1280296; AID1293874; AID1293875; AID1294943; AID1340801; AID1380938; AID1401904; AID1466063; AID1541443; AID1586081; AID1596034; AID1596080; AID1727730; AID1737646; AID1740019; AID1798524; AID1798526; AID1802398; AID1846974; AID1864216; AID1865258; AID1879893; AID1882459; AID1901145; AID1901148; AID292436; AID294382; AID313734; AID316888; AID316899; AID328799; AID364648; AID374820; AID421212; AID488276; AID524999; AID538409; AID622254; AID664383; AID717827; AID764212; AID90208; AID90211; AID90529
Histone deacetylase 9Homo sapiens (human)IC50 (µMol)8.21890.00050.94139.9000AID1293874; AID1293875; AID1294943; AID1340801; AID1380938; AID1548736; AID1578490; AID1596080; AID1737652; AID1740018; AID1802398; AID1864216; AID1865258; AID1901148; AID292436; AID294382; AID316888; AID364648; AID421212; AID524994; AID622254; AID717827; AID90208; AID90211; AID90529
Histone deacetylase 5Homo sapiens (human)IC50 (µMol)6.95280.00070.961010.0000AID1293874; AID1293875; AID1294943; AID1340801; AID1380938; AID1548734; AID1578488; AID1596080; AID1737650; AID1798524; AID1802398; AID1864216; AID1865258; AID1901148; AID292436; AID294382; AID313733; AID316888; AID328798; AID364648; AID374819; AID421212; AID524998; AID622254; AID717827; AID90208; AID90211; AID90529
Histone deacetylase Plasmodium falciparum (malaria parasite P. falciparum)IC50 (µMol)0.94000.00060.16880.9400AID414980
Nuclear receptor corepressor 2Homo sapiens (human)IC50 (µMol)1.18500.00170.59528.0000AID1408543; AID1541444; AID1548728; AID1556401; AID1691039; AID1901146
Nuclear receptor corepressor 2Homo sapiens (human)Ki0.82250.00030.33253.2000AID1873437; AID1873440; AID1873449; AID1873480
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Histone deacetylase 3Homo sapiens (human)EC50 (µMol)1.00000.03001.85126.7000AID93030
Histone deacetylase 4Homo sapiens (human)EC50 (µMol)1.00000.03002.35236.7000AID93030
Histone deacetylase 1Homo sapiens (human)EC50 (µMol)1.00000.03001.98776.7000AID316943; AID93030
Histone deacetylase 1Homo sapiens (human)Kd0.21900.01210.10490.2820AID1802399
Histone deacetylase 7Homo sapiens (human)EC50 (µMol)1.00000.03002.32116.7000AID93030
Histone deacetylase 2Homo sapiens (human)EC50 (µMol)1.00000.03001.85756.7000AID93030
Histone deacetylase 2Homo sapiens (human)Kd0.21900.01210.11300.2820AID1802399
Polyamine deacetylase HDAC10Homo sapiens (human)EC50 (µMol)1.00000.03002.54656.7000AID93030
Histone deacetylase 11 Homo sapiens (human)EC50 (µMol)1.00000.03002.54656.7000AID93030
Histone deacetylase 8Homo sapiens (human)EC50 (µMol)1.00000.03002.27346.7000AID93030
Histone deacetylase 6Homo sapiens (human)EC50 (µMol)1.00000.00521.59986.7000AID93030
Histone deacetylase 9Homo sapiens (human)EC50 (µMol)1.00000.03002.32666.7000AID93030
Histone deacetylase 5Homo sapiens (human)EC50 (µMol)1.00000.03002.54656.7000AID93030
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (418)

Processvia Protein(s)Taxonomy
negative regulation of myotube differentiationHistone deacetylase 3Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIHistone deacetylase 3Homo sapiens (human)
establishment of mitotic spindle orientationHistone deacetylase 3Homo sapiens (human)
in utero embryonic developmentHistone deacetylase 3Homo sapiens (human)
positive regulation of protein phosphorylationHistone deacetylase 3Homo sapiens (human)
chromatin organizationHistone deacetylase 3Homo sapiens (human)
transcription by RNA polymerase IIHistone deacetylase 3Homo sapiens (human)
protein deacetylationHistone deacetylase 3Homo sapiens (human)
regulation of mitotic cell cycleHistone deacetylase 3Homo sapiens (human)
positive regulation of protein ubiquitinationHistone deacetylase 3Homo sapiens (human)
regulation of protein stabilityHistone deacetylase 3Homo sapiens (human)
positive regulation of TOR signalingHistone deacetylase 3Homo sapiens (human)
circadian regulation of gene expressionHistone deacetylase 3Homo sapiens (human)
regulation of multicellular organism growthHistone deacetylase 3Homo sapiens (human)
positive regulation of protein import into nucleusHistone deacetylase 3Homo sapiens (human)
regulation of circadian rhythmHistone deacetylase 3Homo sapiens (human)
negative regulation of apoptotic processHistone deacetylase 3Homo sapiens (human)
negative regulation of DNA-templated transcriptionHistone deacetylase 3Homo sapiens (human)
positive regulation of transcription by RNA polymerase IIHistone deacetylase 3Homo sapiens (human)
negative regulation of JNK cascadeHistone deacetylase 3Homo sapiens (human)
spindle assemblyHistone deacetylase 3Homo sapiens (human)
establishment of skin barrierHistone deacetylase 3Homo sapiens (human)
cellular response to fluid shear stressHistone deacetylase 3Homo sapiens (human)
positive regulation of cold-induced thermogenesisHistone deacetylase 3Homo sapiens (human)
DNA repair-dependent chromatin remodelingHistone deacetylase 3Homo sapiens (human)
cornified envelope assemblyHistone deacetylase 3Homo sapiens (human)
negative regulation of cardiac muscle cell differentiationHistone deacetylase 3Homo sapiens (human)
epigenetic regulation of gene expressionHistone deacetylase 3Homo sapiens (human)
regulation of transcription by RNA polymerase IIBromodomain-containing protein 4Homo sapiens (human)
positive regulation of G2/M transition of mitotic cell cycleBromodomain-containing protein 4Homo sapiens (human)
positive regulation of transcription elongation by RNA polymerase IIBromodomain-containing protein 4Homo sapiens (human)
chromatin organizationBromodomain-containing protein 4Homo sapiens (human)
DNA damage responseBromodomain-containing protein 4Homo sapiens (human)
positive regulation of transcription elongation by RNA polymerase IIBromodomain-containing protein 4Homo sapiens (human)
positive regulation of canonical NF-kappaB signal transductionBromodomain-containing protein 4Homo sapiens (human)
positive regulation of DNA-templated transcriptionBromodomain-containing protein 4Homo sapiens (human)
positive regulation of transcription by RNA polymerase IIBromodomain-containing protein 4Homo sapiens (human)
regulation of inflammatory responseBromodomain-containing protein 4Homo sapiens (human)
positive regulation of T-helper 17 cell lineage commitmentBromodomain-containing protein 4Homo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell activation involved in immune responseInterferon betaHomo sapiens (human)
cell surface receptor signaling pathwayInterferon betaHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to virusInterferon betaHomo sapiens (human)
positive regulation of autophagyInterferon betaHomo sapiens (human)
cytokine-mediated signaling pathwayInterferon betaHomo sapiens (human)
natural killer cell activationInterferon betaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinInterferon betaHomo sapiens (human)
cellular response to interferon-betaInterferon betaHomo sapiens (human)
B cell proliferationInterferon betaHomo sapiens (human)
negative regulation of viral genome replicationInterferon betaHomo sapiens (human)
innate immune responseInterferon betaHomo sapiens (human)
positive regulation of innate immune responseInterferon betaHomo sapiens (human)
regulation of MHC class I biosynthetic processInterferon betaHomo sapiens (human)
negative regulation of T cell differentiationInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon betaHomo sapiens (human)
defense response to virusInterferon betaHomo sapiens (human)
type I interferon-mediated signaling pathwayInterferon betaHomo sapiens (human)
neuron cellular homeostasisInterferon betaHomo sapiens (human)
cellular response to exogenous dsRNAInterferon betaHomo sapiens (human)
cellular response to virusInterferon betaHomo sapiens (human)
negative regulation of Lewy body formationInterferon betaHomo sapiens (human)
negative regulation of T-helper 2 cell cytokine productionInterferon betaHomo sapiens (human)
positive regulation of apoptotic signaling pathwayInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell differentiationInterferon betaHomo sapiens (human)
natural killer cell activation involved in immune responseInterferon betaHomo sapiens (human)
adaptive immune responseInterferon betaHomo sapiens (human)
T cell activation involved in immune responseInterferon betaHomo sapiens (human)
humoral immune responseInterferon betaHomo sapiens (human)
lipid hydroxylationCytochrome P450 3A4Homo sapiens (human)
lipid metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid catabolic processCytochrome P450 3A4Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid metabolic processCytochrome P450 3A4Homo sapiens (human)
cholesterol metabolic processCytochrome P450 3A4Homo sapiens (human)
androgen metabolic processCytochrome P450 3A4Homo sapiens (human)
estrogen metabolic processCytochrome P450 3A4Homo sapiens (human)
alkaloid catabolic processCytochrome P450 3A4Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 3A4Homo sapiens (human)
calcitriol biosynthetic process from calciolCytochrome P450 3A4Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D metabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D catabolic processCytochrome P450 3A4Homo sapiens (human)
retinol metabolic processCytochrome P450 3A4Homo sapiens (human)
retinoic acid metabolic processCytochrome P450 3A4Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 3A4Homo sapiens (human)
aflatoxin metabolic processCytochrome P450 3A4Homo sapiens (human)
oxidative demethylationCytochrome P450 3A4Homo sapiens (human)
proteolysisLeukotriene A-4 hydrolaseHomo sapiens (human)
lipid metabolic processLeukotriene A-4 hydrolaseHomo sapiens (human)
response to zinc ionLeukotriene A-4 hydrolaseHomo sapiens (human)
leukotriene biosynthetic processLeukotriene A-4 hydrolaseHomo sapiens (human)
protein metabolic processLeukotriene A-4 hydrolaseHomo sapiens (human)
peptide catabolic processLeukotriene A-4 hydrolaseHomo sapiens (human)
response to peptide hormoneLeukotriene A-4 hydrolaseHomo sapiens (human)
type I pneumocyte differentiationLeukotriene A-4 hydrolaseHomo sapiens (human)
negative regulation of transcription by RNA polymerase IIAndrogen receptorHomo sapiens (human)
MAPK cascadeAndrogen receptorHomo sapiens (human)
in utero embryonic developmentAndrogen receptorHomo sapiens (human)
regulation of systemic arterial blood pressureAndrogen receptorHomo sapiens (human)
epithelial cell morphogenesisAndrogen receptorHomo sapiens (human)
transcription by RNA polymerase IIAndrogen receptorHomo sapiens (human)
signal transductionAndrogen receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAndrogen receptorHomo sapiens (human)
cell-cell signalingAndrogen receptorHomo sapiens (human)
spermatogenesisAndrogen receptorHomo sapiens (human)
single fertilizationAndrogen receptorHomo sapiens (human)
positive regulation of cell population proliferationAndrogen receptorHomo sapiens (human)
negative regulation of cell population proliferationAndrogen receptorHomo sapiens (human)
positive regulation of gene expressionAndrogen receptorHomo sapiens (human)
male somatic sex determinationAndrogen receptorHomo sapiens (human)
intracellular estrogen receptor signaling pathwayAndrogen receptorHomo sapiens (human)
androgen receptor signaling pathwayAndrogen receptorHomo sapiens (human)
intracellular receptor signaling pathwayAndrogen receptorHomo sapiens (human)
positive regulation of intracellular estrogen receptor signaling pathwayAndrogen receptorHomo sapiens (human)
Leydig cell differentiationAndrogen receptorHomo sapiens (human)
multicellular organism growthAndrogen receptorHomo sapiens (human)
positive regulation of phosphorylationAndrogen receptorHomo sapiens (human)
positive regulation of MAPK cascadeAndrogen receptorHomo sapiens (human)
positive regulation of insulin-like growth factor receptor signaling pathwayAndrogen receptorHomo sapiens (human)
positive regulation of cell differentiationAndrogen receptorHomo sapiens (human)
negative regulation of integrin biosynthetic processAndrogen receptorHomo sapiens (human)
positive regulation of integrin biosynthetic processAndrogen receptorHomo sapiens (human)
positive regulation of DNA-templated transcriptionAndrogen receptorHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIAndrogen receptorHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIIAndrogen receptorHomo sapiens (human)
insulin-like growth factor receptor signaling pathwayAndrogen receptorHomo sapiens (human)
regulation of developmental growthAndrogen receptorHomo sapiens (human)
animal organ formationAndrogen receptorHomo sapiens (human)
male genitalia morphogenesisAndrogen receptorHomo sapiens (human)
epithelial cell proliferationAndrogen receptorHomo sapiens (human)
negative regulation of epithelial cell proliferationAndrogen receptorHomo sapiens (human)
positive regulation of NF-kappaB transcription factor activityAndrogen receptorHomo sapiens (human)
activation of prostate induction by androgen receptor signaling pathwayAndrogen receptorHomo sapiens (human)
morphogenesis of an epithelial foldAndrogen receptorHomo sapiens (human)
lateral sprouting involved in mammary gland duct morphogenesisAndrogen receptorHomo sapiens (human)
prostate gland growthAndrogen receptorHomo sapiens (human)
prostate gland epithelium morphogenesisAndrogen receptorHomo sapiens (human)
epithelial cell differentiation involved in prostate gland developmentAndrogen receptorHomo sapiens (human)
tertiary branching involved in mammary gland duct morphogenesisAndrogen receptorHomo sapiens (human)
mammary gland alveolus developmentAndrogen receptorHomo sapiens (human)
positive regulation of epithelial cell proliferation involved in prostate gland developmentAndrogen receptorHomo sapiens (human)
cellular response to steroid hormone stimulusAndrogen receptorHomo sapiens (human)
cellular response to estrogen stimulusAndrogen receptorHomo sapiens (human)
cellular response to testosterone stimulusAndrogen receptorHomo sapiens (human)
seminiferous tubule developmentAndrogen receptorHomo sapiens (human)
non-membrane-bounded organelle assemblyAndrogen receptorHomo sapiens (human)
positive regulation of miRNA transcriptionAndrogen receptorHomo sapiens (human)
regulation of protein localization to plasma membraneAndrogen receptorHomo sapiens (human)
negative regulation of extrinsic apoptotic signaling pathwayAndrogen receptorHomo sapiens (human)
male gonad developmentAndrogen receptorHomo sapiens (human)
intracellular steroid hormone receptor signaling pathwayAndrogen receptorHomo sapiens (human)
positive regulation of gene expressionTissue factorHomo sapiens (human)
positive regulation of interleukin-8 productionTissue factorHomo sapiens (human)
positive regulation of endothelial cell proliferationTissue factorHomo sapiens (human)
activation of plasma proteins involved in acute inflammatory responseTissue factorHomo sapiens (human)
activation of blood coagulation via clotting cascadeTissue factorHomo sapiens (human)
activation of cysteine-type endopeptidase activity involved in apoptotic processTissue factorHomo sapiens (human)
blood coagulationTissue factorHomo sapiens (human)
positive regulation of platelet-derived growth factor receptor signaling pathwayTissue factorHomo sapiens (human)
protein processingTissue factorHomo sapiens (human)
positive regulation of cell migrationTissue factorHomo sapiens (human)
positive regulation of TOR signalingTissue factorHomo sapiens (human)
positive regulation of angiogenesisTissue factorHomo sapiens (human)
positive regulation of positive chemotaxisTissue factorHomo sapiens (human)
cytokine-mediated signaling pathwayTissue factorHomo sapiens (human)
long-chain fatty acid metabolic processCytochrome P450 2C19Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 2C19Homo sapiens (human)
steroid metabolic processCytochrome P450 2C19Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 2C19Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 2C19Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2C19Homo sapiens (human)
omega-hydroxylase P450 pathwayCytochrome P450 2C19Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIHistone deacetylase 4Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIHistone deacetylase 4Homo sapiens (human)
chromatin remodelingHistone deacetylase 4Homo sapiens (human)
protein deacetylationHistone deacetylase 4Homo sapiens (human)
inflammatory responseHistone deacetylase 4Homo sapiens (human)
nervous system developmentHistone deacetylase 4Homo sapiens (human)
positive regulation of cell population proliferationHistone deacetylase 4Homo sapiens (human)
negative regulation of myotube differentiationHistone deacetylase 4Homo sapiens (human)
negative regulation of transcription by competitive promoter bindingHistone deacetylase 4Homo sapiens (human)
response to denervation involved in regulation of muscle adaptationHistone deacetylase 4Homo sapiens (human)
cardiac muscle hypertrophy in response to stressHistone deacetylase 4Homo sapiens (human)
protein sumoylationHistone deacetylase 4Homo sapiens (human)
B cell differentiationHistone deacetylase 4Homo sapiens (human)
positive regulation of protein sumoylationHistone deacetylase 4Homo sapiens (human)
peptidyl-lysine deacetylationHistone deacetylase 4Homo sapiens (human)
B cell activationHistone deacetylase 4Homo sapiens (human)
regulation of protein bindingHistone deacetylase 4Homo sapiens (human)
negative regulation of DNA-binding transcription factor activityHistone deacetylase 4Homo sapiens (human)
negative regulation of gene expression, epigeneticHistone deacetylase 4Homo sapiens (human)
negative regulation of glycolytic processHistone deacetylase 4Homo sapiens (human)
positive regulation of DNA-templated transcriptionHistone deacetylase 4Homo sapiens (human)
positive regulation of transcription by RNA polymerase IIHistone deacetylase 4Homo sapiens (human)
positive regulation of DNA-binding transcription factor activityHistone deacetylase 4Homo sapiens (human)
type I interferon-mediated signaling pathwayHistone deacetylase 4Homo sapiens (human)
response to interleukin-1Histone deacetylase 4Homo sapiens (human)
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of heart rate by hormonePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of membrane potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
positive regulation of DNA-templated transcriptionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion homeostasisPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cardiac muscle contractionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of ventricular cardiac muscle cell membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cellular response to xenobiotic stimulusPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane depolarization during action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion export across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
negative regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
positive regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
negative regulation of potassium ion export across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion import across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
negative regulation of myotube differentiationHistone deacetylase 1Homo sapiens (human)
negative regulation of apoptotic processHistone deacetylase 1Homo sapiens (human)
positive regulation of signaling receptor activityHistone deacetylase 1Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIHistone deacetylase 1Homo sapiens (human)
chromatin organizationHistone deacetylase 1Homo sapiens (human)
chromatin remodelingHistone deacetylase 1Homo sapiens (human)
DNA methylation-dependent heterochromatin formationHistone deacetylase 1Homo sapiens (human)
regulation of transcription by RNA polymerase IIHistone deacetylase 1Homo sapiens (human)
protein deacetylationHistone deacetylase 1Homo sapiens (human)
endoderm developmentHistone deacetylase 1Homo sapiens (human)
positive regulation of cell population proliferationHistone deacetylase 1Homo sapiens (human)
epidermal cell differentiationHistone deacetylase 1Homo sapiens (human)
positive regulation of gene expressionHistone deacetylase 1Homo sapiens (human)
negative regulation of gene expressionHistone deacetylase 1Homo sapiens (human)
hippocampus developmentHistone deacetylase 1Homo sapiens (human)
neuron differentiationHistone deacetylase 1Homo sapiens (human)
negative regulation of cell migrationHistone deacetylase 1Homo sapiens (human)
negative regulation of transforming growth factor beta receptor signaling pathwayHistone deacetylase 1Homo sapiens (human)
circadian regulation of gene expressionHistone deacetylase 1Homo sapiens (human)
cellular response to platelet-derived growth factor stimulusHistone deacetylase 1Homo sapiens (human)
odontogenesis of dentin-containing toothHistone deacetylase 1Homo sapiens (human)
regulation of cell fate specificationHistone deacetylase 1Homo sapiens (human)
embryonic digit morphogenesisHistone deacetylase 1Homo sapiens (human)
negative regulation of apoptotic processHistone deacetylase 1Homo sapiens (human)
negative regulation of canonical NF-kappaB signal transductionHistone deacetylase 1Homo sapiens (human)
negative regulation by host of viral transcriptionHistone deacetylase 1Homo sapiens (human)
negative regulation of gene expression, epigeneticHistone deacetylase 1Homo sapiens (human)
negative regulation of DNA-templated transcriptionHistone deacetylase 1Homo sapiens (human)
positive regulation of DNA-templated transcriptionHistone deacetylase 1Homo sapiens (human)
positive regulation of transcription by RNA polymerase IIHistone deacetylase 1Homo sapiens (human)
positive regulation of smooth muscle cell proliferationHistone deacetylase 1Homo sapiens (human)
oligodendrocyte differentiationHistone deacetylase 1Homo sapiens (human)
positive regulation of oligodendrocyte differentiationHistone deacetylase 1Homo sapiens (human)
negative regulation of androgen receptor signaling pathwayHistone deacetylase 1Homo sapiens (human)
hair follicle placode formationHistone deacetylase 1Homo sapiens (human)
eyelid development in camera-type eyeHistone deacetylase 1Homo sapiens (human)
fungiform papilla formationHistone deacetylase 1Homo sapiens (human)
negative regulation of canonical Wnt signaling pathwayHistone deacetylase 1Homo sapiens (human)
negative regulation of stem cell population maintenanceHistone deacetylase 1Homo sapiens (human)
positive regulation of stem cell population maintenanceHistone deacetylase 1Homo sapiens (human)
regulation of stem cell differentiationHistone deacetylase 1Homo sapiens (human)
negative regulation of intrinsic apoptotic signaling pathwayHistone deacetylase 1Homo sapiens (human)
heterochromatin formationHistone deacetylase 1Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIHistone deacetylase 7Homo sapiens (human)
vasculogenesisHistone deacetylase 7Homo sapiens (human)
chromatin remodelingHistone deacetylase 7Homo sapiens (human)
protein deacetylationHistone deacetylase 7Homo sapiens (human)
cell-cell junction assemblyHistone deacetylase 7Homo sapiens (human)
protein sumoylationHistone deacetylase 7Homo sapiens (human)
negative regulation of interleukin-2 productionHistone deacetylase 7Homo sapiens (human)
negative regulation of osteoblast differentiationHistone deacetylase 7Homo sapiens (human)
regulation of mRNA processingHistone deacetylase 7Homo sapiens (human)
positive regulation of cell migration involved in sprouting angiogenesisHistone deacetylase 7Homo sapiens (human)
negative regulation of non-canonical NF-kappaB signal transductionHistone deacetylase 7Homo sapiens (human)
positive regulation of signaling receptor activityHistone deacetylase 2Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIHistone deacetylase 2Homo sapiens (human)
response to amphetamineHistone deacetylase 2Homo sapiens (human)
cardiac muscle hypertrophyHistone deacetylase 2Homo sapiens (human)
chromatin remodelingHistone deacetylase 2Homo sapiens (human)
positive regulation of cell population proliferationHistone deacetylase 2Homo sapiens (human)
response to xenobiotic stimulusHistone deacetylase 2Homo sapiens (human)
epidermal cell differentiationHistone deacetylase 2Homo sapiens (human)
positive regulation of epithelial to mesenchymal transitionHistone deacetylase 2Homo sapiens (human)
negative regulation of transcription by competitive promoter bindingHistone deacetylase 2Homo sapiens (human)
negative regulation of neuron projection developmentHistone deacetylase 2Homo sapiens (human)
dendrite developmentHistone deacetylase 2Homo sapiens (human)
negative regulation of cell migrationHistone deacetylase 2Homo sapiens (human)
negative regulation of transforming growth factor beta receptor signaling pathwayHistone deacetylase 2Homo sapiens (human)
response to caffeineHistone deacetylase 2Homo sapiens (human)
heterochromatin formationHistone deacetylase 2Homo sapiens (human)
response to lipopolysaccharideHistone deacetylase 2Homo sapiens (human)
positive regulation of interleukin-1 productionHistone deacetylase 2Homo sapiens (human)
positive regulation of tumor necrosis factor productionHistone deacetylase 2Homo sapiens (human)
circadian regulation of gene expressionHistone deacetylase 2Homo sapiens (human)
positive regulation of collagen biosynthetic processHistone deacetylase 2Homo sapiens (human)
cellular response to heatHistone deacetylase 2Homo sapiens (human)
response to nicotineHistone deacetylase 2Homo sapiens (human)
protein modification processHistone deacetylase 2Homo sapiens (human)
response to cocaineHistone deacetylase 2Homo sapiens (human)
odontogenesis of dentin-containing toothHistone deacetylase 2Homo sapiens (human)
positive regulation of tyrosine phosphorylation of STAT proteinHistone deacetylase 2Homo sapiens (human)
regulation of cell fate specificationHistone deacetylase 2Homo sapiens (human)
embryonic digit morphogenesisHistone deacetylase 2Homo sapiens (human)
negative regulation of apoptotic processHistone deacetylase 2Homo sapiens (human)
negative regulation of DNA-binding transcription factor activityHistone deacetylase 2Homo sapiens (human)
negative regulation of MHC class II biosynthetic processHistone deacetylase 2Homo sapiens (human)
positive regulation of proteolysisHistone deacetylase 2Homo sapiens (human)
negative regulation of DNA-templated transcriptionHistone deacetylase 2Homo sapiens (human)
positive regulation of DNA-templated transcriptionHistone deacetylase 2Homo sapiens (human)
positive regulation of transcription by RNA polymerase IIHistone deacetylase 2Homo sapiens (human)
behavioral response to ethanolHistone deacetylase 2Homo sapiens (human)
positive regulation of oligodendrocyte differentiationHistone deacetylase 2Homo sapiens (human)
response to hyperoxiaHistone deacetylase 2Homo sapiens (human)
hair follicle placode formationHistone deacetylase 2Homo sapiens (human)
negative regulation of dendritic spine developmentHistone deacetylase 2Homo sapiens (human)
eyelid development in camera-type eyeHistone deacetylase 2Homo sapiens (human)
fungiform papilla formationHistone deacetylase 2Homo sapiens (human)
cellular response to hydrogen peroxideHistone deacetylase 2Homo sapiens (human)
cellular response to retinoic acidHistone deacetylase 2Homo sapiens (human)
cellular response to transforming growth factor beta stimulusHistone deacetylase 2Homo sapiens (human)
positive regulation of male mating behaviorHistone deacetylase 2Homo sapiens (human)
negative regulation of stem cell population maintenanceHistone deacetylase 2Homo sapiens (human)
positive regulation of stem cell population maintenanceHistone deacetylase 2Homo sapiens (human)
cellular response to dopamineHistone deacetylase 2Homo sapiens (human)
response to amyloid-betaHistone deacetylase 2Homo sapiens (human)
regulation of stem cell differentiationHistone deacetylase 2Homo sapiens (human)
negative regulation of peptidyl-lysine acetylationHistone deacetylase 2Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIPolyamine deacetylase HDAC10Homo sapiens (human)
DNA repairPolyamine deacetylase HDAC10Homo sapiens (human)
chromatin organizationPolyamine deacetylase HDAC10Homo sapiens (human)
regulation of DNA-templated transcriptionPolyamine deacetylase HDAC10Homo sapiens (human)
macroautophagyPolyamine deacetylase HDAC10Homo sapiens (human)
positive regulation of mismatch repairPolyamine deacetylase HDAC10Homo sapiens (human)
homologous recombinationPolyamine deacetylase HDAC10Homo sapiens (human)
negative regulation of DNA-templated transcriptionPolyamine deacetylase HDAC10Homo sapiens (human)
polyamine deacetylationPolyamine deacetylase HDAC10Homo sapiens (human)
spermidine deacetylationPolyamine deacetylase HDAC10Homo sapiens (human)
epigenetic regulation of gene expressionPolyamine deacetylase HDAC10Homo sapiens (human)
chromatin organizationHistone deacetylase 11 Homo sapiens (human)
oligodendrocyte developmentHistone deacetylase 11 Homo sapiens (human)
epigenetic regulation of gene expressionHistone deacetylase 11 Homo sapiens (human)
single strand break repairNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
negative regulation of transcription by RNA polymerase IINAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
rDNA heterochromatin formationNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
pyrimidine dimer repair by nucleotide-excision repairNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
DNA synthesis involved in DNA repairNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
angiogenesisNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
ovulation from ovarian follicleNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
intracellular glucose homeostasisNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
positive regulation of protein phosphorylationNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
positive regulation of endothelial cell proliferationNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
positive regulation of adaptive immune responseNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
chromatin organizationNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
DNA methylation-dependent heterochromatin formationNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
protein deacetylationNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
triglyceride mobilizationNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
DNA damage responseNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
response to oxidative stressNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
transforming growth factor beta receptor signaling pathwayNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
spermatogenesisNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
regulation of mitotic cell cycleNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
muscle organ developmentNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
positive regulation of cell population proliferationNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
cellular response to starvationNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
negative regulation of gene expressionNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
regulation of centrosome duplicationNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
negative regulation of triglyceride biosynthetic processNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
positive regulation of cholesterol effluxNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
regulation of lipid storageNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
regulation of glucose metabolic processNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
positive regulation of macroautophagyNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
protein ubiquitinationNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
peptidyl-lysine acetylationNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
macrophage differentiationNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
negative regulation of transforming growth factor beta receptor signaling pathwayNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
negative regulation of prostaglandin biosynthetic processNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
heterochromatin formationNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
protein destabilizationNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
negative regulation of TOR signalingNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
regulation of endodeoxyribonuclease activityNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
negative regulation of NF-kappaB transcription factor activityNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
response to insulinNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
circadian regulation of gene expressionNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
leptin-mediated signaling pathwayNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
regulation of smooth muscle cell apoptotic processNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
intracellular triglyceride homeostasisNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
regulation of peroxisome proliferator activated receptor signaling pathwayNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
regulation of cell population proliferationNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
cellular response to glucose starvationNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
negative regulation of phosphorylationNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
response to hydrogen peroxideNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
behavioral response to starvationNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
cholesterol homeostasisNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
regulation of apoptotic processNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
positive regulation of apoptotic processNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
negative regulation of apoptotic processNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
negative regulation of canonical NF-kappaB signal transductionNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
proteasome-mediated ubiquitin-dependent protein catabolic processNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
positive regulation of cysteine-type endopeptidase activity involved in apoptotic processNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
negative regulation of DNA-binding transcription factor activityNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
negative regulation of DNA damage response, signal transduction by p53 class mediatorNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
negative regulation of neuron apoptotic processNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
positive regulation of blood vessel endothelial cell migrationNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
response to leptinNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
positive regulation of MHC class II biosynthetic processNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
negative regulation of fat cell differentiationNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
positive regulation of gluconeogenesisNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
positive regulation of DNA repairNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
positive regulation of angiogenesisNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
negative regulation of cell cycleNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
negative regulation of DNA-templated transcriptionNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
positive regulation of transcription by RNA polymerase IINAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
regulation of transcription by glucoseNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
positive regulation of insulin receptor signaling pathwayNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
white fat cell differentiationNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
negative regulation of helicase activityNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
positive regulation of smooth muscle cell differentiationNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
maintenance of nucleus locationNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
negative regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
fatty acid homeostasisNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
negative regulation of androgen receptor signaling pathwayNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
positive regulation of macrophage cytokine productionNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
cellular response to hydrogen peroxideNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
regulation of bile acid biosynthetic processNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
UV-damage excision repairNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
cellular response to tumor necrosis factorNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
cellular response to hypoxiaNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
cellular response to ionizing radiationNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
regulation of protein serine/threonine kinase activityNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
regulation of brown fat cell differentiationNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
stress-induced premature senescenceNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
energy homeostasisNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
protein depropionylationNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
DNA repair-dependent chromatin remodelingNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
regulation of cellular response to heatNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
negative regulation of signal transduction by p53 class mediatorNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
negative regulation of protein acetylationNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
negative regulation of intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
negative regulation of oxidative stress-induced intrinsic apoptotic signaling pathwayNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
positive regulation of endoplasmic reticulum stress-induced intrinsic apoptotic signaling pathwayNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
positive regulation of adipose tissue developmentNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
cellular response to leukemia inhibitory factorNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
positive regulation of macrophage apoptotic processNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
negative regulation of cAMP-dependent protein kinase activityNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
positive regulation of cAMP-dependent protein kinase activityNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
negative regulation of cellular response to testosterone stimulusNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
negative regulation of peptidyl-lysine acetylationNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
negative regulation of cellular senescenceNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
positive regulation of cellular senescenceNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
positive regulation of double-strand break repairNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIHistone deacetylase 8Homo sapiens (human)
chromatin organizationHistone deacetylase 8Homo sapiens (human)
mitotic sister chromatid cohesionHistone deacetylase 8Homo sapiens (human)
negative regulation of protein ubiquitinationHistone deacetylase 8Homo sapiens (human)
regulation of protein stabilityHistone deacetylase 8Homo sapiens (human)
regulation of telomere maintenanceHistone deacetylase 8Homo sapiens (human)
epigenetic regulation of gene expressionHistone deacetylase 8Homo sapiens (human)
polyamine deacetylationHistone deacetylase 6Homo sapiens (human)
spermidine deacetylationHistone deacetylase 6Homo sapiens (human)
positive regulation of signaling receptor activityHistone deacetylase 6Homo sapiens (human)
protein polyubiquitinationHistone deacetylase 6Homo sapiens (human)
response to amphetamineHistone deacetylase 6Homo sapiens (human)
protein deacetylationHistone deacetylase 6Homo sapiens (human)
protein quality control for misfolded or incompletely synthesized proteinsHistone deacetylase 6Homo sapiens (human)
intracellular protein transportHistone deacetylase 6Homo sapiens (human)
autophagyHistone deacetylase 6Homo sapiens (human)
actin filament organizationHistone deacetylase 6Homo sapiens (human)
negative regulation of microtubule depolymerizationHistone deacetylase 6Homo sapiens (human)
regulation of autophagyHistone deacetylase 6Homo sapiens (human)
positive regulation of epithelial cell migrationHistone deacetylase 6Homo sapiens (human)
negative regulation of hydrogen peroxide metabolic processHistone deacetylase 6Homo sapiens (human)
regulation of macroautophagyHistone deacetylase 6Homo sapiens (human)
axonal transport of mitochondrionHistone deacetylase 6Homo sapiens (human)
negative regulation of protein-containing complex assemblyHistone deacetylase 6Homo sapiens (human)
regulation of protein stabilityHistone deacetylase 6Homo sapiens (human)
protein destabilizationHistone deacetylase 6Homo sapiens (human)
lysosome localizationHistone deacetylase 6Homo sapiens (human)
protein-containing complex disassemblyHistone deacetylase 6Homo sapiens (human)
positive regulation of peptidyl-serine phosphorylationHistone deacetylase 6Homo sapiens (human)
cellular response to heatHistone deacetylase 6Homo sapiens (human)
peptidyl-lysine deacetylationHistone deacetylase 6Homo sapiens (human)
response to immobilization stressHistone deacetylase 6Homo sapiens (human)
cellular response to topologically incorrect proteinHistone deacetylase 6Homo sapiens (human)
erythrocyte enucleationHistone deacetylase 6Homo sapiens (human)
ubiquitin-dependent protein catabolic process via the multivesicular body sorting pathwayHistone deacetylase 6Homo sapiens (human)
negative regulation of protein-containing complex disassemblyHistone deacetylase 6Homo sapiens (human)
regulation of fat cell differentiationHistone deacetylase 6Homo sapiens (human)
negative regulation of gene expression, epigeneticHistone deacetylase 6Homo sapiens (human)
negative regulation of proteolysisHistone deacetylase 6Homo sapiens (human)
negative regulation of DNA-templated transcriptionHistone deacetylase 6Homo sapiens (human)
collateral sproutingHistone deacetylase 6Homo sapiens (human)
negative regulation of axon extension involved in axon guidanceHistone deacetylase 6Homo sapiens (human)
positive regulation of dendrite morphogenesisHistone deacetylase 6Homo sapiens (human)
negative regulation of oxidoreductase activityHistone deacetylase 6Homo sapiens (human)
response to corticosteroneHistone deacetylase 6Homo sapiens (human)
response to misfolded proteinHistone deacetylase 6Homo sapiens (human)
positive regulation of synaptic transmission, glutamatergicHistone deacetylase 6Homo sapiens (human)
cilium assemblyHistone deacetylase 6Homo sapiens (human)
regulation of microtubule-based movementHistone deacetylase 6Homo sapiens (human)
regulation of androgen receptor signaling pathwayHistone deacetylase 6Homo sapiens (human)
dendritic spine morphogenesisHistone deacetylase 6Homo sapiens (human)
cilium disassemblyHistone deacetylase 6Homo sapiens (human)
parkin-mediated stimulation of mitophagy in response to mitochondrial depolarizationHistone deacetylase 6Homo sapiens (human)
regulation of establishment of protein localizationHistone deacetylase 6Homo sapiens (human)
cellular response to hydrogen peroxideHistone deacetylase 6Homo sapiens (human)
aggresome assemblyHistone deacetylase 6Homo sapiens (human)
polyubiquitinated misfolded protein transportHistone deacetylase 6Homo sapiens (human)
response to growth factorHistone deacetylase 6Homo sapiens (human)
cellular response to misfolded proteinHistone deacetylase 6Homo sapiens (human)
cellular response to parathyroid hormone stimulusHistone deacetylase 6Homo sapiens (human)
response to dexamethasoneHistone deacetylase 6Homo sapiens (human)
tubulin deacetylationHistone deacetylase 6Homo sapiens (human)
positive regulation of tubulin deacetylationHistone deacetylase 6Homo sapiens (human)
positive regulation of cellular response to oxidative stressHistone deacetylase 6Homo sapiens (human)
negative regulation of protein acetylationHistone deacetylase 6Homo sapiens (human)
regulation of autophagy of mitochondrionHistone deacetylase 6Homo sapiens (human)
positive regulation of cholangiocyte proliferationHistone deacetylase 6Homo sapiens (human)
negative regulation of aggrephagyHistone deacetylase 6Homo sapiens (human)
epigenetic regulation of gene expressionHistone deacetylase 6Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIHistone deacetylase 9Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIHistone deacetylase 9Homo sapiens (human)
negative regulation of cytokine productionHistone deacetylase 9Homo sapiens (human)
response to amphetamineHistone deacetylase 9Homo sapiens (human)
inflammatory responseHistone deacetylase 9Homo sapiens (human)
heart developmentHistone deacetylase 9Homo sapiens (human)
neuron differentiationHistone deacetylase 9Homo sapiens (human)
B cell differentiationHistone deacetylase 9Homo sapiens (human)
cellular response to insulin stimulusHistone deacetylase 9Homo sapiens (human)
peptidyl-lysine deacetylationHistone deacetylase 9Homo sapiens (human)
B cell activationHistone deacetylase 9Homo sapiens (human)
cholesterol homeostasisHistone deacetylase 9Homo sapiens (human)
negative regulation of gene expression, epigeneticHistone deacetylase 9Homo sapiens (human)
negative regulation of DNA-templated transcriptionHistone deacetylase 9Homo sapiens (human)
regulation of skeletal muscle fiber developmentHistone deacetylase 9Homo sapiens (human)
regulation of striated muscle cell differentiationHistone deacetylase 9Homo sapiens (human)
positive regulation of cell migration involved in sprouting angiogenesisHistone deacetylase 9Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIHistone deacetylase 5Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIHistone deacetylase 5Homo sapiens (human)
inflammatory responseHistone deacetylase 5Homo sapiens (human)
response to xenobiotic stimulusHistone deacetylase 5Homo sapiens (human)
regulation of myotube differentiationHistone deacetylase 5Homo sapiens (human)
negative regulation of myotube differentiationHistone deacetylase 5Homo sapiens (human)
response to activityHistone deacetylase 5Homo sapiens (human)
neuron differentiationHistone deacetylase 5Homo sapiens (human)
B cell differentiationHistone deacetylase 5Homo sapiens (human)
cellular response to insulin stimulusHistone deacetylase 5Homo sapiens (human)
B cell activationHistone deacetylase 5Homo sapiens (human)
response to cocaineHistone deacetylase 5Homo sapiens (human)
regulation of protein bindingHistone deacetylase 5Homo sapiens (human)
negative regulation of gene expression, epigeneticHistone deacetylase 5Homo sapiens (human)
negative regulation of DNA-templated transcriptionHistone deacetylase 5Homo sapiens (human)
positive regulation of transcription by RNA polymerase IIHistone deacetylase 5Homo sapiens (human)
positive regulation of DNA-binding transcription factor activityHistone deacetylase 5Homo sapiens (human)
cellular response to lipopolysaccharideHistone deacetylase 5Homo sapiens (human)
negative regulation of cell migration involved in sprouting angiogenesisHistone deacetylase 5Homo sapiens (human)
negative regulation of transcription by RNA polymerase IINuclear receptor corepressor 2Homo sapiens (human)
lactationNuclear receptor corepressor 2Homo sapiens (human)
response to organonitrogen compoundNuclear receptor corepressor 2Homo sapiens (human)
regulation of cellular ketone metabolic processNuclear receptor corepressor 2Homo sapiens (human)
cerebellum developmentNuclear receptor corepressor 2Homo sapiens (human)
response to estradiolNuclear receptor corepressor 2Homo sapiens (human)
estrous cycleNuclear receptor corepressor 2Homo sapiens (human)
negative regulation of DNA-templated transcriptionNuclear receptor corepressor 2Homo sapiens (human)
negative regulation of androgen receptor signaling pathwayNuclear receptor corepressor 2Homo sapiens (human)
negative regulation of miRNA transcriptionNuclear receptor corepressor 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (148)

Processvia Protein(s)Taxonomy
transcription corepressor bindingHistone deacetylase 3Homo sapiens (human)
chromatin bindingHistone deacetylase 3Homo sapiens (human)
transcription corepressor activityHistone deacetylase 3Homo sapiens (human)
histone deacetylase activityHistone deacetylase 3Homo sapiens (human)
protein bindingHistone deacetylase 3Homo sapiens (human)
enzyme bindingHistone deacetylase 3Homo sapiens (human)
cyclin bindingHistone deacetylase 3Homo sapiens (human)
chromatin DNA bindingHistone deacetylase 3Homo sapiens (human)
protein lysine deacetylase activityHistone deacetylase 3Homo sapiens (human)
histone deacetylase bindingHistone deacetylase 3Homo sapiens (human)
NF-kappaB bindingHistone deacetylase 3Homo sapiens (human)
DNA-binding transcription factor bindingHistone deacetylase 3Homo sapiens (human)
protein decrotonylase activityHistone deacetylase 3Homo sapiens (human)
histone decrotonylase activityHistone deacetylase 3Homo sapiens (human)
protein de-2-hydroxyisobutyrylase activityHistone deacetylase 3Homo sapiens (human)
transcription cis-regulatory region bindingBromodomain-containing protein 4Homo sapiens (human)
p53 bindingBromodomain-containing protein 4Homo sapiens (human)
chromatin bindingBromodomain-containing protein 4Homo sapiens (human)
transcription coregulator activityBromodomain-containing protein 4Homo sapiens (human)
transcription coactivator activityBromodomain-containing protein 4Homo sapiens (human)
protein bindingBromodomain-containing protein 4Homo sapiens (human)
RNA polymerase II CTD heptapeptide repeat kinase activityBromodomain-containing protein 4Homo sapiens (human)
enzyme bindingBromodomain-containing protein 4Homo sapiens (human)
lysine-acetylated histone bindingBromodomain-containing protein 4Homo sapiens (human)
RNA polymerase II C-terminal domain bindingBromodomain-containing protein 4Homo sapiens (human)
P-TEFb complex bindingBromodomain-containing protein 4Homo sapiens (human)
histone reader activityBromodomain-containing protein 4Homo sapiens (human)
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
steroid bindingCytochrome P450 3A4Homo sapiens (human)
iron ion bindingCytochrome P450 3A4Homo sapiens (human)
protein bindingCytochrome P450 3A4Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
retinoic acid 4-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
oxidoreductase activityCytochrome P450 3A4Homo sapiens (human)
oxygen bindingCytochrome P450 3A4Homo sapiens (human)
enzyme bindingCytochrome P450 3A4Homo sapiens (human)
heme bindingCytochrome P450 3A4Homo sapiens (human)
vitamin D3 25-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
caffeine oxidase activityCytochrome P450 3A4Homo sapiens (human)
quinine 3-monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
testosterone 6-beta-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1-alpha,25-dihydroxyvitamin D3 23-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 8,9 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 11,12 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 14,15 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
aromatase activityCytochrome P450 3A4Homo sapiens (human)
vitamin D 24-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 16-alpha-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 2-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1,8-cineole 2-exo-monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
RNA bindingLeukotriene A-4 hydrolaseHomo sapiens (human)
aminopeptidase activityLeukotriene A-4 hydrolaseHomo sapiens (human)
epoxide hydrolase activityLeukotriene A-4 hydrolaseHomo sapiens (human)
leukotriene-A4 hydrolase activityLeukotriene A-4 hydrolaseHomo sapiens (human)
protein bindingLeukotriene A-4 hydrolaseHomo sapiens (human)
peptidase activityLeukotriene A-4 hydrolaseHomo sapiens (human)
zinc ion bindingLeukotriene A-4 hydrolaseHomo sapiens (human)
tripeptide aminopeptidase activityLeukotriene A-4 hydrolaseHomo sapiens (human)
metalloaminopeptidase activityLeukotriene A-4 hydrolaseHomo sapiens (human)
transcription cis-regulatory region bindingAndrogen receptorHomo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingAndrogen receptorHomo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificAndrogen receptorHomo sapiens (human)
RNA polymerase II general transcription initiation factor bindingAndrogen receptorHomo sapiens (human)
transcription coactivator bindingAndrogen receptorHomo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificAndrogen receptorHomo sapiens (human)
chromatin bindingAndrogen receptorHomo sapiens (human)
DNA-binding transcription factor activityAndrogen receptorHomo sapiens (human)
nuclear receptor activityAndrogen receptorHomo sapiens (human)
G protein-coupled receptor activityAndrogen receptorHomo sapiens (human)
signaling receptor bindingAndrogen receptorHomo sapiens (human)
steroid bindingAndrogen receptorHomo sapiens (human)
androgen bindingAndrogen receptorHomo sapiens (human)
protein bindingAndrogen receptorHomo sapiens (human)
beta-catenin bindingAndrogen receptorHomo sapiens (human)
zinc ion bindingAndrogen receptorHomo sapiens (human)
enzyme bindingAndrogen receptorHomo sapiens (human)
ATPase bindingAndrogen receptorHomo sapiens (human)
molecular adaptor activityAndrogen receptorHomo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingAndrogen receptorHomo sapiens (human)
POU domain bindingAndrogen receptorHomo sapiens (human)
molecular condensate scaffold activityAndrogen receptorHomo sapiens (human)
estrogen response element bindingAndrogen receptorHomo sapiens (human)
serine-type endopeptidase activityTissue factorHomo sapiens (human)
protease bindingTissue factorHomo sapiens (human)
protein bindingTissue factorHomo sapiens (human)
phospholipid bindingTissue factorHomo sapiens (human)
cytokine receptor activityTissue factorHomo sapiens (human)
monooxygenase activityCytochrome P450 2C19Homo sapiens (human)
iron ion bindingCytochrome P450 2C19Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 2C19Homo sapiens (human)
oxidoreductase activityCytochrome P450 2C19Homo sapiens (human)
(S)-limonene 6-monooxygenase activityCytochrome P450 2C19Homo sapiens (human)
(S)-limonene 7-monooxygenase activityCytochrome P450 2C19Homo sapiens (human)
oxygen bindingCytochrome P450 2C19Homo sapiens (human)
enzyme bindingCytochrome P450 2C19Homo sapiens (human)
heme bindingCytochrome P450 2C19Homo sapiens (human)
(R)-limonene 6-monooxygenase activityCytochrome P450 2C19Homo sapiens (human)
aromatase activityCytochrome P450 2C19Homo sapiens (human)
long-chain fatty acid omega-1 hydroxylase activityCytochrome P450 2C19Homo sapiens (human)
arachidonic acid epoxygenase activityCytochrome P450 2C19Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2C19Homo sapiens (human)
transcription cis-regulatory region bindingHistone deacetylase 4Homo sapiens (human)
histone bindingHistone deacetylase 4Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingHistone deacetylase 4Homo sapiens (human)
histone deacetylase activityHistone deacetylase 4Homo sapiens (human)
protein bindingHistone deacetylase 4Homo sapiens (human)
zinc ion bindingHistone deacetylase 4Homo sapiens (human)
SUMO transferase activityHistone deacetylase 4Homo sapiens (human)
potassium ion bindingHistone deacetylase 4Homo sapiens (human)
protein lysine deacetylase activityHistone deacetylase 4Homo sapiens (human)
identical protein bindingHistone deacetylase 4Homo sapiens (human)
histone deacetylase bindingHistone deacetylase 4Homo sapiens (human)
molecular adaptor activityHistone deacetylase 4Homo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingHistone deacetylase 4Homo sapiens (human)
DNA-binding transcription factor bindingHistone deacetylase 4Homo sapiens (human)
transcription cis-regulatory region bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inward rectifier potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
delayed rectifier potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
ubiquitin protein ligase bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
identical protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
protein homodimerization activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
C3HC4-type RING finger domain bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activity involved in cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
scaffold protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activity involved in ventricular cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
nucleosomal DNA bindingHistone deacetylase 1Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingHistone deacetylase 1Homo sapiens (human)
RNA polymerase II core promoter sequence-specific DNA bindingHistone deacetylase 1Homo sapiens (human)
core promoter sequence-specific DNA bindingHistone deacetylase 1Homo sapiens (human)
transcription corepressor bindingHistone deacetylase 1Homo sapiens (human)
p53 bindingHistone deacetylase 1Homo sapiens (human)
transcription corepressor activityHistone deacetylase 1Homo sapiens (human)
histone deacetylase activityHistone deacetylase 1Homo sapiens (human)
protein bindingHistone deacetylase 1Homo sapiens (human)
enzyme bindingHistone deacetylase 1Homo sapiens (human)
protein lysine deacetylase activityHistone deacetylase 1Homo sapiens (human)
Krueppel-associated box domain bindingHistone deacetylase 1Homo sapiens (human)
histone deacetylase bindingHistone deacetylase 1Homo sapiens (human)
NF-kappaB bindingHistone deacetylase 1Homo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingHistone deacetylase 1Homo sapiens (human)
E-box bindingHistone deacetylase 1Homo sapiens (human)
DNA-binding transcription factor bindingHistone deacetylase 1Homo sapiens (human)
histone decrotonylase activityHistone deacetylase 1Homo sapiens (human)
promoter-specific chromatin bindingHistone deacetylase 1Homo sapiens (human)
chromatin bindingHistone deacetylase 7Homo sapiens (human)
transcription corepressor activityHistone deacetylase 7Homo sapiens (human)
histone deacetylase activityHistone deacetylase 7Homo sapiens (human)
protein kinase C bindingHistone deacetylase 7Homo sapiens (human)
protein bindingHistone deacetylase 7Homo sapiens (human)
SUMO transferase activityHistone deacetylase 7Homo sapiens (human)
protein kinase bindingHistone deacetylase 7Homo sapiens (human)
protein lysine deacetylase activityHistone deacetylase 7Homo sapiens (human)
metal ion bindingHistone deacetylase 7Homo sapiens (human)
14-3-3 protein bindingHistone deacetylase 7Homo sapiens (human)
DNA-binding transcription factor bindingHistone deacetylase 7Homo sapiens (human)
nucleosomal DNA bindingHistone deacetylase 2Homo sapiens (human)
chromatin bindingHistone deacetylase 2Homo sapiens (human)
RNA bindingHistone deacetylase 2Homo sapiens (human)
histone deacetylase activityHistone deacetylase 2Homo sapiens (human)
protein bindingHistone deacetylase 2Homo sapiens (human)
enzyme bindingHistone deacetylase 2Homo sapiens (human)
heat shock protein bindingHistone deacetylase 2Homo sapiens (human)
protein lysine deacetylase activityHistone deacetylase 2Homo sapiens (human)
histone bindingHistone deacetylase 2Homo sapiens (human)
histone deacetylase bindingHistone deacetylase 2Homo sapiens (human)
NF-kappaB bindingHistone deacetylase 2Homo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingHistone deacetylase 2Homo sapiens (human)
histone decrotonylase activityHistone deacetylase 2Homo sapiens (human)
protein de-2-hydroxyisobutyrylase activityHistone deacetylase 2Homo sapiens (human)
promoter-specific chromatin bindingHistone deacetylase 2Homo sapiens (human)
protein lysine deacetylase activityPolyamine deacetylase HDAC10Homo sapiens (human)
histone deacetylase activityPolyamine deacetylase HDAC10Homo sapiens (human)
protein bindingPolyamine deacetylase HDAC10Homo sapiens (human)
zinc ion bindingPolyamine deacetylase HDAC10Homo sapiens (human)
deacetylase activityPolyamine deacetylase HDAC10Homo sapiens (human)
enzyme bindingPolyamine deacetylase HDAC10Homo sapiens (human)
protein lysine deacetylase activityPolyamine deacetylase HDAC10Homo sapiens (human)
histone deacetylase bindingPolyamine deacetylase HDAC10Homo sapiens (human)
acetylputrescine deacetylase activityPolyamine deacetylase HDAC10Homo sapiens (human)
acetylspermidine deacetylase activityPolyamine deacetylase HDAC10Homo sapiens (human)
histone deacetylase activityHistone deacetylase 11 Homo sapiens (human)
protein bindingHistone deacetylase 11 Homo sapiens (human)
DNA-binding transcription factor bindingHistone deacetylase 11 Homo sapiens (human)
NAD+ ADP-ribosyltransferase activityNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
NAD+-protein ADP-ribosyltransferase activityNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
p53 bindingNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
transcription coactivator activityNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
transcription corepressor activityNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
histone deacetylase activityNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
protein bindingNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
nuclear receptor bindingNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
NAD-dependent histone deacetylase activityNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
deacetylase activityNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
enzyme bindingNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
NAD-dependent histone H3K14 deacetylase activityNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
protein lysine deacetylase activityNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
NAD-dependent protein lysine deacetylase activityNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
histone bindingNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
identical protein bindingNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
HLH domain bindingNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
bHLH transcription factor bindingNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
metal ion bindingNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
NAD-dependent histone H3K9 deacetylase activityNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
NAD-dependent histone H4K16 deacetylase activityNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
mitogen-activated protein kinase bindingNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
lysine-acetylated histone bindingNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
protein-propionyllysine depropionylase activityNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
DNA-binding transcription factor bindingNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
histone H4K12 deacetylase activityNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
histone H3K deacetylase activityNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
NAD-dependent histone decrotonylase activityNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
keratin filament bindingNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
promoter-specific chromatin bindingNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
NAD+ bindingNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
histone deacetylase activityHistone deacetylase 8Homo sapiens (human)
protein bindingHistone deacetylase 8Homo sapiens (human)
Hsp70 protein bindingHistone deacetylase 8Homo sapiens (human)
protein lysine deacetylase activityHistone deacetylase 8Homo sapiens (human)
metal ion bindingHistone deacetylase 8Homo sapiens (human)
Hsp90 protein bindingHistone deacetylase 8Homo sapiens (human)
DNA-binding transcription factor bindingHistone deacetylase 8Homo sapiens (human)
histone decrotonylase activityHistone deacetylase 8Homo sapiens (human)
acetylspermidine deacetylase activityHistone deacetylase 6Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingHistone deacetylase 6Homo sapiens (human)
transcription corepressor bindingHistone deacetylase 6Homo sapiens (human)
actin bindingHistone deacetylase 6Homo sapiens (human)
histone deacetylase activityHistone deacetylase 6Homo sapiens (human)
protein bindingHistone deacetylase 6Homo sapiens (human)
beta-catenin bindingHistone deacetylase 6Homo sapiens (human)
microtubule bindingHistone deacetylase 6Homo sapiens (human)
zinc ion bindingHistone deacetylase 6Homo sapiens (human)
enzyme bindingHistone deacetylase 6Homo sapiens (human)
polyubiquitin modification-dependent protein bindingHistone deacetylase 6Homo sapiens (human)
ubiquitin protein ligase bindingHistone deacetylase 6Homo sapiens (human)
protein lysine deacetylase activityHistone deacetylase 6Homo sapiens (human)
histone deacetylase bindingHistone deacetylase 6Homo sapiens (human)
tubulin deacetylase activityHistone deacetylase 6Homo sapiens (human)
alpha-tubulin bindingHistone deacetylase 6Homo sapiens (human)
ubiquitin bindingHistone deacetylase 6Homo sapiens (human)
tau protein bindingHistone deacetylase 6Homo sapiens (human)
beta-tubulin bindingHistone deacetylase 6Homo sapiens (human)
misfolded protein bindingHistone deacetylase 6Homo sapiens (human)
Hsp90 protein bindingHistone deacetylase 6Homo sapiens (human)
dynein complex bindingHistone deacetylase 6Homo sapiens (human)
transcription factor bindingHistone deacetylase 6Homo sapiens (human)
transcription corepressor activityHistone deacetylase 9Homo sapiens (human)
histone deacetylase activityHistone deacetylase 9Homo sapiens (human)
protein kinase C bindingHistone deacetylase 9Homo sapiens (human)
protein bindingHistone deacetylase 9Homo sapiens (human)
histone H3K14 deacetylase activityHistone deacetylase 9Homo sapiens (human)
histone H3K9 deacetylase activityHistone deacetylase 9Homo sapiens (human)
protein lysine deacetylase activityHistone deacetylase 9Homo sapiens (human)
histone H4K16 deacetylase activityHistone deacetylase 9Homo sapiens (human)
histone deacetylase bindingHistone deacetylase 9Homo sapiens (human)
metal ion bindingHistone deacetylase 9Homo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingHistone deacetylase 9Homo sapiens (human)
DNA-binding transcription factor bindingHistone deacetylase 9Homo sapiens (human)
transcription cis-regulatory region bindingHistone deacetylase 5Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingHistone deacetylase 5Homo sapiens (human)
transcription corepressor bindingHistone deacetylase 5Homo sapiens (human)
chromatin bindingHistone deacetylase 5Homo sapiens (human)
histone deacetylase activityHistone deacetylase 5Homo sapiens (human)
protein kinase C bindingHistone deacetylase 5Homo sapiens (human)
protein bindingHistone deacetylase 5Homo sapiens (human)
protein lysine deacetylase activityHistone deacetylase 5Homo sapiens (human)
identical protein bindingHistone deacetylase 5Homo sapiens (human)
histone deacetylase bindingHistone deacetylase 5Homo sapiens (human)
metal ion bindingHistone deacetylase 5Homo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingHistone deacetylase 5Homo sapiens (human)
DNA-binding transcription factor bindingHistone deacetylase 5Homo sapiens (human)
DNA bindingNuclear receptor corepressor 2Homo sapiens (human)
chromatin bindingNuclear receptor corepressor 2Homo sapiens (human)
transcription corepressor activityNuclear receptor corepressor 2Homo sapiens (human)
Notch bindingNuclear receptor corepressor 2Homo sapiens (human)
protein bindingNuclear receptor corepressor 2Homo sapiens (human)
nuclear glucocorticoid receptor bindingNuclear receptor corepressor 2Homo sapiens (human)
histone deacetylase bindingNuclear receptor corepressor 2Homo sapiens (human)
nuclear retinoid X receptor bindingNuclear receptor corepressor 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (62)

Processvia Protein(s)Taxonomy
nucleusHistone deacetylase 3Homo sapiens (human)
nucleoplasmHistone deacetylase 3Homo sapiens (human)
cytoplasmHistone deacetylase 3Homo sapiens (human)
Golgi apparatusHistone deacetylase 3Homo sapiens (human)
cytosolHistone deacetylase 3Homo sapiens (human)
plasma membraneHistone deacetylase 3Homo sapiens (human)
mitotic spindleHistone deacetylase 3Homo sapiens (human)
histone deacetylase complexHistone deacetylase 3Homo sapiens (human)
transcription repressor complexHistone deacetylase 3Homo sapiens (human)
nucleusHistone deacetylase 3Homo sapiens (human)
condensed nuclear chromosomeBromodomain-containing protein 4Homo sapiens (human)
nucleusBromodomain-containing protein 4Homo sapiens (human)
nucleoplasmBromodomain-containing protein 4Homo sapiens (human)
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
cytoplasmCytochrome P450 3A4Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 3A4Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 3A4Homo sapiens (human)
extracellular regionLeukotriene A-4 hydrolaseHomo sapiens (human)
nucleoplasmLeukotriene A-4 hydrolaseHomo sapiens (human)
cytosolLeukotriene A-4 hydrolaseHomo sapiens (human)
extracellular exosomeLeukotriene A-4 hydrolaseHomo sapiens (human)
tertiary granule lumenLeukotriene A-4 hydrolaseHomo sapiens (human)
ficolin-1-rich granule lumenLeukotriene A-4 hydrolaseHomo sapiens (human)
cytosolLeukotriene A-4 hydrolaseHomo sapiens (human)
nucleusLeukotriene A-4 hydrolaseHomo sapiens (human)
plasma membraneAndrogen receptorHomo sapiens (human)
nucleusAndrogen receptorHomo sapiens (human)
nucleoplasmAndrogen receptorHomo sapiens (human)
cytoplasmAndrogen receptorHomo sapiens (human)
cytosolAndrogen receptorHomo sapiens (human)
nuclear speckAndrogen receptorHomo sapiens (human)
chromatinAndrogen receptorHomo sapiens (human)
protein-containing complexAndrogen receptorHomo sapiens (human)
nucleusAndrogen receptorHomo sapiens (human)
extracellular spaceTissue factorHomo sapiens (human)
plasma membraneTissue factorHomo sapiens (human)
external side of plasma membraneTissue factorHomo sapiens (human)
cell surfaceTissue factorHomo sapiens (human)
membraneTissue factorHomo sapiens (human)
collagen-containing extracellular matrixTissue factorHomo sapiens (human)
serine-type peptidase complexTissue factorHomo sapiens (human)
plasma membraneTissue factorHomo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2C19Homo sapiens (human)
plasma membraneCytochrome P450 2C19Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C19Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C19Homo sapiens (human)
cytoplasmCytochrome P450 2C19Homo sapiens (human)
nucleusHistone deacetylase 4Homo sapiens (human)
nucleoplasmHistone deacetylase 4Homo sapiens (human)
cytoplasmHistone deacetylase 4Homo sapiens (human)
cytosolHistone deacetylase 4Homo sapiens (human)
nuclear speckHistone deacetylase 4Homo sapiens (human)
histone deacetylase complexHistone deacetylase 4Homo sapiens (human)
chromatinHistone deacetylase 4Homo sapiens (human)
transcription repressor complexHistone deacetylase 4Homo sapiens (human)
plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cell surfacePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
perinuclear region of cytoplasmPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel complexPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inward rectifier potassium channel complexPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
nucleusHistone deacetylase 1Homo sapiens (human)
nucleoplasmHistone deacetylase 1Homo sapiens (human)
cytoplasmHistone deacetylase 1Homo sapiens (human)
cytosolHistone deacetylase 1Homo sapiens (human)
NuRD complexHistone deacetylase 1Homo sapiens (human)
neuronal cell bodyHistone deacetylase 1Homo sapiens (human)
Sin3-type complexHistone deacetylase 1Homo sapiens (human)
histone deacetylase complexHistone deacetylase 1Homo sapiens (human)
chromatinHistone deacetylase 1Homo sapiens (human)
heterochromatinHistone deacetylase 1Homo sapiens (human)
transcription repressor complexHistone deacetylase 1Homo sapiens (human)
protein-containing complexHistone deacetylase 1Homo sapiens (human)
nucleusHistone deacetylase 1Homo sapiens (human)
nucleusHistone deacetylase 7Homo sapiens (human)
nucleoplasmHistone deacetylase 7Homo sapiens (human)
cytoplasmHistone deacetylase 7Homo sapiens (human)
cytosolHistone deacetylase 7Homo sapiens (human)
chromosome, telomeric regionHistone deacetylase 2Homo sapiens (human)
nucleusHistone deacetylase 2Homo sapiens (human)
nucleoplasmHistone deacetylase 2Homo sapiens (human)
cytoplasmHistone deacetylase 2Homo sapiens (human)
NuRD complexHistone deacetylase 2Homo sapiens (human)
Sin3-type complexHistone deacetylase 2Homo sapiens (human)
histone deacetylase complexHistone deacetylase 2Homo sapiens (human)
chromatinHistone deacetylase 2Homo sapiens (human)
protein-containing complexHistone deacetylase 2Homo sapiens (human)
ESC/E(Z) complexHistone deacetylase 2Homo sapiens (human)
nucleusHistone deacetylase 2Homo sapiens (human)
nucleusPolyamine deacetylase HDAC10Homo sapiens (human)
nucleoplasmPolyamine deacetylase HDAC10Homo sapiens (human)
cytoplasmPolyamine deacetylase HDAC10Homo sapiens (human)
cytosolPolyamine deacetylase HDAC10Homo sapiens (human)
intracellular membrane-bounded organellePolyamine deacetylase HDAC10Homo sapiens (human)
histone deacetylase complexPolyamine deacetylase HDAC10Homo sapiens (human)
nucleusHistone deacetylase 11 Homo sapiens (human)
plasma membraneHistone deacetylase 11 Homo sapiens (human)
histone deacetylase complexHistone deacetylase 11 Homo sapiens (human)
nucleolusNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
cytoplasmNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
ESC/E(Z) complexNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
cytosolNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
fibrillar centerNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
nucleusNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
nuclear envelopeNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
nuclear inner membraneNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
nucleoplasmNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
nucleolusNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
cytoplasmNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
mitochondrionNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
cytosolNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
PML bodyNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
eNoSc complexNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
chromatinNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
euchromatinNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
heterochromatinNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
chromatin silencing complexNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
rDNA heterochromatinNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
nucleusNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
nuclear inner membraneNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
nucleoplasmNAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)
nuclear chromosomeHistone deacetylase 8Homo sapiens (human)
nucleusHistone deacetylase 8Homo sapiens (human)
nucleoplasmHistone deacetylase 8Homo sapiens (human)
cytoplasmHistone deacetylase 8Homo sapiens (human)
histone deacetylase complexHistone deacetylase 8Homo sapiens (human)
nucleusHistone deacetylase 8Homo sapiens (human)
nucleusHistone deacetylase 6Homo sapiens (human)
nucleoplasmHistone deacetylase 6Homo sapiens (human)
cytoplasmHistone deacetylase 6Homo sapiens (human)
multivesicular bodyHistone deacetylase 6Homo sapiens (human)
centrosomeHistone deacetylase 6Homo sapiens (human)
cytosolHistone deacetylase 6Homo sapiens (human)
microtubuleHistone deacetylase 6Homo sapiens (human)
caveolaHistone deacetylase 6Homo sapiens (human)
inclusion bodyHistone deacetylase 6Homo sapiens (human)
aggresomeHistone deacetylase 6Homo sapiens (human)
axonHistone deacetylase 6Homo sapiens (human)
dendriteHistone deacetylase 6Homo sapiens (human)
cell leading edgeHistone deacetylase 6Homo sapiens (human)
ciliary basal bodyHistone deacetylase 6Homo sapiens (human)
perikaryonHistone deacetylase 6Homo sapiens (human)
perinuclear region of cytoplasmHistone deacetylase 6Homo sapiens (human)
axon cytoplasmHistone deacetylase 6Homo sapiens (human)
histone deacetylase complexHistone deacetylase 6Homo sapiens (human)
microtubule associated complexHistone deacetylase 6Homo sapiens (human)
nucleusHistone deacetylase 9Homo sapiens (human)
nucleoplasmHistone deacetylase 9Homo sapiens (human)
cytoplasmHistone deacetylase 9Homo sapiens (human)
histone deacetylase complexHistone deacetylase 9Homo sapiens (human)
transcription regulator complexHistone deacetylase 9Homo sapiens (human)
histone methyltransferase complexHistone deacetylase 9Homo sapiens (human)
nucleusHistone deacetylase 5Homo sapiens (human)
nucleoplasmHistone deacetylase 5Homo sapiens (human)
cytoplasmHistone deacetylase 5Homo sapiens (human)
Golgi apparatusHistone deacetylase 5Homo sapiens (human)
cytosolHistone deacetylase 5Homo sapiens (human)
nuclear speckHistone deacetylase 5Homo sapiens (human)
histone deacetylase complexHistone deacetylase 5Homo sapiens (human)
nucleusNuclear receptor corepressor 2Homo sapiens (human)
nucleoplasmNuclear receptor corepressor 2Homo sapiens (human)
membraneNuclear receptor corepressor 2Homo sapiens (human)
nuclear matrixNuclear receptor corepressor 2Homo sapiens (human)
nuclear bodyNuclear receptor corepressor 2Homo sapiens (human)
chromatinNuclear receptor corepressor 2Homo sapiens (human)
transcription repressor complexNuclear receptor corepressor 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (920)

Assay IDTitleYearJournalArticle
AID1798524HDAC Activity Assay from Article 10.1021/jm800079s: \\A novel series of potent and selective ketone histone deacetylase inhibitors with antitumor activity in vivo.\\2008Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8
A novel series of potent and selective ketone histone deacetylase inhibitors with antitumor activity in vivo.
AID1802398Enzymatic HDAC Activity Assay from Article 10.1074/jbc.M113.490706: \\Histone deacetylase (HDAC) inhibitor kinetic rate constants correlate with cellular histone acetylation but not transcription and cell viability.\\2013The Journal of biological chemistry, Sep-13, Volume: 288, Issue:37
Histone deacetylase (HDAC) inhibitor kinetic rate constants correlate with cellular histone acetylation but not transcription and cell viability.
AID1797850HDAC Enzyme Activity Assay from Article 10.1021/jm701079h: \\Novel aminophenyl benzamide-type histone deacetylase inhibitors with enhanced potency and selectivity.\\2007Journal of medicinal chemistry, Nov-15, Volume: 50, Issue:23
Novel aminophenyl benzamide-type histone deacetylase inhibitors with enhanced potency and selectivity.
AID1798526HDAC Activity Assay from Article 10.1016/j.bmcl.2008.02.025: \\Probing the elusive catalytic activity of vertebrate class IIa histone deacetylases.\\2008Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6
Probing the elusive catalytic activity of vertebrate class IIa histone deacetylases.
AID1802399Proteros Reporter Displacement Assay from Article 10.1074/jbc.M113.490706: \\Histone deacetylase (HDAC) inhibitor kinetic rate constants correlate with cellular histone acetylation but not transcription and cell viability.\\2013The Journal of biological chemistry, Sep-13, Volume: 288, Issue:37
Histone deacetylase (HDAC) inhibitor kinetic rate constants correlate with cellular histone acetylation but not transcription and cell viability.
AID1799021pfHDAC-1 Enzyme Assay from Article 10.1021/jm801654y: \\Identification and characterization of small molecule inhibitors of a class I histone deacetylase from Plasmodium falciparum.\\2009Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
Identification and characterization of small molecule inhibitors of a class I histone deacetylase from Plasmodium falciparum.
AID1347123qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347126qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347113qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347116qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347129qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347121qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347119qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347115qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID686947qHTS for small molecule inhibitors of Yes1 kinase: Primary Screen2013Bioorganic & medicinal chemistry letters, Aug-01, Volume: 23, Issue:15
Identification of potent Yes1 kinase inhibitors using a library screening approach.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347109qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347118qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347124qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347112qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347125qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347117qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347128qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347114qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347111qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347110qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells)2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347122qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347127qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1346134Human histone deacetylase 1 (3.5.1.- Histone deacetylases (HDACs))2010Nature chemical biology, Mar, Volume: 6, Issue:3
Chemical phylogenetics of histone deacetylases.
AID1346077Human histone deacetylase 3 (3.5.1.- Histone deacetylases (HDACs))2010Nature chemical biology, Mar, Volume: 6, Issue:3
Chemical phylogenetics of histone deacetylases.
AID1346090Human histone deacetylase 9 (3.5.1.- Histone deacetylases (HDACs))2008The Biochemical journal, Jan-15, Volume: 409, Issue:2
Determination of the class and isoform selectivity of small-molecule histone deacetylase inhibitors.
AID1346077Human histone deacetylase 3 (3.5.1.- Histone deacetylases (HDACs))2008The Biochemical journal, Jan-15, Volume: 409, Issue:2
Determination of the class and isoform selectivity of small-molecule histone deacetylase inhibitors.
AID1346082Human histone deacetylase 2 (3.5.1.- Histone deacetylases (HDACs))2010Nature chemical biology, Mar, Volume: 6, Issue:3
Chemical phylogenetics of histone deacetylases.
AID1346134Human histone deacetylase 1 (3.5.1.- Histone deacetylases (HDACs))2008The Biochemical journal, Jan-15, Volume: 409, Issue:2
Determination of the class and isoform selectivity of small-molecule histone deacetylase inhibitors.
AID1346082Human histone deacetylase 2 (3.5.1.- Histone deacetylases (HDACs))2008The Biochemical journal, Jan-15, Volume: 409, Issue:2
Determination of the class and isoform selectivity of small-molecule histone deacetylase inhibitors.
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID385685Inhibition of flag-tagged HDAC4 by pull-down assay2007Proceedings of the National Academy of Sciences of the United States of America, Oct-30, Volume: 104, Issue:44
Unraveling the hidden catalytic activity of vertebrate class IIa histone deacetylases.
AID1548274Antiproliferative activity against bortezomib resistant human KM3/BTZ cells incubated for 48 hrs by MTT assay
AID417069Activation of mouse Wnt3a signaling expressed in HEK293 STF cells assessed as increase in transcriptional activity after 24 hrs by luciferase reporter gene-based lactate dehydrogenase assay2009Bioorganic & medicinal chemistry, Mar-15, Volume: 17, Issue:6
Psammaplin A as a general activator of cell-based signaling assays via HDAC inhibition and studies on some bromotyrosine derivatives.
AID1853065Inhibition of HDAC1-CoREST-LSD1 (unknown origin) using Boc-(Ac)Lys-AMC as substrate preincubated with compound for 1 hrs followed by substrate addition and measured after 1 hrs by fluorescent assay2022RSC medicinal chemistry, Dec-14, Volume: 13, Issue:12
A 'click' chemistry approach to novel entinostat (MS-275) based class I histone deacetylase proteolysis targeting chimeras.
AID1901159Antiproliferative activity against human MDA-MB-231 cells measured after 48 hrs by MTT assay2022Bioorganic & medicinal chemistry, 02-15, Volume: 56Synthesis and biological evaluation of aminobenzamides containing purine moiety as class I histone deacetylases inhibitors.
AID664385Inhibition of SIRT12012European journal of medicinal chemistry, Jul, Volume: 53Appraisal of GABA and PABA as linker: design and synthesis of novel benzamide based histone deacetylase inhibitors.
AID1466057Growth inhibition of human PC3 cells after 48 hrs by sulforhodamine B assay2017European journal of medicinal chemistry, Jul-07, Volume: 1344-Indolyl-N-hydroxyphenylacrylamides as potent HDAC class I and IIB inhibitors in vitro and in vivo.
AID1467233Inhibition of recombinant C-terminal His-tagged HDAC11 (unknown origin) expressed in baculovirus infected Sf9 cells at 5 uM using Ac-Arg-Gly-Lys(Ac)-AMC as substrate pretreated followed by substrate addition after 30 mins by fluorometric method2017Bioorganic & medicinal chemistry letters, 07-01, Volume: 27, Issue:13
Stabilizing HDAC11 with SAHA to assay slow-binding benzamide inhibitors.
AID1541562Inhibition of class 1 HDAC in human Cal27CisR cells assessed as increase in histone H3 acetylation at 1 uM measured after 24 hrs by immunoblot analysis2019Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
Synthesis of Peptoid-Based Class I-Selective Histone Deacetylase Inhibitors with Chemosensitizing Properties.
AID374828Antiproliferative activity against human G401 cells after 72 hrs by celltiter-blue cell viability assay2009Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
Discovery of a potent class I selective ketone histone deacetylase inhibitor with antitumor activity in vivo and optimized pharmacokinetic properties.
AID1732162Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay2021European journal of medicinal chemistry, Apr-05, Volume: 215CAP rigidification of MS-275 and chidamide leads to enhanced antiproliferative effects mediated through HDAC1, 2 and tubulin polymerization inhibition.
AID392619Cytotoxicity against human DU145 cells by MTT assay2009Bioorganic & medicinal chemistry letters, Feb-15, Volume: 19, Issue:4
N-Benzyl-1-heteroaryl-3-(trifluoromethyl)-1H-pyrazole-5-carboxamides as inhibitors of co-activator associated arginine methyltransferase 1 (CARM1).
AID1556404Cytotoxicity against mouse RAW264.7 cells assessed as cell viability at 1 to 5 uM incubated for 24 hrs by MTS assay2019European journal of medicinal chemistry, Sep-01, Volume: 177Inhibitory selectivity among class I HDACs has a major impact on inflammatory gene expression in macrophages.
AID609496Cardiac safety index, Ratio of IC50 for human ERG to IC50 for human HCT116 cells2011Bioorganic & medicinal chemistry letters, Aug-15, Volume: 21, Issue:16
The design, synthesis and structure-activity relationships of novel isoindoline-based histone deacetylase inhibitors.
AID1846961Antiproliferative activity against human YCC-11 cells assessed as inhibition of cell viability
AID374829Antiproliferative activity against human A2780 cells after 72 hrs by celltiter-blue cell viability assay2009Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
Discovery of a potent class I selective ketone histone deacetylase inhibitor with antitumor activity in vivo and optimized pharmacokinetic properties.
AID1596058Cell cycle arrest in human SMMC7721 cells assessed as accumulation at G0/G1 phase at 1 uM incubated for 48 hrs by propidium iodide staining based flow cytometry (Rvb=77%)2019European journal of medicinal chemistry, Jul-01, Volume: 173Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (HDAC) inhibitors.
AID1280296Inhibition of KDAC6 in human K562 cells using [3H]acetylated histone as substrate incubated for 10 mins by liquid scintillation counting method2016Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
Design and Synthesis of Simplified Largazole Analogues as Isoform-Selective Human Lysine Deacetylase Inhibitors.
AID650218Induction of cell cycle arrest in human HCT116 cells assessed as accumulation at G2/M phase at 10 uM after 24 hrs by flow cytometry (Rvb = 9.5 %)2012Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
Anti-tumor activity of new orally bioavailable 2-amino-5-(thiophen-2-yl)benzamide-series histone deacetylase inhibitors, possessing an aqueous soluble functional group as a surface recognition domain.
AID1596055Cell cycle arrest in human SMMC7721 cells assessed as accumulation at G0/G1 phase at 0.25 uM incubated for 48 hrs by propidium iodide staining based flow cytometry (Rvb=77%)2019European journal of medicinal chemistry, Jul-01, Volume: 173Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (HDAC) inhibitors.
AID1454687Drug uptake in iv dosed rat brain after 90 mins by PET imaging method relative to control2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Class I HDAC Inhibitors: Potential New Epigenetic Therapeutics for Alcohol Use Disorder (AUD).
AID1401926Cell cycle arrest in human SMMC7721 cells assessed as accumulation of cells at G0/G1 phase at 4 umol/L after 72 hrs by propidium iodide staining-based flow cytometric analysis (Rvb = 80.65%)2018European journal of medicinal chemistry, Jan-01, Volume: 143Design, synthesis and biological evaluation of novel 2-aminobenzamides containing dithiocarbamate moiety as histone deacetylase inhibitors and potent antitumor agents.
AID1881854Inhibition of HDAC2 (unknown origin)2022European journal of medicinal chemistry, Jan-05, Volume: 227NO-HDAC dual inhibitors.
AID328798Inhibition of HDAC5 expressed in Escherichia coli2008Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8
A novel series of potent and selective ketone histone deacetylase inhibitors with antitumor activity in vivo.
AID488273Inhibition of HDAC12010Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
On the inhibition of histone deacetylase 8.
AID610086Inhibition of HDAC by fluorescence assay2011Bioorganic & medicinal chemistry letters, Aug-15, Volume: 21, Issue:16
Design, synthesis and docking studies on benzamide derivatives as histone deacetylase inhibitors.
AID1548305Induction of cell cycle arrest in bortezomib resistant human KM3/BTZ cells assessed as accumulation at G2/M phase at 100 nM incubated for 24 hrs in presence of bortezomib by propidium iodide staining based flow cytometry (Rvb = 9.1%)
AID1596042Antiproliferative activity against human HCT116 cells assessed as reduction in cell growth at 2 uM incubated for 72 hrs by CCK-8 assay relative to control2019European journal of medicinal chemistry, Jul-01, Volume: 173Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (HDAC) inhibitors.
AID1706071Increase in LPS/IFNgamma-induced IL6 mRNA expression in mouse RAW26.7 cells at 1 uM incubated for 20 hrs followed by LPS/IFNgamma stimulation and measured after 4 hrs by RT-qPCR analysis2020European journal of medicinal chemistry, Dec-15, Volume: 208Induced protein degradation of histone deacetylases 3 (HDAC3) by proteolysis targeting chimera (PROTAC).
AID525024Inhibition of HDAC in human CFBE41o- cell line assessed as increase in CFTR mRNA at 1 uM by RT-PCR2010Nature chemical biology, Jan, Volume: 6, Issue:1
Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis.
AID650211Toxicity in human HCT116 cells xenografted in BALB/c- nu.nu mouse assessed as relative body weight change at 45 mg/kg, po administered every alternate days for 14 days measured up to day 162012Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
Anti-tumor activity of new orally bioavailable 2-amino-5-(thiophen-2-yl)benzamide-series histone deacetylase inhibitors, possessing an aqueous soluble functional group as a surface recognition domain.
AID316899Inhibition of HDAC62008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Histone deacetylase inhibitors: from bench to clinic.
AID538413Selectivity index, ratio of IC50 for recombinant human HDAC1 to IC50 for recombinant human HDAC62010Bioorganic & medicinal chemistry letters, Dec-01, Volume: 20, Issue:23
Inhibitors selective for HDAC6 in enzymes and cells.
AID1873471Inhibition of full length C-terminal His-tagged HDAC1 (unknown origin) assessed as dissociation half-life of EI complex using (Ac-Leu-Gly-Lys(Ac)-AMC as substrate measured every 30 sec for 60 mins by fluorescence based assay2022ACS medicinal chemistry letters, May-12, Volume: 13, Issue:5
Determination of Slow-Binding HDAC Inhibitor Potency and Subclass Selectivity.
AID748114Inhibition of HDAC1 (unknown origin) after 60 mins by fluorescence assay2013Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
Discovery of the first histone deacetylase 6/8 dual inhibitors.
AID1737666Induction of cell cycle arrest in human MDA-MB-231 cells assessed as accumulation of cells at subG1 phase at 16 uM for 48 hrs by PI staining based flow cytometry analysis
AID1676600Binding affinity to zinc ion assessed as accounting ratio by measuring total compound detected/total compound adsorbed at 2.55 umol by immobilized metal-ion affinity chromatography2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors.
AID1401910Induction of apoptosis in human SMMC7721 cells assessed as late apoptotic cells at 0.125 umol/L after 72 hrs by Alexa Fluor 488 Annexin/propidium iodide staining-based flow cytometric analysis (Rvb = 0.29%)2018European journal of medicinal chemistry, Jan-01, Volume: 143Design, synthesis and biological evaluation of novel 2-aminobenzamides containing dithiocarbamate moiety as histone deacetylase inhibitors and potent antitumor agents.
AID1596049Inhibition of human recombinant His-tagged HDAC1 (482 residues) expressed in baculovirus infected insect cells using FLUOR DE LYS SIRT1 as substrate incubated for 10 mins followed by substrate addition and measured after 30 mins by fluorescence method2019European journal of medicinal chemistry, Jul-01, Volume: 173Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (HDAC) inhibitors.
AID1853066Inhibition of HDAC2-CoREST-LSD1 (unknown origin) using Boc-(Ac)Lys-AMC as substrate preincubated with compound for 1 hrs followed by substrate addition and measured after 1 hrs by fluorescent assay2022RSC medicinal chemistry, Dec-14, Volume: 13, Issue:12
A 'click' chemistry approach to novel entinostat (MS-275) based class I histone deacetylase proteolysis targeting chimeras.
AID328807Antiproliferative activity against human A549 cells by CellTiter-Blue cell viability assay2008Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8
A novel series of potent and selective ketone histone deacetylase inhibitors with antitumor activity in vivo.
AID1586083Inhibition of human HDAC8 using RHKAcKAc as substrate by fluorescence assay2019European journal of medicinal chemistry, Jan-15, Volume: 1621-Arylsulfonyl indoline-benzamides as a new antitubulin agents, with inhibition of histone deacetylase.
AID1263144Inhibition of human recombinant HDAC3 using Boc-Lys(Ac)-AMC as substrate after 30 mins by fluorescence assay2015Bioorganic & medicinal chemistry, Dec-15, Volume: 23, Issue:24
Design, synthesis and evaluation of antiestrogen and histone deacetylase inhibitor molecular hybrids.
AID1873427Inhibition of HDAC3 (unknown origin) at 2 uM preincubated for 1 hr followed by 100-fold dilution and subsequent substrate addition measured after 1 hr2022Bioorganic & medicinal chemistry letters, 08-15, Volume: 70Comparison of three zinc binding groups for HDAC inhibitors - A potency, selectivity and enzymatic kinetics study.
AID525011Inhibition of HDAC expressed in hamster BHK cell line assessed as increase in plasma membrane Fdelta508 CFTR protein at 5 uM by immunofluorescence method2010Nature chemical biology, Jan, Volume: 6, Issue:1
Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis.
AID777593Effect on HDAC in human HaCaT cells assessed as upregulation of miR-16-1# at 10 uM after 1 hr by RT-PCR analysis2013ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
Synthesis and Biological Evaluation of the First Example of NO-Donor Histone Deacetylase Inhibitor.
AID1466061Inhibition of recombinant human full length HDAC1 using Fluor-de-Lys as substrate after 60 mins by spectrofluorimetric analysis2017European journal of medicinal chemistry, Jul-07, Volume: 1344-Indolyl-N-hydroxyphenylacrylamides as potent HDAC class I and IIB inhibitors in vitro and in vivo.
AID1401900Antiproliferative activity against human HCT116 cells after 72 hrs by CCK-8 assay2018European journal of medicinal chemistry, Jan-01, Volume: 143Design, synthesis and biological evaluation of novel 2-aminobenzamides containing dithiocarbamate moiety as histone deacetylase inhibitors and potent antitumor agents.
AID414981Antimalarial activity against Plasmodium falciparum 3D7 by [3H]hypoxanthine uptake2009Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
Identification and characterization of small molecule inhibitors of a class I histone deacetylase from Plasmodium falciparum.
AID488363Antitumor activity against human HCT116 cells xenografted in BALB/c nu/nu mouse assessed as reduction of tumor mass at 45 mg/kg, po administered on days 2, 4, 7, 9, 11, 14 and 16 measured on day 18 relative to control2010Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
New orally bioavailable 2-aminobenzamide-type histone deacetylase inhibitor possessing a (2-hydroxyethyl)(4-(thiophen-2-yl)benzyl)amino group.
AID1847014Toxicity in C57BL/6 mouse allografted with mouse B16-F10 cells assessed as body weight loss at 100 mg/kg, ip administered for 14 days
AID664040Growth inhibition of human HCT116 cells after 2 days by MTT assay2012European journal of medicinal chemistry, Jul, Volume: 53Appraisal of GABA and PABA as linker: design and synthesis of novel benzamide based histone deacetylase inhibitors.
AID1235133Cytotoxicity against human HCT116 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay2015European journal of medicinal chemistry, Jul-15, Volume: 100Design, synthesis and antiproliferative activities of novel benzamides derivatives as HDAC inhibitors.
AID1431812Selectivity ratio of IC50 for human KDAC1 to IC50 for human KDAC32017European journal of medicinal chemistry, Feb-15, Volume: 127Design and synthesis of benzodiazepine analogs as isoform-selective human lysine deacetylase inhibitors.
AID622254Inhibition of human HDAC in HeLa cells after 30 mins by Fluor de Lys fluorescence assay2011Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20
The structural requirements of histone deacetylase inhibitors: Suberoylanilide hydroxamic acid analogs modified at the C3 position display isoform selectivity.
AID777572Modulation of mouse C2C12 cell proliferation at 0.1 uM after 72 hrs2013ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
Synthesis and Biological Evaluation of the First Example of NO-Donor Histone Deacetylase Inhibitor.
AID1887685Cytotoxicity against human MGC-803 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay2022European journal of medicinal chemistry, Jan-05, Volume: 227Design, synthesis and biological evaluation of novel o-aminobenzamide derivatives as potential anti-gastric cancer agents in vitro and in vivo.
AID664041Growth inhibition of human U251 cells after 2 days by MTT assay2012European journal of medicinal chemistry, Jul, Volume: 53Appraisal of GABA and PABA as linker: design and synthesis of novel benzamide based histone deacetylase inhibitors.
AID1466381Antiproliferative activity against human HL60 cells after 48 hrs by MTT assay2017European journal of medicinal chemistry, Jul-07, Volume: 134Selective HDAC inhibitors with potent oral activity against leukemia and colorectal cancer: Design, structure-activity relationship and anti-tumor activity study.
AID670717Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay2012Bioorganic & medicinal chemistry, Jul-15, Volume: 20, Issue:14
Synthesis, biological evaluation and molecular docking studies of 3-(1,3-diphenyl-1H-pyrazol-4-yl)-N-phenylacrylamide derivatives as inhibitors of HDAC activity.
AID316887Antiproliferative activity against human MKN45 cells2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Histone deacetylase inhibitors: from bench to clinic.
AID1596057Cell cycle arrest in human SMMC7721 cells assessed as accumulation at G2/M phase at 0.25 uM incubated for 48 hrs by propidium iodide staining based flow cytometry (Rvb=16.17%)2019European journal of medicinal chemistry, Jul-01, Volume: 173Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (HDAC) inhibitors.
AID1676592Binding affinity to Gallium ion assessed as performance ratio ratio by measuring product of accounting ratio and retention ratio at 2.55 umol by immobilized metal-ion affinity chromatography2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors.
AID664380Inhibition of HDAC32012European journal of medicinal chemistry, Jul, Volume: 53Appraisal of GABA and PABA as linker: design and synthesis of novel benzamide based histone deacetylase inhibitors.
AID1596062Cell cycle arrest in human SMMC7721 cells assessed as accumulation at S phase at 4 uM incubated for 48 hrs by propidium iodide staining based flow cytometry (Rvb=6.83%)2019European journal of medicinal chemistry, Jul-01, Volume: 173Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (HDAC) inhibitors.
AID1578491Inhibition of recombinant full length human HDAC10 expressed in baculovirus infected Sf9 cells using FAM-RHKK-Ac as substrate incubated for 17 hrs by electrophoretic mobility shift assay2020ACS medicinal chemistry letters, Jan-09, Volume: 11, Issue:1
Class I/IIb-Selective HDAC Inhibitor Exhibits Oral Bioavailability and Therapeutic Efficacy in Acute Myeloid Leukemia.
AID1596034Inhibition of human recombinant His-tagged HDAC6 expressed in baculovirus infected insect cells using FLUOR DE LYS SIRT1 as substrate preincubated for 10 mins followed by substrate addition and measured after 30 mins by fluorescence method2019European journal of medicinal chemistry, Jul-01, Volume: 173Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (HDAC) inhibitors.
AID1466388Antiproliferative activity against HEL cells after 48 hrs by MTT assay2017European journal of medicinal chemistry, Jul-07, Volume: 134Selective HDAC inhibitors with potent oral activity against leukemia and colorectal cancer: Design, structure-activity relationship and anti-tumor activity study.
AID1401917Induction of apoptosis in human SMMC7721 cells assessed as early apoptotic cells at 4 umol/L after 72 hrs by Alexa Fluor 488 Annexin/propidium iodide staining-based flow cytometric analysis (Rvb = 0.09%)2018European journal of medicinal chemistry, Jan-01, Volume: 143Design, synthesis and biological evaluation of novel 2-aminobenzamides containing dithiocarbamate moiety as histone deacetylase inhibitors and potent antitumor agents.
AID1676590Binding affinity to Nickel cation assessed as retention ratio by measuring compound detected in elution fraction/total compound detected at 2.55 umol by immobilized metal-ion affinity chromatography2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors.
AID1901175Inhibition of HDAC1/HDAC2/HDAC3 in human HCT-116 cells assessed as increase in accumulation of acetylated H3K9 at 5 uM preincubated for 6 hrs followed by compound washout and measured up to 48 hrs by Western blot analysis2022Bioorganic & medicinal chemistry, 02-15, Volume: 56Synthesis and biological evaluation of aminobenzamides containing purine moiety as class I histone deacetylases inhibitors.
AID1864219Binding affinity to 5' FAM-labeled c-myc G4-quadruplex DNA Pu22 (unknown origin) at 50 uM by fluorescence quench assay2022Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
Discovery of a Novel G-Quadruplex and Histone Deacetylase (HDAC) Dual-Targeting Agent for the Treatment of Triple-Negative Breast Cancer.
AID519591Selectivity index, ratio of IC50 for human WI38 cells to IC50 for chloroquine-resistant Plasmodium falciparum Dd22008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Potent antimalarial activity of histone deacetylase inhibitor analogues.
AID1864216Inhibition of HDAC in human HeLa nuclear extract incubated for 30 mins by fluorescence-based Glo-luminescence assay2022Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
Discovery of a Novel G-Quadruplex and Histone Deacetylase (HDAC) Dual-Targeting Agent for the Treatment of Triple-Negative Breast Cancer.
AID777594Effect on HDAC in human HaCaT cells assessed as downregulation of miR-589 at 10 uM after 1 hr by RT-PCR analysis2013ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
Synthesis and Biological Evaluation of the First Example of NO-Donor Histone Deacetylase Inhibitor.
AID613341Inhibition of human ERG by automated Q-patch assay2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Optimization of the in vitro cardiac safety of hydroxamate-based histone deacetylase inhibitors.
AID1431821Selectivity ratio of IC50 for human KDAC6 to IC50 for human KDAC82017European journal of medicinal chemistry, Feb-15, Volume: 127Design and synthesis of benzodiazepine analogs as isoform-selective human lysine deacetylase inhibitors.
AID1917926Inhibition of HDAC1 (unknown origin)2022Bioorganic & medicinal chemistry letters, 11-15, Volume: 76Zinc-dependent deacetylases (HDACs) as potential targets for treating Alzheimer's disease.
AID1401901Inhibition of HDAC in human HeLa cell extract using Fluor de Lys-Green as substrate preincubated for 5 mins followed by substrate addition and measured after 1 hr by fluorescence assay2018European journal of medicinal chemistry, Jan-01, Volume: 143Design, synthesis and biological evaluation of novel 2-aminobenzamides containing dithiocarbamate moiety as histone deacetylase inhibitors and potent antitumor agents.
AID1401923Cell cycle arrest in human SMMC7721 cells assessed as accumulation of cells at G0/G1 phase at 1 umol/L after 72 hrs by propidium iodide staining-based flow cytometric analysis (Rvb = 80.65%)2018European journal of medicinal chemistry, Jan-01, Volume: 143Design, synthesis and biological evaluation of novel 2-aminobenzamides containing dithiocarbamate moiety as histone deacetylase inhibitors and potent antitumor agents.
AID360095Inhibition of TNF-alpha-induced tissue factor activity in HUVEC preincubated for 4 hrs assessed after 4 hrs of TNFalpha challenge by one stage clotting assay2007The Journal of biological chemistry, Sep-28, Volume: 282, Issue:39
Histone deacetylase inhibitors suppress TF-kappaB-dependent agonist-driven tissue factor expression in endothelial cells and monocytes.
AID1915581Cytotoxicity against human DU-145 cells2021European journal of medicinal chemistry, Jan-01, Volume: 209Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors.
AID1380964Inhibition of HDAC1/HDAC2/HDAC3 in human HeLa cells assessed as increase in intracellular acetyl-histone H4 levels at 1 uM after 6 hrs by Western blot analysis2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Discovery of Novel Pazopanib-Based HDAC and VEGFR Dual Inhibitors Targeting Cancer Epigenetics and Angiogenesis Simultaneously.
AID1873439Inhibition of full length C-terminal His-tagged HDAC1 (unknown origin) assessed as inhibition constant (Ki) using (Ac-Leu-Gly-Lys(Ac)-AMC as substrate measured every 30 sec for 60 mins by fluorescence based assay2022ACS medicinal chemistry letters, May-12, Volume: 13, Issue:5
Determination of Slow-Binding HDAC Inhibitor Potency and Subclass Selectivity.
AID1847021Toxicity in C57BL/6 mouse allografted with mouse B16-F10 cells assessed as morphological abnormalities in liver at 5 mg/kg, ip administered for 14 days in presence of (2-phenylthiazol-4-yl)(3,4,5-trimethoxyphenyl)methanone by H and E staining based analys
AID1424833Induction of apoptosis in human MV4-11 cells at 5 uM after 24 to 48 hrs by Annexin V-PI staining based flow cytometry2018European journal of medicinal chemistry, May-25, Volume: 152Design and biological evaluation of tetrahydro-β-carboline derivatives as highly potent histone deacetylase 6 (HDAC6) inhibitors.
AID1293874Inhibition of HDAC in human HeLa nuclear extract using fluor de lys as substrate after 10 to 15 mins by spectrofluorometry2016Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
Identification of new quinic acid derivatives as histone deacetylase inhibitors by fluorescence-based cellular assay.
AID316892Inhibition of HDAC12008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Histone deacetylase inhibitors: from bench to clinic.
AID328794Inhibition of HDAC22008Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8
A novel series of potent and selective ketone histone deacetylase inhibitors with antitumor activity in vivo.
AID420329Inhibition of HDAC from RT extract2009Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
Non-isotopic dual parameter competition assay suitable for high-throughput screening of histone deacetylases.
AID1727731Inhibition of His-tagged BRD4 bromodomain 1 (unknown origin) using [Lys (5,8,12,16) Ac] H4(1-21) as substrate by fluorescence based assay2021European journal of medicinal chemistry, Jan-01, Volume: 209Discovery of selective HDAC/BRD4 dual inhibitors as epigenetic probes.
AID708276Growth inhibition of human Bel7404 cells incubated for 72 hrs by WST dye reduction assay2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Pharmacokinetic optimization of class-selective histone deacetylase inhibitors and identification of associated candidate predictive biomarkers of hepatocellular carcinoma tumor response.
AID1308513Inhibition of recombinant HDAC1 (unknown origin) using of Fluor-de-Lys substrate incubated for 10 mins by fluorimetric assay2016Bioorganic & medicinal chemistry letters, 06-15, Volume: 26, Issue:12
Targeting epigenetic reader and eraser: Rational design, synthesis and in vitro evaluation of dimethylisoxazoles derivatives as BRD4/HDAC dual inhibitors.
AID1737645Inhibition of human recombinant HDAC2 expressed in baculovirus using fluorogenic peptide p53 residues 379-382 (RHKK(Ac)AMC) as substrate by Fluorescence analysis
AID1401892Antiproliferative activity against human A375 cells at 8 uM after 72 hrs by CCK-8 assay relative to control2018European journal of medicinal chemistry, Jan-01, Volume: 143Design, synthesis and biological evaluation of novel 2-aminobenzamides containing dithiocarbamate moiety as histone deacetylase inhibitors and potent antitumor agents.
AID1453362Inhibition of class 2 HDAC in HEL cells using Boc-Lys (triflouroacetyl)-AMC as substrate preincubated for 3 hrs followed by substrate addition measured after 3 hrs by fluorescence assay2017Bioorganic & medicinal chemistry, 06-15, Volume: 25, Issue:12
Design, synthesis and anti-tumor activity study of novel histone deacetylase inhibitors containing isatin-based caps and o-phenylenediamine-based zinc binding groups.
AID201624Compound was tested for antiproliferative activity against human SK-BR-3 cancer cell lines2003Journal of medicinal chemistry, Dec-18, Volume: 46, Issue:26
Synthesis and biological evaluation of 3-(4-substituted-phenyl)-N-hydroxy-2-propenamides, a new class of histone deacetylase inhibitors.
AID1431818Selectivity ratio of IC50 for human KDAC8 to IC50 for human KDAC32017European journal of medicinal chemistry, Feb-15, Volume: 127Design and synthesis of benzodiazepine analogs as isoform-selective human lysine deacetylase inhibitors.
AID1467234Inhibition of recombinant C-terminal His-tagged HDAC11 (unknown origin) expressed in baculovirus infected Sf9 cells using Ac-Arg-Gly-Lys(Ac)-AMC as substrate pretreated for 3 hrs followed by substrate addition after 30 mins by fluorometric method2017Bioorganic & medicinal chemistry letters, 07-01, Volume: 27, Issue:13
Stabilizing HDAC11 with SAHA to assay slow-binding benzamide inhibitors.
AID525020Inhibition of HDAC in human CFBE41o- cell line assessed as total CFTR protein level including CFTR glycoform at 1 uM by immunoblot analysis2010Nature chemical biology, Jan, Volume: 6, Issue:1
Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis.
AID1453364Inhibition of HDAC2 (unknown origin) using Boc-Lys (acetyl)-AMC as substrate preincubated for 1 hr followed by substrate addition measured after 1 hr by fluorescence assay2017Bioorganic & medicinal chemistry, 06-15, Volume: 25, Issue:12
Design, synthesis and anti-tumor activity study of novel histone deacetylase inhibitors containing isatin-based caps and o-phenylenediamine-based zinc binding groups.
AID524998Inhibition of HDAC5 by in vitro deacetylation assay2010Nature chemical biology, Jan, Volume: 6, Issue:1
Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis.
AID1706072Increase in LPS/IFNgamma-induced TNFalpha mRNA expression in mouse RAW26.7 cells at 1 uM incubated for 20 hrs followed by LPS/IFNgamma stimulation and measured after 4 hrs by RT-qPCR analysis2020European journal of medicinal chemistry, Dec-15, Volume: 208Induced protein degradation of histone deacetylases 3 (HDAC3) by proteolysis targeting chimera (PROTAC).
AID613298In vitro cardiac safety index, ratio of IC50 for human ERG to IC50 for human HCT116 cells2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Optimization of the in vitro cardiac safety of hydroxamate-based histone deacetylase inhibitors.
AID519593Selectivity index, ratio of IC50 for human WI38 cells to IC50 for chloroquine-sensitive Plasmodium falciparum 3D72008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Potent antimalarial activity of histone deacetylase inhibitor analogues.
AID329915Inhibition of human HDAC4 in U937 cells by immunoprecipitation assay2008Bioorganic & medicinal chemistry letters, Apr-15, Volume: 18, Issue:8
Novel uracil-based 2-aminoanilide and 2-aminoanilide-like derivatives: histone deacetylase inhibition and in-cell activities.
AID1401897Antiproliferative activity against human HeLa cells after 72 hrs by CCK-8 assay2018European journal of medicinal chemistry, Jan-01, Volume: 143Design, synthesis and biological evaluation of novel 2-aminobenzamides containing dithiocarbamate moiety as histone deacetylase inhibitors and potent antitumor agents.
AID1586067Growth inhibition of human KB cells after 48 hrs by SRB assay2019European journal of medicinal chemistry, Jan-15, Volume: 1621-Arylsulfonyl indoline-benzamides as a new antitubulin agents, with inhibition of histone deacetylase.
AID1466395Antitumor activity against human U937 cells xenografted in BALB/c nude mouse assessed as tumor growth inhibition at 50 mg/kg/day administered via oral gavage for 13 days measured every 3 days2017European journal of medicinal chemistry, Jul-07, Volume: 134Selective HDAC inhibitors with potent oral activity against leukemia and colorectal cancer: Design, structure-activity relationship and anti-tumor activity study.
AID1732172Induction of cell cycle arrest in human MDA-MB-231 cells assessed as sub-G1 phase at 8 uM incubated for 72 hrs by PI staining based flow cytometry analysis (Rvb = 0.8 %)2021European journal of medicinal chemistry, Apr-05, Volume: 215CAP rigidification of MS-275 and chidamide leads to enhanced antiproliferative effects mediated through HDAC1, 2 and tubulin polymerization inhibition.
AID1380944Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Discovery of Novel Pazopanib-Based HDAC and VEGFR Dual Inhibitors Targeting Cancer Epigenetics and Angiogenesis Simultaneously.
AID374821Inhibition of wild type His-tagged HDAC7 catalytic domain T515-L952 expressed in Escherichia coli2009Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
Discovery of a potent class I selective ketone histone deacetylase inhibitor with antitumor activity in vivo and optimized pharmacokinetic properties.
AID316925Inhibition of human HepG2 cells2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Histone deacetylase inhibitors: from bench to clinic.
AID1454688Half life in human at 6 mg/m2, po2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Class I HDAC Inhibitors: Potential New Epigenetic Therapeutics for Alcohol Use Disorder (AUD).
AID1740019Inhibition of recombinant human HDAC6 using pan-HDAC substrate incubated for 3 hrs by fluorescence method2020Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
Thirty Years of HDAC Inhibitors: 2020 Insight and Hindsight.
AID1431815Selectivity ratio of IC50 for human KDAC1 to IC50 for human KDAC82017European journal of medicinal chemistry, Feb-15, Volume: 127Design and synthesis of benzodiazepine analogs as isoform-selective human lysine deacetylase inhibitors.
AID1596039Antiproliferative activity against human A549 cells assessed as reduction in cell growth at 8 uM incubated for 72 hrs by CCK-8 assay relative to control2019European journal of medicinal chemistry, Jul-01, Volume: 173Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (HDAC) inhibitors.
AID1676593Binding affinity to Gallium ion assessed as retention ratio by measuring compound detected in elution fraction/total compound detected at 2.55 umol by immobilized metal-ion affinity chromatography2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors.
AID328808Antiproliferative activity against human G401 cells by CellTiter-Blue cell viability assay2008Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8
A novel series of potent and selective ketone histone deacetylase inhibitors with antitumor activity in vivo.
AID1467242Inhibition of recombinant C-terminal His-tagged HDAC11 (unknown origin) expressed in baculovirus infected Sf9 cells at 2 uM using Ac-Arg-Gly-Lys(Ac)-AMC as substrate pretreated for 3 hrs followed by substrate addition after 30 mins by fluorometric method 2017Bioorganic & medicinal chemistry letters, 07-01, Volume: 27, Issue:13
Stabilizing HDAC11 with SAHA to assay slow-binding benzamide inhibitors.
AID374820Inhibition of C-terminal FLAG-tagged HDAC6 expressed in mammalian cells2009Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
Discovery of a potent class I selective ketone histone deacetylase inhibitor with antitumor activity in vivo and optimized pharmacokinetic properties.
AID1203895Antiproliferative activity against human U937 cells assessed as inhibition of cell growth after 72 hrs by MTT-based assay2015European journal of medicinal chemistry, , Volume: 96Discovery and preliminary evaluation of 2-aminobenzamide and hydroxamate derivatives containing 1,2,4-oxadiazole moiety as potent histone deacetylase inhibitors.
AID364648Inhibition of human recombinant HDAC by fluorimetric assay2008Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17
Design, synthesis and biological evaluation of novel compounds with conjugated structure as anti-tumor agents.
AID1401903Inhibition of human recombinant HDAC2 using Fluor de Lys-Green as substrate preincubated for 5 mins followed by substrate addition and measured after 1 hr by fluorescence assay2018European journal of medicinal chemistry, Jan-01, Volume: 143Design, synthesis and biological evaluation of novel 2-aminobenzamides containing dithiocarbamate moiety as histone deacetylase inhibitors and potent antitumor agents.
AID1548735Inhibition of recombinant human N-terminal GST-tagged HDAC7 (518 to end residues) expressed in baculovirus infected Sf9 cells using Boc-Lys (trifluoroacetyl)-AMC as substrate preincubated for 1 hr followed by substrate addition and measured after 2 hrs by2020Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
Design of Hydrazide-Bearing HDACIs Based on Panobinostat and Their p53 and FLT3-ITD Dependency in Antileukemia Activity.
AID1474454Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay2017European journal of medicinal chemistry, May-26, Volume: 132Design, synthesis and biological evaluation of novel coumarin-based benzamides as potent histone deacetylase inhibitors and anticancer agents.
AID1548293Induction of apoptosis in bortezomib resistant human KM3/BTZ cells assessed as early apoptotic cells level at 50 nM incubated for 24 hrs in presence of bortezomib by Annexin V-FITC/PI staining based FCAS analysis (Rvb = 1.39%)
AID1474462Cytotoxicity against HUVEC after 48 hrs by MTT assay2017European journal of medicinal chemistry, May-26, Volume: 132Design, synthesis and biological evaluation of novel coumarin-based benzamides as potent histone deacetylase inhibitors and anticancer agents.
AID488366Cell cycle arrest in human HCT116 cells assessed as accumulation at subG1 phase at 10 uM after 48 hrs by flow cytometry analysis2010Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
New orally bioavailable 2-aminobenzamide-type histone deacetylase inhibitor possessing a (2-hydroxyethyl)(4-(thiophen-2-yl)benzyl)amino group.
AID488368Cell cycle arrest in human HCT116 cells assessed as accumulation at G0/G1 phase at 10 uM after 48 hrs by flow cytometry analysis2010Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
New orally bioavailable 2-aminobenzamide-type histone deacetylase inhibitor possessing a (2-hydroxyethyl)(4-(thiophen-2-yl)benzyl)amino group.
AID1231814Antiproliferative activity against human U937 cells incubated for 72 hrs by MTT assay2015Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13
Discovery, bioactivity and docking simulation of Vorinostat analogues containing 1,2,4-oxadiazole moiety as potent histone deacetylase inhibitors and antitumor agents.
AID1466380Inhibition of class 1 HDAC in human HL60 cells using Boc-Ac-Lys-AMC as substrate incubated for 3 hrs followed by substrate addition measured after 3 hrs by fluorescence assay2017European journal of medicinal chemistry, Jul-07, Volume: 134Selective HDAC inhibitors with potent oral activity against leukemia and colorectal cancer: Design, structure-activity relationship and anti-tumor activity study.
AID324948Inhibition of HDAC1 in HEK293 cells2008Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6
Probing the elusive catalytic activity of vertebrate class IIa histone deacetylases.
AID1548284Induction of apoptosis in bortezomib resistant human KM3/BTZ cells assessed as viable cells level at 50 nM incubated for 24 hrs by Annexin V-FITC/PI staining based FCAS analysis (Rvb = 98.1%)
AID1401912Induction of apoptosis in human SMMC7721 cells assessed as viable cells at 1 umol/L after 72 hrs by Alexa Fluor 488 Annexin/propidium iodide staining-based flow cytometric analysis (Rvb = 97.14%)2018European journal of medicinal chemistry, Jan-01, Volume: 143Design, synthesis and biological evaluation of novel 2-aminobenzamides containing dithiocarbamate moiety as histone deacetylase inhibitors and potent antitumor agents.
AID1548734Inhibition of recombinant human HDAC5 using Boc-Lys (trifluoroacetyl)-AMC as substrate preincubated for 1 hr followed by substrate addition and measured after 2 hrs by fluorescence based micro plate reader analysis2020Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
Design of Hydrazide-Bearing HDACIs Based on Panobinostat and Their p53 and FLT3-ITD Dependency in Antileukemia Activity.
AID1380952Inhibition of HDAC1 (unknown origin) using fluorogenic substrate preincubated for 5 mins followed by substrate addition measured after 30 mins by fluorescence-based assay2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Discovery of Novel Pazopanib-Based HDAC and VEGFR Dual Inhibitors Targeting Cancer Epigenetics and Angiogenesis Simultaneously.
AID1474456Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay2017European journal of medicinal chemistry, May-26, Volume: 132Design, synthesis and biological evaluation of novel coumarin-based benzamides as potent histone deacetylase inhibitors and anticancer agents.
AID329916Induction of histone H4 hyperacetylation in human U937 cells2008Bioorganic & medicinal chemistry letters, Apr-15, Volume: 18, Issue:8
Novel uracil-based 2-aminoanilide and 2-aminoanilide-like derivatives: histone deacetylase inhibition and in-cell activities.
AID1732201Induction of cell cycle arrest in human MDA-MB-231 cells assessed as increase in accumulation of G1 phase at 4 uM incubated for 24 hrs by PI staining based flow cytometry analysis2021European journal of medicinal chemistry, Apr-05, Volume: 215CAP rigidification of MS-275 and chidamide leads to enhanced antiproliferative effects mediated through HDAC1, 2 and tubulin polymerization inhibition.
AID1466064Inhibition of recombinant human full length HDAC8 using Fluor-de-Lys as substrate after 60 mins by spectrofluorimetric analysis2017European journal of medicinal chemistry, Jul-07, Volume: 1344-Indolyl-N-hydroxyphenylacrylamides as potent HDAC class I and IIB inhibitors in vitro and in vivo.
AID1189850Cytotoxicity against human HuH7 cells assessed as inhibition of cell viability after 3 days by CellTiter 96 assay2015Journal of medicinal chemistry, Jan-22, Volume: 58, Issue:2
Hydroxamic acids block replication of hepatitis C virus.
AID1901163Antiproliferative activity against human K562 cells measured after 48 hrs by MTT assay2022Bioorganic & medicinal chemistry, 02-15, Volume: 56Synthesis and biological evaluation of aminobenzamides containing purine moiety as class I histone deacetylases inhibitors.
AID1846955Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell viability measured for 48 hrs by microplate reader based MTT assay
AID1441699Inhibition of recombinant human LTA4H aminopeptidase activity expressed in Escherichia coli BL21 (DE3) pLysS assessed as formation of p-NA from Ala-p-NA at 10 uM preincubated for 10 mins followed by substrate addition measured after 10 mins2017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Drug Repurposing of Histone Deacetylase Inhibitors That Alleviate Neutrophilic Inflammation in Acute Lung Injury and Idiopathic Pulmonary Fibrosis via Inhibiting Leukotriene A4 Hydrolase and Blocking LTB4 Biosynthesis.
AID374818Inhibition of human C-terminal FLAG-tagged HDAC3 in HEK293 cells2009Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
Discovery of a potent class I selective ketone histone deacetylase inhibitor with antitumor activity in vivo and optimized pharmacokinetic properties.
AID1541441Inhibition of human full length N-terminal GST-tagged HDAC6 expressed in baculovirus infected Sf9 insect cells at 10 uM ZMAL as substrate incubated for 90 mins by fluorescence assay relative to control2019Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
Synthesis of Peptoid-Based Class I-Selective Histone Deacetylase Inhibitors with Chemosensitizing Properties.
AID316896Inhibition of human HDAC12008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Histone deacetylase inhibitors: from bench to clinic.
AID1401902Inhibition of human recombinant HDAC1 using Fluor de Lys-Green as substrate preincubated for 5 mins followed by substrate addition and measured after 1 hr by fluorescence assay2018European journal of medicinal chemistry, Jan-01, Volume: 143Design, synthesis and biological evaluation of novel 2-aminobenzamides containing dithiocarbamate moiety as histone deacetylase inhibitors and potent antitumor agents.
AID492802Inhibition of human recombinant HDAC4 at 5 uM after 15 mins by fluorimetric assay2010Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12
Synthesis and biological characterization of the histone deacetylase inhibitor largazole and C7- modified analogues.
AID1876491Antiproliferative activity against human U-251 cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay2022European journal of medicinal chemistry, Jan-05, Volume: 227Novel piperazine based benzamide derivatives as potential anti-glioblastoma agents inhibiting cell proliferation and cell cycle progression.
AID664039Inhibition of HDAC1 using Fluor de Lys as substrate by fluorescence analysis2012European journal of medicinal chemistry, Jul, Volume: 53Appraisal of GABA and PABA as linker: design and synthesis of novel benzamide based histone deacetylase inhibitors.
AID777606Induction of NO release in human HaCaT cells at 10 uM after 1 to 5 hrs by DAF-2D-based FACS analysis relative to DMSO-treated control2013ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
Synthesis and Biological Evaluation of the First Example of NO-Donor Histone Deacetylase Inhibitor.
AID1888470Antiproliferative activity against human LNCAP cells assessed as reduction in cell viability at 100 uM incubated for 5 days2022Bioorganic & medicinal chemistry letters, 01-01, Volume: 55Dual-function antiandrogen/HDACi hybrids based on enzalutamide and entinostat.
AID421212Inhibition of HDAC from human HeLa cells assessed as of histone H3 acetylation2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Recent advances in the development of polyamine analogues as antitumor agents.
AID50586Inhibitory concentration against colon HCT116 cell line2003Journal of medicinal chemistry, Feb-27, Volume: 46, Issue:5
Development of potential antitumor agents. Synthesis and biological evaluation of a new set of sulfonamide derivatives as histone deacetylase inhibitors.
AID1181316Induction of granulocytic differentiation in human U937 cells assessed as increase in CD11c expression at 5 uM after 48 hrs by FACS method2014Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
1,3,4-Oxadiazole-containing histone deacetylase inhibitors: anticancer activities in cancer cells.
AID1453363Inhibition of HDAC1 (unknown origin) using Boc-Lys (acetyl)-AMC as substrate preincubated for 1 hr followed by substrate addition measured after 1 hr by fluorescence assay2017Bioorganic & medicinal chemistry, 06-15, Volume: 25, Issue:12
Design, synthesis and anti-tumor activity study of novel histone deacetylase inhibitors containing isatin-based caps and o-phenylenediamine-based zinc binding groups.
AID670718Antiproliferative activity against human A549 cells after 48 hrs by MTT assay2012Bioorganic & medicinal chemistry, Jul-15, Volume: 20, Issue:14
Synthesis, biological evaluation and molecular docking studies of 3-(1,3-diphenyl-1H-pyrazol-4-yl)-N-phenylacrylamide derivatives as inhibitors of HDAC activity.
AID1873449Inhibition of full length C-terminal His-tagged HDAC3 (unknown origin)/N-terminal GST-tagged NCoR2 (unknown origin) assessed as apparent inhibition constant using (Ac-Leu-Gly-Lys(Ac)-AMC as substrate preincubated with enzyme for 0.5 to 2 hrs followed by s2022ACS medicinal chemistry letters, May-12, Volume: 13, Issue:5
Determination of Slow-Binding HDAC Inhibitor Potency and Subclass Selectivity.
AID364642Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay2008Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17
Design, synthesis and biological evaluation of novel compounds with conjugated structure as anti-tumor agents.
AID525035Inhibition of CFTR transcription assessed as decrease of CFTR protein level at 50 uM by immunoblot method2010Nature chemical biology, Jan, Volume: 6, Issue:1
Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis.
AID488276Inhibition of HDAC62010Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
On the inhibition of histone deacetylase 8.
AID1873440Inhibition of full length C-terminal His-tagged HDAC3 (unknown origin)/N-terminal GST-tagged NCoR2 (unknown origin) assessed as equilibrium inhibition constant (Ki,1) using (Ac-Leu-Gly-Lys(Ac)-AMC as substrate measured every 30 sec for 60 mins by fluoresc2022ACS medicinal chemistry letters, May-12, Volume: 13, Issue:5
Determination of Slow-Binding HDAC Inhibitor Potency and Subclass Selectivity.
AID1676588Binding affinity to Zinc ion assessed as performance ratio ratio by measuring product of accounting ratio and retention ratio at 2.55 umol by immobilized metal-ion affinity chromatography2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors.
AID316936Inhibition of HDAC72008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Histone deacetylase inhibitors: from bench to clinic.
AID519583Antimalarial activity against chloroquine-resistant Plasmodium falciparum Dd2 infected in O+ human erythrocytes by [3H]hypoxanthine incorporation assay2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Potent antimalarial activity of histone deacetylase inhibitor analogues.
AID1887684Cytotoxicity against human BGC-823 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay2022European journal of medicinal chemistry, Jan-05, Volume: 227Design, synthesis and biological evaluation of novel o-aminobenzamide derivatives as potential anti-gastric cancer agents in vitro and in vivo.
AID1263145Inhibition of human recombinant HDAC6 using Boc-Lys(Ac)-AMC as substrate after 30 mins by fluorescence assay2015Bioorganic & medicinal chemistry, Dec-15, Volume: 23, Issue:24
Design, synthesis and evaluation of antiestrogen and histone deacetylase inhibitor molecular hybrids.
AID1466062Inhibition of recombinant human full length HDAC4 using Fluor-de-Lys as substrate after 60 mins by spectrofluorimetric analysis2017European journal of medicinal chemistry, Jul-07, Volume: 1344-Indolyl-N-hydroxyphenylacrylamides as potent HDAC class I and IIB inhibitors in vitro and in vivo.
AID1737641Antiproliferative activity against human HepG2 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
AID519592Selectivity index, ratio of IC50 for breast fibroblasts to IC50 for chloroquine-resistant Plasmodium falciparum Dd22008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Potent antimalarial activity of histone deacetylase inhibitor analogues.
AID1556408Inhibition of HDAC1/2 in LPS/IFNgamma-stimulated mouse RAW264.7 cells assessed as upregulation of iNOS gene expression at 1 uM pretreated for 16 hrs followed by LPS stimulation and measured after 4 hrs by RT-qPCR analysis2019European journal of medicinal chemistry, Sep-01, Volume: 177Inhibitory selectivity among class I HDACs has a major impact on inflammatory gene expression in macrophages.
AID1548728Inhibition of recombinant human C-terminal GST/His-tagged HDAC3 (1 to 428 residues) co-expressed with human N-terminal GST-tagged NCOR2 (395 to 489 residues) in baculovirus infected Sf9 cells using Boc-Lys(acetyl)-AMC as substrate preincubated for 1 hr fo2020Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
Design of Hydrazide-Bearing HDACIs Based on Panobinostat and Their p53 and FLT3-ITD Dependency in Antileukemia Activity.
AID1466063Inhibition of recombinant human full length HDAC6 using Fluor-de-Lys as substrate after 60 mins by spectrofluorimetric analysis2017European journal of medicinal chemistry, Jul-07, Volume: 1344-Indolyl-N-hydroxyphenylacrylamides as potent HDAC class I and IIB inhibitors in vitro and in vivo.
AID1879900Inhibition of HDAC1 in human MV4-11 cells assessed as accumulation of acetylated histone H3 at 5 uM measured by immunoblotting method2022European journal of medicinal chemistry, Apr-15, Volume: 234Identification of histone deacetylase 10 (HDAC10) inhibitors that modulate autophagy in transformed cells.
AID1732165Inhibition of HDAC3 (unknown origin) using fluorogenic-(RHKKAc) as substrate by fluorescence assay2021European journal of medicinal chemistry, Apr-05, Volume: 215CAP rigidification of MS-275 and chidamide leads to enhanced antiproliferative effects mediated through HDAC1, 2 and tubulin polymerization inhibition.
AID1453359Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay2017Bioorganic & medicinal chemistry, 06-15, Volume: 25, Issue:12
Design, synthesis and anti-tumor activity study of novel histone deacetylase inhibitors containing isatin-based caps and o-phenylenediamine-based zinc binding groups.
AID650229Inhibition of HDAC12012Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
Anti-tumor activity of new orally bioavailable 2-amino-5-(thiophen-2-yl)benzamide-series histone deacetylase inhibitors, possessing an aqueous soluble functional group as a surface recognition domain.
AID1846954Inhibition of recombinant HDAC3 (unknown origin) at 1 uM relative to control
AID374830Antiproliferative activity against human MCF7 cells after 72 hrs by celltiter-blue cell viability assay2009Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
Discovery of a potent class I selective ketone histone deacetylase inhibitor with antitumor activity in vivo and optimized pharmacokinetic properties.
AID1453366Selectivity ratio of IC50 for HDAC2 (unknown origin) to IC50 for HDAC1 (unknown origin)2017Bioorganic & medicinal chemistry, 06-15, Volume: 25, Issue:12
Design, synthesis and anti-tumor activity study of novel histone deacetylase inhibitors containing isatin-based caps and o-phenylenediamine-based zinc binding groups.
AID524999Inhibition of HDAC6 by in vitro deacetylation assay2010Nature chemical biology, Jan, Volume: 6, Issue:1
Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis.
AID1676597Binding affinity to cupric ion assessed as performance ratio ratio by measuring product of accounting ratio and retention ratio at 2.55 umol by immobilized metal-ion affinity chromatography2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors.
AID488360Antitumor activity against human HCT116 cells xenografted in BALB/c nu/nu mouse assessed as reduction of tumor growth at 45 mg/kg, po administered on days 2, 4, 7, 9, 11, 14 and 162010Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
New orally bioavailable 2-aminobenzamide-type histone deacetylase inhibitor possessing a (2-hydroxyethyl)(4-(thiophen-2-yl)benzyl)amino group.
AID1873444Inhibition of full length C-terminal FLAG-tagged HDAC2 (unknown origin) assessed as rate constant (k-2) of EI complex using (Ac-Leu-Gly-Lys(Ac)-AMC as substrate measured every 30 sec for 60 mins by fluorescence based assay2022ACS medicinal chemistry letters, May-12, Volume: 13, Issue:5
Determination of Slow-Binding HDAC Inhibitor Potency and Subclass Selectivity.
AID1548302Induction of cell cycle arrest in bortezomib resistant human KM3/BTZ cells assessed as accumulation at G2/M phase at 100 nM incubated for 24 hrs by propidium iodide staining based flow cytometry (Rvb = 9.1%)
AID1467243Inhibition of recombinant C-terminal His-tagged HDAC11 (unknown origin) expressed in baculovirus infected Sf9 cells at 2 uM using Ac-Arg-Gly-Lys(Ac)-AMC as substrate pretreated for 3 hrs followed by substrate addition after 30 mins in presence of 0.2 uM S2017Bioorganic & medicinal chemistry letters, 07-01, Volume: 27, Issue:13
Stabilizing HDAC11 with SAHA to assay slow-binding benzamide inhibitors.
AID313730Inhibition of HDAC22008Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2
Optimization of biaryl Selective HDAC1&2 Inhibitors (SHI-1:2).
AID1846980Selectivity index, ratio of IC50 for Inhibition of full length N-terminal GST-tagged human recombinant HDAC7 (501 to 952 residues) expressed in Baculovirus system using Ac-Leu-Gly-Lys (Ac)-AMC as substrate to IC50 for inhibition of full length recombinant
AID1401906Selectivity ratio of IC50 for human recombinant HDAC2 to IC50 for human recombinant HDAC62018European journal of medicinal chemistry, Jan-01, Volume: 143Design, synthesis and biological evaluation of novel 2-aminobenzamides containing dithiocarbamate moiety as histone deacetylase inhibitors and potent antitumor agents.
AID1876490Antiproliferative activity against human U-87 MG cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay2022European journal of medicinal chemistry, Jan-05, Volume: 227Novel piperazine based benzamide derivatives as potential anti-glioblastoma agents inhibiting cell proliferation and cell cycle progression.
AID717813Inhibition of HDAC in human Hela cell lysate using Fluor-de-Lys as substrate assessed as remaining activity at 7.81 x 10'-6 M pretreated for 30 mins before substrate addition by fluorescence assay2012Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23
The structural requirements of histone deacetylase inhibitors: suberoylanilide hydroxamic acid analogs modified at the C6 position.
AID102521Inhibitory concentration against lung H446 cell line2003Journal of medicinal chemistry, Feb-27, Volume: 46, Issue:5
Development of potential antitumor agents. Synthesis and biological evaluation of a new set of sulfonamide derivatives as histone deacetylase inhibitors.
AID488369Cell cycle arrest in human HCT116 cells assessed as accumulation at S phase at 10 uM after 24 hrs by flow cytometry analysis2010Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
New orally bioavailable 2-aminobenzamide-type histone deacetylase inhibitor possessing a (2-hydroxyethyl)(4-(thiophen-2-yl)benzyl)amino group.
AID1676591Binding affinity to Nickel cation assessed as accounting ratio by measuring total compound detected/total compound adsorbed at 2.55 umol by immobilized metal-ion affinity chromatography2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors.
AID1401924Cell cycle arrest in human SMMC7721 cells assessed as accumulation of cells at S phase at 1 umol/L after 72 hrs by propidium iodide staining-based flow cytometric analysis (Rvb = 5.21%)2018European journal of medicinal chemistry, Jan-01, Volume: 143Design, synthesis and biological evaluation of novel 2-aminobenzamides containing dithiocarbamate moiety as histone deacetylase inhibitors and potent antitumor agents.
AID316888Inhibition of HDAC from human SNU16 cells2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Histone deacetylase inhibitors: from bench to clinic.
AID1846974Inhibition of full length N-terminal GST-tagged human recombinant HDAC6 (1 to 1215 residues) expressed in Baculovirus infected Sf9 cells using Ac-Leu-Gly-Lys (Ac)-AMC as substrate pretreated for 5 mins followed by substrate addition and measured after 30
AID328809Antiproliferative activity against human A2780 cells by CellTiter-Blue cell viability assay2008Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8
A novel series of potent and selective ketone histone deacetylase inhibitors with antitumor activity in vivo.
AID1732209Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay2021European journal of medicinal chemistry, Apr-05, Volume: 215CAP rigidification of MS-275 and chidamide leads to enhanced antiproliferative effects mediated through HDAC1, 2 and tubulin polymerization inhibition.
AID519590Toxicity in breast fibroblasts2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Potent antimalarial activity of histone deacetylase inhibitor analogues.
AID1737665Induction of apoptosis in human MDA-MB-231 cells assessed as increase in cleaved PARP-1 level incubated for 24 hrs by Western blot analysis
AID488370Cell cycle arrest in human HCT116 cells assessed as accumulation at S phase at 10 uM after 48 hrs by flow cytometry analysis2010Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
New orally bioavailable 2-aminobenzamide-type histone deacetylase inhibitor possessing a (2-hydroxyethyl)(4-(thiophen-2-yl)benzyl)amino group.
AID328801Inhibition of HDAC8 expressed in Escherichia coli2008Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8
A novel series of potent and selective ketone histone deacetylase inhibitors with antitumor activity in vivo.
AID1846976Inhibition of full length C-terminal his-tagged human recombinant HDAC8 (142 to 143 residues) expressed in baculovirus in Sf9 insect cells using Ac-Leu-Gly-Lys (Tfa)-AMC as substrate pretreated for 5 mins followed by substrate addition and measured after
AID1548297Induction of apoptosis in bortezomib resistant human KM3/BTZ cells assessed as early apoptotic cells level at 200 nM incubated for 24 hrs in presence of bortezomib by Annexin V-FITC/PI staining based FCAS analysis (Rvb = 1.39%)
AID1596044Antiproliferative activity against human SMMC7721 cells assessed as reduction in cell growth at 2 uM incubated for 72 hrs by CCK-8 assay relative to control2019European journal of medicinal chemistry, Jul-01, Volume: 173Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (HDAC) inhibitors.
AID329928Inhibition of human HDAC4 in U937 cells assessed as residual activity at 5 uM2008Bioorganic & medicinal chemistry letters, Apr-15, Volume: 18, Issue:8
Novel uracil-based 2-aminoanilide and 2-aminoanilide-like derivatives: histone deacetylase inhibition and in-cell activities.
AID1732190Cytotoxicity against human HH cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay2021European journal of medicinal chemistry, Apr-05, Volume: 215CAP rigidification of MS-275 and chidamide leads to enhanced antiproliferative effects mediated through HDAC1, 2 and tubulin polymerization inhibition.
AID1231809Inhibition of recombinant HDAC8 (unknown origin) incubated for 10 mins using Boc-Lys(acetyl)-AMC fluorogenic substrate by homogeneous fluorescence release assay2015Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13
Discovery, bioactivity and docking simulation of Vorinostat analogues containing 1,2,4-oxadiazole moiety as potent histone deacetylase inhibitors and antitumor agents.
AID1732192Cytotoxicity against human HL-60 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay2021European journal of medicinal chemistry, Apr-05, Volume: 215CAP rigidification of MS-275 and chidamide leads to enhanced antiproliferative effects mediated through HDAC1, 2 and tubulin polymerization inhibition.
AID764214Inhibition of human recombinant HDAC1 using p53 residues 379-382 (RHKKAc) as substrate2013Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
Novel N-hydroxyfurylacrylamide-based histone deacetylase (HDAC) inhibitors with branched CAP group (Part 2).
AID650224Induction of cell cycle arrest in human HCT116 cells assessed as accumulation at SubG1 phase at 10 uM after 24 hrs by flow cytometry (Rvb = 5.7 %)2012Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
Anti-tumor activity of new orally bioavailable 2-amino-5-(thiophen-2-yl)benzamide-series histone deacetylase inhibitors, possessing an aqueous soluble functional group as a surface recognition domain.
AID1596075Induction of apoptosis in human SMMC7721 cells assessed as necrotic cells at 4 uM incubated for 48 hrs by Annexin-V-FITC/propidium iodide staining based flow cytometry (Rvb=1.88%)2019European journal of medicinal chemistry, Jul-01, Volume: 173Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (HDAC) inhibitors.
AID1732158Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay2021European journal of medicinal chemistry, Apr-05, Volume: 215CAP rigidification of MS-275 and chidamide leads to enhanced antiproliferative effects mediated through HDAC1, 2 and tubulin polymerization inhibition.
AID374826Antiproliferative activity against human P53 expressing HCT116 cells after 72 hrs by celltiter-blue cell viability assay2009Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
Discovery of a potent class I selective ketone histone deacetylase inhibitor with antitumor activity in vivo and optimized pharmacokinetic properties.
AID1732164Inhibition of HDAC2 (unknown origin) using fluorogenic-(RHKKAc) as substrate by fluorescence assay2021European journal of medicinal chemistry, Apr-05, Volume: 215CAP rigidification of MS-275 and chidamide leads to enhanced antiproliferative effects mediated through HDAC1, 2 and tubulin polymerization inhibition.
AID1732169Antiproliferative activity against HDACi-resistant human YCC3/7 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay2021European journal of medicinal chemistry, Apr-05, Volume: 215CAP rigidification of MS-275 and chidamide leads to enhanced antiproliferative effects mediated through HDAC1, 2 and tubulin polymerization inhibition.
AID777591Effect on HDAC in human HaCaT cells assessed as upregulation of miR-661 at 10 uM after 1 hr by RT-PCR analysis2013ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
Synthesis and Biological Evaluation of the First Example of NO-Donor Histone Deacetylase Inhibitor.
AID420317Displacement of Atto700-HA from Bordetella / Alcaligenes strain FB188 HDAH by fluorescence anisotropy2009Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
Non-isotopic dual parameter competition assay suitable for high-throughput screening of histone deacetylases.
AID1727732Inhibition of His-tagged BRD4 bromodomain 2 (unknown origin) using [Lys (5,8,12,16) Ac] H4(1-21) as substrate by fluorescence based assay2021European journal of medicinal chemistry, Jan-01, Volume: 209Discovery of selective HDAC/BRD4 dual inhibitors as epigenetic probes.
AID1401925Cell cycle arrest in human SMMC7721 cells assessed as accumulation of cells at G2/M phase at 1 umol/L after 72 hrs by propidium iodide staining-based flow cytometric analysis (Rvb = 14.14%)2018European journal of medicinal chemistry, Jan-01, Volume: 143Design, synthesis and biological evaluation of novel 2-aminobenzamides containing dithiocarbamate moiety as histone deacetylase inhibitors and potent antitumor agents.
AID1548292Induction of apoptosis in bortezomib resistant human KM3/BTZ cells assessed as viable cells level at 50 nM incubated for 24 hrs in presence of bortezomib by Annexin V-FITC/PI staining based FCAS analysis (Rvb = 98.1%)
AID610087Anticancer activity against human HCT116 cells after 72 hrs by MTT assay2011Bioorganic & medicinal chemistry letters, Aug-15, Volume: 21, Issue:16
Design, synthesis and docking studies on benzamide derivatives as histone deacetylase inhibitors.
AID43458Inhibitory concentration against breast MCF-7 cell line2003Journal of medicinal chemistry, Feb-27, Volume: 46, Issue:5
Development of potential antitumor agents. Synthesis and biological evaluation of a new set of sulfonamide derivatives as histone deacetylase inhibitors.
AID1401899Antiproliferative activity against human NCI-H1299 cells after 72 hrs by CCK-8 assay2018European journal of medicinal chemistry, Jan-01, Volume: 143Design, synthesis and biological evaluation of novel 2-aminobenzamides containing dithiocarbamate moiety as histone deacetylase inhibitors and potent antitumor agents.
AID1691036Antiproliferative activity against human KB7D cells incubated for 48 hrs by SRB assay
AID161227Inhibitory concentration against prostate DU145 cell line2003Journal of medicinal chemistry, Feb-27, Volume: 46, Issue:5
Development of potential antitumor agents. Synthesis and biological evaluation of a new set of sulfonamide derivatives as histone deacetylase inhibitors.
AID764213Inhibition of human recombinant HDAC4 using p53 residues 379-382 (RHKKAc) as substrate2013Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
Novel N-hydroxyfurylacrylamide-based histone deacetylase (HDAC) inhibitors with branched CAP group (Part 2).
AID538409Inhibition of recombinant human HDAC6 using Boc-Lys(Ac)-AMC as substrate by fluorometric analysis2010Bioorganic & medicinal chemistry letters, Dec-01, Volume: 20, Issue:23
Inhibitors selective for HDAC6 in enzymes and cells.
AID1586069Growth inhibition of human MKN45 cells after 48 hrs by SRB assay2019European journal of medicinal chemistry, Jan-15, Volume: 1621-Arylsulfonyl indoline-benzamides as a new antitubulin agents, with inhibition of histone deacetylase.
AID1901174Inhibition of HDAC1/HDAC2/HDAC3 in human HCT-116 cells assessed as increase in accumulation of acetylated H4K5 at 5 uM treated for 48 hrs by Western blot analysis2022Bioorganic & medicinal chemistry, 02-15, Volume: 56Synthesis and biological evaluation of aminobenzamides containing purine moiety as class I histone deacetylases inhibitors.
AID496803Inhibition of human HDAC32010Nature chemical biology, Mar, Volume: 6, Issue:3
Chemical phylogenetics of histone deacetylases.
AID1596040Antiproliferative activity against human A549 cells assessed as reduction in cell growth at 2 uM incubated for 72 hrs by CCK-8 assay relative to control2019European journal of medicinal chemistry, Jul-01, Volume: 173Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (HDAC) inhibitors.
AID1293872Inhibition of HDAC in mouse C127-LT cells assessed as activation of EGFP expression at 1 uM after 24 hrs by fluorescence microscopy2016Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
Identification of new quinic acid derivatives as histone deacetylase inhibitors by fluorescence-based cellular assay.
AID1881855Inhibition of HDAC3 (unknown origin)2022European journal of medicinal chemistry, Jan-05, Volume: 227NO-HDAC dual inhibitors.
AID1873438Inhibition of full length C-terminal FLAG-tagged HDAC2 (unknown origin) assessed as inhibition constant (Ki) using (Ac-Leu-Gly-Lys(Ac)-AMC as substrate measured every 30 sec for 60 mins by fluorescence based assay2022ACS medicinal chemistry letters, May-12, Volume: 13, Issue:5
Determination of Slow-Binding HDAC Inhibitor Potency and Subclass Selectivity.
AID1556409Inhibition of HDAC1/2 in LPS/IFNgamma-stimulated mouse RAW264.7 cells assessed as upregulation of IL-10 gene expression at 1 uM pretreated for 16 hrs followed by LPS stimulation and measured after 4 hrs by RT-qPCR analysis2019European journal of medicinal chemistry, Sep-01, Volume: 177Inhibitory selectivity among class I HDACs has a major impact on inflammatory gene expression in macrophages.
AID1596068Induction of apoptosis in human SMMC7721 cells assessed as viable cells at 1 uM incubated for 48 hrs by Annexin-V-FITC/propidium iodide staining based flow cytometry (Rvb=93.5%)2019European journal of medicinal chemistry, Jul-01, Volume: 173Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (HDAC) inhibitors.
AID1431813Selectivity ratio of IC50 for human KDAC6 to IC50 for human KDAC12017European journal of medicinal chemistry, Feb-15, Volume: 127Design and synthesis of benzodiazepine analogs as isoform-selective human lysine deacetylase inhibitors.
AID292436Inhibition of HDAC in HeLa cells2007Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
Trithiocarbonates: exploration of a new head group for HDAC inhibitors.
AID1401894Antiproliferative activity against human HeLa cells at 8 uM after 72 hrs by CCK-8 assay relative to control2018European journal of medicinal chemistry, Jan-01, Volume: 143Design, synthesis and biological evaluation of novel 2-aminobenzamides containing dithiocarbamate moiety as histone deacetylase inhibitors and potent antitumor agents.
AID1453361Inhibition of class 1 HDAC in HEL cells using Boc-Lys (acetyl)-AMC as substrate preincubated for 3 hrs followed by substrate addition measured after 3 hrs by fluorescence assay2017Bioorganic & medicinal chemistry, 06-15, Volume: 25, Issue:12
Design, synthesis and anti-tumor activity study of novel histone deacetylase inhibitors containing isatin-based caps and o-phenylenediamine-based zinc binding groups.
AID1901161Antiproliferative activity against human A549 cells measured after 48 hrs by MTT assay2022Bioorganic & medicinal chemistry, 02-15, Volume: 56Synthesis and biological evaluation of aminobenzamides containing purine moiety as class I histone deacetylases inhibitors.
AID364641Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay2008Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17
Design, synthesis and biological evaluation of novel compounds with conjugated structure as anti-tumor agents.
AID1431816Selectivity ratio of IC50 for human KDAC6 to IC50 for human KDAC32017European journal of medicinal chemistry, Feb-15, Volume: 127Design and synthesis of benzodiazepine analogs as isoform-selective human lysine deacetylase inhibitors.
AID1865259Inhibition of wild type SHP2 (unknown origin) using DiFMUP as substrate preincubated for 30 mins followed by substrate addition and measured after 30 mins by microplate reader method2022Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
Discovery of Novel Src Homology-2 Domain-Containing Phosphatase 2 and Histone Deacetylase Dual Inhibitors with Potent Antitumor Efficacy and Enhanced Antitumor Immunity.
AID1737655Cytotoxicity against human K562 cells assessed as inhibition of cell viability incubated for 72 hrs by MTS assay
AID1737664Induction of cell cycle arrest in human MDA-MB-231 cells assessed as accumulation of cells at G1 phase at 4 uM for 24 hrs in presence of nocodazole by PI staining based flow cytometry analysis
AID1474452Selectivity ratio of IC50 for HDAC1 (unknown origin) to IC50 for HDAC in human HCT116 cells2017European journal of medicinal chemistry, May-26, Volume: 132Design, synthesis and biological evaluation of novel coumarin-based benzamides as potent histone deacetylase inhibitors and anticancer agents.
AID1596053Inhibition of cell migration in human SMMC7721 cells at 0.5 uM measured after 48 hrs by microscopic analysis2019European journal of medicinal chemistry, Jul-01, Volume: 173Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (HDAC) inhibitors.
AID1263142Antagonist activity at luciferase-fused ERalpha in human HEK293 cells expressing eYFP assessed as reduction of E2-induced estrogenic activity after 2 hrs by BRET assay2015Bioorganic & medicinal chemistry, Dec-15, Volume: 23, Issue:24
Design, synthesis and evaluation of antiestrogen and histone deacetylase inhibitor molecular hybrids.
AID1541443Inhibition of human full length N-terminal GST-tagged HDAC6 expressed in baculovirus infected Sf9 insect cells ZMAL as substrate incubated for 90 mins by fluorescence assay2019Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
Synthesis of Peptoid-Based Class I-Selective Histone Deacetylase Inhibitors with Chemosensitizing Properties.
AID329917Induction of alpha tubulin hyperacetylation in human U937 cells2008Bioorganic & medicinal chemistry letters, Apr-15, Volume: 18, Issue:8
Novel uracil-based 2-aminoanilide and 2-aminoanilide-like derivatives: histone deacetylase inhibition and in-cell activities.
AID269160Antitumor activity against human HCT116 cells xenografted in mouse at 20 mg/kg, ip2006Bioorganic & medicinal chemistry letters, Aug-01, Volume: 16, Issue:15
Substituted N-(2-aminophenyl)-benzamides, (E)-N-(2-aminophenyl)-acrylamides and their analogues: novel classes of histone deacetylase inhibitors.
AID1691034Antiproliferative activity against human KB cells incubated for 48 hrs by SRB assay
AID1732207Cytotoxicity against human NCI-H661 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay2021European journal of medicinal chemistry, Apr-05, Volume: 215CAP rigidification of MS-275 and chidamide leads to enhanced antiproliferative effects mediated through HDAC1, 2 and tubulin polymerization inhibition.
AID613340Antiproliferative activity against human H1299 cells2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Optimization of the in vitro cardiac safety of hydroxamate-based histone deacetylase inhibitors.
AID1324233Inhibition of HDAC6 in human LNCAP cells assessed as inhibition of DHT-induced alpha-tubulin deacetylation by measuring increase in alpha-tubulin acetylation at 10 uM measured after 24 hrs relative to control2016Bioorganic & medicinal chemistry letters, 11-01, Volume: 26, Issue:21
Targeting prostate cancer with compounds possessing dual activity as androgen receptor antagonists and HDAC6 inhibitors.
AID1548294Induction of apoptosis in bortezomib resistant human KM3/BTZ cells assessed as late apoptotic cells level at 50 nM incubated for 24 hrs in presence of bortezomib by Annexin V-FITC/PI staining based FCAS analysis (Rvb = 0.38%)
AID1474460Inhibition of HDAC in human HCT116 cells using Boc-Lys (epsilon-Ac)-AMC as substrate pretreated for 18 hrs followed by substrate addition after 3 hrs by fluorescence assay2017European journal of medicinal chemistry, May-26, Volume: 132Design, synthesis and biological evaluation of novel coumarin-based benzamides as potent histone deacetylase inhibitors and anticancer agents.
AID650226Inhibition of HDAC1 in human HCT116 cells assessed as hyperacetylation of histone H3 at 10 uM after 24 hrs by Western blot analysis2012Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
Anti-tumor activity of new orally bioavailable 2-amino-5-(thiophen-2-yl)benzamide-series histone deacetylase inhibitors, possessing an aqueous soluble functional group as a surface recognition domain.
AID1732161Cytotoxicity against human DLD-1 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay2021European journal of medicinal chemistry, Apr-05, Volume: 215CAP rigidification of MS-275 and chidamide leads to enhanced antiproliferative effects mediated through HDAC1, 2 and tubulin polymerization inhibition.
AID316931Inhibition of HDAC32008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Histone deacetylase inhibitors: from bench to clinic.
AID1901167Inhibition of HDAC1/HDAC2/HDAC3 in human HCT-116 cells assessed as increase in accumulation of acetylated H4K5 at 5 uM measured after 24 hrs by Western blot analysis2022Bioorganic & medicinal chemistry, 02-15, Volume: 56Synthesis and biological evaluation of aminobenzamides containing purine moiety as class I histone deacetylases inhibitors.
AID525021Inhibition of HDAC in human CFBE41o- cell line assessed as total CFTR protein level including CFTR glycoform at 5 uM by immunoblot analysis2010Nature chemical biology, Jan, Volume: 6, Issue:1
Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis.
AID1691035Antiproliferative activity against human KB-VIN cells incubated for 48 hrs by SRB assay
AID328796Inhibition of HDAC4 expressed in Escherichia coli2008Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8
A novel series of potent and selective ketone histone deacetylase inhibitors with antitumor activity in vivo.
AID1466059Growth inhibition of human MDA-MB-231 cells after 48 hrs by sulforhodamine B assay2017European journal of medicinal chemistry, Jul-07, Volume: 1344-Indolyl-N-hydroxyphenylacrylamides as potent HDAC class I and IIB inhibitors in vitro and in vivo.
AID1901158Antiproliferative activity against human HCT-116 cells measured after 48 hrs by MTT assay2022Bioorganic & medicinal chemistry, 02-15, Volume: 56Synthesis and biological evaluation of aminobenzamides containing purine moiety as class I histone deacetylases inhibitors.
AID1596060Cell cycle arrest in human SMMC7721 cells assessed as accumulation at G2/M phase at 1 uM incubated for 48 hrs by propidium iodide staining based flow cytometry (Rvb=16.17%)2019European journal of medicinal chemistry, Jul-01, Volume: 173Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (HDAC) inhibitors.
AID1676599Binding affinity to cupric ion assessed as accounting ratio by measuring total compound detected/total compound adsorbed at 2.55 umol by immobilized metal-ion affinity chromatography2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors.
AID1737667Induction of apoptosis in human MDA-MB-231 cells assessed as increase in cleaved caspase-3 level incubated for 24 hrs by Western blot analysis
AID1474459Antiproliferative activity against human A2780 cells after 48 hrs by MTT assay2017European journal of medicinal chemistry, May-26, Volume: 132Design, synthesis and biological evaluation of novel coumarin-based benzamides as potent histone deacetylase inhibitors and anticancer agents.
AID1596043Antiproliferative activity against human SMMC7721 cells assessed as reduction in cell growth at 8 uM incubated for 72 hrs by CCK-8 assay relative to control2019European journal of medicinal chemistry, Jul-01, Volume: 173Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (HDAC) inhibitors.
AID525005Inhibition of HDAC7 in Fdelta508 CFTR-expressing human CFBE41o- monolayers assessed as increase in short circuit currents at 0.5 uM2010Nature chemical biology, Jan, Volume: 6, Issue:1
Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis.
AID8302Compound was tested for antiproliferative activity against human A549 cancer cell lines using MTT assay2003Journal of medicinal chemistry, Dec-18, Volume: 46, Issue:26
Synthesis and biological evaluation of 3-(4-substituted-phenyl)-N-hydroxy-2-propenamides, a new class of histone deacetylase inhibitors.
AID1235135Cytotoxicity against human A549 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay2015European journal of medicinal chemistry, Jul-15, Volume: 100Design, synthesis and antiproliferative activities of novel benzamides derivatives as HDAC inhibitors.
AID1737639Cytotoxicity against human HDACi-sensitive YCC-11 cells assessed as reduction in cell growth incubated for 72 hrs by MTS assay
AID385431Inhibition of TNF-alpha-induced tissue factor activity in HUVEC at 30 uM preincubated for 4 hrs assessed after 4 hrs of TNFalpha challenge by one stage clotting assay2007The Journal of biological chemistry, Sep-28, Volume: 282, Issue:39
Histone deacetylase inhibitors suppress TF-kappaB-dependent agonist-driven tissue factor expression in endothelial cells and monocytes.
AID708274Growth inhibition of human SKHEP1 cells incubated for 72 hrs by WST dye reduction assay2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Pharmacokinetic optimization of class-selective histone deacetylase inhibitors and identification of associated candidate predictive biomarkers of hepatocellular carcinoma tumor response.
AID1548289Induction of apoptosis in bortezomib resistant human KM3/BTZ cells assessed as early apoptotic cells level at 200 nM incubated for 24 hrs by Annexin V-FITC/PI staining based FCAS analysis (Rvb = 1.39%)
AID1578487Inhibition of recombinant full length human HDAC4 expressed in baculovirus infected Sf9 cells using FAM-RHKK-TFAc as substrate incubated for 1.5 hrs by electrophoretic mobility shift assay2020ACS medicinal chemistry letters, Jan-09, Volume: 11, Issue:1
Class I/IIb-Selective HDAC Inhibitor Exhibits Oral Bioavailability and Therapeutic Efficacy in Acute Myeloid Leukemia.
AID1453360Antiproliferative activity against human SK-N-BE(2) cells after 48 hrs by MTT assay2017Bioorganic & medicinal chemistry, 06-15, Volume: 25, Issue:12
Design, synthesis and anti-tumor activity study of novel histone deacetylase inhibitors containing isatin-based caps and o-phenylenediamine-based zinc binding groups.
AID1235134Cytotoxicity against human MCF7 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay2015European journal of medicinal chemistry, Jul-15, Volume: 100Design, synthesis and antiproliferative activities of novel benzamides derivatives as HDAC inhibitors.
AID316941Inhibition of HDAC92008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Histone deacetylase inhibitors: from bench to clinic.
AID1479828Inhibition of class 1 HDAC in human MV4-11 cells assessed as induction of histone hyperacetylation at 5 uM after 24 hrs by Western blot method2018Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
Marbostat-100 Defines a New Class of Potent and Selective Antiinflammatory and Antirheumatic Histone Deacetylase 6 Inhibitors.
AID90211Inhibitory activity against Histone deacetylase (HDAC) in K 562 erythroleukemia cells2003Bioorganic & medicinal chemistry letters, Nov-17, Volume: 13, Issue:22
Heterocyclic ketones as inhibitors of histone deacetylase.
AID44724Inhibitory concentration against bladder T24 cell line2003Journal of medicinal chemistry, Feb-27, Volume: 46, Issue:5
Development of potential antitumor agents. Synthesis and biological evaluation of a new set of sulfonamide derivatives as histone deacetylase inhibitors.
AID1691040Inhibition of human recombinant HDAC8 using RHKAcKAc-AMC as substrate measured after 60 mins by fluorescence assay
AID50591Inhibitory concentration against colon SW48 cell line2003Journal of medicinal chemistry, Feb-27, Volume: 46, Issue:5
Development of potential antitumor agents. Synthesis and biological evaluation of a new set of sulfonamide derivatives as histone deacetylase inhibitors.
AID1401908Induction of apoptosis in human SMMC7721 cells assessed as viable cells at 0.125 umol/L after 72 hrs by Alexa Fluor 488 Annexin/propidium iodide staining-based flow cytometric analysis (Rvb = 97.14%)2018European journal of medicinal chemistry, Jan-01, Volume: 143Design, synthesis and biological evaluation of novel 2-aminobenzamides containing dithiocarbamate moiety as histone deacetylase inhibitors and potent antitumor agents.
AID1732167Inhibition of HDAC10 (unknown origin) using fluorogenic-(RHKKAc) as substrate by fluorescence assay2021European journal of medicinal chemistry, Apr-05, Volume: 215CAP rigidification of MS-275 and chidamide leads to enhanced antiproliferative effects mediated through HDAC1, 2 and tubulin polymerization inhibition.
AID777588Effect on HDAC in human HaCaT cells assessed as upregulation of miR-126# at 10 uM after 1 hr by RT-PCR analysis2013ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
Synthesis and Biological Evaluation of the First Example of NO-Donor Histone Deacetylase Inhibitor.
AID1293873Inhibition of HDAC in mouse C127-LT cells assessed as activation of EGFP expression at 10 uM after 24 hrs by fluorescence microscopy2016Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
Identification of new quinic acid derivatives as histone deacetylase inhibitors by fluorescence-based cellular assay.
AID328805Antiproliferative activity against human HeLa cells by CellTiter-Blue cell viability assay2008Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8
A novel series of potent and selective ketone histone deacetylase inhibitors with antitumor activity in vivo.
AID607635Inhibition of HDAC6 in human Hela cells assessed as increase in alpha-tubulin acetylation at 0.6 uM after 16 hrs by immunofluorescence microscopy2011Bioorganic & medicinal chemistry letters, Jul-15, Volume: 21, Issue:14
A novel HDAC inhibitor with a hydroxy-pyrimidine scaffold.
AID1466058Growth inhibition of human A549 cells after 48 hrs by sulforhodamine B assay2017European journal of medicinal chemistry, Jul-07, Volume: 1344-Indolyl-N-hydroxyphenylacrylamides as potent HDAC class I and IIB inhibitors in vitro and in vivo.
AID1873446Inhibition of full length C-terminal His-tagged HDAC3 (unknown origin)/N-terminal GST-tagged NCoR2 (unknown origin) assessed as rate constant (k2) of EI complex using (Ac-Leu-Gly-Lys(Ac)-AMC as substrate measured every 30 sec for 60 mins by fluorescence b2022ACS medicinal chemistry letters, May-12, Volume: 13, Issue:5
Determination of Slow-Binding HDAC Inhibitor Potency and Subclass Selectivity.
AID90348Ability to inhibit recombinant human histone deacetylase 1 (HDAC-1).2004Bioorganic & medicinal chemistry letters, Jan-05, Volume: 14, Issue:1
(2-amino-phenyl)-amides of omega-substituted alkanoic acids as new histone deacetylase inhibitors.
AID1596063Cell cycle arrest in human SMMC7721 cells assessed as accumulation at G2/M phase at 4 uM incubated for 48 hrs by propidium iodide staining based flow cytometry (Rvb=16.17%)2019European journal of medicinal chemistry, Jul-01, Volume: 173Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (HDAC) inhibitors.
AID1732202Induction of cell cycle arrest in human MDA-MB-231 cells assessed as increase in accumulation of G2/M phase at 2.5 uM incubated for 24 hrs by PI staining based flow cytometry analysis2021European journal of medicinal chemistry, Apr-05, Volume: 215CAP rigidification of MS-275 and chidamide leads to enhanced antiproliferative effects mediated through HDAC1, 2 and tubulin polymerization inhibition.
AID1454683Decrease in alcohol intake in rat model of voluntary heavy drinking assessed as decrease in motivation to consume alcohol at 500 uM, icv administered twice relative to control2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Class I HDAC Inhibitors: Potential New Epigenetic Therapeutics for Alcohol Use Disorder (AUD).
AID1446910Inhibition of Schistosoma mansoni KDAC8 at 30 uM using (FAM)-labeled peptide as substrate after 60 mins by microfluidic assay2017Bioorganic & medicinal chemistry, 04-01, Volume: 25, Issue:7
Structural insights of SmKDAC8 inhibitors: Targeting Schistosoma epigenetics through a combined structure-based 3D QSAR, in vitro and synthesis strategy.
AID1548301Induction of cell cycle arrest in bortezomib resistant human KM3/BTZ cells assessed as accumulation at S phase at 100 nM incubated for 24 hrs by propidium iodide staining based flow cytometry (Rvb = 46%)
AID1727733Antiproliferative activity against human MV4-11 cells assessed as cell viability after 72 hrs by CCK8 assay2021European journal of medicinal chemistry, Jan-01, Volume: 209Discovery of selective HDAC/BRD4 dual inhibitors as epigenetic probes.
AID1431817Selectivity ratio of IC50 for human KDAC3 to IC50 for human KDAC62017European journal of medicinal chemistry, Feb-15, Volume: 127Design and synthesis of benzodiazepine analogs as isoform-selective human lysine deacetylase inhibitors.
AID1596051Selectivity ratio of IC50 for human recombinant His-tagged HDAC6 expressed in baculovirus infected insect cells to IC50 of human recombinant His-tagged HDAC1 (482 residues) expressed in baculovirus infected insect cells2019European journal of medicinal chemistry, Jul-01, Volume: 173Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (HDAC) inhibitors.
AID1548288Induction of apoptosis in bortezomib resistant human KM3/BTZ cells assessed as viable cells level at 200 nM incubated for 24 hrs by Annexin V-FITC/PI staining based FCAS analysis (Rvb = 98.1%)
AID313736Inhibition of HDAC82008Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2
Optimization of biaryl Selective HDAC1&2 Inhibitors (SHI-1:2).
AID1294934Inhibition of HDAC in human HeLa nuclear extract using Boc-acetyl-lysine-AMC as substrate incubated for 30 mins in dark by microplate reader analysis2016European journal of medicinal chemistry, Jun-30, Volume: 116Computer-aided identification of new histone deacetylase 6 selective inhibitor with anti-sepsis activity.
AID1737651Inhibition of human recombinant HDAC7 expressed in baculovirus using fluorogenic peptide p53 residues 379-382 (RHKK(Ac)AMC) as substrate by Fluorescence analysis
AID1556400Inhibition of human recombinant C-terminal FLAG-tagged HDAC2 using Boc-Lys-(epsilon-Ac)-AMC as fluorogenic substrate incubated for 90 mins by fluorescence based assay2019European journal of medicinal chemistry, Sep-01, Volume: 177Inhibitory selectivity among class I HDACs has a major impact on inflammatory gene expression in macrophages.
AID1737653Inhibition of human recombinant HDAC10 expressed in baculovirus using fluorogenic peptide p53 residues 379-382 (RHKK(Ac)AMC) as substrate by Fluorescence analysis
AID1873450Inhibition of full length C-terminal FLAG-tagged HDAC2 (unknown origin) assessed as apparent inhibition constant using (Ac-Leu-Gly-Lys(Ac)-AMC as substrate preincubated with enzyme for 0.5 to 2 hrs followed by substrate addition and measured after 30 mins2022ACS medicinal chemistry letters, May-12, Volume: 13, Issue:5
Determination of Slow-Binding HDAC Inhibitor Potency and Subclass Selectivity.
AID650213Antitumor activity against human HCT116 cells xenografted in BALB/c nu/nu mouse assessed as suppression of tumor growth at 45 mg/kg, po administered every alternate days for 14 days measured up to day 16 relative to control2012Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
Anti-tumor activity of new orally bioavailable 2-amino-5-(thiophen-2-yl)benzamide-series histone deacetylase inhibitors, possessing an aqueous soluble functional group as a surface recognition domain.
AID1873448Inhibition of full length C-terminal His-tagged HDAC1 (unknown origin) assessed as rate constant (k2) of EI complex using (Ac-Leu-Gly-Lys(Ac)-AMC as substrate measured every 30 sec for 60 mins by fluorescence based assay2022ACS medicinal chemistry letters, May-12, Volume: 13, Issue:5
Determination of Slow-Binding HDAC Inhibitor Potency and Subclass Selectivity.
AID329919Induction of apoptosis in human U937 cells2008Bioorganic & medicinal chemistry letters, Apr-15, Volume: 18, Issue:8
Novel uracil-based 2-aminoanilide and 2-aminoanilide-like derivatives: histone deacetylase inhibition and in-cell activities.
AID1380943Antiproliferative activity against human HeLa cells after 72 hrs by MTT assay2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Discovery of Novel Pazopanib-Based HDAC and VEGFR Dual Inhibitors Targeting Cancer Epigenetics and Angiogenesis Simultaneously.
AID488361Toxicity in human HCT116 cells xenografted BALB/c nu/nu mouse assessed increase of running behavior at 45 mg/kg, po administered on days 2, 4, 7, 9, 11, 14 and 162010Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
New orally bioavailable 2-aminobenzamide-type histone deacetylase inhibitor possessing a (2-hydroxyethyl)(4-(thiophen-2-yl)benzyl)amino group.
AID1548295Induction of apoptosis in bortezomib resistant human KM3/BTZ cells assessed as necrotic cells level at 50 nM incubated for 24 hrs in presence of bortezomib by Annexin V-FITC/PI staining based FCAS analysis (Rvb = 0.11%)
AID1915555Inhibition of human recombinant HDAC1 (unknown origin) using MAZ1600 as substrate preincubated for 3 hrs followed by substrate addition by multilabel plate reader method2021European journal of medicinal chemistry, Jan-01, Volume: 209Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors.
AID1441631Inhibition of recombinant human LTA4H Epoxide Hydrolase expressed in Escherichia coli BL21 (DE3) pLysS preincubated for 10 mins followed by addition of LTA4 as substrate measured after 15 mins by reverse-phase HPLC analysis2017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Drug Repurposing of Histone Deacetylase Inhibitors That Alleviate Neutrophilic Inflammation in Acute Lung Injury and Idiopathic Pulmonary Fibrosis via Inhibiting Leukotriene A4 Hydrolase and Blocking LTB4 Biosynthesis.
AID488365Cell cycle arrest in human HCT116 cells assessed as accumulation at subG1 phase at 10 uM after 24 hrs by flow cytometry analysis2010Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
New orally bioavailable 2-aminobenzamide-type histone deacetylase inhibitor possessing a (2-hydroxyethyl)(4-(thiophen-2-yl)benzyl)amino group.
AID1548278Induction of apoptosis in bortezomib resistant human KM3/BTZ cells at 100 nM in presence of bortezomib incubated for 24 hrs by TUNEL assay
AID525026Inhibition of HDAC in human CFBE41o- cell line assessed as correction of mutant Fdelta508 CFTR trafficking to cell surface as glycoform at 5 uM by Immunoblot analysis2010Nature chemical biology, Jan, Volume: 6, Issue:1
Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis.
AID1453356Antiproliferative activity against human K562 cells after 48 hrs by MTT assay2017Bioorganic & medicinal chemistry, 06-15, Volume: 25, Issue:12
Design, synthesis and anti-tumor activity study of novel histone deacetylase inhibitors containing isatin-based caps and o-phenylenediamine-based zinc binding groups.
AID1530562Antiplasmodial activity against asynchronous form of Plasmodium falciparum 3D7 infected in human erythrocytes assessed as parasite growth inhibition at 10 uM after 48 hrs by SYBR green1 staining based flow cytometry relative to control2019European journal of medicinal chemistry, Jan-01, Volume: 161Identification of novel quinazoline derivatives as potent antiplasmodial agents.
AID90837Inhibitory concentration ratio against HDAC6/HDAC12003Journal of medicinal chemistry, Nov-20, Volume: 46, Issue:24
Histone deacetylase inhibitors.
AID777596Effect on HDAC in human HaCaT cells assessed as downregulation of miR-663B at 10 uM after 1 hr by RT-PCR analysis2013ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
Synthesis and Biological Evaluation of the First Example of NO-Donor Histone Deacetylase Inhibitor.
AID1401928Cell cycle arrest in human SMMC7721 cells assessed as accumulation of cells at G2/M phase at 4 umol/L after 72 hrs by propidium iodide staining-based flow cytometric analysis (Rvb = 14.14%)2018European journal of medicinal chemistry, Jan-01, Volume: 143Design, synthesis and biological evaluation of novel 2-aminobenzamides containing dithiocarbamate moiety as histone deacetylase inhibitors and potent antitumor agents.
AID1380939Inhibition of VEGFR-2 (unknown origin) at 0.2 uM after 40 mins by kinase-Glo assay relative to control2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Discovery of Novel Pazopanib-Based HDAC and VEGFR Dual Inhibitors Targeting Cancer Epigenetics and Angiogenesis Simultaneously.
AID492801Inhibition of human recombinant HDAC1 at 5 uM after 15 mins by fluorimetric assay2010Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12
Synthesis and biological characterization of the histone deacetylase inhibitor largazole and C7- modified analogues.
AID777599Effect on HDAC in human HaCaT cells assessed as upregulation of miR-193b# at 10 uM after 1 hr by RT-PCR analysis2013ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
Synthesis and Biological Evaluation of the First Example of NO-Donor Histone Deacetylase Inhibitor.
AID551597Inhibition of HDAC32011Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
Application of p21 and klf2 reporter gene assays to identify selective histone deacetylase inhibitors for cancer therapy.
AID1189854Therapeutic index, ratio of CC50 for human HuH7 cells to EC50 for HCV genotype 1b infected in human Huh7 cells2015Journal of medicinal chemistry, Jan-22, Volume: 58, Issue:2
Hydroxamic acids block replication of hepatitis C virus.
AID1431814Selectivity ratio of IC50 for human KDAC8 to IC50 for human KDAC12017European journal of medicinal chemistry, Feb-15, Volume: 127Design and synthesis of benzodiazepine analogs as isoform-selective human lysine deacetylase inhibitors.
AID324957Inhibition of HDAC6 in HEK293 cells at 10 uM2008Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6
Probing the elusive catalytic activity of vertebrate class IIa histone deacetylases.
AID303014Inhibition of human recombinant HDAC12007Journal of medicinal chemistry, Nov-15, Volume: 50, Issue:23
Novel aminophenyl benzamide-type histone deacetylase inhibitors with enhanced potency and selectivity.
AID525034In vivo inhibition of HDAC2010Nature chemical biology, Jan, Volume: 6, Issue:1
Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis.
AID1548285Induction of apoptosis in bortezomib resistant human KM3/BTZ cells assessed as early apoptotic cells level at 50 nM incubated for 24 hrs by Annexin V-FITC/PI staining based FCAS analysis (Rvb = 1.39%)
AID650225Inhibition of HDAC2 in human HCT116 cells assessed as hyperacetylation of histone H3 at 10 uM after 24 hrs by Western blot analysis2012Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
Anti-tumor activity of new orally bioavailable 2-amino-5-(thiophen-2-yl)benzamide-series histone deacetylase inhibitors, possessing an aqueous soluble functional group as a surface recognition domain.
AID708270Growth inhibition of human HGC27 cells incubated for 72 hrs by WST dye reduction assay2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Pharmacokinetic optimization of class-selective histone deacetylase inhibitors and identification of associated candidate predictive biomarkers of hepatocellular carcinoma tumor response.
AID1821968Antiproliferative activity against human YCC-11 cells assessed as cell growth inhibition
AID1737648Inhibition of human recombinant HDAC3 expressed in baculovirus using fluorogenic peptide p53 residues 379-382 (RHKK(Ac)AMC) as substrate by Fluorescence analysis
AID1740016Inhibition of recombinant human HDAC4 using pan-HDAC substrate incubated for 3 hrs by fluorescence method2020Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
Thirty Years of HDAC Inhibitors: 2020 Insight and Hindsight.
AID1901176Inhibition of HDAC1/HDAC2/HDAC3 in human HCT-116 cells assessed as increase in accumulation of acetylated H4K5 at 5 uM preincubated for 6 hrs followed by compound washout and measured up to 48 hrs by Western blot analysis2022Bioorganic & medicinal chemistry, 02-15, Volume: 56Synthesis and biological evaluation of aminobenzamides containing purine moiety as class I histone deacetylases inhibitors.
AID620534Reactivation of MeCp2 mutant expression in human GM11272 cells after 6 days by PCR method2011Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
Clonal Rett Syndrome cell lines to test compounds for activation of wild-type MeCP2 expression.
AID524994Inhibition of HDAC9 by in vitro deacetylation assay2010Nature chemical biology, Jan, Volume: 6, Issue:1
Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis.
AID488362Toxicity in human HCT116 cells xenografted BALB/c nu/nu mouse assessed weight loss at 45 mg/kg, po administered on days 2, 4, 7, 9, 11, 142010Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
New orally bioavailable 2-aminobenzamide-type histone deacetylase inhibitor possessing a (2-hydroxyethyl)(4-(thiophen-2-yl)benzyl)amino group.
AID1401915Induction of apoptosis in human SMMC7721 cells assessed as necrotic cells at 1 umol/L after 72 hrs by Alexa Fluor 488 Annexin/propidium iodide staining-based flow cytometric analysis (Rvb = 2.48%)2018European journal of medicinal chemistry, Jan-01, Volume: 143Design, synthesis and biological evaluation of novel 2-aminobenzamides containing dithiocarbamate moiety as histone deacetylase inhibitors and potent antitumor agents.
AID1821969Antiproliferative activity against human YCC3/7 cells assessed as cell growth inhibition
AID1401909Induction of apoptosis in human SMMC7721 cells assessed as early apoptotic cells at 0.125 umol/L after 72 hrs by Alexa Fluor 488 Annexin/propidium iodide staining-based flow cytometric analysis (Rvb = 0.09%)2018European journal of medicinal chemistry, Jan-01, Volume: 143Design, synthesis and biological evaluation of novel 2-aminobenzamides containing dithiocarbamate moiety as histone deacetylase inhibitors and potent antitumor agents.
AID717814Inhibition of HDAC in human Hela cell lysate using Fluor-de-Lys as substrate assessed as remaining activity at 3.91 x 10'-6 M pretreated for 30 mins before substrate addition by fluorescence assay2012Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23
The structural requirements of histone deacetylase inhibitors: suberoylanilide hydroxamic acid analogs modified at the C6 position.
AID1401916Induction of apoptosis in human SMMC7721 cells assessed as viable cells at 4 umol/L after 72 hrs by Alexa Fluor 488 Annexin/propidium iodide staining-based flow cytometric analysis (Rvb = 97.14%)2018European journal of medicinal chemistry, Jan-01, Volume: 143Design, synthesis and biological evaluation of novel 2-aminobenzamides containing dithiocarbamate moiety as histone deacetylase inhibitors and potent antitumor agents.
AID374812Antiproliferative activity against human P53-deficient HeLa cells after 72 hrs by celltiter-blue cell viability assay2009Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
Discovery of a potent class I selective ketone histone deacetylase inhibitor with antitumor activity in vivo and optimized pharmacokinetic properties.
AID1882460Displacement of [3H]-acetylated histones from HDAC1 derived from human K562 cell nuclear extract incubated for 10 mins by liquid scintillation counting method2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Chasing a Breath of Fresh Air in Cystic Fibrosis (CF): Therapeutic Potential of Selective HDAC6 Inhibitors to Tackle Multiple Pathways in CF Pathophysiology.
AID328795Inhibition of HDAC32008Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8
A novel series of potent and selective ketone histone deacetylase inhibitors with antitumor activity in vivo.
AID1466412Induction of apoptosis in human HL60 cells assessed as increase in cleaved PARP level at 5 uM after 48 hrs by Western blot analysis2017European journal of medicinal chemistry, Jul-07, Volume: 134Selective HDAC inhibitors with potent oral activity against leukemia and colorectal cancer: Design, structure-activity relationship and anti-tumor activity study.
AID1737649Inhibition of human recombinant HDAC4 expressed in baculovirus using fluorogenic peptide p53 residues 379-382 (RHKK(Ac)AMC) as substrate by Fluorescence analysis
AID1454685Lipophilicity, log D of the compound at pH 7.42018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Class I HDAC Inhibitors: Potential New Epigenetic Therapeutics for Alcohol Use Disorder (AUD).
AID708277Growth inhibition of human Bel7402 cells incubated for 72 hrs by WST dye reduction assay2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Pharmacokinetic optimization of class-selective histone deacetylase inhibitors and identification of associated candidate predictive biomarkers of hepatocellular carcinoma tumor response.
AID717827Inhibition of HDAC in human Hela cell lysate using Fluor-de-Lys as substrate compound pretreated for 30 mins before substrate addition by fluorescence assay2012Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23
The structural requirements of histone deacetylase inhibitors: suberoylanilide hydroxamic acid analogs modified at the C6 position.
AID1231808Inhibition of recombinant HDAC2 (unknown origin) incubated for 10 mins using Boc-Lys(acetyl)-AMC fluorogenic substrate by homogeneous fluorescence release assay2015Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13
Discovery, bioactivity and docking simulation of Vorinostat analogues containing 1,2,4-oxadiazole moiety as potent histone deacetylase inhibitors and antitumor agents.
AID1454682Decrease in alcohol intake in rat model of voluntary heavy drinking assessed as decrease in operant alcohol self-administration at 500 uM, icv administered twice relative to control2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Class I HDAC Inhibitors: Potential New Epigenetic Therapeutics for Alcohol Use Disorder (AUD).
AID1203890Inhibition of recombinant HDAC2 (unknown origin) using fluorogenic substrate Boc-Lys (acetyl)-AMC after 20 mins by homogeneous fluorescence release assay2015European journal of medicinal chemistry, , Volume: 96Discovery and preliminary evaluation of 2-aminobenzamide and hydroxamate derivatives containing 1,2,4-oxadiazole moiety as potent histone deacetylase inhibitors.
AID1203894Antiproliferative activity against human NCI-H661 cells assessed as inhibition of cell growth after 72 hrs by MTT-based assay2015European journal of medicinal chemistry, , Volume: 96Discovery and preliminary evaluation of 2-aminobenzamide and hydroxamate derivatives containing 1,2,4-oxadiazole moiety as potent histone deacetylase inhibitors.
AID1453367Selectivity ratio of IC50 for HDAC3 (unknown origin) to IC50 for HDAC1 (unknown origin)2017Bioorganic & medicinal chemistry, 06-15, Volume: 25, Issue:12
Design, synthesis and anti-tumor activity study of novel histone deacetylase inhibitors containing isatin-based caps and o-phenylenediamine-based zinc binding groups.
AID1917928Inhibition of HDAC3 (unknown origin)2022Bioorganic & medicinal chemistry letters, 11-15, Volume: 76Zinc-dependent deacetylases (HDACs) as potential targets for treating Alzheimer's disease.
AID488367Cell cycle arrest in human HCT116 cells assessed as accumulation at G0/G1 phase at 10 uM after 24 hrs by flow cytometry analysis2010Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
New orally bioavailable 2-aminobenzamide-type histone deacetylase inhibitor possessing a (2-hydroxyethyl)(4-(thiophen-2-yl)benzyl)amino group.
AID1732196Inhibition of HDAC in human MDA-MB-231 cells assessed as increase in p21 expression at 4 uM incubated for 24 hrs by Western blot analysis2021European journal of medicinal chemistry, Apr-05, Volume: 215CAP rigidification of MS-275 and chidamide leads to enhanced antiproliferative effects mediated through HDAC1, 2 and tubulin polymerization inhibition.
AID613343Inhibition of human ERG at 30 uM2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Optimization of the in vitro cardiac safety of hydroxamate-based histone deacetylase inhibitors.
AID316885Antiproliferative activity against human A549 cells2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Histone deacetylase inhibitors: from bench to clinic.
AID1737646Inhibition of human recombinant HDAC6 expressed in baculovirus using fluorogenic peptide p53 residues 379-382 (RHKK(Ac)AMC) as substrate by Fluorescence analysis
AID328799Inhibition of HDAC6 at 10 uM2008Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8
A novel series of potent and selective ketone histone deacetylase inhibitors with antitumor activity in vivo.
AID1727730Inhibition of HDAC6 (unknown origin) by fluorescence based assay2021European journal of medicinal chemistry, Jan-01, Volume: 209Discovery of selective HDAC/BRD4 dual inhibitors as epigenetic probes.
AID374819Inhibition of wild type His-tagged HDAC5 catalytic domain T678-L1122 expressed in Escherichia coli2009Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
Discovery of a potent class I selective ketone histone deacetylase inhibitor with antitumor activity in vivo and optimized pharmacokinetic properties.
AID1586082Inhibition of human HDAC7 using Boc-Lys(trifluoroacetyl)-AMC as substrate by fluorescence assay2019European journal of medicinal chemistry, Jan-15, Volume: 1621-Arylsulfonyl indoline-benzamides as a new antitubulin agents, with inhibition of histone deacetylase.
AID1846958Antiproliferative activity against human A549 cells assessed as inhibition of cell viability measured for 48 hrs by microplate reader based CCK-8 assay
AID313734Inhibition of HDAC62008Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2
Optimization of biaryl Selective HDAC1&2 Inhibitors (SHI-1:2).
AID1231813Antiproliferative activity against human NCI-H661 cells incubated for 72 hrs by MTT assay2015Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13
Discovery, bioactivity and docking simulation of Vorinostat analogues containing 1,2,4-oxadiazole moiety as potent histone deacetylase inhibitors and antitumor agents.
AID1293875Inhibition of HDAC in human HeLa cells using Boc-Lys(AC)-AMC as substrate after 24 to 48 hrs by spectrofluorometry2016Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
Identification of new quinic acid derivatives as histone deacetylase inhibitors by fluorescence-based cellular assay.
AID328810Antiproliferative activity against human renal epithelial cells by CellTiter-Blue cell viability assay2008Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8
A novel series of potent and selective ketone histone deacetylase inhibitors with antitumor activity in vivo.
AID1586078Inhibition of human HDAC2 using RHKKAc as substrate by fluorescence assay2019European journal of medicinal chemistry, Jan-15, Volume: 1621-Arylsulfonyl indoline-benzamides as a new antitubulin agents, with inhibition of histone deacetylase.
AID1401898Antiproliferative activity against human SMMC7721 cells after 72 hrs by CCK-8 assay2018European journal of medicinal chemistry, Jan-01, Volume: 143Design, synthesis and biological evaluation of novel 2-aminobenzamides containing dithiocarbamate moiety as histone deacetylase inhibitors and potent antitumor agents.
AID1873442Inhibition of full length C-terminal His-tagged HDAC1 (unknown origin) assessed as equilibrium inhibition constant (Ki,1) using (Ac-Leu-Gly-Lys(Ac)-AMC as substrate measured every 30 sec for 60 mins by fluorescence based assay2022ACS medicinal chemistry letters, May-12, Volume: 13, Issue:5
Determination of Slow-Binding HDAC Inhibitor Potency and Subclass Selectivity.
AID1280295Inhibition of KDAC3 in human K562 cells using [3H]acetylated histone as substrate incubated for 10 mins by liquid scintillation counting method2016Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
Design and Synthesis of Simplified Largazole Analogues as Isoform-Selective Human Lysine Deacetylase Inhibitors.
AID1847001Induction of apoptosis in mouse B16-F10 cells assessed as early apoptotic cells at 100 nM incubated for 48 hrs by Annexin V-FITC/PI analysis (Rvb = 1.68 %)
AID777595Effect on HDAC in human HaCaT cells assessed as downregulation of miR-766 at 10 uM after 1 hr by RT-PCR analysis2013ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
Synthesis and Biological Evaluation of the First Example of NO-Donor Histone Deacetylase Inhibitor.
AID488274Inhibition of HDAC22010Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
On the inhibition of histone deacetylase 8.
AID374822Inhibition of C-terminal His-tagged HDAC8 expressed in Escherichia coli2009Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
Discovery of a potent class I selective ketone histone deacetylase inhibitor with antitumor activity in vivo and optimized pharmacokinetic properties.
AID1596077Cytotoxicity against mouse NIH/3T3 cells assessed as reduction in cell viability after 48 hrs by CCK8 assay2019European journal of medicinal chemistry, Jul-01, Volume: 173Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (HDAC) inhibitors.
AID1596050Inhibition of human recombinant His-tagged HDAC2 (1 to 582 residues) expressed in baculovirus infected insect cells using FLUOR DE LYS Green as substrate preincubated for 10 mins followed by substrate addition and measured after 30 mins by fluorescence me2019European journal of medicinal chemistry, Jul-01, Volume: 173Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (HDAC) inhibitors.
AID1466390Antiproliferative activity against human U937 cells after 48 hrs by MTT assay2017European journal of medicinal chemistry, Jul-07, Volume: 134Selective HDAC inhibitors with potent oral activity against leukemia and colorectal cancer: Design, structure-activity relationship and anti-tumor activity study.
AID1486671Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay2017Bioorganic & medicinal chemistry, 08-01, Volume: 25, Issue:15
Design, synthesis and tumor cell growth inhibitory activity of 3-nitro-2H-cheromene derivatives as histone deacetylaes inhibitors.
AID1732160Cytotoxicity against human HeLa cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay2021European journal of medicinal chemistry, Apr-05, Volume: 215CAP rigidification of MS-275 and chidamide leads to enhanced antiproliferative effects mediated through HDAC1, 2 and tubulin polymerization inhibition.
AID1887683Cytotoxicity against human AGS cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay2022European journal of medicinal chemistry, Jan-05, Volume: 227Design, synthesis and biological evaluation of novel o-aminobenzamide derivatives as potential anti-gastric cancer agents in vitro and in vivo.
AID1676595Binding affinity to Ferric ion assessed as performance ratio ratio by measuring product of accounting ratio and retention ratio at 2.55 umol by immobilized metal-ion affinity chromatography2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors.
AID1732166Inhibition of HDAC8 (unknown origin) using fluorogenic-(RHKKAc) as substrate by fluorescence assay2021European journal of medicinal chemistry, Apr-05, Volume: 215CAP rigidification of MS-275 and chidamide leads to enhanced antiproliferative effects mediated through HDAC1, 2 and tubulin polymerization inhibition.
AID1441630Inhibition of recombinant human LTA4H aminopeptidase activity expressed in Escherichia coli BL21 (DE3) pLysS assessed as formation of p-NA from Ala-p-NA preincubated for 10 mins followed by substrate addition measured after 10 mins2017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Drug Repurposing of Histone Deacetylase Inhibitors That Alleviate Neutrophilic Inflammation in Acute Lung Injury and Idiopathic Pulmonary Fibrosis via Inhibiting Leukotriene A4 Hydrolase and Blocking LTB4 Biosynthesis.
AID609492Thermodynamic solubility of the compound at pH 6.82011Bioorganic & medicinal chemistry letters, Aug-15, Volume: 21, Issue:16
The design, synthesis and structure-activity relationships of novel isoindoline-based histone deacetylase inhibitors.
AID1380953Inhibition of HDAC2 (unknown origin) using fluorogenic Boc-Lys(acetyl)-AMC as substrate preincubated for 5 mins followed by substrate addition measured after 30 mins by fluorescence-based assay2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Discovery of Novel Pazopanib-Based HDAC and VEGFR Dual Inhibitors Targeting Cancer Epigenetics and Angiogenesis Simultaneously.
AID329927Inhibition of human HDAC1 in U937 cells assessed as residual activity at 5 uM2008Bioorganic & medicinal chemistry letters, Apr-15, Volume: 18, Issue:8
Novel uracil-based 2-aminoanilide and 2-aminoanilide-like derivatives: histone deacetylase inhibition and in-cell activities.
AID613295Antiproliferative activity against human HCT116 cells assessed as growth inhibition2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Optimization of the in vitro cardiac safety of hydroxamate-based histone deacetylase inhibitors.
AID748113Inhibition of HDAC2 (unknown origin) after 60 mins by fluorescence assay2013Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
Discovery of the first histone deacetylase 6/8 dual inhibitors.
AID1441700Inhibition of recombinant human LTA4H Epoxide Hydrolase expressed in Escherichia coli BL21 (DE3) pLysS at 10 uM preincubated for 10 mins followed by addition of LTA4 as substrate measured after 15 mins by reverse-phase HPLC analysis2017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Drug Repurposing of Histone Deacetylase Inhibitors That Alleviate Neutrophilic Inflammation in Acute Lung Injury and Idiopathic Pulmonary Fibrosis via Inhibiting Leukotriene A4 Hydrolase and Blocking LTB4 Biosynthesis.
AID610090Anticancer activity against human A2780 cells after 72 hrs by MTT assay2011Bioorganic & medicinal chemistry letters, Aug-15, Volume: 21, Issue:16
Design, synthesis and docking studies on benzamide derivatives as histone deacetylase inhibitors.
AID1380938Inhibition of HDAC in human HeLa cell nuclear extract using fluorogenic Boc-Lys(acetyl)-AMC as substrate preincubated for 5 mins followed by substrate addition measured after 30 mins by fluorescence-based assay2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Discovery of Novel Pazopanib-Based HDAC and VEGFR Dual Inhibitors Targeting Cancer Epigenetics and Angiogenesis Simultaneously.
AID524995Inhibition of HDAC10 by in vitro deacetylation assay2010Nature chemical biology, Jan, Volume: 6, Issue:1
Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis.
AID1764296Inhibition of HDAC6 in human CAL-27 cells assessed as accumulation of acetylated alpha-tubulin at 1 uM for 24 hrs by Western blot analysis2021European journal of medicinal chemistry, Feb-05, Volume: 211Synergistic induction of apoptosis in resistant head and neck carcinoma and leukemia by alkoxyamide-based histone deacetylase inhibitors.
AID1847002Induction of apoptosis in mouse B16-F10 cells assessed as late apoptotic cells at 100 nM incubated for 48 hrs by Annexin V-FITC/PI analysis (Rvb = 0.00 %)
AID1596048Antiproliferative activity against human HCT116 cells assessed as reduction in cell growth incubated for 72 hrs by CCK-8 assay2019European journal of medicinal chemistry, Jul-01, Volume: 173Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (HDAC) inhibitors.
AID329914Inhibition of human HDAC1 in U937 cells by immunoprecipitation assay2008Bioorganic & medicinal chemistry letters, Apr-15, Volume: 18, Issue:8
Novel uracil-based 2-aminoanilide and 2-aminoanilide-like derivatives: histone deacetylase inhibition and in-cell activities.
AID1466408Induction of apoptosis in human HL60 cells assessed as decrease in procaspase-3 level at 5 uM after 48 hrs by Western blot analysis2017European journal of medicinal chemistry, Jul-07, Volume: 134Selective HDAC inhibitors with potent oral activity against leukemia and colorectal cancer: Design, structure-activity relationship and anti-tumor activity study.
AID328832Toxicity in ip dosed BALB/c mouse assessed as maximum tolerated dose2008Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8
A novel series of potent and selective ketone histone deacetylase inhibitors with antitumor activity in vivo.
AID1847000Induction of apoptosis in mouse B16-F10 cells assessed as viable cells at 100 nM incubated for 48 hrs by Annexin V-FITC/PI analysis (Rvb = 98.3 %)
AID1879890Inhibition of recombinant human HDAC1 using ZMAL (Z-(Ac)Lys-AMC as substrate incubated for 20 mins and measured by homogenous fluorescence assay2022European journal of medicinal chemistry, Apr-15, Volume: 234Identification of histone deacetylase 10 (HDAC10) inhibitors that modulate autophagy in transformed cells.
AID777600Effect on HDAC in human HaCaT cells assessed as upregulation of miR-21# at 10 uM after 1 hr by RT-PCR analysis2013ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
Synthesis and Biological Evaluation of the First Example of NO-Donor Histone Deacetylase Inhibitor.
AID1466413Toxicity in BALB/c nude mouse xenografted with human U937 cells assessed as body weight loss at 100 mg/kg/day administered via oral gavage for 13 days2017European journal of medicinal chemistry, Jul-07, Volume: 134Selective HDAC inhibitors with potent oral activity against leukemia and colorectal cancer: Design, structure-activity relationship and anti-tumor activity study.
AID364644Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay2008Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17
Design, synthesis and biological evaluation of novel compounds with conjugated structure as anti-tumor agents.
AID777590Effect on HDAC in human HaCaT cells assessed as upregulation of miR-1227 at 10 uM after 1 hr by RT-PCR analysis2013ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
Synthesis and Biological Evaluation of the First Example of NO-Donor Histone Deacetylase Inhibitor.
AID1203893Antiproliferative activity against human A549 cells assessed as inhibition of cell growth after 72 hrs by MTT-based assay2015European journal of medicinal chemistry, , Volume: 96Discovery and preliminary evaluation of 2-aminobenzamide and hydroxamate derivatives containing 1,2,4-oxadiazole moiety as potent histone deacetylase inhibitors.
AID1548296Induction of apoptosis in bortezomib resistant human KM3/BTZ cells assessed as viable cells level at 200 nM incubated for 24 hrs in presence of bortezomib by Annexin V-FITC/PI staining based FCAS analysis (Rvb = 98.1%)
AID1486674Inhibition of HDAC1 (unknown origin) at 10 uM using Ac-Leu-GlyLys(Ac)-AMC as substrate preincubated for 10 mins followed by substrate addition measured after 30 mins by fluorescence analysis2017Bioorganic & medicinal chemistry, 08-01, Volume: 25, Issue:15
Design, synthesis and tumor cell growth inhibitory activity of 3-nitro-2H-cheromene derivatives as histone deacetylaes inhibitors.
AID1888465Anti-androgenic activity at androgen receptor (unknown origin) expressed in HEK293 cells by BRET assay2022Bioorganic & medicinal chemistry letters, 01-01, Volume: 55Dual-function antiandrogen/HDACi hybrids based on enzalutamide and entinostat.
AID1525779Inhibition of HADC3 (unknown origin)2020Journal of medicinal chemistry, 01-09, Volume: 63, Issue:1
Old but Gold: Tracking the New Guise of Histone Deacetylase 6 (HDAC6) Enzyme as a Biomarker and Therapeutic Target in Rare Diseases.
AID1676601Binding affinity to Zinc ion assessed as retention ratio by measuring compound detected in elution fraction/total compound detected at 2.55 umol by immobilized metal-ion affinity chromatography2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors.
AID80683In vitro antiproliferative activity against human cancer cell line HCT116 using MTT assay2004Bioorganic & medicinal chemistry letters, Jan-05, Volume: 14, Issue:1
(2-amino-phenyl)-amides of omega-substituted alkanoic acids as new histone deacetylase inhibitors.
AID1586085Inhibition of human HDAC10 using RHKKAc as substrate by fluorescence assay2019European journal of medicinal chemistry, Jan-15, Volume: 1621-Arylsulfonyl indoline-benzamides as a new antitubulin agents, with inhibition of histone deacetylase.
AID1466393Antiproliferative activity against human ES2 cells after 48 hrs by MTT assay2017European journal of medicinal chemistry, Jul-07, Volume: 134Selective HDAC inhibitors with potent oral activity against leukemia and colorectal cancer: Design, structure-activity relationship and anti-tumor activity study.
AID385692Inhibition of HDAC4 catalytic domain expressed in HEK293 cells upto 10,000 nM by Biomol assay2007Proceedings of the National Academy of Sciences of the United States of America, Oct-30, Volume: 104, Issue:44
Unraveling the hidden catalytic activity of vertebrate class IIa histone deacetylases.
AID525025Inhibition of HDAC in human CFBE41o- cell line assessed as increase in CFTR mRNA at 0.1 uM by RT-PCR2010Nature chemical biology, Jan, Volume: 6, Issue:1
Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis.
AID1380948Antiproliferative activity against human HEL cells after 72 hrs by MTT assay2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Discovery of Novel Pazopanib-Based HDAC and VEGFR Dual Inhibitors Targeting Cancer Epigenetics and Angiogenesis Simultaneously.
AID610088Anticancer activity against human MDA-MB-231 cells after 72 hrs by MTT assay2011Bioorganic & medicinal chemistry letters, Aug-15, Volume: 21, Issue:16
Design, synthesis and docking studies on benzamide derivatives as histone deacetylase inhibitors.
AID1486675Inhibition of HDAC2 (unknown origin) at 10 uM using Ac-Leu-GlyLys(Ac)-AMC as substrate preincubated for 10 mins followed by substrate addition measured after 30 mins by fluorescence analysis2017Bioorganic & medicinal chemistry, 08-01, Volume: 25, Issue:15
Design, synthesis and tumor cell growth inhibitory activity of 3-nitro-2H-cheromene derivatives as histone deacetylaes inhibitors.
AID764212Inhibition of human recombinant HDAC6 using p53 residues 379-382 (RHKKAc) as substrate2013Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
Novel N-hydroxyfurylacrylamide-based histone deacetylase (HDAC) inhibitors with branched CAP group (Part 2).
AID1453365Inhibition of HDAC3 (unknown origin) using Boc-Lys (acetyl)-AMC as substrate preincubated for 1 hr followed by substrate addition measured after 1 hr by fluorescence assay2017Bioorganic & medicinal chemistry, 06-15, Volume: 25, Issue:12
Design, synthesis and anti-tumor activity study of novel histone deacetylase inhibitors containing isatin-based caps and o-phenylenediamine-based zinc binding groups.
AID1556401Inhibition of human recombinant C-terminal His-tagged HDAC3/NCOR2 using Boc-Lys-(epsilon-Ac)-AMC as fluorogenic substrate incubated for 90 mins by fluorescence based assay2019European journal of medicinal chemistry, Sep-01, Volume: 177Inhibitory selectivity among class I HDACs has a major impact on inflammatory gene expression in macrophages.
AID1901146Inhibition of C-terminal His-tagged human HDAC3 (1 to 428 residues)/N-terminal GST tagged human NCOR2 (395 to 489) expressed in baculovirus infected Sf9 insect cells using fluorogenic HDAC substrate measured after 30 mins by fluorimetry2022Bioorganic & medicinal chemistry, 02-15, Volume: 56Synthesis and biological evaluation of aminobenzamides containing purine moiety as class I histone deacetylases inhibitors.
AID519589Toxicity in human WI38 cells2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Potent antimalarial activity of histone deacetylase inhibitor analogues.
AID1737644Inhibition of human recombinant HDAC1 expressed in baculovirus using fluorogenic peptide p53 residues 379-382 (RHKK(Ac)AMC) as substrate by Fluorescence analysis
AID1294943Inhibition of HDAC in human HeLa cells using fluor de Lys as substrate incubated for 20 mins by microplate spectrofluorometric analysis2016European journal of medicinal chemistry, Jun-30, Volume: 116Computer-aided identification of new histone deacetylase 6 selective inhibitor with anti-sepsis activity.
AID1917927Inhibition of HDAC2 (unknown origin)2022Bioorganic & medicinal chemistry letters, 11-15, Volume: 76Zinc-dependent deacetylases (HDACs) as potential targets for treating Alzheimer's disease.
AID777598Effect on HDAC in human HaCaT cells assessed as downregulation of miR-935 at 10 uM after 1 hr by RT-PCR analysis2013ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
Synthesis and Biological Evaluation of the First Example of NO-Donor Histone Deacetylase Inhibitor.
AID1541444Inhibition of human recombinant full length C-terminal His-tagged HDAC3 (1 to 428 residues)/N-terminal GST-tagged NCOR2 (395 to 489 residues) expressed in baculovirus infected Sf9 insect cells using Boc-Lys(epsilon-acetyl)-AMC as substrate incubated for 92019Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
Synthesis of Peptoid-Based Class I-Selective Histone Deacetylase Inhibitors with Chemosensitizing Properties.
AID329918Induction of p21 expression in human U937 cells2008Bioorganic & medicinal chemistry letters, Apr-15, Volume: 18, Issue:8
Novel uracil-based 2-aminoanilide and 2-aminoanilide-like derivatives: histone deacetylase inhibition and in-cell activities.
AID1403468Cytotoxicity against human HaCaT cells assessed as increase in dead cells 0.1 to 100 uM after 72 hrs by Trypan Blue-based assay2018European journal of medicinal chemistry, Jan-20, Volume: 144Structural and biological characterization of new hybrid drugs joining an HDAC inhibitor to different NO-donors.
AID329926Induction of granulocytic differentiation in human U937 cells assessed as CD11c expression at 5 uM after 30 hrs2008Bioorganic & medicinal chemistry letters, Apr-15, Volume: 18, Issue:8
Novel uracil-based 2-aminoanilide and 2-aminoanilide-like derivatives: histone deacetylase inhibition and in-cell activities.
AID524997Inhibition of HDAC7 by in vitro deacetylation assay2010Nature chemical biology, Jan, Volume: 6, Issue:1
Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis.
AID1847023Cardiotoxicity in C57BL/6 mouse ssessed as shortening of QTc level by ECG analysis
AID1548732Inhibition of recombinant full length human C-terminal His-tagged HDAC8 expressed in baculovirus infected Sf9 cells using Boc-Lys (trifluoroacetyl)-AMC as substrate preincubated for 1 hr followed by substrate addition and measured after 2 hrs by fluoresce2020Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
Design of Hydrazide-Bearing HDACIs Based on Panobinostat and Their p53 and FLT3-ITD Dependency in Antileukemia Activity.
AID1873472Inhibition of full length C-terminal FLAG-tagged HDAC2 (unknown origin) assessed as dissociation half-life of EI complex using (Ac-Leu-Gly-Lys(Ac)-AMC as substrate measured every 30 sec for 60 mins by fluorescence based assay2022ACS medicinal chemistry letters, May-12, Volume: 13, Issue:5
Determination of Slow-Binding HDAC Inhibitor Potency and Subclass Selectivity.
AID1474453Inhibition of HDAC in human A2780 cells using Boc-Lys (epsilon-Ac)-AMC as substrate pretreated for 18 hrs followed by substrate addition after 3 hrs by fluorescence assay2017European journal of medicinal chemistry, May-26, Volume: 132Design, synthesis and biological evaluation of novel coumarin-based benzamides as potent histone deacetylase inhibitors and anticancer agents.
AID274110Inhibition of HDAC1 (mean IC50)2006Bioorganic & medicinal chemistry letters, Dec-01, Volume: 16, Issue:23
A series of novel, potent, and selective histone deacetylase inhibitors.
AID1578490Inhibition of recombinant human HDAC9 (604-1066 residues) expressed in baculovirus infected Sf9 cells using FAM-RHKK-TFAc as substrate incubated for 3 hrs by electrophoretic mobility shift assay2020ACS medicinal chemistry letters, Jan-09, Volume: 11, Issue:1
Class I/IIb-Selective HDAC Inhibitor Exhibits Oral Bioavailability and Therapeutic Efficacy in Acute Myeloid Leukemia.
AID313729Inhibition of HDAC12008Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2
Optimization of biaryl Selective HDAC1&2 Inhibitors (SHI-1:2).
AID1486677Inhibition of HDAC1 (unknown origin) using Ac-Leu-GlyLys(Ac)-AMC as substrate preincubated for 10 mins followed by substrate addition measured after 30 mins by fluorescence analysis2017Bioorganic & medicinal chemistry, 08-01, Volume: 25, Issue:15
Design, synthesis and tumor cell growth inhibitory activity of 3-nitro-2H-cheromene derivatives as histone deacetylaes inhibitors.
AID1737663Induction of cell cycle arrest in human MDA-MB-231 cells assessed as reduction in population between G1 to G2/M phases at 4 uM for 24 hrs by PI staining based flow cytometry analysis
AID1901156Inhibition of HDAC4 (unknown origin) using FAM-RHKK(Ac)-NH2/FAM-RHKK(trifluoroacetyl)-NH2 as substrate preincubated for 15 mins followed by substrate addition and measured after 3 hrs by microfluidic chip based fluorescence assay2022Bioorganic & medicinal chemistry, 02-15, Volume: 56Synthesis and biological evaluation of aminobenzamides containing purine moiety as class I histone deacetylases inhibitors.
AID1530563Antiplasmodial activity against asynchronous form of Plasmodium falciparum 3D7 infected in human erythrocytes assessed as parasite growth inhibition after 48 hrs by SYBR green1 staining based flow cytometry2019European journal of medicinal chemistry, Jan-01, Volume: 161Identification of novel quinazoline derivatives as potent antiplasmodial agents.
AID1846997Induction of cell cycle arrest in mouse B16-F10 cells assessed as accumulation of cells in G2/M phase at 100 nM measured after 48 hrs by PI/RNaseA staining based flow cytometry analysis (Rvb= 5.76%)
AID1466055Inhibition of recombinant human full length HDAC2 using Fluor-de-Lys as substrate after 60 mins by spectrofluorimetric analysis2017European journal of medicinal chemistry, Jul-07, Volume: 1344-Indolyl-N-hydroxyphenylacrylamides as potent HDAC class I and IIB inhibitors in vitro and in vivo.
AID1548892Induction of apoptosis in human MV4-11 cells harboring wild type p53/FLT3-ITD mutant assessed as cleavage of pro-caspase 3 at 1000 to 5000 nM after 24 hrs by Western blot analysis2020Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
Design of Hydrazide-Bearing HDACIs Based on Panobinostat and Their p53 and FLT3-ITD Dependency in Antileukemia Activity.
AID385436Inhibition of LPS-induced tissue factor activity in HUVEC at 30 uM preincubated for 4 hrs assessed after 4 hrs of LPS challenge by one stage clotting assay2007The Journal of biological chemistry, Sep-28, Volume: 282, Issue:39
Histone deacetylase inhibitors suppress TF-kappaB-dependent agonist-driven tissue factor expression in endothelial cells and monocytes.
AID328793Inhibition of HDAC12008Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8
A novel series of potent and selective ketone histone deacetylase inhibitors with antitumor activity in vivo.
AID1486676Inhibition of HDAC6 (unknown origin) at 10 uM using Ac-Leu-GlyLys(Ac)-AMC as substrate preincubated for 10 mins followed by substrate addition measured after 30 mins by fluorescence analysis2017Bioorganic & medicinal chemistry, 08-01, Volume: 25, Issue:15
Design, synthesis and tumor cell growth inhibitory activity of 3-nitro-2H-cheromene derivatives as histone deacetylaes inhibitors.
AID1596069Induction of apoptosis in human SMMC7721 cells assessed as early apoptotic cells at 1 uM incubated for 48 hrs by Annexin-V-FITC/propidium iodide staining based flow cytometry (Rvb=2.88%)2019European journal of medicinal chemistry, Jul-01, Volume: 173Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (HDAC) inhibitors.
AID1847015Antitumor activity against mouse B16-F10 cells allografted in C57BL/6 mouse assessed as reduction in tumor weight at 10 mg/kg, ip administered for 14 days in presence of (2-phenylthiazol-4-yl)(3,4,5-trimethoxyphenyl)methanone
AID1401913Induction of apoptosis in human SMMC7721 cells assessed as early apoptotic cells at 1 umol/L after 72 hrs by Alexa Fluor 488 Annexin/propidium iodide staining-based flow cytometric analysis (Rvb = 0.09%)2018European journal of medicinal chemistry, Jan-01, Volume: 143Design, synthesis and biological evaluation of novel 2-aminobenzamides containing dithiocarbamate moiety as histone deacetylase inhibitors and potent antitumor agents.
AID1431819Selectivity ratio of IC50 for human KDAC3 to IC50 for human KDAC82017European journal of medicinal chemistry, Feb-15, Volume: 127Design and synthesis of benzodiazepine analogs as isoform-selective human lysine deacetylase inhibitors.
AID1737642Cytotoxicity in human MDA-MB-468 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
AID609498Half life in human liver microsomes2011Bioorganic & medicinal chemistry letters, Aug-15, Volume: 21, Issue:16
The design, synthesis and structure-activity relationships of novel isoindoline-based histone deacetylase inhibitors.
AID1691039Inhibition of human recombinant HDAC3/NCOR2 using RHKKAc-AMC as substrate measured after 60 mins by fluorescence assay
AID1401918Induction of apoptosis in human SMMC7721 cells assessed as late apoptotic cells at 4 umol/L after 72 hrs by Alexa Fluor 488 Annexin/propidium iodide staining-based flow cytometric analysis (Rvb = 0.29%)2018European journal of medicinal chemistry, Jan-01, Volume: 143Design, synthesis and biological evaluation of novel 2-aminobenzamides containing dithiocarbamate moiety as histone deacetylase inhibitors and potent antitumor agents.
AID708272Growth inhibition of human SGC7901 cells incubated for 72 hrs by WST dye reduction assay2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Pharmacokinetic optimization of class-selective histone deacetylase inhibitors and identification of associated candidate predictive biomarkers of hepatocellular carcinoma tumor response.
AID1380954Inhibition of HDAC3 (unknown origin) using fluorogenic Boc-Lys(acetyl)-AMC as substrate preincubated for 5 mins followed by substrate addition measured after 30 mins by fluorescence-based assay2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Discovery of Novel Pazopanib-Based HDAC and VEGFR Dual Inhibitors Targeting Cancer Epigenetics and Angiogenesis Simultaneously.
AID1401927Cell cycle arrest in human SMMC7721 cells assessed as accumulation of cells at S phase at 4 umol/L after 72 hrs by propidium iodide staining-based flow cytometric analysis (Rvb = 5.21%)2018European journal of medicinal chemistry, Jan-01, Volume: 143Design, synthesis and biological evaluation of novel 2-aminobenzamides containing dithiocarbamate moiety as histone deacetylase inhibitors and potent antitumor agents.
AID1732168Antiproliferative activity against HDACi-sensitive human YCC-11 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay2021European journal of medicinal chemistry, Apr-05, Volume: 215CAP rigidification of MS-275 and chidamide leads to enhanced antiproliferative effects mediated through HDAC1, 2 and tubulin polymerization inhibition.
AID329922Inhibition of human HDAC4 in U937 cells at 5 uM2008Bioorganic & medicinal chemistry letters, Apr-15, Volume: 18, Issue:8
Novel uracil-based 2-aminoanilide and 2-aminoanilide-like derivatives: histone deacetylase inhibition and in-cell activities.
AID1596052Selectivity ratio of IC50 for human recombinant His-tagged HDAC6 expressed in baculovirus infected insect cells to IC50 of human recombinant His-tagged HDAC2 (1 to 582 residues) expressed in baculovirus infected insect cells2019European journal of medicinal chemistry, Jul-01, Volume: 173Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (HDAC) inhibitors.
AID1737656Cytotoxicity against human KG -1 cells assessed as inhibition of cell viability incubated for 72 hrs by MTS assay
AID650221Induction of cell cycle arrest in human HCT116 cells assessed as accumulation at G0/G1 phase at 10 uM after 48 hrs by flow cytometry (Rvb = 81.9 %)2012Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
Anti-tumor activity of new orally bioavailable 2-amino-5-(thiophen-2-yl)benzamide-series histone deacetylase inhibitors, possessing an aqueous soluble functional group as a surface recognition domain.
AID78450Tested for antiproliferative activity against HCT116 colorectal human carcinoma cell using WST-1 assay2002Bioorganic & medicinal chemistry letters, May-20, Volume: 12, Issue:10
Novel histone deacetylase inhibitors: N-hydroxycarboxamides possessing a terminal bicyclic aryl group.
AID1466401Antitumor activity against human HCT116 cells xenografted in BALB/c nude mouse assessed as tumor growth inhibition at 50 mg/kg/day administered via oral gavage for 16 days measured every 3 days2017European journal of medicinal chemistry, Jul-07, Volume: 134Selective HDAC inhibitors with potent oral activity against leukemia and colorectal cancer: Design, structure-activity relationship and anti-tumor activity study.
AID316891Inhibition of HDAC2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Histone deacetylase inhibitors: from bench to clinic.
AID1882459Displacement of [3H]-acetylated histones HDAC6 derived from human K562 cell nuclear extract incubated for 10 mins by liquid scintillation counting method2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Chasing a Breath of Fresh Air in Cystic Fibrosis (CF): Therapeutic Potential of Selective HDAC6 Inhibitors to Tackle Multiple Pathways in CF Pathophysiology.
AID1887682Cytotoxicity against human SGC-7901 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay2022European journal of medicinal chemistry, Jan-05, Volume: 227Design, synthesis and biological evaluation of novel o-aminobenzamide derivatives as potential anti-gastric cancer agents in vitro and in vivo.
AID650230Antiproliferative activity against human HCT116 cells after 3 days by WST-1 assay2012Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
Anti-tumor activity of new orally bioavailable 2-amino-5-(thiophen-2-yl)benzamide-series histone deacetylase inhibitors, possessing an aqueous soluble functional group as a surface recognition domain.
AID73169Inhibitory concentration against normal fibroblast MRHF cell line2003Journal of medicinal chemistry, Feb-27, Volume: 46, Issue:5
Development of potential antitumor agents. Synthesis and biological evaluation of a new set of sulfonamide derivatives as histone deacetylase inhibitors.
AID1846962Antiproliferative activity against human YCC3/7 cells assessed as inhibition of cell viability
AID1887690Cytotoxicity against human HGC-27 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay2022European journal of medicinal chemistry, Jan-05, Volume: 227Design, synthesis and biological evaluation of novel o-aminobenzamide derivatives as potential anti-gastric cancer agents in vitro and in vivo.
AID708279Growth inhibition of human SMMC7721 cells incubated for 72 hrs by WST dye reduction assay2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Pharmacokinetic optimization of class-selective histone deacetylase inhibitors and identification of associated candidate predictive biomarkers of hepatocellular carcinoma tumor response.
AID650227Solubility of the compound in 10 % DMSO/Water2012Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
Anti-tumor activity of new orally bioavailable 2-amino-5-(thiophen-2-yl)benzamide-series histone deacetylase inhibitors, possessing an aqueous soluble functional group as a surface recognition domain.
AID316895Inhibition of human MCF7 cells2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Histone deacetylase inhibitors: from bench to clinic.
AID664379Inhibition of HDAC12012European journal of medicinal chemistry, Jul, Volume: 53Appraisal of GABA and PABA as linker: design and synthesis of novel benzamide based histone deacetylase inhibitors.
AID313733Inhibition of HDAC52008Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2
Optimization of biaryl Selective HDAC1&2 Inhibitors (SHI-1:2).
AID313732Inhibition of HDAC42008Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2
Optimization of biaryl Selective HDAC1&2 Inhibitors (SHI-1:2).
AID90349Inhibitory activity against Histone deacetylase (HDAC) from SNU-16 (human gastric adenocarcinoma) cells2003Journal of medicinal chemistry, Dec-18, Volume: 46, Issue:26
Synthesis and biological evaluation of 3-(4-substituted-phenyl)-N-hydroxy-2-propenamides, a new class of histone deacetylase inhibitors.
AID1873441Inhibition of full length C-terminal FLAG-tagged HDAC2 (unknown origin) assessed as equilibrium inhibition constant (Ki,1) using (Ac-Leu-Gly-Lys(Ac)-AMC as substrate measured every 30 sec for 60 mins by fluorescence based assay2022ACS medicinal chemistry letters, May-12, Volume: 13, Issue:5
Determination of Slow-Binding HDAC Inhibitor Potency and Subclass Selectivity.
AID1881853Inhibition of HDAC1 (unknown origin)2022European journal of medicinal chemistry, Jan-05, Volume: 227NO-HDAC dual inhibitors.
AID1740014Inhibition of recombinant human HDAC3 using pan-HDAC substrate incubated for 3 hrs by fluorescence method2020Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
Thirty Years of HDAC Inhibitors: 2020 Insight and Hindsight.
AID1548244Inhibition of HDAC1/2 in human HeLa cell nuclear extracts pre-incubated for 5 mins before fluorogenic substrate Boc-Lys (acetyl)-AMC or Boc-Lys (triflouroacetyl)-AMC addition and measured after 30 mins by fluorescence based assay
AID1732191Cytotoxicity against human HuT78 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay2021European journal of medicinal chemistry, Apr-05, Volume: 215CAP rigidification of MS-275 and chidamide leads to enhanced antiproliferative effects mediated through HDAC1, 2 and tubulin polymerization inhibition.
AID1308514Inhibition of human BRD4 expressed in Escherichia coli BL21(DE3)-R3-pRARE2 by bromodomain alphascreen peptide displacement assay2016Bioorganic & medicinal chemistry letters, 06-15, Volume: 26, Issue:12
Targeting epigenetic reader and eraser: Rational design, synthesis and in vitro evaluation of dimethylisoxazoles derivatives as BRD4/HDAC dual inhibitors.
AID1380968Inhibition of VEGF-stimulated VEGFR2 phosphorylation in human HUVEC cells at 100 nM preincubated for 2 hrs followed by VEGF stimulation by Western blot analysis2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Discovery of Novel Pazopanib-Based HDAC and VEGFR Dual Inhibitors Targeting Cancer Epigenetics and Angiogenesis Simultaneously.
AID1541558Inhibition of HDAC6 in human Cal27CisR cells assessed as acetylation of alpha-tubulin at 1 uM measured after 24 hrs by immunoblot analysis2019Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
Synthesis of Peptoid-Based Class I-Selective Histone Deacetylase Inhibitors with Chemosensitizing Properties.
AID1403469Cytotoxicity against mouse C2C12 cells assessed as increase in dead cells 0.5 to 10 uM after 72 hrs by Trypan Blue-based assay2018European journal of medicinal chemistry, Jan-20, Volume: 144Structural and biological characterization of new hybrid drugs joining an HDAC inhibitor to different NO-donors.
AID1596080Inhibition of HDAC in human HeLa cell nuclear extract using fluor-de-lys-green as substrate preincubated for 10 mins followed by substrate addition and measured after 30 mins by fluorescence assay2019European journal of medicinal chemistry, Jul-01, Volume: 173Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (HDAC) inhibitors.
AID1556399Inhibition of human recombinant C-terminal His/FLAG-tagged HDAC1 using Boc-Lys-(epsilon-Ac)-AMC as fluorogenic substrate incubated for 90 mins by fluorescence based assay2019European journal of medicinal chemistry, Sep-01, Volume: 177Inhibitory selectivity among class I HDACs has a major impact on inflammatory gene expression in macrophages.
AID525022Inhibition of HDAC in human CFBE41o- cell line assessed as increase in total CFTR protein level including CFTR glycoform at 0.1 uM by immunoblot analysis2010Nature chemical biology, Jan, Volume: 6, Issue:1
Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis.
AID1403455Inhibition of FLAG-tagged HDAC2 (unknown origin) expressed in HEK293T cells using acetylated lysine side chain as substrate after 1 hr by colorimetric detection based assay2018European journal of medicinal chemistry, Jan-20, Volume: 144Structural and biological characterization of new hybrid drugs joining an HDAC inhibitor to different NO-donors.
AID1453357Antiproliferative activity against human MOLT4 cells after 48 hrs by MTT assay2017Bioorganic & medicinal chemistry, 06-15, Volume: 25, Issue:12
Design, synthesis and anti-tumor activity study of novel histone deacetylase inhibitors containing isatin-based caps and o-phenylenediamine-based zinc binding groups.
AID414980Inhibition of Plasmodium falciparum HDAC1 expressed in Drosophila melanogaster S2 cells2009Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
Identification and characterization of small molecule inhibitors of a class I histone deacetylase from Plasmodium falciparum.
AID1474455Antiproliferative activity against human A549 cells after 48 hrs by MTT assay2017European journal of medicinal chemistry, May-26, Volume: 132Design, synthesis and biological evaluation of novel coumarin-based benzamides as potent histone deacetylase inhibitors and anticancer agents.
AID1676602Binding affinity to ferric ion assessed as accounting ratio by measuring total compound detected/total compound adsorbed at 2.55 umol by immobilized metal-ion affinity chromatography2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors.
AID1691038Inhibition of recombinant human C-terminal GST-tagged HDAC2 (1 to 488 residues) expressed in baculovirus infected insect cells using RHKKAc-AMC as substrate measured after 60 mins by fluorescence assay
AID1737647Inhibition of human recombinant HDAC8 expressed in baculovirus using fluorogenic peptide p53 residues 379-382 (RHKK(Ac)AMC) as substrate by Fluorescence analysis
AID708273Growth inhibition of human MGC803 cells incubated for 72 hrs by WST dye reduction assay2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Pharmacokinetic optimization of class-selective histone deacetylase inhibitors and identification of associated candidate predictive biomarkers of hepatocellular carcinoma tumor response.
AID1901160Antiproliferative activity against human HepG2 cells measured after 48 hrs by MTT assay2022Bioorganic & medicinal chemistry, 02-15, Volume: 56Synthesis and biological evaluation of aminobenzamides containing purine moiety as class I histone deacetylases inhibitors.
AID1380940Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Discovery of Novel Pazopanib-Based HDAC and VEGFR Dual Inhibitors Targeting Cancer Epigenetics and Angiogenesis Simultaneously.
AID1596072Induction of apoptosis in human SMMC7721 cells assessed as viable cells at 4 uM incubated for 48 hrs by Annexin-V-FITC/propidium iodide staining based flow cytometry (Rvb=93.5%)2019European journal of medicinal chemistry, Jul-01, Volume: 173Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (HDAC) inhibitors.
AID1596041Antiproliferative activity against human HCT116 cells assessed as reduction in cell growth at 8 uM incubated for 72 hrs by CCK-8 assay relative to control2019European journal of medicinal chemistry, Jul-01, Volume: 173Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (HDAC) inhibitors.
AID1901166Inhibition of HDAC1/HDAC2/HDAC3 in human HCT-116 cells assessed as increase in accumulation of acetylated H3K9 at 5 uM measured after 24 hrs by Western blot analysis2022Bioorganic & medicinal chemistry, 02-15, Volume: 56Synthesis and biological evaluation of aminobenzamides containing purine moiety as class I histone deacetylases inhibitors.
AID292437Antiproliferative activity against HeLa cells by alamar blue assay2007Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
Trithiocarbonates: exploration of a new head group for HDAC inhibitors.
AID1479838Cell cycle arrest in human MV4-11 cells assessed as accumulation at sub-G1 phase at 5 uM after 24 hrs by propidium iodide staining-based flow cytometric method2018Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
Marbostat-100 Defines a New Class of Potent and Selective Antiinflammatory and Antirheumatic Histone Deacetylase 6 Inhibitors.
AID1431822Selectivity ratio of IC50 for human KDAC1 to IC50 for human KDAC62017European journal of medicinal chemistry, Feb-15, Volume: 127Design and synthesis of benzodiazepine analogs as isoform-selective human lysine deacetylase inhibitors.
AID1737657Cytotoxicity against human THP-1 cells assessed as inhibition of cell viability incubated for 72 hrs by MTS assay
AID1596033Antiproliferative activity against human SMMC7721 cells assessed as reduction in cell growth incubated for 72 hrs by CCK-8 assay2019European journal of medicinal chemistry, Jul-01, Volume: 173Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (HDAC) inhibitors.
AID1474461Inhibition of HDAC1 (unknown origin) using deacetylase fluorogenic substrate pretreated for 5 mins followed by substrate addition after 30 mins by fluorescence assay2017European journal of medicinal chemistry, May-26, Volume: 132Design, synthesis and biological evaluation of novel coumarin-based benzamides as potent histone deacetylase inhibitors and anticancer agents.
AID1676589Binding affinity to Nickel cation assessed as performance ratio ratio by measuring product of accounting ratio and retention ratio at 2.55 umol by immobilized metal-ion affinity chromatography2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors.
AID1441632Binding affinity to recombinant human LTA4H hydrolase assessed as change in melting temperature at 50 uM by SYPRO orange dye-based thermofluor assay2017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Drug Repurposing of Histone Deacetylase Inhibitors That Alleviate Neutrophilic Inflammation in Acute Lung Injury and Idiopathic Pulmonary Fibrosis via Inhibiting Leukotriene A4 Hydrolase and Blocking LTB4 Biosynthesis.
AID1181308Inhibition of HDAC1 in human U937 cells assessed as increase in p21WAF1/CIP1 level at 5 uM by Western blotting method2014Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
1,3,4-Oxadiazole-containing histone deacetylase inhibitors: anticancer activities in cancer cells.
AID1403456Inhibition of human FLAG-tagged HDAC3 expressed in HEK293T cells using acetylated lysine side chain as substrate after 1 hr by colorimetric detection based assay2018European journal of medicinal chemistry, Jan-20, Volume: 144Structural and biological characterization of new hybrid drugs joining an HDAC inhibitor to different NO-donors.
AID1578485Inhibition of recombinant full length human HDAC1 expressed in baculovirus infected Sf9 cells using FAM-RHKK-Ac as substrate incubated for 17 hrs by electrophoretic mobility shift assay2020ACS medicinal chemistry letters, Jan-09, Volume: 11, Issue:1
Class I/IIb-Selective HDAC Inhibitor Exhibits Oral Bioavailability and Therapeutic Efficacy in Acute Myeloid Leukemia.
AID492813Inhibition of HDAC in human NB4 cells assessed as increase in histone H3 acetylation at 5 uM after 24 hrs by Western blot analysis2010Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12
Synthesis and biological characterization of the histone deacetylase inhibitor largazole and C7- modified analogues.
AID328828Antitumor activity against human HCT116 cells xenografted BALB/c mouse assessed as tumor growth inhibition at 60 mg/kg, ip administered for 5 days per week for 2.5 weeks2008Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8
A novel series of potent and selective ketone histone deacetylase inhibitors with antitumor activity in vivo.
AID1846971Inhibition of recombinant HDAC1 (unknown origin) at 1 uM
AID609489Inhibition of purified recombinant HDAC12011Bioorganic & medicinal chemistry letters, Aug-15, Volume: 21, Issue:16
The design, synthesis and structure-activity relationships of novel isoindoline-based histone deacetylase inhibitors.
AID93030Effect on induced hyperacetylation of histones in whole cells2004Bioorganic & medicinal chemistry letters, Jan-05, Volume: 14, Issue:1
(2-amino-phenyl)-amides of omega-substituted alkanoic acids as new histone deacetylase inhibitors.
AID664382Inhibition of HDAC42012European journal of medicinal chemistry, Jul, Volume: 53Appraisal of GABA and PABA as linker: design and synthesis of novel benzamide based histone deacetylase inhibitors.
AID1401922Cell cycle arrest in human SMMC7721 cells assessed as accumulation of cells at G2/M phase at 0.125 umol/L after 72 hrs by propidium iodide staining-based flow cytometric analysis (Rvb = 14.14%)2018European journal of medicinal chemistry, Jan-01, Volume: 143Design, synthesis and biological evaluation of novel 2-aminobenzamides containing dithiocarbamate moiety as histone deacetylase inhibitors and potent antitumor agents.
AID286793Increase in histone H3 acetylation in U937 cells at 5 uM after 24 hrs by Western blot analysis2007Journal of medicinal chemistry, May-17, Volume: 50, Issue:10
Bispyridinium dienes: histone deacetylase inhibitors with selective activities.
AID1556406Inhibition of HDAC1/2 in LPS/IFNgamma-stimulated mouse RAW264.7 cells assessed as upregulation of TNF-alpha gene expression at 1 uM pretreated for 16 hrs followed by LPS stimulation and measured after 4 hrs by RT-qPCR analysis2019European journal of medicinal chemistry, Sep-01, Volume: 177Inhibitory selectivity among class I HDACs has a major impact on inflammatory gene expression in macrophages.
AID1401911Induction of apoptosis in human SMMC7721 cells assessed as necrotic cells at 0.125 umol/L after 72 hrs by Alexa Fluor 488 Annexin/propidium iodide staining-based flow cytometric analysis (Rvb = 2.48%)2018European journal of medicinal chemistry, Jan-01, Volume: 143Design, synthesis and biological evaluation of novel 2-aminobenzamides containing dithiocarbamate moiety as histone deacetylase inhibitors and potent antitumor agents.
AID1380945Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Discovery of Novel Pazopanib-Based HDAC and VEGFR Dual Inhibitors Targeting Cancer Epigenetics and Angiogenesis Simultaneously.
AID1873480Inhibition of full length C-terminal His-tagged HDAC3 (unknown origin)/N-terminal GST-tagged NCoR2 (unknown origin) assessed as inhibition constant of EI complex in the first binding step using (Ac-Leu-Gly-Lys(Ac)-AMC as substrate in the presence of inosi2022ACS medicinal chemistry letters, May-12, Volume: 13, Issue:5
Determination of Slow-Binding HDAC Inhibitor Potency and Subclass Selectivity.
AID1732159Cytotoxicity against human MDA-MB-468 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay2021European journal of medicinal chemistry, Apr-05, Volume: 215CAP rigidification of MS-275 and chidamide leads to enhanced antiproliferative effects mediated through HDAC1, 2 and tubulin polymerization inhibition.
AID1596047Antiproliferative activity against human A549 cells assessed as reduction in cell growth incubated for 72 hrs by CCK-8 assay2019European journal of medicinal chemistry, Jul-01, Volume: 173Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (HDAC) inhibitors.
AID1466410Induction of apoptosis in human HL60 cells assessed as increase in cleaved caspase-3 level at 5 uM after 48 hrs by Western blot analysis2017European journal of medicinal chemistry, Jul-07, Volume: 134Selective HDAC inhibitors with potent oral activity against leukemia and colorectal cancer: Design, structure-activity relationship and anti-tumor activity study.
AID488357Cytotoxicity against human HCT116 cells after 3 days by WST-1 assay2010Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
New orally bioavailable 2-aminobenzamide-type histone deacetylase inhibitor possessing a (2-hydroxyethyl)(4-(thiophen-2-yl)benzyl)amino group.
AID609494Inhibition of CYP3A42011Bioorganic & medicinal chemistry letters, Aug-15, Volume: 21, Issue:16
The design, synthesis and structure-activity relationships of novel isoindoline-based histone deacetylase inhibitors.
AID1454684Decrease in alcohol intake in rat model of voluntary heavy drinking assessed as decrease in relapse phenomenon after period of abstinence at 500 uM, icv administered twice relative to control2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Class I HDAC Inhibitors: Potential New Epigenetic Therapeutics for Alcohol Use Disorder (AUD).
AID294382Inhibition of HDAC by fluorescent assay2007Bioorganic & medicinal chemistry letters, Apr-15, Volume: 17, Issue:8
Structural requirements of HDAC inhibitors: SAHA analogs functionalized adjacent to the hydroxamic acid.
AID1486678Inhibition of HDAC2 (unknown origin) using Ac-Leu-GlyLys(Ac)-AMC as substrate preincubated for 10 mins followed by substrate addition measured after 30 mins by fluorescence analysis2017Bioorganic & medicinal chemistry, 08-01, Volume: 25, Issue:15
Design, synthesis and tumor cell growth inhibitory activity of 3-nitro-2H-cheromene derivatives as histone deacetylaes inhibitors.
AID1401890Antiproliferative activity against human MGC803 cells at 8 uM after 72 hrs by CCK-8 assay relative to control2018European journal of medicinal chemistry, Jan-01, Volume: 143Design, synthesis and biological evaluation of novel 2-aminobenzamides containing dithiocarbamate moiety as histone deacetylase inhibitors and potent antitumor agents.
AID708275Growth inhibition of human QGY7701 cells incubated for 72 hrs by WST dye reduction assay2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Pharmacokinetic optimization of class-selective histone deacetylase inhibitors and identification of associated candidate predictive biomarkers of hepatocellular carcinoma tumor response.
AID1380965Inhibition of HDAC6 in human HeLa cells assessed as increase in intracellular acetyl-tubulin levels at 1 uM after 6 hrs by Western blot analysis2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Discovery of Novel Pazopanib-Based HDAC and VEGFR Dual Inhibitors Targeting Cancer Epigenetics and Angiogenesis Simultaneously.
AID329921Inhibition of human HDAC1 in U937 cells at 5 uM2008Bioorganic & medicinal chemistry letters, Apr-15, Volume: 18, Issue:8
Novel uracil-based 2-aminoanilide and 2-aminoanilide-like derivatives: histone deacetylase inhibition and in-cell activities.
AID316934Inhibition of HDAC42008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Histone deacetylase inhibitors: from bench to clinic.
AID1466060Growth inhibition of human AsPC1 cells after 48 hrs by sulforhodamine B assay2017European journal of medicinal chemistry, Jul-07, Volume: 1344-Indolyl-N-hydroxyphenylacrylamides as potent HDAC class I and IIB inhibitors in vitro and in vivo.
AID1293876Inhibition of HDAC in human HeLa nuclear extract assessed as accumulation of acetylated histone H3 after 24 hrs by western blot analysis2016Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
Identification of new quinic acid derivatives as histone deacetylase inhibitors by fluorescence-based cellular assay.
AID1873443Inhibition of full length C-terminal His-tagged HDAC3 (unknown origin)/N-terminal GST-tagged NCoR2 (unknown origin) assessed as rate constant (k-2) of EI complex using (Ac-Leu-Gly-Lys(Ac)-AMC as substrate measured every 30 sec for 60 mins by fluorescence 2022ACS medicinal chemistry letters, May-12, Volume: 13, Issue:5
Determination of Slow-Binding HDAC Inhibitor Potency and Subclass Selectivity.
AID1449332Inhibition of HDAC6 in human CAL27 cells assessed as accumulation of acetylated alpha tubulin at 1 uM after 24 hrs by immunoblot analysis2017Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
Alkoxyurea-Based Histone Deacetylase Inhibitors Increase Cisplatin Potency in Chemoresistant Cancer Cell Lines.
AID1873437Inhibition of full length C-terminal His-tagged HDAC3 (unknown origin)/N-terminal GST-tagged NCoR2 (unknown origin) assessed as inhibition constant (Ki) using (Ac-Leu-Gly-Lys(Ac)-AMC as substrate measured every 30 sec for 60 mins by fluorescence based ass2022ACS medicinal chemistry letters, May-12, Volume: 13, Issue:5
Determination of Slow-Binding HDAC Inhibitor Potency and Subclass Selectivity.
AID1596067Induction of apoptosis in human SMMC7721 cells assessed as necrotic cells at 0.25 uM incubated for 48 hrs by Annexin-V-FITC/propidium iodide staining based flow cytometry (Rvb=1.88%)2019European journal of medicinal chemistry, Jul-01, Volume: 173Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (HDAC) inhibitors.
AID1706069Increase in LPS/IFNgamma-induced IL-10 mRNA expression in mouse RAW26.7 cells at 1 uM incubated for 20 hrs followed by LPS/IFNgamma stimulation and measured after 4 hrs by RT-qPCR analysis2020European journal of medicinal chemistry, Dec-15, Volume: 208Induced protein degradation of histone deacetylases 3 (HDAC3) by proteolysis targeting chimera (PROTAC).
AID1865258Inhibition of recombinant human HDAC using fluorogenic substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by fluorescence based microplate reader analysis2022Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
Discovery of Novel Src Homology-2 Domain-Containing Phosphatase 2 and Histone Deacetylase Dual Inhibitors with Potent Antitumor Efficacy and Enhanced Antitumor Immunity.
AID1740018Inhibition of recombinant human HDAC9 using pan-HDAC substrate incubated for 3 hrs by fluorescence method2020Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
Thirty Years of HDAC Inhibitors: 2020 Insight and Hindsight.
AID1408543Inhibition of His6-tagged HDAC3/SMRT (395 to 489 residues) (unknown origin) co-expressed in baculovirus infected sf9 cells using (FAM)-labeled acetylated peptide substrate after 17 hrs by caliper microfluidic mobility shift assay2018European journal of medicinal chemistry, Sep-05, Volume: 157HDAC3 is a potential validated target for cancer: An overview on the benzamide-based selective HDAC3 inhibitors through comparative SAR/QSAR/QAAR approaches.
AID1231812Antiproliferative activity against human A549 cells incubated for 72 hrs by MTT assay2015Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13
Discovery, bioactivity and docking simulation of Vorinostat analogues containing 1,2,4-oxadiazole moiety as potent histone deacetylase inhibitors and antitumor agents.
AID1879896Inhibition of recombinant human HDAC8 using H2N-Arg- His-Lys(Ac)-Lys(Ac)-AMC as substrate incubated for 90 mins and measured after 20 mins by fluorescence assay2022European journal of medicinal chemistry, Apr-15, Volume: 234Identification of histone deacetylase 10 (HDAC10) inhibitors that modulate autophagy in transformed cells.
AID1486672Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay2017Bioorganic & medicinal chemistry, 08-01, Volume: 25, Issue:15
Design, synthesis and tumor cell growth inhibitory activity of 3-nitro-2H-cheromene derivatives as histone deacetylaes inhibitors.
AID1873447Inhibition of full length C-terminal FLAG-tagged HDAC2 (unknown origin) assessed as rate constant (k2) of EI complex using (Ac-Leu-Gly-Lys(Ac)-AMC as substrate measured every 30 sec for 60 mins by fluorescence based assay2022ACS medicinal chemistry letters, May-12, Volume: 13, Issue:5
Determination of Slow-Binding HDAC Inhibitor Potency and Subclass Selectivity.
AID777605Inhibition of HDAC activity in human HaCaT cell lysate at 1 to 50 uM after 1 hr by colorimetry2013ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
Synthesis and Biological Evaluation of the First Example of NO-Donor Histone Deacetylase Inhibitor.
AID1737662Induction of cell cycle arrest in human MDA-MB-231 cells assessed as reduction in population at S phase at 4 uM for 24 hrs by PI staining based flow cytometry analysis
AID748112Inhibition of HDAC3 (unknown origin) after 60 mins by fluorescence assay2013Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
Discovery of the first histone deacetylase 6/8 dual inhibitors.
AID286792Effect on alpha tubulin acetylation in U937 cells at 1 uM after 24 hrs by Western blot analysis2007Journal of medicinal chemistry, May-17, Volume: 50, Issue:10
Bispyridinium dienes: histone deacetylase inhibitors with selective activities.
AID1401893Antiproliferative activity against human HeLa cells at 2 uM after 72 hrs by CCK-8 assay relative to control2018European journal of medicinal chemistry, Jan-01, Volume: 143Design, synthesis and biological evaluation of novel 2-aminobenzamides containing dithiocarbamate moiety as histone deacetylase inhibitors and potent antitumor agents.
AID777592Effect on HDAC in human HaCaT cells assessed as downregulation of miR-744# at 10 uM after 1 hr by RT-PCR analysis2013ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
Synthesis and Biological Evaluation of the First Example of NO-Donor Histone Deacetylase Inhibitor.
AID1737652Inhibition of human recombinant HDAC9 expressed in baculovirus using fluorogenic peptide p53 residues 379-382 (RHKK(Ac)AMC) as substrate by Fluorescence analysis
AID1474463Therapeutic index, ratio of IC50 for HUVEC to IC50 for human HCT116 cells2017European journal of medicinal chemistry, May-26, Volume: 132Design, synthesis and biological evaluation of novel coumarin-based benzamides as potent histone deacetylase inhibitors and anticancer agents.
AID1740012Inhibition of recombinant human HDAC1 using pan-HDAC substrate incubated for 3 hrs by fluorescence method2020Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
Thirty Years of HDAC Inhibitors: 2020 Insight and Hindsight.
AID1846975Inhibition of full length N-terminal GST-tagged human recombinant HDAC7 (501 to 952 residues) expressed in Baculovirus system using Ac-Leu-Gly-Lys (Ac)-AMC as substrate pretreated for 5 mins followed by substrate addition and measured after 30 mins
AID1847020Toxicity in C57BL/6 mouse allografted with mouse B16-F10 cells assessed as morphological abnormalities in liver at 10 mg/kg, ip administered for 14 days by H and E staining based analysis
AID524991Inhibition of HDAC7 in human homozygous Fdelta508 primary bronchial epithelial cells assessed as increase in short circuit currents at 1 uM for 4, 6, and 8 days relative to control2010Nature chemical biology, Jan, Volume: 6, Issue:1
Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis.
AID1454689Half life in human at 2 mg/m2 dosed twice a week2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Class I HDAC Inhibitors: Potential New Epigenetic Therapeutics for Alcohol Use Disorder (AUD).
AID1548727Inhibition of recombinant human HDAC2 expressed in baculovirus expression system using Boc-Lys(acetyl)-AMC as substrate preincubated for 1 hr followed by substrate addition and measured after 2 hrs by fluorescence based micro plate reader analysis2020Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
Design of Hydrazide-Bearing HDACIs Based on Panobinostat and Their p53 and FLT3-ITD Dependency in Antileukemia Activity.
AID488358Inhibition of HDAC12010Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
New orally bioavailable 2-aminobenzamide-type histone deacetylase inhibitor possessing a (2-hydroxyethyl)(4-(thiophen-2-yl)benzyl)amino group.
AID1486670Antiproliferative activity against human A549 cells after 48 hrs by MTT assay2017Bioorganic & medicinal chemistry, 08-01, Volume: 25, Issue:15
Design, synthesis and tumor cell growth inhibitory activity of 3-nitro-2H-cheromene derivatives as histone deacetylaes inhibitors.
AID496802Inhibition of human HDAC22010Nature chemical biology, Mar, Volume: 6, Issue:3
Chemical phylogenetics of histone deacetylases.
AID328806Antiproliferative activity against human HCT116 cells by CellTiter-Blue cell viability assay2008Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8
A novel series of potent and selective ketone histone deacetylase inhibitors with antitumor activity in vivo.
AID650217Induction of cell cycle arrest in human HCT116 cells assessed as accumulation at G2/M phase at 10 uM after 48 hrs by flow cytometry (Rvb = 5.4 %)2012Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
Anti-tumor activity of new orally bioavailable 2-amino-5-(thiophen-2-yl)benzamide-series histone deacetylase inhibitors, possessing an aqueous soluble functional group as a surface recognition domain.
AID1901162Antiproliferative activity against human SGC-7901 cells measured after 48 hrs by MTT assay2022Bioorganic & medicinal chemistry, 02-15, Volume: 56Synthesis and biological evaluation of aminobenzamides containing purine moiety as class I histone deacetylases inhibitors.
AID1764298Inhibition of class-1 HDAC in human CAL-27 cells assessed as induction of histone H-3 acetylation at 1 uM for 24 hrs by Western blot analysis2021European journal of medicinal chemistry, Feb-05, Volume: 211Synergistic induction of apoptosis in resistant head and neck carcinoma and leukemia by alkoxyamide-based histone deacetylase inhibitors.
AID1548290Induction of apoptosis in bortezomib resistant human KM3/BTZ cells assessed as late apoptotic cells level at 200 nM incubated for 24 hrs by Annexin V-FITC/PI staining based FCAS analysis (Rvb = 0.38%)
AID717815Inhibition of HDAC in human Hela cell lysate using Fluor-de-Lys as substrate assessed as remaining activity at 1.95 x 10'-6 M pretreated for 30 mins before substrate addition by fluorescence assay2012Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23
The structural requirements of histone deacetylase inhibitors: suberoylanilide hydroxamic acid analogs modified at the C6 position.
AID1846970Inhibition of recombinant HDAC3 (unknown origin) at 1 uM
AID1454686Drug uptake in iv dosed baboon brain after 90 mins by PET imaging method relative to control2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Class I HDAC Inhibitors: Potential New Epigenetic Therapeutics for Alcohol Use Disorder (AUD).
AID374811Inhibition of human C-terminal FLAG-tagged HDAC1 in HEK293 cells2009Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
Discovery of a potent class I selective ketone histone deacetylase inhibitor with antitumor activity in vivo and optimized pharmacokinetic properties.
AID1915537Inhibition of HDAC1 (unknown origin)2021European journal of medicinal chemistry, Jan-01, Volume: 209Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors.
AID1847017Toxicity in C57BL/6 mouse allografted with mouse B16-F10 cells assessed as morphological abnormalities in kidney at 10 mg/kg, ip administered for 14 days by H and E staining based analysis
AID1453355Inhibition of HDAC in human HeLa nuclear extract using Boc-Lys (acetyl)-AMC as substrate preincubated for 1 hr followed by substrate addition measured after 1 hr by fluorescence assay2017Bioorganic & medicinal chemistry, 06-15, Volume: 25, Issue:12
Design, synthesis and anti-tumor activity study of novel histone deacetylase inhibitors containing isatin-based caps and o-phenylenediamine-based zinc binding groups.
AID1203896Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth after 72 hrs by MTT-based assay2015European journal of medicinal chemistry, , Volume: 96Discovery and preliminary evaluation of 2-aminobenzamide and hydroxamate derivatives containing 1,2,4-oxadiazole moiety as potent histone deacetylase inhibitors.
AID316920Antitumor activity against human HCT116 cells xenografted in nude mouse model at 20 mg/kg, ip2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Histone deacetylase inhibitors: from bench to clinic.
AID43462Inhibitory concentration against breast MDA-MB-231 cell line2003Journal of medicinal chemistry, Feb-27, Volume: 46, Issue:5
Development of potential antitumor agents. Synthesis and biological evaluation of a new set of sulfonamide derivatives as histone deacetylase inhibitors.
AID650220Induction of cell cycle arrest in human HCT116 cells assessed as accumulation at S phase at 10 uM after 24 hrs by flow cytometry (Rvb = 10.6 %)2012Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
Anti-tumor activity of new orally bioavailable 2-amino-5-(thiophen-2-yl)benzamide-series histone deacetylase inhibitors, possessing an aqueous soluble functional group as a surface recognition domain.
AID1846973Inhibition of recombinant HDAC3 (unknown origin) using Ac-Leu-Gly-Lys (Ac)-AMC as substrate pretreated for 5 mins followed by substrate addition and measured after 30 mins
AID551596Inhibition of HDAC22011Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
Application of p21 and klf2 reporter gene assays to identify selective histone deacetylase inhibitors for cancer therapy.
AID492806Cell cycle arrest in human NB4 cells assessed as increase in accumulation at pre-G1 phase at 5 uM after 24 hrs by FACS analysis2010Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12
Synthesis and biological characterization of the histone deacetylase inhibitor largazole and C7- modified analogues.
AID1691037Inhibition of recombinant human full-length C-terminal FLAG-His tagged HDAC1 (1 to 482 residues) expressed in Sf21 insect cells using RHK-K(Ac)-AMC as substrate measured after 60 mins by fluorescence assay
AID420319Inhibition of Bordetella / Alcaligenes strain FB188 HDAH by fluorogenic enzyme assay2009Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
Non-isotopic dual parameter competition assay suitable for high-throughput screening of histone deacetylases.
AID1203889Inhibition of recombinant HDAC1 (unknown origin) using fluorogenic substrate Boc-Lys (acetyl)-AMC after 20 mins by homogeneous fluorescence release assay2015European journal of medicinal chemistry, , Volume: 96Discovery and preliminary evaluation of 2-aminobenzamide and hydroxamate derivatives containing 1,2,4-oxadiazole moiety as potent histone deacetylase inhibitors.
AID1556405Inhibition of HDAC1 in LPS/IFNgamma-stimulated mouse RAW blue cells assessed as upregulation of NFkappaB transcriptional activity by measuring increase in SEAP activity at 1 to 2.5 uM pretreated for 16 hrs followed by LPS stimulation and measured after 4 2019European journal of medicinal chemistry, Sep-01, Volume: 177Inhibitory selectivity among class I HDACs has a major impact on inflammatory gene expression in macrophages.
AID1596070Induction of apoptosis in human SMMC7721 cells assessed as late apoptotic cells at 1 uM incubated for 48 hrs by Annexin-V-FITC/propidium iodide staining based flow cytometry (Rvb=1.73%)2019European journal of medicinal chemistry, Jul-01, Volume: 173Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (HDAC) inhibitors.
AID1586084Inhibition of human HDAC9 using Boc-Lys(trifluoroacetyl)-AMC as substrate by fluorescence assay2019European journal of medicinal chemistry, Jan-15, Volume: 1621-Arylsulfonyl indoline-benzamides as a new antitubulin agents, with inhibition of histone deacetylase.
AID316903Inhibition of human HCT116 cells2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Histone deacetylase inhibitors: from bench to clinic.
AID488372Cell cycle arrest in human HCT116 cells assessed as accumulation at G2/M phase at 10 uM after 48 hrs by flow cytometry analysis2010Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
New orally bioavailable 2-aminobenzamide-type histone deacetylase inhibitor possessing a (2-hydroxyethyl)(4-(thiophen-2-yl)benzyl)amino group.
AID1203892Antiproliferative activity against human HCT116 cells assessed as inhibition of cell growth after 72 hrs by MTT-based assay2015European journal of medicinal chemistry, , Volume: 96Discovery and preliminary evaluation of 2-aminobenzamide and hydroxamate derivatives containing 1,2,4-oxadiazole moiety as potent histone deacetylase inhibitors.
AID1431811Selectivity ratio of IC50 for human KDAC3 to IC50 for human KDAC12017European journal of medicinal chemistry, Feb-15, Volume: 127Design and synthesis of benzodiazepine analogs as isoform-selective human lysine deacetylase inhibitors.
AID1548300Induction of cell cycle arrest in bortezomib resistant human KM3/BTZ cells assessed as accumulation at G1 phase at 100 nM incubated for 24 hrs by propidium iodide staining based flow cytometry (Rvb = 42%)
AID269168Antitumor activity against human SW48 cells xenografted in mouse at 20 mg/kg, ip2006Bioorganic & medicinal chemistry letters, Aug-01, Volume: 16, Issue:15
Substituted N-(2-aminophenyl)-benzamides, (E)-N-(2-aminophenyl)-acrylamides and their analogues: novel classes of histone deacetylase inhibitors.
AID1474451Selectivity ratio of IC50 for HDAC1 (unknown origin) to IC50 for HDAC in human A2780 cells2017European journal of medicinal chemistry, May-26, Volume: 132Design, synthesis and biological evaluation of novel coumarin-based benzamides as potent histone deacetylase inhibitors and anticancer agents.
AID1901145Inhibition of recombinant human N-terminal GST-tagged HDAC6 (1 to 1215 residues) expressed in Sf9 insect cells using fluorogenic HDAC substrate 3 measured after 30 mins by fluorimetry2022Bioorganic & medicinal chemistry, 02-15, Volume: 56Synthesis and biological evaluation of aminobenzamides containing purine moiety as class I histone deacetylases inhibitors.
AID1380956Inhibition of HDAC8 (unknown origin) using fluorogenic Boc-Lys(trifluoroacetyl)-AMC as substrate preincubated for 5 mins followed by substrate addition measured after 30 mins by fluorescence-based assay2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Discovery of Novel Pazopanib-Based HDAC and VEGFR Dual Inhibitors Targeting Cancer Epigenetics and Angiogenesis Simultaneously.
AID1846972Inhibition of full length recombinant human HDAC1 (1 to 482 residues) expressed in Baculovirus system using Ac-Leu-Gly-Lys (Ac)-AMC as substrate pretreated for 5 mins followed by substrate addition and measured after 30 mins
AID1740013Inhibition of recombinant human HDAC2 using pan-HDAC substrate incubated for 3 hrs by fluorescence method2020Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
Thirty Years of HDAC Inhibitors: 2020 Insight and Hindsight.
AID1181306Inhibition of HDAC1 in human U937 cells assessed as increase in acetyl-histone H3 level at 5 uM by Western blotting method2014Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
1,3,4-Oxadiazole-containing histone deacetylase inhibitors: anticancer activities in cancer cells.
AID421211Antitumor activity against mouse ML1 cells2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Recent advances in the development of polyamine analogues as antitumor agents.
AID1887681Cytotoxicity against human GES1 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay2022European journal of medicinal chemistry, Jan-05, Volume: 227Design, synthesis and biological evaluation of novel o-aminobenzamide derivatives as potential anti-gastric cancer agents in vitro and in vivo.
AID1181307Inhibition of HDAC6 in human U937 cells assessed as increase in acetyl-alpha-tubulin level at 5 uM by Western blotting method2014Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
1,3,4-Oxadiazole-containing histone deacetylase inhibitors: anticancer activities in cancer cells.
AID551595Inhibition of HDAC12011Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
Application of p21 and klf2 reporter gene assays to identify selective histone deacetylase inhibitors for cancer therapy.
AID1548303Induction of cell cycle arrest in bortezomib resistant human KM3/BTZ cells assessed as accumulation at G1 phase at 100 nM incubated for 24 hrs in presence of bortezomib by propidium iodide staining based flow cytometry (Rvb = 42%)
AID1525777Inhibition of HADC1 (unknown origin)2020Journal of medicinal chemistry, 01-09, Volume: 63, Issue:1
Old but Gold: Tracking the New Guise of Histone Deacetylase 6 (HDAC6) Enzyme as a Biomarker and Therapeutic Target in Rare Diseases.
AID1596071Induction of apoptosis in human SMMC7721 cells assessed as necrotic cells at 1 uM incubated for 48 hrs by Annexin-V-FITC/propidium iodide staining based flow cytometry (Rvb=1.88%)2019European journal of medicinal chemistry, Jul-01, Volume: 173Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (HDAC) inhibitors.
AID1424827Inhibition of class 1 HDAC in human MV4-11 cells assessed as hyperacetylation of histone H3 at 200 nM after 24 hrs by Western blot analysis2018European journal of medicinal chemistry, May-25, Volume: 152Design and biological evaluation of tetrahydro-β-carboline derivatives as highly potent histone deacetylase 6 (HDAC6) inhibitors.
AID1847034In vivo inhibition of HDAC in tumor of mouse B16-F10 cells xenografted in C57BL/6 mouse assessed as increase in acetylated histone-H3 expression by H and E staining based immunohistochemistry method
AID324951Inhibition of HDAC4 H976Y mutant expressed in Escherichia coli at 10 uM2008Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6
Probing the elusive catalytic activity of vertebrate class IIa histone deacetylases.
AID1901148Inhibition of HDAC in human HeLa cell nuclear extracts using color de Lys as substrate measured after 30 mins by colorimetric assay2022Bioorganic & medicinal chemistry, 02-15, Volume: 56Synthesis and biological evaluation of aminobenzamides containing purine moiety as class I histone deacetylases inhibitors.
AID1467241Inhibition of recombinant C-terminal His-tagged HDAC11 (unknown origin) expressed in baculovirus infected Sf9 cells using Ac-Arg-Gly-Lys(Ac)-AMC as substrate pretreated for 3 hrs followed by substrate addition after 30 mins in presence of 0.2 uM SAHA by f2017Bioorganic & medicinal chemistry letters, 07-01, Volume: 27, Issue:13
Stabilizing HDAC11 with SAHA to assay slow-binding benzamide inhibitors.
AID1541446Inhibition of recombinant human full length C-terminal His/FLAG-tagged HDAC1 expressed in baculovirus infected Sf9 insect cells using ZMAL as substrate incubated for 90 mins by fluorescence assay2019Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
Synthesis of Peptoid-Based Class I-Selective Histone Deacetylase Inhibitors with Chemosensitizing Properties.
AID1548733Inhibition of recombinant human HDAC4 using Boc-Lys (trifluoroacetyl)-AMC as substrate preincubated for 1 hr followed by substrate addition and measured after 2 hrs by fluorescence based micro plate reader analysis2020Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
Design of Hydrazide-Bearing HDACIs Based on Panobinostat and Their p53 and FLT3-ITD Dependency in Antileukemia Activity.
AID1732163Inhibition of HDAC1 (unknown origin) using fluorogenic-(RHKKAc) as substrate by fluorescence assay2021European journal of medicinal chemistry, Apr-05, Volume: 215CAP rigidification of MS-275 and chidamide leads to enhanced antiproliferative effects mediated through HDAC1, 2 and tubulin polymerization inhibition.
AID1847024Cardiotoxicity in C57BL/6 mouse ssessed as shortening of QTc level in presence of (2-phenylthiazol-4-yl)(3,4,5-trimethoxyphenyl)methanone by ECG analysis
AID1578486Inhibition of recombinant full length human HDAC2 expressed in baculovirus infected Sf9 cells using FAM-RHKK-Ac as substrate incubated for 17 hrs by electrophoretic mobility shift assay2020ACS medicinal chemistry letters, Jan-09, Volume: 11, Issue:1
Class I/IIb-Selective HDAC Inhibitor Exhibits Oral Bioavailability and Therapeutic Efficacy in Acute Myeloid Leukemia.
AID1586079Inhibition of human HDAC3 using RHKKAc as substrate by fluorescence assay2019European journal of medicinal chemistry, Jan-15, Volume: 1621-Arylsulfonyl indoline-benzamides as a new antitubulin agents, with inhibition of histone deacetylase.
AID524996Inhibition of HDAC8 by in vitro deacetylation assay2010Nature chemical biology, Jan, Volume: 6, Issue:1
Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis.
AID525003Inhibition of HDAC1 by in vitro deacetylation assay2010Nature chemical biology, Jan, Volume: 6, Issue:1
Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis.
AID496801Inhibition of human HDAC12010Nature chemical biology, Mar, Volume: 6, Issue:3
Chemical phylogenetics of histone deacetylases.
AID609495Ratio of IC50 for CYP3A4 to IC50 for human HCT116 cells2011Bioorganic & medicinal chemistry letters, Aug-15, Volume: 21, Issue:16
The design, synthesis and structure-activity relationships of novel isoindoline-based histone deacetylase inhibitors.
AID1263146Antiproliferative activity against human MCF7 cells treated for 48 hrs followed by refreshed every 96 hrs measured on day 10 by Lowry assay2015Bioorganic & medicinal chemistry, Dec-15, Volume: 23, Issue:24
Design, synthesis and evaluation of antiestrogen and histone deacetylase inhibitor molecular hybrids.
AID1548291Induction of apoptosis in bortezomib resistant human KM3/BTZ cells assessed as necrotic cells level at 200 nM incubated for 24 hrs by Annexin V-FITC/PI staining based FCAS analysis (Rvb = 0.11%)
AID1401914Induction of apoptosis in human SMMC7721 cells assessed as late apoptotic cells at 1 umol/L after 72 hrs by Alexa Fluor 488 Annexin/propidium iodide staining-based flow cytometric analysis (Rvb = 0.29%)2018European journal of medicinal chemistry, Jan-01, Volume: 143Design, synthesis and biological evaluation of novel 2-aminobenzamides containing dithiocarbamate moiety as histone deacetylase inhibitors and potent antitumor agents.
AID1846959Antiproliferative activity against mouse B16-F10 cells assessed as inhibition of cell viability measured for 48 hrs in presence of (2-phenylthiazol-4-yl)(3,4,5-trimethoxyphenyl)methanone by microplate reader based MTT assay
AID1596038Antiproliferative activity against human HeLa cells assessed as reduction in cell growth at 2 uM incubated for 72 hrs by CCK-8 assay relative to control2019European journal of medicinal chemistry, Jul-01, Volume: 173Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (HDAC) inhibitors.
AID525000Inhibition of HDAC4 by in vitro deacetylation assay2010Nature chemical biology, Jan, Volume: 6, Issue:1
Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis.
AID316898Inhibition of HDAC22008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Histone deacetylase inhibitors: from bench to clinic.
AID374831Antiproliferative activity against human U937 cells after 72 hrs by celltiter-blue cell viability assay2009Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
Discovery of a potent class I selective ketone histone deacetylase inhibitor with antitumor activity in vivo and optimized pharmacokinetic properties.
AID70208Inhibitory concentration against normal epithelial HMEC cell line2003Journal of medicinal chemistry, Feb-27, Volume: 46, Issue:5
Development of potential antitumor agents. Synthesis and biological evaluation of a new set of sulfonamide derivatives as histone deacetylase inhibitors.
AID1380947Antiproliferative activity against human KG1 cells after 72 hrs by MTT assay2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Discovery of Novel Pazopanib-Based HDAC and VEGFR Dual Inhibitors Targeting Cancer Epigenetics and Angiogenesis Simultaneously.
AID1380955Inhibition of HDAC6 (unknown origin) using fluorogenic Boc-Lys(acetyl)-AMC as substrate preincubated for 5 mins followed by substrate addition measured after 30 mins by fluorescence-based assay2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Discovery of Novel Pazopanib-Based HDAC and VEGFR Dual Inhibitors Targeting Cancer Epigenetics and Angiogenesis Simultaneously.
AID1596066Induction of apoptosis in human SMMC7721 cells assessed as late apoptotic cells at 0.25 uM incubated for 48 hrs by Annexin-V-FITC/propidium iodide staining based flow cytometry (Rvb=1.73%)2019European journal of medicinal chemistry, Jul-01, Volume: 173Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (HDAC) inhibitors.
AID717811Inhibition of HDAC in human Hela cell lysate using Fluor-de-Lys as substrate assessed as remaining activity at 6.25 x 10'-5 M pretreated for 30 mins before substrate addition by fluorescence assay2012Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23
The structural requirements of histone deacetylase inhibitors: suberoylanilide hydroxamic acid analogs modified at the C6 position.
AID1596065Induction of apoptosis in human SMMC7721 cells assessed as early apoptotic cells at 0.25 uM incubated for 48 hrs by Annexin-V-FITC/propidium iodide staining based flow cytometry (Rvb=2.88%)2019European journal of medicinal chemistry, Jul-01, Volume: 173Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (HDAC) inhibitors.
AID1732193Cytotoxicity against human KG-1 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay2021European journal of medicinal chemistry, Apr-05, Volume: 215CAP rigidification of MS-275 and chidamide leads to enhanced antiproliferative effects mediated through HDAC1, 2 and tubulin polymerization inhibition.
AID1879893Inhibition of recombinant human HDAC6 using ZMAL (Z-(Ac)Lys-AMC as substrate incubated for 20 mins and measured by homogenous fluorescence assay2022European journal of medicinal chemistry, Apr-15, Volume: 234Identification of histone deacetylase 10 (HDAC10) inhibitors that modulate autophagy in transformed cells.
AID525023Inhibition of HDAC in human CFBE41o- cell line assessed as increase in CFTR mRNA at 5 uM by RT-PCR2010Nature chemical biology, Jan, Volume: 6, Issue:1
Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis.
AID328800Inhibition of HDAC7 expressed in Escherichia coli2008Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8
A novel series of potent and selective ketone histone deacetylase inhibitors with antitumor activity in vivo.
AID1541554Inhibition of class 1 HDAC in human CAL27 cells assessed as increase in histone H3 acetylation at 1 uM measured after 24 hrs by immunoblot analysis2019Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
Synthesis of Peptoid-Based Class I-Selective Histone Deacetylase Inhibitors with Chemosensitizing Properties.
AID1479842Cell cycle arrest in human HEL cells at 5 uM after 24 hrs by propidium iodide staining-based flow cytometric method2018Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
Marbostat-100 Defines a New Class of Potent and Selective Antiinflammatory and Antirheumatic Histone Deacetylase 6 Inhibitors.
AID670719Inhibition of HDAC1 in human HeLa cell lysate using KI-104 as substrate after 40 mins by fluorescence analysis2012Bioorganic & medicinal chemistry, Jul-15, Volume: 20, Issue:14
Synthesis, biological evaluation and molecular docking studies of 3-(1,3-diphenyl-1H-pyrazol-4-yl)-N-phenylacrylamide derivatives as inhibitors of HDAC activity.
AID1847035In vivo inhibition of HDAC in tumor of mouse B16-F10 cells xenografted in C57BL/6 mouse assessed as increase in acetylated histone-H3 expression in presence of (2-phenylthiazol-4-yl)(3,4,5-trimethoxyphenyl)methanone by H and E staining based immunohistoch
AID1876492Antiproliferative activity against rat C6 cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay2022European journal of medicinal chemistry, Jan-05, Volume: 227Novel piperazine based benzamide derivatives as potential anti-glioblastoma agents inhibiting cell proliferation and cell cycle progression.
AID488359Solubility in 10% DMSO-water2010Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
New orally bioavailable 2-aminobenzamide-type histone deacetylase inhibitor possessing a (2-hydroxyethyl)(4-(thiophen-2-yl)benzyl)amino group.
AID1864220Binding affinity to 5' FAM and 3' TAMRA-labeled c-myc G4-quadruplex DNA Pu22 (unknown origin) assessed as change in melting temperature at 1 uM by fluorescence resonance energy transfer assay2022Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
Discovery of a Novel G-Quadruplex and Histone Deacetylase (HDAC) Dual-Targeting Agent for the Treatment of Triple-Negative Breast Cancer.
AID1401905Selectivity ratio of IC50 for human recombinant HDAC1 to IC50 for human recombinant HDAC62018European journal of medicinal chemistry, Jan-01, Volume: 143Design, synthesis and biological evaluation of novel 2-aminobenzamides containing dithiocarbamate moiety as histone deacetylase inhibitors and potent antitumor agents.
AID1486673Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay2017Bioorganic & medicinal chemistry, 08-01, Volume: 25, Issue:15
Design, synthesis and tumor cell growth inhibitory activity of 3-nitro-2H-cheromene derivatives as histone deacetylaes inhibitors.
AID1901147Inhibition of recombinant human full-length C-terminal Flag-His6-tagged HDAC1 (1 to 482 residues) expressed in Sf9 insect cells using fluorogenic HDAC substrate measured after 30 mins by fluorimetry2022Bioorganic & medicinal chemistry, 02-15, Volume: 56Synthesis and biological evaluation of aminobenzamides containing purine moiety as class I histone deacetylases inhibitors.
AID1676594Binding affinity to gallium ion assessed as accounting ratio by measuring total compound detected/total compound adsorbed at 2.55 umol by immobilized metal-ion affinity chromatography2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors.
AID1727729Inhibition of HDAC1 (unknown origin) by fluorescence based assay2021European journal of medicinal chemistry, Jan-01, Volume: 209Discovery of selective HDAC/BRD4 dual inhibitors as epigenetic probes.
AID1596059Cell cycle arrest in human SMMC7721 cells assessed as accumulation at S phase at 1 uM incubated for 48 hrs by propidium iodide staining based flow cytometry (Rvb=6.83%)2019European journal of medicinal chemistry, Jul-01, Volume: 173Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (HDAC) inhibitors.
AID1737650Inhibition of human recombinant HDAC5 expressed in baculovirus using fluorogenic peptide p53 residues 379-382 (RHKK(Ac)AMC) as substrate by Fluorescence analysis
AID1479843Cell cycle arrest in human Jurkat cells at 5 uM after 24 hrs by propidium iodide staining-based flow cytometric method2018Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
Marbostat-100 Defines a New Class of Potent and Selective Antiinflammatory and Antirheumatic Histone Deacetylase 6 Inhibitors.
AID324949Inhibition of HDAC3 in HEK293 cells2008Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6
Probing the elusive catalytic activity of vertebrate class IIa histone deacetylases.
AID329931Induction of apoptosis in human U937 cells at 5 uM after 30 hrs2008Bioorganic & medicinal chemistry letters, Apr-15, Volume: 18, Issue:8
Novel uracil-based 2-aminoanilide and 2-aminoanilide-like derivatives: histone deacetylase inhibition and in-cell activities.
AID1324232Antagonist activity at AR in human LNCAP cells assessed as suppression of DHT-induced AR protein level at 10 uM measured after 24 hrs relative to control2016Bioorganic & medicinal chemistry letters, 11-01, Volume: 26, Issue:21
Targeting prostate cancer with compounds possessing dual activity as androgen receptor antagonists and HDAC6 inhibitors.
AID538408Inhibition of recombinant human HDAC1 using Cbz-Lys(TFAc)-AMC as substrate by fluorometric analysis2010Bioorganic & medicinal chemistry letters, Dec-01, Volume: 20, Issue:23
Inhibitors selective for HDAC6 in enzymes and cells.
AID1401891Antiproliferative activity against human A375 cells at 2 uM after 72 hrs by CCK-8 assay relative to control2018European journal of medicinal chemistry, Jan-01, Volume: 143Design, synthesis and biological evaluation of novel 2-aminobenzamides containing dithiocarbamate moiety as histone deacetylase inhibitors and potent antitumor agents.
AID1706070Increase in LPS/IFNgamma-induced iNOS mRNA expression in mouse RAW26.7 cells at 1 uM incubated for 20 hrs followed by LPS/IFNgamma stimulation and measured after 4 hrs by RT-qPCR analysis2020European journal of medicinal chemistry, Dec-15, Volume: 208Induced protein degradation of histone deacetylases 3 (HDAC3) by proteolysis targeting chimera (PROTAC).
AID1901154Inhibition of HDAC8 (unknown origin) using FAM-RHKK(Ac)-NH2/FAM-RHKK(trifluoroacetyl)-NH2 as substrate preincubated for 15 mins followed by substrate addition and measured after 3 hrs by microfluidic chip based fluorescence assay2022Bioorganic & medicinal chemistry, 02-15, Volume: 56Synthesis and biological evaluation of aminobenzamides containing purine moiety as class I histone deacetylases inhibitors.
AID717812Inhibition of HDAC in human Hela cell lysate using Fluor-de-Lys as substrate assessed as remaining activity at 1.56 x 10'-5 M pretreated for 30 mins before substrate addition by fluorescence assay2012Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23
The structural requirements of histone deacetylase inhibitors: suberoylanilide hydroxamic acid analogs modified at the C6 position.
AID1403454Inhibition of human FLAG-tagged HDAC1 expressed in HEK293T cells using acetylated lysine side chain as substrate after 1 hr by colorimetric detection based assay2018European journal of medicinal chemistry, Jan-20, Volume: 144Structural and biological characterization of new hybrid drugs joining an HDAC inhibitor to different NO-donors.
AID328831Toxicity against human HCT116 cells xenografted BALB/c mouse assessed as body weight loss at 25 mg/kg, ip administered 5 days per week for 2.5 weeks2008Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8
A novel series of potent and selective ketone histone deacetylase inhibitors with antitumor activity in vivo.
AID1380950Antiproliferative activity against human K562 cells after 72 hrs by MTT assay2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Discovery of Novel Pazopanib-Based HDAC and VEGFR Dual Inhibitors Targeting Cancer Epigenetics and Angiogenesis Simultaneously.
AID650228Inhibition of HDAC22012Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
Anti-tumor activity of new orally bioavailable 2-amino-5-(thiophen-2-yl)benzamide-series histone deacetylase inhibitors, possessing an aqueous soluble functional group as a surface recognition domain.
AID1846956Antiproliferative activity against mouse B16-F10 cells assessed as inhibition of cell viability measured for 48 hrs by microplate reader based MTT assay
AID1263143Antagonist activity at ERalpha in human T47D-KBLuc cells assessed as inhibition of E2-induced transcriptional activity by luciferase reporter gene assay2015Bioorganic & medicinal chemistry, Dec-15, Volume: 23, Issue:24
Design, synthesis and evaluation of antiestrogen and histone deacetylase inhibitor molecular hybrids.
AID1853011Inhibition of HDAC3-SMRT (unknown origin) using Boc-(Ac)Lys-AMC as substrate preincubated with compound for 1 hrs followed by substrate addition and measured after 1 hrs by fluorescent assay2022RSC medicinal chemistry, Dec-14, Volume: 13, Issue:12
A 'click' chemistry approach to novel entinostat (MS-275) based class I histone deacetylase proteolysis targeting chimeras.
AID1847013Antitumor activity against mouse B16-F10 cells allografted in C57BL/6 mouse assessed as tumor growth inhibition at 10 mg/kg, ip administered for 14 days
AID670720Inhibition of HDAC2 in human HeLa cell lysate using KI-104 as substrate after 40 mins by fluorescence analysis2012Bioorganic & medicinal chemistry, Jul-15, Volume: 20, Issue:14
Synthesis, biological evaluation and molecular docking studies of 3-(1,3-diphenyl-1H-pyrazol-4-yl)-N-phenylacrylamide derivatives as inhibitors of HDAC activity.
AID1691061Induction of apoptosis in human KB7D cells assessed as increase in activated gammaH2AX expression at 5 uM measured after 24 hrs by Western blot analysis
AID102520Inhibitory concentration against lung A549 cell line2003Journal of medicinal chemistry, Feb-27, Volume: 46, Issue:5
Development of potential antitumor agents. Synthesis and biological evaluation of a new set of sulfonamide derivatives as histone deacetylase inhibitors.
AID1881857Vasodilating activity in rat aorta in presence of ODQ2022European journal of medicinal chemistry, Jan-05, Volume: 227NO-HDAC dual inhibitors.
AID1737640Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
AID488371Cell cycle arrest in human HCT116 cells assessed as accumulation at G2/M phase at 10 uM after 24 hrs by flow cytometry analysis2010Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
New orally bioavailable 2-aminobenzamide-type histone deacetylase inhibitor possessing a (2-hydroxyethyl)(4-(thiophen-2-yl)benzyl)amino group.
AID1873428Inhibition of HDAC2 (unknown origin) at 2 uM preincubated for 1 hr followed by 100-fold dilution and subsequent substrate addition measured after 1 hr2022Bioorganic & medicinal chemistry letters, 08-15, Volume: 70Comparison of three zinc binding groups for HDAC inhibitors - A potency, selectivity and enzymatic kinetics study.
AID1380942Antiproliferative activity against human AGS cells after 72 hrs by MTT assay2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Discovery of Novel Pazopanib-Based HDAC and VEGFR Dual Inhibitors Targeting Cancer Epigenetics and Angiogenesis Simultaneously.
AID1676598Binding affinity to cupric ion assessed as retention ratio by measuring compound detected in elution fraction/total compound detected at 2.55 umol by immobilized metal-ion affinity chromatography2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors.
AID488275Inhibition of HDAC32010Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
On the inhibition of histone deacetylase 8.
AID1596045Antiproliferative activity against human A375 cells assessed as reduction in cell growth incubated for 72 hrs by CCK-8 assay2019European journal of medicinal chemistry, Jul-01, Volume: 173Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (HDAC) inhibitors.
AID1548730Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability after 48 hrs by CellTiter-Blue dye based spectrophotometric analysis2020Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
Design of Hydrazide-Bearing HDACIs Based on Panobinostat and Their p53 and FLT3-ITD Dependency in Antileukemia Activity.
AID1189851Antiviral activity against HCV genotype 1b infected in human Huh7 cells after 3 days by luciferase reporter gene assay2015Journal of medicinal chemistry, Jan-22, Volume: 58, Issue:2
Hydroxamic acids block replication of hepatitis C virus.
AID303015Inhibition of human recombinant HDAC22007Journal of medicinal chemistry, Nov-15, Volume: 50, Issue:23
Novel aminophenyl benzamide-type histone deacetylase inhibitors with enhanced potency and selectivity.
AID609490Antiproliferative activity against human HCT116 cells2011Bioorganic & medicinal chemistry letters, Aug-15, Volume: 21, Issue:16
The design, synthesis and structure-activity relationships of novel isoindoline-based histone deacetylase inhibitors.
AID316927Inhibition of human CCD1059SK cells2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Histone deacetylase inhibitors: from bench to clinic.
AID1586081Inhibition of human HDAC6 using RHKKAc as substrate by fluorescence assay2019European journal of medicinal chemistry, Jan-15, Volume: 1621-Arylsulfonyl indoline-benzamides as a new antitubulin agents, with inhibition of histone deacetylase.
AID316893Inhibition of HDAC82008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Histone deacetylase inhibitors: from bench to clinic.
AID1596074Induction of apoptosis in human SMMC7721 cells assessed as late apoptotic cells at 4 uM incubated for 48 hrs by Annexin-V-FITC/propidium iodide staining based flow cytometry (Rvb=1.73%)2019European journal of medicinal chemistry, Jul-01, Volume: 173Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (HDAC) inhibitors.
AID274117Inhibition of HeLa cell proliferation2006Bioorganic & medicinal chemistry letters, Dec-01, Volume: 16, Issue:23
A series of novel, potent, and selective histone deacetylase inhibitors.
AID420324Inhibition of HDAC1 by fluorogenic enzyme assay2009Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
Non-isotopic dual parameter competition assay suitable for high-throughput screening of histone deacetylases.
AID1882461Displacement of [3H]-acetylated histones from HDAC3 derived from human K562 cell nuclear extract incubated for 10 mins by liquid scintillation counting method2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Chasing a Breath of Fresh Air in Cystic Fibrosis (CF): Therapeutic Potential of Selective HDAC6 Inhibitors to Tackle Multiple Pathways in CF Pathophysiology.
AID764209Partition coefficient, log D of the compound at pH 7.4 by Avdeef-Tsinman potentiometric titration method2013Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
Novel N-hydroxyfurylacrylamide-based histone deacetylase (HDAC) inhibitors with branched CAP group (Part 2).
AID488364Inhibition of HDAC1 in human HCT116 cells assessed as induction of hyperacetylation of histone H3 at 10 uM after 24 hrs by Western blot analysis2010Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
New orally bioavailable 2-aminobenzamide-type histone deacetylase inhibitor possessing a (2-hydroxyethyl)(4-(thiophen-2-yl)benzyl)amino group.
AID1686358Cytotoxicity against human MV4-11 cells assessed as reduction in cell viability incubated for 48 hrs by Cell-titer-blue cell viability assay2016Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21
Development of Allosteric Hydrazide-Containing Class I Histone Deacetylase Inhibitors for Use in Acute Myeloid Leukemia.
AID1466056Inhibition of HDAC in human HeLa cell nuclear extract using Ac-Lys(Ac)-pNA as substrate after 30 mins by fluorescence assay2017European journal of medicinal chemistry, Jul-07, Volume: 1344-Indolyl-N-hydroxyphenylacrylamides as potent HDAC class I and IIB inhibitors in vitro and in vivo.
AID1737668Induction of apoptosis in human MDA-MB-231 cells assessed as increase in cleaved caspase-8 level incubated for 24 hrs by Western blot analysis
AID1548275Antiproliferative activity against bortezomib resistant human KM3/BTZ cells in presence of bortezomib incubated for 48 hrs by MTT assay
AID1873473Inhibition of full length C-terminal His-tagged HDAC3 (unknown origin)/N-terminal GST-tagged NCoR2 (unknown origin) assessed as dissociation half-life of EI complex using (Ac-Leu-Gly-Lys(Ac)-AMC as substrate measured every 30 sec for 60 mins by fluorescen2022ACS medicinal chemistry letters, May-12, Volume: 13, Issue:5
Determination of Slow-Binding HDAC Inhibitor Potency and Subclass Selectivity.
AID1873429Mixed-type inhibition of HDAC3 (unknown origin) at 3.90625 to 62.5 nM by Lineweaver-Burk plot analysis2022Bioorganic & medicinal chemistry letters, 08-15, Volume: 70Comparison of three zinc binding groups for HDAC inhibitors - A potency, selectivity and enzymatic kinetics study.
AID329920Induction of granulocytic differentiation in human U937 cells2008Bioorganic & medicinal chemistry letters, Apr-15, Volume: 18, Issue:8
Novel uracil-based 2-aminoanilide and 2-aminoanilide-like derivatives: histone deacetylase inhibition and in-cell activities.
AID374817Inhibition of human C-terminal FLAG-tagged HDAC2 in HEK293 cells2009Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
Discovery of a potent class I selective ketone histone deacetylase inhibitor with antitumor activity in vivo and optimized pharmacokinetic properties.
AID316926Inhibition of human SW620 cells2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Histone deacetylase inhibitors: from bench to clinic.
AID492812Induction of p21WAF1/CIP1 expression in human NB4 cells at 5 uM after 24 hrs by Western blot analysis2010Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12
Synthesis and biological characterization of the histone deacetylase inhibitor largazole and C7- modified analogues.
AID777589Effect on HDAC in human HaCaT cells assessed as downregulation of miR-941 at 10 uM after 1 hr by RT-PCR analysis2013ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
Synthesis and Biological Evaluation of the First Example of NO-Donor Histone Deacetylase Inhibitor.
AID1401896Antiproliferative activity against human MGC803 cells after 72 hrs by CCK-8 assay2018European journal of medicinal chemistry, Jan-01, Volume: 143Design, synthesis and biological evaluation of novel 2-aminobenzamides containing dithiocarbamate moiety as histone deacetylase inhibitors and potent antitumor agents.
AID1596073Induction of apoptosis in human SMMC7721 cells assessed as early apoptotic cells at 4 uM incubated for 48 hrs by Annexin-V-FITC/propidium iodide staining based flow cytometry (Rvb=2.88%)2019European journal of medicinal chemistry, Jul-01, Volume: 173Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (HDAC) inhibitors.
AID609497Half life in rat liver microsomes2011Bioorganic & medicinal chemistry letters, Aug-15, Volume: 21, Issue:16
The design, synthesis and structure-activity relationships of novel isoindoline-based histone deacetylase inhibitors.
AID1479845Induction of apoptosis in human PBMC at 5 uM after 24 hrs by Annexin V/propidium iodide staining-based flow cytometric method2018Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
Marbostat-100 Defines a New Class of Potent and Selective Antiinflammatory and Antirheumatic Histone Deacetylase 6 Inhibitors.
AID1380949Antiproliferative activity against human MOLT4 cells after 72 hrs by MTT assay2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Discovery of Novel Pazopanib-Based HDAC and VEGFR Dual Inhibitors Targeting Cancer Epigenetics and Angiogenesis Simultaneously.
AID328797Inhibition of HDAC4 gain-of-function phenotype expressed in Escherichia coli2008Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8
A novel series of potent and selective ketone histone deacetylase inhibitors with antitumor activity in vivo.
AID1556407Inhibition of HDAC1/2 in LPS/IFNgamma-stimulated mouse RAW264.7 cells assessed as upregulation of IL-6 gene expression at 1 uM pretreated for 16 hrs followed by LPS stimulation and measured after 4 hrs by RT-qPCR analysis2019European journal of medicinal chemistry, Sep-01, Volume: 177Inhibitory selectivity among class I HDACs has a major impact on inflammatory gene expression in macrophages.
AID1380946Antiproliferative activity against human HT1080 cells after 72 hrs by MTT assay2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Discovery of Novel Pazopanib-Based HDAC and VEGFR Dual Inhibitors Targeting Cancer Epigenetics and Angiogenesis Simultaneously.
AID1764256Induction of histone H-3 expression in human CAL-27 cells for 24 hrs by Western blot analysis2021European journal of medicinal chemistry, Feb-05, Volume: 211Synergistic induction of apoptosis in resistant head and neck carcinoma and leukemia by alkoxyamide-based histone deacetylase inhibitors.
AID1486669Antiproliferative activity against human K562 cells after 48 hrs by MTT assay2017Bioorganic & medicinal chemistry, 08-01, Volume: 25, Issue:15
Design, synthesis and tumor cell growth inhibitory activity of 3-nitro-2H-cheromene derivatives as histone deacetylaes inhibitors.
AID316943Inhibition of human HDAC1 assessed as histone H4 acetylation in cell based assay2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Histone deacetylase inhibitors: from bench to clinic.
AID488277Inhibition of HDAC82010Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
On the inhibition of histone deacetylase 8.
AID1915580Cytotoxicity against human K562 cells2021European journal of medicinal chemistry, Jan-01, Volume: 209Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors.
AID1474457Antiproliferative activity against human HL60 cells after 48 hrs by MTT assay2017European journal of medicinal chemistry, May-26, Volume: 132Design, synthesis and biological evaluation of novel coumarin-based benzamides as potent histone deacetylase inhibitors and anticancer agents.
AID316935Inhibition of HDAC52008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Histone deacetylase inhibitors: from bench to clinic.
AID613114Cell cycle arrest in human U937 cells assessed as accumulation at G1 phase at 5 uM after 30 hrs by propidium iodide staining based flow cytometry2011Bioorganic & medicinal chemistry, Jun-15, Volume: 19, Issue:12
Epigenetic profiling of the antitumor natural product psammaplin A and its analogues.
AID1280294Inhibition of KDAC1 in human K562 cells using [3H]acetylated histone as substrate incubated for 10 mins by liquid scintillation counting method2016Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
Design and Synthesis of Simplified Largazole Analogues as Isoform-Selective Human Lysine Deacetylase Inhibitors.
AID1847037Antitumor activity against mouse B16-F10 cells allografted in C57BL/6 mouse assessed as tumor growth inhibition at 10 mg/kg, ip administered for 14 days in presence of (2-phenylthiazol-4-yl)(3,4,5-trimethoxyphenyl)methanone
AID708271Growth inhibition of human BGC823 cells incubated for 72 hrs by WST dye reduction assay2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Pharmacokinetic optimization of class-selective histone deacetylase inhibitors and identification of associated candidate predictive biomarkers of hepatocellular carcinoma tumor response.
AID1888466Inhibition of purified human HDAC1 using Ac-Leu-Gly-(e-Ac)Lys-AMC by fluorometric HDAC assay2022Bioorganic & medicinal chemistry letters, 01-01, Volume: 55Dual-function antiandrogen/HDACi hybrids based on enzalutamide and entinostat.
AID1596036Antiproliferative activity against human A375 cells assessed as reduction in cell growth at 2 uM incubated for 72 hrs by CCK-8 assay relative to control2019European journal of medicinal chemistry, Jul-01, Volume: 173Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (HDAC) inhibitors.
AID1548726Inhibition of recombinant HDAC1 (unknown origin) using Boc-Lys(acetyl)-AMC as substrate preincubated for 1 hr followed by substrate addition and measured after 2 hrs by fluorescence based micro plate reader analysis2020Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
Design of Hydrazide-Bearing HDACIs Based on Panobinostat and Their p53 and FLT3-ITD Dependency in Antileukemia Activity.
AID269169Antitumor activity against human A549 cells xenografted in mouse at 20 mg/kg, ip2006Bioorganic & medicinal chemistry letters, Aug-01, Volume: 16, Issue:15
Substituted N-(2-aminophenyl)-benzamides, (E)-N-(2-aminophenyl)-acrylamides and their analogues: novel classes of histone deacetylase inhibitors.
AID1578488Inhibition of recombinant full length human HDAC5 expressed in baculovirus infected Sf9 cells using FAM-RHKK-TFAc as substrate incubated for 3 hrs by electrophoretic mobility shift assay2020ACS medicinal chemistry letters, Jan-09, Volume: 11, Issue:1
Class I/IIb-Selective HDAC Inhibitor Exhibits Oral Bioavailability and Therapeutic Efficacy in Acute Myeloid Leukemia.
AID313735Inhibition of HDAC72008Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2
Optimization of biaryl Selective HDAC1&2 Inhibitors (SHI-1:2).
AID1737643Cytotoxicity in human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
AID286791Effect on alpha tubulin acetylation in U937 cells at 5 uM after 24 hrs by Western blot analysis2007Journal of medicinal chemistry, May-17, Volume: 50, Issue:10
Bispyridinium dienes: histone deacetylase inhibitors with selective activities.
AID1586077Inhibition of human HDAC1 using RHKKAc as substrate by fluorescence assay2019European journal of medicinal chemistry, Jan-15, Volume: 1621-Arylsulfonyl indoline-benzamides as a new antitubulin agents, with inhibition of histone deacetylase.
AID90347Inhibition of human histone deacetylase (mixture of HDAC1 and HDAC2) prepared from K562 erythroleukemia cells.2002Bioorganic & medicinal chemistry letters, Dec-02, Volume: 12, Issue:23
Trifluoromethyl ketones as inhibitors of histone deacetylase.
AID1578489Inhibition of recombinant full length human HDAC7 expressed in baculovirus infected Sf9 cells using FAM-RHKK-TFAc as substrate incubated for 3 hrs by electrophoretic mobility shift assay2020ACS medicinal chemistry letters, Jan-09, Volume: 11, Issue:1
Class I/IIb-Selective HDAC Inhibitor Exhibits Oral Bioavailability and Therapeutic Efficacy in Acute Myeloid Leukemia.
AID1548287Induction of apoptosis in bortezomib resistant human KM3/BTZ cells assessed as necrotic cells level at 50 nM incubated for 24 hrs by Annexin V-FITC/PI staining based FCAS analysis (Rvb = 0.11%)
AID1732171Induction of cell cycle arrest in human MDA-MB-231 cells assessed as sub-G1 phase at 4 uM incubated for 72 hrs by PI staining based flow cytometry analysis (Rvb = 0.8 %)2021European journal of medicinal chemistry, Apr-05, Volume: 215CAP rigidification of MS-275 and chidamide leads to enhanced antiproliferative effects mediated through HDAC1, 2 and tubulin polymerization inhibition.
AID525033Inhibition of HDAC in human primary bronchial epithelial cells assessed as induction of mutant Fdelta508 CFTR protein apical surface localization at 5 uM2010Nature chemical biology, Jan, Volume: 6, Issue:1
Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis.
AID106868Compound was tested for antiproliferative activity against human MKN45 cancer cell lines2003Journal of medicinal chemistry, Dec-18, Volume: 46, Issue:26
Synthesis and biological evaluation of 3-(4-substituted-phenyl)-N-hydroxy-2-propenamides, a new class of histone deacetylase inhibitors.
AID1727745Induction of cell cycle arrest in human MV4-11 cells assessed as accumulation at G0/G1 phase after 24 hrs by flow cytometry2021European journal of medicinal chemistry, Jan-01, Volume: 209Discovery of selective HDAC/BRD4 dual inhibitors as epigenetic probes.
AID1873426Inhibition of HDAC1 (unknown origin) at 2 uM preincubated for 1 hr followed by 100-fold dilution and subsequent substrate addition measured after 1 hr2022Bioorganic & medicinal chemistry letters, 08-15, Volume: 70Comparison of three zinc binding groups for HDAC inhibitors - A potency, selectivity and enzymatic kinetics study.
AID1431820Selectivity ratio of IC50 for human KDAC8 to IC50 for human KDAC62017European journal of medicinal chemistry, Feb-15, Volume: 127Design and synthesis of benzodiazepine analogs as isoform-selective human lysine deacetylase inhibitors.
AID1203891Inhibition of recombinant HDAC8 (unknown origin) using fluorogenic substrate Boc-Lys (acetyl)-AMC after 20 mins by homogeneous fluorescence release assay2015European journal of medicinal chemistry, , Volume: 96Discovery and preliminary evaluation of 2-aminobenzamide and hydroxamate derivatives containing 1,2,4-oxadiazole moiety as potent histone deacetylase inhibitors.
AID1740017Inhibition of recombinant human HDAC7 using pan-HDAC substrate incubated for 3 hrs by fluorescence method2020Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
Thirty Years of HDAC Inhibitors: 2020 Insight and Hindsight.
AID1596061Cell cycle arrest in human SMMC7721 cells assessed as accumulation at G0/G1 phase at 4 uM incubated for 48 hrs by propidium iodide staining based flow cytometry (Rvb=77%)2019European journal of medicinal chemistry, Jul-01, Volume: 173Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (HDAC) inhibitors.
AID764208Intrinsic aqueous solubility of the compound at pH 7.4 by Avdeef-Tsinman potentiometric titration method2013Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
Novel N-hydroxyfurylacrylamide-based histone deacetylase (HDAC) inhibitors with branched CAP group (Part 2).
AID1446915Inhibition of Schistosoma mansoni KDAC8 using (FAM)-labeled peptide as substrate after 60 mins by microfluidic assay2017Bioorganic & medicinal chemistry, 04-01, Volume: 25, Issue:7
Structural insights of SmKDAC8 inhibitors: Targeting Schistosoma epigenetics through a combined structure-based 3D QSAR, in vitro and synthesis strategy.
AID1449333Inhibition of HDAC6 in human Cal27CisR cells assessed accumulation of acetylated alpha tubulin at 1 uM after 24 hrs by immunoblot analysis2017Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
Alkoxyurea-Based Histone Deacetylase Inhibitors Increase Cisplatin Potency in Chemoresistant Cancer Cell Lines.
AID1541445Inhibition of recombinant human full length C-terminal FLAG-tagged HDAC2 expressed in baculovirus infected Sf9 insect cells using Boc-Lys(epsilon-acetyl)-AMC as substrate incubated for 90 mins by fluorescence assay2019Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
Synthesis of Peptoid-Based Class I-Selective Histone Deacetylase Inhibitors with Chemosensitizing Properties.
AID610089Anticancer activity against human DU145 cells after 72 hrs by MTT assay2011Bioorganic & medicinal chemistry letters, Aug-15, Volume: 21, Issue:16
Design, synthesis and docking studies on benzamide derivatives as histone deacetylase inhibitors.
AID525001Inhibition of HDAC2 by in vitro deacetylation assay2010Nature chemical biology, Jan, Volume: 6, Issue:1
Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis.
AID650222Induction of cell cycle arrest in human HCT116 cells assessed as accumulation at G0/G1 phase at 10 uM after 24 hrs by flow cytometry (Rvb = 74.2 %)2012Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
Anti-tumor activity of new orally bioavailable 2-amino-5-(thiophen-2-yl)benzamide-series histone deacetylase inhibitors, possessing an aqueous soluble functional group as a surface recognition domain.
AID1596046Antiproliferative activity against human HeLa cells assessed as reduction in cell growth incubated for 72 hrs by CCK-8 assay2019European journal of medicinal chemistry, Jul-01, Volume: 173Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (HDAC) inhibitors.
AID316922Antitumor activity against human SW48 cells xenografted in nude mouse model at 20 mg/kg, ip2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Histone deacetylase inhibitors: from bench to clinic.
AID609493Inhibition of human ERG by automated patch clamp assay2011Bioorganic & medicinal chemistry letters, Aug-15, Volume: 21, Issue:16
The design, synthesis and structure-activity relationships of novel isoindoline-based histone deacetylase inhibitors.
AID324954Inhibition of wild type HDAC4 expressed in Escherichia coli at 10 uM2008Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6
Probing the elusive catalytic activity of vertebrate class IIa histone deacetylases.
AID650223Induction of cell cycle arrest in human HCT116 cells assessed as accumulation at SubG1 phase at 10 uM after 48 hrs by flow cytometry (Rvb = 2.3 %)2012Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
Anti-tumor activity of new orally bioavailable 2-amino-5-(thiophen-2-yl)benzamide-series histone deacetylase inhibitors, possessing an aqueous soluble functional group as a surface recognition domain.
AID1541550Inhibition of HDAC6 in human CAL27 cells assessed as acetylation of alpha-tubulin at 1 uM measured after 24 hrs by immunoblot analysis2019Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
Synthesis of Peptoid-Based Class I-Selective Histone Deacetylase Inhibitors with Chemosensitizing Properties.
AID385686Inhibition of flag-tagged HDAC4 by Biomol assay2007Proceedings of the National Academy of Sciences of the United States of America, Oct-30, Volume: 104, Issue:44
Unraveling the hidden catalytic activity of vertebrate class IIa histone deacetylases.
AID607634Inhibition of HDAC6 in human Hela cells assessed as increase in total lysine acetylation at 0.6 uM after 16 hrs by immunofluorescence microscopy2011Bioorganic & medicinal chemistry letters, Jul-15, Volume: 21, Issue:14
A novel HDAC inhibitor with a hydroxy-pyrimidine scaffold.
AID1466403Antitumor activity against human HCT116 cells xenografted in BALB/c nude mouse assessed as relative tumor increment ratio at 50 mg/kg/day administered via oral gavage for 16 days measured every 3 days2017European journal of medicinal chemistry, Jul-07, Volume: 134Selective HDAC inhibitors with potent oral activity against leukemia and colorectal cancer: Design, structure-activity relationship and anti-tumor activity study.
AID1847003Induction of apoptosis in mouse B16-F10 cells assessed as necrotic cells at 100 nM incubated for 48 hrs by Annexin V-FITC/PI analysis (Rvb = 0.012 %)
AID1231807Inhibition of recombinant HDAC1 (unknown origin) incubated for 10 mins using Boc-Lys(acetyl)-AMC fluorogenic substrate by homogeneous fluorescence release assay2015Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13
Discovery, bioactivity and docking simulation of Vorinostat analogues containing 1,2,4-oxadiazole moiety as potent histone deacetylase inhibitors and antitumor agents.
AID1466397Antitumor activity against human U937 cells xenografted in BALB/c nude mouse assessed as relative tumor increment ratio at 50 mg/kg/day administered via oral gavage for 13 days measured every 3 days2017European journal of medicinal chemistry, Jul-07, Volume: 134Selective HDAC inhibitors with potent oral activity against leukemia and colorectal cancer: Design, structure-activity relationship and anti-tumor activity study.
AID420322Inhibition of Bordetella / Alcaligenes strain FB188 HDAC6 by fluorogenic enzyme assay2009Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
Non-isotopic dual parameter competition assay suitable for high-throughput screening of histone deacetylases.
AID1846957Antiproliferative activity against human Jurkat cells assessed as inhibition of cell viability measured for 48 hrs by microplate reader based CCK-8 assay
AID313731Inhibition of HDAC32008Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2
Optimization of biaryl Selective HDAC1&2 Inhibitors (SHI-1:2).
AID1873479Inhibition of full length C-terminal His-tagged HDAC3 (unknown origin)/N-terminal GST-tagged NCoR2 (unknown origin) using (Ac-Leu-Gly-Lys(Ac)-AMC as substrate preincubated with enzyme and inositol hexa phosphate for 2 hrs followed by substrate addition an2022ACS medicinal chemistry letters, May-12, Volume: 13, Issue:5
Determination of Slow-Binding HDAC Inhibitor Potency and Subclass Selectivity.
AID1453358Antiproliferative activity against HEL cells after 48 hrs by MTT assay2017Bioorganic & medicinal chemistry, 06-15, Volume: 25, Issue:12
Design, synthesis and anti-tumor activity study of novel histone deacetylase inhibitors containing isatin-based caps and o-phenylenediamine-based zinc binding groups.
AID777597Effect on HDAC in human HaCaT cells assessed as downregulation of miR-629 at 10 uM after 1 hr by RT-PCR analysis2013ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
Synthesis and Biological Evaluation of the First Example of NO-Donor Histone Deacetylase Inhibitor.
AID1466392Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay2017European journal of medicinal chemistry, Jul-07, Volume: 134Selective HDAC inhibitors with potent oral activity against leukemia and colorectal cancer: Design, structure-activity relationship and anti-tumor activity study.
AID360094Inhibition of LPS-induced tissue factor activity in HUVEC preincubated for 4 hrs assessed after 4 hrs of LPS challenge by one stage clotting assay2007The Journal of biological chemistry, Sep-28, Volume: 282, Issue:39
Histone deacetylase inhibitors suppress TF-kappaB-dependent agonist-driven tissue factor expression in endothelial cells and monocytes.
AID1548299Induction of apoptosis in bortezomib resistant human KM3/BTZ cells assessed as necrotic cells level at 200 nM incubated for 24 hrs in presence of bortezomib by Annexin V-FITC/PI staining based FCAS analysis (Rvb = 0.11%)
AID385691Inhibition of flag-tagged HDAC4 expressed in HEK293 cells upto 10,000 nM by Biomol assay2007Proceedings of the National Academy of Sciences of the United States of America, Oct-30, Volume: 104, Issue:44
Unraveling the hidden catalytic activity of vertebrate class IIa histone deacetylases.
AID1454739Lipophilicity, log P of the compound at pH 7.42018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Class I HDAC Inhibitors: Potential New Epigenetic Therapeutics for Alcohol Use Disorder (AUD).
AID1401904Inhibition of human recombinant HDAC6 using Fluor de Lys-Green as substrate preincubated for 5 mins followed by substrate addition and measured after 1 hr by fluorescence assay2018European journal of medicinal chemistry, Jan-01, Volume: 143Design, synthesis and biological evaluation of novel 2-aminobenzamides containing dithiocarbamate moiety as histone deacetylase inhibitors and potent antitumor agents.
AID90666Inhibitory activity on partially purified recombinant human Histone deacetylase 1 (HDAC-1)2003Journal of medicinal chemistry, Feb-27, Volume: 46, Issue:5
Development of potential antitumor agents. Synthesis and biological evaluation of a new set of sulfonamide derivatives as histone deacetylase inhibitors.
AID316918Antitumor activity against human A549 cells xenografted in nude mouse model at 20 mg/kg, ip2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Histone deacetylase inhibitors: from bench to clinic.
AID519594Selectivity index, ratio of IC50 for breast fibroblasts to IC50 for chloroquine-sensitive Plasmodium falciparum 3D72008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Potent antimalarial activity of histone deacetylase inhibitor analogues.
AID1732208Cytotoxicity against human NCI-H1299 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay2021European journal of medicinal chemistry, Apr-05, Volume: 215CAP rigidification of MS-275 and chidamide leads to enhanced antiproliferative effects mediated through HDAC1, 2 and tubulin polymerization inhibition.
AID90529Inhibitory concentration against histone deacetylase2003Journal of medicinal chemistry, Nov-20, Volume: 46, Issue:24
Histone deacetylase inhibitors.
AID1466399Toxicity in BALB/c nude mouse xenografted with human U937 cells assessed as body weight at 50 mg/kg/day administered via oral gavage for 13 days (Rvb = 25.39 +/- 1.18 g)2017European journal of medicinal chemistry, Jul-07, Volume: 134Selective HDAC inhibitors with potent oral activity against leukemia and colorectal cancer: Design, structure-activity relationship and anti-tumor activity study.
AID1401895Antiproliferative activity against human A375 cells after 72 hrs by CCK-8 assay2018European journal of medicinal chemistry, Jan-01, Volume: 143Design, synthesis and biological evaluation of novel 2-aminobenzamides containing dithiocarbamate moiety as histone deacetylase inhibitors and potent antitumor agents.
AID1548736Inhibition of recombinant human C-terminal His-tagged HDAC9 (604 to 1066 residues) expressed in baculovirus infected Sf9 cells using Boc-Lys (trifluoroacetyl)-AMC as substrate preincubated for 1 hr followed by substrate addition and measured after 2 hrs b2020Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
Design of Hydrazide-Bearing HDACIs Based on Panobinostat and Their p53 and FLT3-ITD Dependency in Antileukemia Activity.
AID1586080Inhibition of human HDAC4 using Boc-Lys(trifluoroacetyl)-AMC as substrate by fluorescence assay2019European journal of medicinal chemistry, Jan-15, Volume: 1621-Arylsulfonyl indoline-benzamides as a new antitubulin agents, with inhibition of histone deacetylase.
AID1881856Vasodilating activity in rat aorta2022European journal of medicinal chemistry, Jan-05, Volume: 227NO-HDAC dual inhibitors.
AID1401889Antiproliferative activity against human MGC803 cells at 2 uM after 72 hrs by CCK-8 assay relative to control2018European journal of medicinal chemistry, Jan-01, Volume: 143Design, synthesis and biological evaluation of novel 2-aminobenzamides containing dithiocarbamate moiety as histone deacetylase inhibitors and potent antitumor agents.
AID1466389Antiproliferative activity against human K562 cells after 48 hrs by MTT assay2017European journal of medicinal chemistry, Jul-07, Volume: 134Selective HDAC inhibitors with potent oral activity against leukemia and colorectal cancer: Design, structure-activity relationship and anti-tumor activity study.
AID1466404Toxicity in BALB/c nude mouse xenografted with human HCT116 cells assessed as body weight at 50 mg/kg/day administered via oral gavage for 16 days (Rvb = 19.91 +/- 1.26 g)2017European journal of medicinal chemistry, Jul-07, Volume: 134Selective HDAC inhibitors with potent oral activity against leukemia and colorectal cancer: Design, structure-activity relationship and anti-tumor activity study.
AID1548286Induction of apoptosis in bortezomib resistant human KM3/BTZ cells assessed as late apoptotic cells level at 50 nM incubated for 24 hrs by Annexin V-FITC/PI staining based FCAS analysis (Rvb = 0.38%)
AID1596037Antiproliferative activity against human HeLa cells assessed as reduction in cell growth at 8 uM incubated for 72 hrs by CCK-8 assay relative to control2019European journal of medicinal chemistry, Jul-01, Volume: 173Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (HDAC) inhibitors.
AID650219Induction of cell cycle arrest in human HCT116 cells assessed as accumulation at S phase at 10 uM after 48 hrs by flow cytometry (Rvb = 10.4 %)2012Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
Anti-tumor activity of new orally bioavailable 2-amino-5-(thiophen-2-yl)benzamide-series histone deacetylase inhibitors, possessing an aqueous soluble functional group as a surface recognition domain.
AID1401919Induction of apoptosis in human SMMC7721 cells assessed as necrotic cells at 4 umol/L after 72 hrs by Alexa Fluor 488 Annexin/propidium iodide staining-based flow cytometric analysis (Rvb = 2.48%)2018European journal of medicinal chemistry, Jan-01, Volume: 143Design, synthesis and biological evaluation of novel 2-aminobenzamides containing dithiocarbamate moiety as histone deacetylase inhibitors and potent antitumor agents.
AID1676596Binding affinity to Ferric ion assessed as retention ratio by measuring compound detected in elution fraction/total compound detected at 2.55 umol by immobilized metal-ion affinity chromatography2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors.
AID1474458Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay2017European journal of medicinal chemistry, May-26, Volume: 132Design, synthesis and biological evaluation of novel coumarin-based benzamides as potent histone deacetylase inhibitors and anticancer agents.
AID374827Antiproliferative activity against human P53 expressing A549 cells after 72 hrs by celltiter-blue cell viability assay2009Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
Discovery of a potent class I selective ketone histone deacetylase inhibitor with antitumor activity in vivo and optimized pharmacokinetic properties.
AID1235132Inhibition of HDAC1 (unknown origin) preincubated for 5 mins followed by fluorogenic substrate addition measured after 30 mins by microplate reader analysis2015European journal of medicinal chemistry, Jul-15, Volume: 100Design, synthesis and antiproliferative activities of novel benzamides derivatives as HDAC inhibitors.
AID1548276Antiproliferative activity against bortezomib resistant human KM3/BTZ cells assessed combination index in presence of bortezomib at 1:1 compound to bortezomib ratio incubated for 48 hrs by MTT assay
AID1873445Inhibition of full length C-terminal His-tagged HDAC1 (unknown origin) assessed as rate constant (k-2) of EI complex using (Ac-Leu-Gly-Lys(Ac)-AMC as substrate measured every 30 sec for 60 mins by fluorescence based assay2022ACS medicinal chemistry letters, May-12, Volume: 13, Issue:5
Determination of Slow-Binding HDAC Inhibitor Potency and Subclass Selectivity.
AID1401921Cell cycle arrest in human SMMC7721 cells assessed as accumulation of cells at S phase at 0.125 umol/L after 72 hrs by propidium iodide staining-based flow cytometric analysis (Rvb = 5.21%)2018European journal of medicinal chemistry, Jan-01, Volume: 143Design, synthesis and biological evaluation of novel 2-aminobenzamides containing dithiocarbamate moiety as histone deacetylase inhibitors and potent antitumor agents.
AID525002Inhibition of HDAC3 by in vitro deacetylation assay2010Nature chemical biology, Jan, Volume: 6, Issue:1
Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis.
AID777601Induction of HDAC4 nuclear shuttling in human HaCaT cells at 10 uM after 1 hr by immunofluorescence method relative to DMSO-treated control2013ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
Synthesis and Biological Evaluation of the First Example of NO-Donor Histone Deacetylase Inhibitor.
AID1596035Antiproliferative activity against human A375 cells assessed as reduction in cell growth at 8 uM incubated for 72 hrs by CCK-8 assay relative to control2019European journal of medicinal chemistry, Jul-01, Volume: 173Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (HDAC) inhibitors.
AID316886Antiproliferative activity against human SKBR3 cells2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Histone deacetylase inhibitors: from bench to clinic.
AID1847012Upregulation of AC-H3 in mouse B16-F10 cells incubated for 12 hrs by Western blot analysis
AID1466391Antiproliferative activity against human U266 cells after 48 hrs by MTT assay2017European journal of medicinal chemistry, Jul-07, Volume: 134Selective HDAC inhibitors with potent oral activity against leukemia and colorectal cancer: Design, structure-activity relationship and anti-tumor activity study.
AID1548298Induction of apoptosis in bortezomib resistant human KM3/BTZ cells assessed as late apoptotic cells level at 200 nM incubated for 24 hrs in presence of bortezomib by Annexin V-FITC/PI staining based FCAS analysis (Rvb = 0.38%)
AID1901173Inhibition of HDAC1/HDAC2/HDAC3 in human HCT-116 cells assessed as increase in accumulation of acetylated H3K9 at 5 uM treated for 48 hrs by Western blot analysis2022Bioorganic & medicinal chemistry, 02-15, Volume: 56Synthesis and biological evaluation of aminobenzamides containing purine moiety as class I histone deacetylases inhibitors.
AID1380941Antiproliferative activity against human ACHN cells after 72 hrs by MTT assay2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Discovery of Novel Pazopanib-Based HDAC and VEGFR Dual Inhibitors Targeting Cancer Epigenetics and Angiogenesis Simultaneously.
AID664384Inhibition of HDAC102012European journal of medicinal chemistry, Jul, Volume: 53Appraisal of GABA and PABA as linker: design and synthesis of novel benzamide based histone deacetylase inhibitors.
AID1548304Induction of cell cycle arrest in bortezomib resistant human KM3/BTZ cells assessed as accumulation at S phase at 100 nM incubated for 24 hrs in presence of bortezomib by propidium iodide staining based flow cytometry (Rvb = 46%)
AID1596056Cell cycle arrest in human SMMC7721 cells assessed as accumulation at S phase at 0.25 uM incubated for 48 hrs by propidium iodide staining based flow cytometry (Rvb=6.83%)2019European journal of medicinal chemistry, Jul-01, Volume: 173Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (HDAC) inhibitors.
AID322414Antiproliferative activity against human LNCap by MTT assay2008Bioorganic & medicinal chemistry, Mar-15, Volume: 16, Issue:6
Improved synthesis of histone deacetylase inhibitors (HDIs) (MS-275 and CI-994) and inhibitory effects of HDIs alone or in combination with RAMBAs or retinoids on growth of human LNCaP prostate cancer cells and tumor xenografts.
AID519584Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 infected in O+ human erythrocytes by [3H]hypoxanthine incorporation assay2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Potent antimalarial activity of histone deacetylase inhibitor analogues.
AID1586068Growth inhibition of human A549 cells after 48 hrs by SRB assay2019European journal of medicinal chemistry, Jan-15, Volume: 1621-Arylsulfonyl indoline-benzamides as a new antitubulin agents, with inhibition of histone deacetylase.
AID1280297Inhibition of KDAC8 in human K562 cells using [3H]acetylated histone as substrate incubated for 10 mins by liquid scintillation counting method2016Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
Design and Synthesis of Simplified Largazole Analogues as Isoform-Selective Human Lysine Deacetylase Inhibitors.
AID664381Inhibition of HDAC82012European journal of medicinal chemistry, Jul, Volume: 53Appraisal of GABA and PABA as linker: design and synthesis of novel benzamide based histone deacetylase inhibitors.
AID90208Inhibitory activity against partially purified histone deacetylase of human leukemia K562 cells.1999Journal of medicinal chemistry, Jul-29, Volume: 42, Issue:15
Synthesis and histone deacetylase inhibitory activity of new benzamide derivatives.
AID664383Inhibition of HDAC62012European journal of medicinal chemistry, Jul, Volume: 53Appraisal of GABA and PABA as linker: design and synthesis of novel benzamide based histone deacetylase inhibitors.
AID1737654Cytotoxicity against human HDACi-sensitive YCC3 cells assessed as reduction in cell growth incubated for 72 hrs by MTS assay
AID1740015Inhibition of recombinant human HDAC8 using pan-HDAC substrate incubated for 3 hrs by fluorescence method2020Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
Thirty Years of HDAC Inhibitors: 2020 Insight and Hindsight.
AID1847018Toxicity in C57BL/6 mouse allografted with mouse B16-F10 cells assessed as morphological abnormalities in kidney at 5 mg/kg, ip administered for 14 days in presence of (2-phenylthiazol-4-yl)(3,4,5-trimethoxyphenyl)methanone by H and E staining based analy
AID1596064Induction of apoptosis in human SMMC7721 cells assessed as viable cells at 0.25 uM incubated for 48 hrs by Annexin-V-FITC/propidium iodide staining based flow cytometry (Rvb=93.5%)2019European journal of medicinal chemistry, Jul-01, Volume: 173Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (HDAC) inhibitors.
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1745854NCATS anti-infectives library activity on HEK293 viability as a counter-qHTS vs the C. elegans viability qHTS2023Disease models & mechanisms, 03-01, Volume: 16, Issue:3
In vivo quantitative high-throughput screening for drug discovery and comparative toxicology.
AID1745855NCATS anti-infectives library activity on the primary C. elegans qHTS viability assay2023Disease models & mechanisms, 03-01, Volume: 16, Issue:3
In vivo quantitative high-throughput screening for drug discovery and comparative toxicology.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (550)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's2 (0.36)18.2507
2000's125 (22.73)29.6817
2010's312 (56.73)24.3611
2020's111 (20.18)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 42.81

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index42.81 (24.57)
Research Supply Index6.38 (2.92)
Research Growth Index6.91 (4.65)
Search Engine Demand Index62.74 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (42.81)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials31 (5.57%)5.53%
Reviews32 (5.75%)6.00%
Case Studies1 (0.18%)4.05%
Observational0 (0.00%)0.25%
Other493 (88.51%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (71)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Phase I Study of GSK525762C and Entinostat in Advanced and Refractory Solid Tumors and Lymphomas [NCT03925428]Phase 10 participants (Actual)Interventional2020-09-18Withdrawn(stopped due to Other - Protocol moved to Disapproved)
A Phase Ib Study of Entinostat and FOLFOX in Subjects With Pancreatic Adenocarcinoma [NCT03760614]Phase 10 participants (Actual)Interventional2021-01-31Withdrawn(stopped due to Lack of Funding)
A Phase 1, Randomized, Open-Label, Continuation Study of Entinostat in Combination With Pembrolizumab in Patients With Advanced Solid Tumors (SNDX-275-0141, MK3475-460/KEYNOTE-460) [NCT02909452]Phase 130 participants (Actual)Interventional2016-09-20Completed
Phase I/II Study of High Dose Interleukin 2, Aldesleukin, in Combination With the Histone Deacetylase Inhibitor Entinostat in Patients With Metastatic Renal Cell Carcinoma [NCT01038778]Phase 1/Phase 247 participants (Actual)Interventional2009-10-29Active, not recruiting
A Phase 1b Study of the Anti-PD1 Antibody Pembrolizumab in Combination With the Histone Deacetylase Inhibitor, Entinostat for Treatment of Patients With Myelodysplastic Syndromes After DNA Methyltransferase Inhibitor Therapy Failure [NCT02936752]Phase 127 participants (Anticipated)Interventional2017-04-03Active, not recruiting
A Phase II Study of Pembrolizumab and Entinostat in Patients With Relapsed and Refractory Lymphomas [NCT03179930]Phase 247 participants (Anticipated)Interventional2017-06-07Recruiting
A Phase I Study of Entinostat in Combination With Enzalutamide for Treatment of Patients With Castration-Resistant Prostate Cancer [NCT03829930]Phase 16 participants (Actual)Interventional2019-05-01Terminated(stopped due to Sponsor discontinued the drug)
A Randomized Surgical Window Pilot Investigation of the Relationship of Short Term Medroxyprogesterone Acetate (NSC #26386) Compared to Medroxyprogesterone Acetate Plus Entinostat (NSC #706995) on the Morphologic, Biochemical, and Molecular Changes in Pri [NCT03018249]Early Phase 150 participants (Actual)Interventional2017-10-11Completed
A Phase 2, Randomized, Double-Blind, Multicenter Study of Fulvestrant With and Without Entinostat in Postmenopausal Women With Hormone Receptor-Positive Advanced Breast Cancer [NCT02115594]Phase 20 participants (Actual)Interventional2014-04-30Withdrawn(stopped due to Internal decision)
A Phase I/II Study of Combination Immunotherapy for Advanced Cancers Including HPV-Associated Malignancies, Small Bowel, and Colon Cancers [NCT04708470]Phase 1/Phase 290 participants (Anticipated)Interventional2021-10-05Recruiting
A Phase 2 Multicenter Study of the Effect of the Addition of SNDX-275 to Continued Aromatase Inhibitor (AI) Therapy in Postmenopausal Women With ER+ Breast Cancer Whose Disease is Progressing [NCT00828854]Phase 227 participants (Actual)Interventional2008-10-01Completed
A Phase I Study of the Histone Deacetylase Inhibitor Entinostat (SNDX-275, NSC 706995) Plus Clofarabine for Philadelphia Chromosome-Negative, Poor Risk Acute Lymphoblastic Leukemia or Bilineage/Biphenotypic Leukemia in Newly Diagnosed Older Adults or in A [NCT01132573]Phase 127 participants (Actual)Interventional2010-04-30Completed
A Phase II Study to Evaluate the Safety, Pharmacodynamics, and Efficacy of Entinostat in Combination With Nivolumab Plus Ipilimumab in Patients With Renal Cell Carcinoma Previously Treated With Nivolumab Plus Ipilimumab [NCT03552380]Phase 218 participants (Anticipated)Interventional2018-08-31Active, not recruiting
A Phase I/II Study of Olaparib With Entinostat in the Treatment of Recurrent, Platinum-Refractory or Resistant, Homologous Recombination Repair Proficient Ovarian, Primary Peritoneal, and Fallopian Tube Cancers [NCT03924245]Phase 13 participants (Actual)Interventional2020-10-01Terminated(stopped due to Change in participant landscape and other treatment availability)
A Phase I Study of Sorafenib in Combination With the Histone Deacetylase Inhibitor, Entinostat in Patients With Advanced Cancers [NCT01159301]Phase 144 participants (Actual)Interventional2010-06-30Terminated
A Pilot Study of the Combination of Entinostat With Capecitabine in High Risk Breast Cancer After Neo-adjuvant Therapy [NCT03473639]Phase 113 participants (Actual)Interventional2019-01-29Completed
A Phase 1b Trial of Sequential Combinations of BN-Brachyury, Entinostat, Ado-trastuzuamb Emtansine and M7824 in Advanced Stage Breast Cancer (BrEAsT) [NCT04296942]Phase 11 participants (Actual)Interventional2021-05-04Terminated(stopped due to One participant was accrued, and the study was stopped due to new safety data from the company for M7824 and slow accrual.)
A Phase 2, Randomized, Double-Blind, Multicenter Study of Exemestane With and Without SNDX-275 in Postmenopausal Women With Locally Recurrent or Metastatic Estrogen Receptor-Positive Breast Cancer, Progressing on Treatment With a Non-Steroidal Aromatase I [NCT00676663]Phase 2130 participants (Actual)Interventional2008-06-13Completed
A Randomized Phase II Trial to Simultaneously Evaluate Two Schedules of the Histone Deacetylase Inhibitor Entinostat in Combination With 5-Azacytidine (5AC, NSC 102816) in Elderly Patients With Acute Myeloid Leukemia (AML) [NCT01305499]Phase 252 participants (Actual)Interventional2011-07-01Active, not recruiting
A Phase 1, Open-Label, Parallel-Cohort, Single-Dose Study to Evaluate the Pharmacokinetics of Entinostat in Adult Subjects With Normal and Impaired Renal Function [NCT03192111]Phase 140 participants (Actual)Interventional2017-07-27Completed
A Randomized Phase III Clinical Study of Entinostat/Placebo in Combination With Exemestane in Chinese Patients With Hormone Receptor-positive Advanced Breast Cancer [NCT03538171]Phase 3375 participants (Actual)Interventional2018-05-15Active, not recruiting
Breaking Innate PD-1 Inhibitor (PD1i) Resistance Using Epigenetic Modifiers; Antitumor Efficacy and Correlative Analyses of Entinostat Plus Pembrolizumab in Non-Inflamed Metastatic Melanoma (MM) [NCT03765229]Phase 211 participants (Actual)Interventional2019-03-22Completed
A Phase 1 Cardiac Safety Study of Entinostat in Men and Women With Advanced Solid Tumors [NCT02897778]Phase 130 participants (Actual)Interventional2016-08-24Completed
An Open-Label, 3-Part, 2-Period Study to Examine the Effect of Omeprazole (Part 1), Famotidine (Part 2), and of an Acidic Beverage (Part 3) on the Single-Dose Pharmacokinetics of Entinostat in Healthy Adult Subjects [NCT02922933]Phase 166 participants (Actual)Interventional2016-10-25Completed
A Randomized, Placebo-controlled, Double-blind, Multicenter Phase 2 Study With a Lead in Phase of Erlotinib With or Without SNDX-275 in Patients With NSCLC After Failure In Up to Two Prior Chemotherapeutic Regimens for Advanced Disease [NCT00602030]Phase 1/Phase 2141 participants (Actual)Interventional2008-01-08Completed
A Phase I/II Study of Entinostat in Combination With 5-Azacytidine in Patients With Recurrent Advanced Non-Small Cell Lung Cancer [NCT00387465]Phase 1/Phase 294 participants (Actual)Interventional2006-08-31Completed
A Phase 2 Multi-Center Study of Entinostat (SNDX-275) in Patients With Relapsed or Refractory Hodgkin's Lymphoma [NCT00866333]Phase 249 participants (Actual)Interventional2009-04-13Terminated(stopped due to Terminated prior to completion of accrual per corporate decision.)
Phase II Study of Azacitidine and Entinostat (SNDX-275) in Patients With Advanced Breast Cancer [NCT01349959]Phase 258 participants (Actual)Interventional2011-04-21Active, not recruiting
A Phase I and Pharmacokinetic Study to Evaluate Histone Deacetylase Inhibitor, Entinostat in Chinese Postmenopausal Women Patients With Locally Recurrent or Metastatic Breast Cancer [NCT02833155]Phase 119 participants (Actual)Interventional2016-08-29Completed
Phase I Clinical-Labratory Study of the Histone Deacetylase (HDA) Inhibitor MS-275 in Adults With Refractory and Relapsed Hematologic Malignancies [NCT00015925]Phase 10 participants Interventional2001-02-28Completed
A 2-Stage, Open-Label, Randomized, Single-Dose, Crossover Study to Determine the Effect of the Timing of a Meal on the Pharmacokinetics of Entinostat in Healthy Adult Subjects [NCT02922946]Phase 147 participants (Actual)Interventional2016-10-11Completed
GCC 0927 A Pilot and Phase II Study of Entinostat and Anastrozole/Tamoxifen in Women With Triple Negative Breast Cancer to Evaluate Biomarkers and Surrogates for Response [NCT01234532]Phase 25 participants (Actual)Interventional2010-10-31Terminated(stopped due to low accrual)
A Phase 2, Exploratory Study of Erlotinib and SNDX-275 in Patients With Non-small Cell Lung Carcinoma Who Are Progressing on Erlotinib [NCT00750698]Phase 28 participants (Actual)Interventional2008-08-31Terminated(stopped due to Due to business reasons, enrollment on the study was halted and the study terminated. The decision to close enrollment was not due to any safety concern.)
A Phase Ib/II, Open-Label, Multicenter, Randomized Umbrella Study Evaluating the Efficacy and Safety of Multiple Immunotherapy-Based Treatment Combinations in Patients With Hormone Receptor-Positive HER2-Negative Breast Cancer (MORPHEUS-HR+ Breast Cancer) [NCT03280563]Phase 1/Phase 2138 participants (Actual)Interventional2017-12-26Active, not recruiting
A Randomized Phase II Trial of Azacitidine With or Without the Histone Deacetylase Inhibitor Entinostat for the Treatment of Myelodysplastic Syndrome, Chronic Myelomonocytic Leukemia (Dysplastic Type), and Acute Myeloid Leukemia With Multilineage Dysplasi [NCT00313586]Phase 2197 participants (Actual)Interventional2006-08-31Completed
Genome-Wide Methylation and Gene Re-expression Analysis of Resectable Lung Tumor Tissue Pairs Obtained Pre- and Post-Treatment With 5-Azacytidine and Entinostat [NCT01886573]Phase 140 participants (Anticipated)Interventional2013-06-30Terminated
A Phase II Study of and Oral Histone Deacytylase Inhibitor, MS-275 (NSC 706995), in Combination With Sargramostim (GM-CSF, Berlex, Inc.) Treating Relapsed and Refractory Myeloid Malignancies [NCT00462605]Phase 224 participants (Actual)Interventional2007-04-30Completed
Phase I/II Evaluation of a Cancer Lysate Vaccine and Montanide(R) ISA-51 VG With Entinostat and Nivolumab as Adjuvant Therapy Following Chemoradiation Therapy With or Without Surgery for Locally Advanced Esophageal Cancer [NCT05898828]Phase 1/Phase 250 participants (Anticipated)Interventional2024-01-03Recruiting
A Phase 1b/2, Open-label, Dose Escalation Study of Entinostat in Combination With Pembrolizumab in Patients With Non-small Cell Lung Cancer, With Expansion Cohorts in Patients With Non-small Cell Lung Cancer, Melanoma, and Mismatch Repair-Proficient Color [NCT02437136]Phase 1/Phase 2196 participants (Actual)Interventional2015-07-31Completed
Phase II Study of Azacitadine and Entinostat in Patients With Metastatic Colorectal Cancer [NCT01105377]Phase 247 participants (Actual)Interventional2010-04-30Completed
A Phase II Randomized, Open Label Study of High Dose Interleukin 2 vs High Dose Interleukin 2 Plus Entinostat in Advanced Renal Cell Carcinoma [NCT03501381]Phase 246 participants (Anticipated)Interventional2018-05-24Active, not recruiting
Study of KHK2375 in Subjects With Advanced or Recurrent Breast Cancer [NCT03291886]Phase 2133 participants (Actual)Interventional2017-09-22Completed
Phase II Study of MS-275, a Histone Deacetylase Inhibitor, Comparing 2 Dosage Schedules in Patients With Metastatic Melanoma [NCT00185302]Phase 228 participants (Actual)Interventional2004-12-31Completed
Phase 1 Study of KHK2375 in Subjects With Advanced or Recurrent Breast Cancer [NCT02623751]Phase 115 participants (Actual)Interventional2015-11-30Completed
A Phase 1 Study of Entinostat, an Oral Histone Deacetylase Inhibitor, in Pediatric Patients With Recurrent or Refractory Solid Tumors, Including CNS Tumors and Lymphoma [NCT02780804]Phase 121 participants (Actual)Interventional2017-01-06Completed
A Phase I Study to Assess the Food Effect on the Pharmacokinetics of Entinostat in Postmenopausal Women With Locally Recurrent or Metastatic ER+ Breast Cancer and Men and Women With Progressive Non-Small Cell Lung Cancer [NCT01594398]Phase 114 participants (Actual)Interventional2012-05-31Completed
A Randomized Phase III Trial of Endocrine Therapy Plus Entinostat/Placebo in Patients With Hormone Receptor-Positive Advanced Breast Cancer [NCT02115282]Phase 3608 participants (Actual)Interventional2014-03-29Active, not recruiting
A Phase I Study of an Oral Histone Deacetylase Inhibitor, MS-275 (NSC 706995, IND 61,198), in Combination With 13-Cis-Retinoic Acid in Metastatic Progressive Cancer. [NCT00098891]Phase 124 participants (Actual)Interventional2004-10-31Completed
A Dose-Finding Trial of the Histone Deacetylase Inhibitor MS-275 (NSC 706995) in Combination With 5-Azacitidine (5AC, NSC 102816) in Patients With Myelodysplastic Syndromes (MDS), Chronic Myelomonocytic Leukemia (CMMoL) and Acute Myeloid Leukemia (AML) [NCT00101179]Phase 163 participants (Actual)Interventional2004-11-03Completed
A Phase I Study of an Oral Histone Deacetylase Inhibitor, MS-275, in Refractory Solid Tumors and Lymphomas [NCT00020579]Phase 175 participants (Anticipated)Interventional2001-03-31Completed
A Phase I/II Study to Evaluate the Safety, Pharmacodynamics and Efficacy of Atezolizumab in Combination With Entinostat and Bevacizumab in Patients With Advanced Renal Cell Carcinoma [NCT03024437]Phase 1/Phase 272 participants (Anticipated)Interventional2017-06-29Suspended(stopped due to Major review underway)
A Phase 1/2 Study of SNDX-275 in Combination With Imatinib for Relapsed/Refractory Philadelphia Chromosome Positive Acute Lymphoblastic Leukemia [NCT01383447]Phase 1/Phase 22 participants (Actual)Interventional2010-10-31Terminated(stopped due to This study was halted prematurely by the NCI for low accrual.)
Phase I and Phase I Trastuzumab Cohort Study of Entinostat, Lapatinib and Trastuzumab in Patients With HER2-Positive Metastatic Breast Cancer in Whom Trastuzumab Has Failed [NCT01434303]Phase 137 participants (Actual)Interventional2012-01-10Completed
A Phase I, Multicenter, Open Label Study on the Effects of SNDX-275 on Expression of Biomarkers in Subjects With Newly Diagnosed Breast Cancer [NCT00754312]Phase 11 participants (Actual)Interventional2008-06-30Terminated
Randomized Phase II Trial of Adjuvant Combined Epigenetic Therapy With 5-Azacitidine and Entinostat in Resected Stage I Non-small Cell Lung Cancer Versus Standard Care [NCT01207726]Phase 213 participants (Actual)Interventional2010-09-30Terminated(stopped due to Slow Accrual due to patients not wanting daily clinic administration of 5AZA and/or 6 months of treatment after surgery.)
A Multicenter Phase II Open Label Study to Evaluate Efficacy of Concomitant Use of Pembrolizumab and Entinostat in Adult Patients With Metastatic Uveal Melanoma [NCT02697630]Phase 229 participants (Actual)Interventional2018-02-21Completed
A Phase 2 Clinical Trial of Entinostat in Combination With Nivolumab for Patients With Previously Treated Unresectable or Metastatic Cholangiocarcinoma and Pancreatic Adenocarcinoma [NCT03250273]Phase 244 participants (Actual)Interventional2017-11-06Completed
A Non-randomized, Non-comparative, Open-label, Window Trial of Entinostat Given With or Without Exemestane in Patients With Newly Diagnosed, Stage I-IIIC, Hormone Receptor - Positive (HR+) or Triple Negative Breast Cancer (TNBC) [NCT03361800]Early Phase 15 participants (Actual)Interventional2018-11-28Terminated(stopped due to Funding withdrawn.)
An Open Label, 2-Period Study to Assess the Effect of Entinostat on the Pharmacokinetics of Midazolam in Healthy Adult Subjects [NCT03187015]Phase 126 participants (Actual)Interventional2017-05-23Completed
Phase I/II Trial of Regorafenib, Hydroxychloroquine, and Entinostat in Metastatic Colorectal Cancer [NCT03215264]Phase 120 participants (Actual)Interventional2017-10-02Completed
A Phase 2 Single-Arm Multicenter Study of Entinostat in Patients With Relapsed or Refractory Abdominal Neuroendocrine (NE) Tumors [NCT03211988]Phase 25 participants (Actual)Interventional2017-12-23Terminated(stopped due to Lack of funding and drug supply)
A Phase II Study of Epigenetic Therapy With Azacitidine and Entinostat With Concurrent Nivolumab in Subjects With Metastatic Non-Small Cell Lung Cancer. [NCT01928576]Phase 2101 participants (Actual)Interventional2013-11-06Completed
A Randomized, Placebo-controlled, Double-blind, Multicenter Phase 2 Study of Atezolizumab With or Without Entinostat in Patients With Advanced Triple Negative Breast Cancer, With a Phase 1b Lead in Phase [NCT02708680]Phase 1/Phase 289 participants (Actual)Interventional2016-05-31Completed
Phase Ib/II Study of ZEN003694 and Entinostat in Advanced and Refractory Solid Tumors and Lymphomas [NCT05053971]Phase 1/Phase 230 participants (Anticipated)Interventional2022-11-16Recruiting
A Randomized Phase II Trial of Cytotoxic Chemotherapy With or Without Epigenetic Priming in Patients With Advanced Non-Small Cell Lung Cancer [NCT01935947]Phase 217 participants (Actual)Interventional2013-05-31Terminated
Window of Opportunity Platform Study to Define Immunogenomic Changes With Pembrolizumab Alone and in Rational Combinations in Muscle-Invasive Bladder Cancer [NCT03978624]Phase 220 participants (Anticipated)Interventional2020-09-23Active, not recruiting
A Randomized, Placebo-controlled, Double-blind, Multicenter Phase 1b/2 Study of Avelumab With or Without Entinostat in Patients With Advanced Epithelial Ovarian Cancer Which Has Progressed or Recurred After First-line Platinum-based Chemotherapy and at Le [NCT02915523]Phase 1/Phase 2140 participants (Actual)Interventional2017-01-10Completed
A Phase 1, Two-Cohort, Open-Label, Drug-Drug Interaction Study of Entinostat and Exemestane in Postmenopausal Women With Locally Recurrent or Metastatic ER+ Breast Cancer [NCT02820961]Phase 161 participants (Actual)Interventional2016-06-29Completed
A Phase 1 Study Evaluating Safety, Tolerability, and Preliminary Antitumor Activity of Entinostat and Nivolumab With or Without Ipilimumab in Advanced Solid Tumors [NCT02453620]Phase 157 participants (Actual)Interventional2016-02-12Active, not recruiting
A Phase 1 Study of Entinostat in Combination With Atezolizumab / Carboplatin / Etoposide in Previously Untreated Extensive-Stage Small Cell Lung Cancer [NCT04631029]Phase 13 participants (Actual)Interventional2021-04-27Completed
INFORM2 Exploratory Multinational Phase I/II Combination Study of Nivolumab and Entinostat in Children and Adolescents With Refractory High-risk Malignancies [NCT03838042]Phase 1/Phase 2128 participants (Anticipated)Interventional2020-05-26Recruiting
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00313586 (1) [back to overview]Proportion of Patients With Clinical Response
NCT00387465 (9) [back to overview](Phase I) Maximum Tolerated Dose (MTD) of Azacitidine When Given Together With Entinostat as Determined by Number of Participants Experiencing Dose-limiting Toxicity (DLT)
NCT00387465 (9) [back to overview]Effect of Entinostat and Azacitidine on DNA Methylation and Response
NCT00387465 (9) [back to overview]Overall Survival
NCT00387465 (9) [back to overview]Pharmacokinetic Profile of Azacitidine as Measured by AUC (ng*hr/mL)
NCT00387465 (9) [back to overview]Pharmacokinetic Profile of Azacitidine as Measured by Cmax
NCT00387465 (9) [back to overview]Pharmacokinetic Profile of Azacitidine as Measured by Half-life
NCT00387465 (9) [back to overview]Pharmacokinetic Profile of Azacytidine as Measured by Tmax
NCT00387465 (9) [back to overview]Progression-free Survival
NCT00387465 (9) [back to overview]Average Steady State Trough Concentration (ng/mL) of Entinostat
NCT00462605 (1) [back to overview]Clinical Activity Assessed by Change in Peripheral Blood Counts
NCT00602030 (16) [back to overview]6-Month PFS Rate in the Double-blind Phase
NCT00602030 (16) [back to overview]Number of Participants With Grade 3 or 4 Laboratory Variables in the Double-blind Phase
NCT00602030 (16) [back to overview]Number of Participants With Treatment-Emergent Adverse Events (TEAEs) and Serious Adverse Events (SAEs) by Severity in the Double-blind Phase
NCT00602030 (16) [back to overview]Tmax: Time to Cmax of Entinostat in the Lead-in Phase
NCT00602030 (16) [back to overview]Vital Sign Values: Diastolic Blood Pressure in the Double-blind Phase
NCT00602030 (16) [back to overview]Vital Sign Values: Heart Rate in the Double-blind Phase
NCT00602030 (16) [back to overview]Vital Sign Values: Respiration Rate in the Double-blind Phase
NCT00602030 (16) [back to overview]Vital Sign Values: Systolic Blood Pressure in the Double-blind Phase
NCT00602030 (16) [back to overview]Vital Sign Values: Temperature in the Double-blind Phase
NCT00602030 (16) [back to overview]Vital Sign Values: Weight in the Double-blind Phase
NCT00602030 (16) [back to overview]4-Month Progression-free Survival (PFS) Rate in the Double-blind Phase
NCT00602030 (16) [back to overview]Identification of Safe-dose for the Phase 2 Double-blind Phase in the Lead-in Phase
NCT00602030 (16) [back to overview]Objective Response Rate (ORR) in the Double-blind Phase
NCT00602030 (16) [back to overview]AUC(0-24): Area Under the Concentration-time Curve From Time 0 to 24 Hours in the Lead-in Phase
NCT00602030 (16) [back to overview]AUC(0-last): Area Under the Concentration-time Curve From Time 0 to Last Quantifiable Concentration in the Lead-in Phase
NCT00602030 (16) [back to overview]Cmax: Maximum Plasma Concentration of Entinostat in the Lead-in Phase
NCT00676663 (5) [back to overview]Clinical Benefit Rate (CBR)
NCT00676663 (5) [back to overview]Objective Response Rate (ORR)
NCT00676663 (5) [back to overview]Overall Survival (OS)
NCT00676663 (5) [back to overview]Progression-free Survival (PFS)
NCT00676663 (5) [back to overview]Number of Participants With Treatment-Emergent Adverse Events (TEAEs) and Serious Adverse Events (SAEs)
NCT00828854 (4) [back to overview]Objective Response Rate (ORR) During the First 6 Cycles of Study Treatment
NCT00828854 (4) [back to overview]Progression-Free Survival (PFS)
NCT00828854 (4) [back to overview]Number of Participants With Adverse Events (AEs)
NCT00828854 (4) [back to overview]Clinical Benefit Rate (CBR)
NCT00866333 (4) [back to overview]Percentage of Participants With Best Overall Response Based on the Participant's Best Response That is Documented Within the First 6 Cycles of Protocol Therapy
NCT00866333 (4) [back to overview]Duration of Objective Response for Participants Achieving CR or PR
NCT00866333 (4) [back to overview]Percentage of Participants With Best Overall Response Based on the Participant's Best Response Documented Through the Entire Course of Protocol Therapy
NCT00866333 (4) [back to overview]Number of Participants With Serious Adverse Events (SAE) and Adverse Events (AEs)
NCT01038778 (8) [back to overview]Incidence of Toxicities
NCT01038778 (8) [back to overview]Incidence of Toxicity (Phase I)
NCT01038778 (8) [back to overview]Overall Response Rate (Complete Plus Partial) (Phase II)
NCT01038778 (8) [back to overview]Overall Survival
NCT01038778 (8) [back to overview]Progression-free Survival
NCT01038778 (8) [back to overview]Time-to-tumor Progression
NCT01038778 (8) [back to overview]Dose-limiting Toxicities of Entinostat When Combined With Aldesleukin Within the Phase I
NCT01038778 (8) [back to overview]Changes in the Level of Specific T Lymphocytes
NCT01105377 (2) [back to overview]Confirmed Tumor Response
NCT01105377 (2) [back to overview]Time to Progression
NCT01234532 (5) [back to overview]Change in HER2
NCT01234532 (5) [back to overview]Change in Proliferative Index (Ki67) (Phase II)
NCT01234532 (5) [back to overview]Number of Participants With Adverse Events
NCT01234532 (5) [back to overview]Recommended Phase II Dose of Entinostat in Combination With Anastrozole (Pilot)
NCT01234532 (5) [back to overview]Change in Estrogen-receptor (ER) Expression (Phase II)
NCT01349959 (8) [back to overview]Clinical Benefit Rate
NCT01349959 (8) [back to overview]Confirmed Response Rate (Percentage of Participants With Complete or Partial Response Noted as the Objective Status on Two Consecutive Evaluations at Least 4 Weeks Apart) Assessed by RECIST
NCT01349959 (8) [back to overview]Confirmed Response Rate to Azacitidine and Entinostat Plus the Addition of Hormone Therapy
NCT01349959 (8) [back to overview]Feasibility of the Addition of Hormone Therapy, Evaluated by Calculating the Number of Patients With Disease Progression That go on to Receive Hormonal Therapy
NCT01349959 (8) [back to overview]Number of Participants With Change in Expression of Relevant Genes (e.g., ER Alpha and RAR Beta) Evaluated by Reverse Transcriptase Polymerase Chain Reaction (RT-PCR)
NCT01349959 (8) [back to overview]Number of Participants With Change in Gene Methylation Evaluated Using Quantitative Multiple Methylation-specific Polymerase Chain Reaction (QM-MSP)
NCT01349959 (8) [back to overview]Overall Survival
NCT01349959 (8) [back to overview]Progression-free Survival (PFS)
NCT02115282 (9) [back to overview]Time-to-treatment Deterioration (TTD)
NCT02115282 (9) [back to overview]Patient-reported Fatigue
NCT02115282 (9) [back to overview]Lysine Acetylation Change in CD45 Blood Mononuclear Cells Between C1D1 and C1D15 and PFS in Patients on Arm A
NCT02115282 (9) [back to overview]Objective Response Rate (ORR)
NCT02115282 (9) [back to overview]Overall Survival (OS)
NCT02115282 (9) [back to overview]Patient-reported Diarrhea
NCT02115282 (9) [back to overview]Patient-reported Health-related Quality of Life
NCT02115282 (9) [back to overview]Patient-reported Nausea and Anorexia
NCT02115282 (9) [back to overview]Progression-free Survival (PFS)
NCT02708680 (7) [back to overview]Phase 1b: Participants Experiencing DLT
NCT02708680 (7) [back to overview]Phase 2 Expansion: Overall Survival (OS)
NCT02708680 (7) [back to overview]Phase 2 Expansion: Duration of Progression-free Survival (PFS) Using Response Evaluation Criteria in Solid Tumors Version 1.1 (RECIST 1.1)
NCT02708680 (7) [back to overview]Phase 2 Expansion: Duration of PFS Using Immune Response RECIST (irRECIST)
NCT02708680 (7) [back to overview]Phase 2 Expansion: Overall Response Rate (ORR) Using RECIST 1.1 and irRECIST
NCT02708680 (7) [back to overview]Phase 2 Expansion: Clinical Benefit Rate (CBR) Using RECIST 1.1 and irRECIST
NCT02708680 (7) [back to overview]Phase 1b: Determination of the RP2D
NCT02780804 (7) [back to overview]Total Area Under the Plasma Concentration Curve of Entinostat: AUC
NCT02780804 (7) [back to overview]Antitumor Activity of Entinostat
NCT02780804 (7) [back to overview]Frequency of Adverse Events for Entinostat
NCT02780804 (7) [back to overview]Half-life of Entinostat
NCT02780804 (7) [back to overview]Maximum Tolerated Dose (MTD) or Recommended Phase 2 Dose (R2PD) of Entinostat
NCT02780804 (7) [back to overview]Peak Plasma Concentration of Entinostat: C-Max
NCT02780804 (7) [back to overview]Time to Reach Maximum Plasma Concentration of Entinostat: T-Max
NCT03018249 (4) [back to overview]Percent of Participants With a Ki67 Response
NCT03018249 (4) [back to overview]The Frequency and Severity of CTCAE Version 4.0 Graded Adverse Events (AE)
NCT03018249 (4) [back to overview]Percentage of Participants With a Histologic Response
NCT03018249 (4) [back to overview]Mean Post-treatment Tumor Progesterone Receptor H-score (Histology Score)
NCT03215264 (1) [back to overview]Maximum Tolerated Dose (MTD) of Hydroxychloroquine and Entinostat in Combination With Regorafenib
NCT03250273 (11) [back to overview]Overall Survival (OS) at 24 Months
NCT03250273 (11) [back to overview]Overall Survival (OS) at 36 Months
NCT03250273 (11) [back to overview]Overall Survival (OS) at 6 Months
NCT03250273 (11) [back to overview]Progression Free Survival (PFS) at 12 Months
NCT03250273 (11) [back to overview]Progression Free Survival (PFS) at 24 Months
NCT03250273 (11) [back to overview]Progression Free Survival (PFS) at 6 Months
NCT03250273 (11) [back to overview]Overall Survival (OS)
NCT03250273 (11) [back to overview]Overall Survival (OS) at 12 Months
NCT03250273 (11) [back to overview]Objective Response Rate (ORR) Using Response Evaluation Criteria for Solid Tumors (RECIST 1.1)
NCT03250273 (11) [back to overview]Number of Patients Experiencing a Grade 3 or Above Treatment-related Adverse Event (AE)
NCT03250273 (11) [back to overview]Duration of Response (DOR)
NCT04296942 (4) [back to overview]Number of Participants With Serious and Non-serious Adverse Events Assessed by the Common Terminology Criteria for Adverse Events (CTCAE v5.0)
NCT04296942 (4) [back to overview]Progression-free Survival (PFS) in Triple Negative Breast Cancer (TNBC)
NCT04296942 (4) [back to overview]Overall Response (Partial Response + Complete Response) for Participants With Triple Negative Breast Cancer (TNBC)
NCT04296942 (4) [back to overview]Number of Participants Experiencing at Least One Grade 3 to 5 Adverse Events for Each of the Three Combinations of Agents
NCT04631029 (4) [back to overview]Number of Participants Experiencing Grade 3 and 4 Adverse Events
NCT04631029 (4) [back to overview]Number of Participants Who Received 3 or More Cycles of the Combination of Entinostat, Atezolizumab, Carboplatin, and Etoposide
NCT04631029 (4) [back to overview]Number of Participants With Dose Limiting Toxicities
NCT04631029 (4) [back to overview]Progression Free Survival (PFS) Rate

Proportion of Patients With Clinical Response

"Clinical response is defined as a complete response (CR), partial response (PR) or trilineage response (TR) graded according to the following criteria:~World Health Organization classification of the acute leukemias and myelodysplastic syndrome (by Bennett)~Myelodysplastic syndromes standardized response criteria: further definition (by Cheson et al.)~Report of an international working group to standardize response criteria for myelodysplastic syndromes (by Cheson et al.)" (NCT00313586)
Timeframe: Assessed every 3 months if patient is < 2 years from study entry, every 6 months if patient is 2 - 5 years from study entry.

InterventionProportion of patients (Number)
Arm A (Azacitidine; Non-treatment-induced Cohort)0.32
Arm B (Azacitidine + Entinostat; Non-treatment-induced Cohort)0.27
Arm A (Azacitidine; Treatment-induced Cohort)0.46
Arm B (Azacitidine + Entinostat; Treatment-induced Cohort)0.17

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(Phase I) Maximum Tolerated Dose (MTD) of Azacitidine When Given Together With Entinostat as Determined by Number of Participants Experiencing Dose-limiting Toxicity (DLT)

DLT is defined by the National Cancer Institute Common Terminology Criteria for Adverse Events (NCI CTCAE) v3.0 (NCT00387465)
Timeframe: Up to 28 days

InterventionParticipants (Count of Participants)
Phase I - 30mg/m2 Azacitidine0
Phase I - 40mg/m2 Azacitidine0

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Effect of Entinostat and Azacitidine on DNA Methylation and Response

"Number of participants with decrease in DNA methylation (methylation-signature positive) on Day 10 or Day 29, and either stable disease or objective response (OR) as defined by RECIST 1.0. Per RECIST 1.0, progression is defined as a 20% increase in the sum of the longest diameter of target lesions, or a measurable increase in a non-target lesion, or the appearance of new lesions; PR is defined as >=30% decrease in the sum of the longest diameter of target lesions, complete response is defined as disappearance of all target lesions; OR=CR+PR." (NCT00387465)
Timeframe: Baseline and days 10 and 29

InterventionParticipants (Count of Participants)
Azacitidine 40mg/m2 With Entinostat8

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Overall Survival

Determined by the method determined by Kaplan and Meier. 95% confidence intervals will be estimated. (NCT00387465)
Timeframe: Up to 1 year

Interventionmonths (Median)
Azacitidine 40mg/m2 With Entinostat6.4

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Pharmacokinetic Profile of Azacitidine as Measured by AUC (ng*hr/mL)

(NCT00387465)
Timeframe: Day 1

Interventionng*hr/mL (Mean)
Azacitidine 40mg/m2 With Entinostat675

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Pharmacokinetic Profile of Azacitidine as Measured by Cmax

Maximal concentration (ng/mL) of azacitidine (NCT00387465)
Timeframe: Day 1

Interventionng/mL (Mean)
Azacitidine 40mg/m2 With Entinostat468

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Pharmacokinetic Profile of Azacitidine as Measured by Half-life

(NCT00387465)
Timeframe: Day 1

Interventionhours (Mean)
Azacitidine 40mg/m2 With Entinostat1.12

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Pharmacokinetic Profile of Azacytidine as Measured by Tmax

Time to maximal concentration of azacitidine in the blood. (NCT00387465)
Timeframe: Day 1

Interventionhours (Median)
Azacitidine 40mg/m2 With Entinostat0.5

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Progression-free Survival

Progression is defined using Response Evaluation Criteria In Solid Tumors Criteria (RECIST v1.0), as a 20% increase in the sum of the longest diameter of target lesions, or a measurable increase in a non-target lesion, or the appearance of new lesions. Determined by the method determined by Kaplan and Meier. 95% confidence intervals will be estimated. (NCT00387465)
Timeframe: Up to 1 year

Interventionweeks (Median)
Azacitidine 40mg/m2 With Entinostat7.4

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Average Steady State Trough Concentration (ng/mL) of Entinostat

(NCT00387465)
Timeframe: Day 10 and 17

Interventionng/mL (Mean)
Day 10Day 17
Azacitidine 40mg/m2 With Entinostat0.841.10

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Clinical Activity Assessed by Change in Peripheral Blood Counts

(NCT00462605)
Timeframe: Baseline and after 2 cycles

Interventioncell/mm^3 (Mean)
ANC +/- SEM at baselineANC +/- SEM after 2 cycles
Arm I5781137

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6-Month PFS Rate in the Double-blind Phase

PFS rate at 6 months is defined as the percentage of participants who are progression-free at 6 months. (NCT00602030)
Timeframe: Month 6

Interventionpercentage of participants (Number)
Double-blind Phase: Erlotinib + Placebo10.8
Double-blind Phase: Erlotinib + Entinostat 10 mg11.9

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Number of Participants With Grade 3 or 4 Laboratory Variables in the Double-blind Phase

Laboratory tests included tests of Hematology and Chemistry. The individual laboratory values were graded by the investigator using the Common Terminology Criteria for Adverse Events (CTCAE) version 3.0 scale where Grade 1=Mild, Grade 2=Moderate, Grade 3=Severe, medically significant, Grade 4=Life-threatening and 5=Death. (NCT00602030)
Timeframe: Day 1 and 15 of each cycle to safety follow-up 30 days past last dose (up to 7 months)

,
InterventionParticipants (Count of Participants)
White Blood Count decreasedAbsolute Neutrophil Count decreasedLymphocytes decreasedPlatelets decreasedPhosphorus decreasedAlanine aminotransferase increasedSodium decreasedGlucose increasedAlbumin decreasedPotassium decreasedAspartate aminotransferase increasedBilirubin increasedCreatinine abnormalMagnesium decreasedPotassium increasedCalcium increasedCalcium decreased
Double-blind Phase: Erlotinib + Entinostat 10 mg121826643222011100
Double-blind Phase: Erlotinib + Placebo11914152420310021

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Number of Participants With Treatment-Emergent Adverse Events (TEAEs) and Serious Adverse Events (SAEs) by Severity in the Double-blind Phase

"An AE is defined as any untoward medical occurrence in a patient or clinical investigation patient administered a pharmaceutical product and that does not necessarily have a causal relationship with this treatment. Worsening of a pre-existing medical condition was considered an AE if there was either an increase in severity, frequency, or duration of the condition or an association with significantly worse outcomes. A TEAE is an AE that starts after the administration of study drug.~A SAE is any AE that is fatal, life threatening, requires in-patient hospitalization or prolongation of existing hospitalization, results in persistent or significant disability/incapacity, is a congenital anomaly/birth effect or other significant medical hazard.~TEAE severity was graded according to the Common Terminology Criteria for Adverse Events (CTCAE) version 3.0 scale where Grade 1=Mild, Grade 2=Moderate, Grade 3=Severe, medically significant, Grade 4=Life-threatening and 5=Death." (NCT00602030)
Timeframe: First dose of study drug to within 30 days past last dose (Up to 7 months)

,
InterventionParticipants (Count of Participants)
Any SAEAny TEAEGrade 1 TEAEGrade 2 TEAEGrade 3 TEAEGrade 4 TEAEGrade 5 TEAE
Double-blind Phase: Erlotinib + Entinostat 10 mg326511234612
Double-blind Phase: Erlotinib + Placebo296371620515

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Tmax: Time to Cmax of Entinostat in the Lead-in Phase

(NCT00602030)
Timeframe: Day 1 predose and 0.5, 1, 2, 4 and 6 hours after dose; Days 2 and 8 predose (entinostat alone); Day 15 predose and 0.5, 1, 2, 4, 6 and 24 hours after dose

,
Interventionhour (Mean)
Day 1 (entinostat alone)Day 15 (entinostat + erlotinib)
Lead-in Phase: Erlotinib + Entinostat 10 mg0.501.3
Lead-in Phase: Erlotinib + Entinostat 5 mg0.831.0

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Vital Sign Values: Diastolic Blood Pressure in the Double-blind Phase

(NCT00602030)
Timeframe: Day 1 and 15 of each cycle to safety follow-up 30 days past last dose (up to 7 months)

,
Interventionmm Hg (Mean)
BaselineMinimum Post-Baseline ValueMaximum Post-Baseline Value
Double-blind Phase: Erlotinib + Entinostat 10 mg72.161.378.5
Double-blind Phase: Erlotinib + Placebo72.564.778.8

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Vital Sign Values: Heart Rate in the Double-blind Phase

(NCT00602030)
Timeframe: Day 1 and 15 of each cycle to safety follow-up 30 days past last dose (up to 7 months)

,
Interventionbeats per minute (bpm) (Mean)
BaselineMinimum Post-Baseline ValueMaximum Post-Baseline Value
Double-blind Phase: Erlotinib + Entinostat 10 mg85.679.7102.1
Double-blind Phase: Erlotinib + Placebo87.578.598.2

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Vital Sign Values: Respiration Rate in the Double-blind Phase

(NCT00602030)
Timeframe: Day 1 and 15 of each cycle to safety follow-up 30 days past last dose (up to 7 months)

,
Interventionbreaths per minute (Mean)
BaselineMinimum Post-Baseline ValueMaximum Post-Baseline Value
Double-blind Phase: Erlotinib + Entinostat 10 mg17.916.620.1
Double-blind Phase: Erlotinib + Placebo18.517.220.2

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Vital Sign Values: Systolic Blood Pressure in the Double-blind Phase

(NCT00602030)
Timeframe: Day 1 and 15 of each cycle to safety follow-up 30 days past last dose (up to 7 months)

,
Interventionmm Hg (Mean)
BaselineMinimum Post-Baseline ValueMaximum Post-Baseline Value
Double-blind Phase: Erlotinib + Entinostat 10 mg126.0105.0132.5
Double-blind Phase: Erlotinib + Placebo125.3112.4135.5

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Vital Sign Values: Temperature in the Double-blind Phase

(NCT00602030)
Timeframe: Day 1 and 15 of each cycle to safety follow-up 30 days past last dose (up to 7 months)

,
Interventiondegrees Celsius (C) (Mean)
BaselineMinimum Post-Baseline ValueMaximum Post-Baseline Value
Double-blind Phase: Erlotinib + Entinostat 10 mg97.697.098.5
Double-blind Phase: Erlotinib + Placebo97.596.998.2

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Vital Sign Values: Weight in the Double-blind Phase

(NCT00602030)
Timeframe: Day 1 and 15 of each cycle to safety follow-up 30 days past last dose (up to 7 months)

,
Interventionkilograms (kg) (Mean)
BaselineMinimum Post-Baseline ValueMaximum Post-Baseline Value
Double-blind Phase: Erlotinib + Entinostat 10 mg74.370.074.3
Double-blind Phase: Erlotinib + Placebo77.973.577.6

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4-Month Progression-free Survival (PFS) Rate in the Double-blind Phase

PFS rate at 4 months was defined as the percentage of participants who are progression-free at 4 months. (NCT00602030)
Timeframe: Month 4

Interventionpercentage of participants (Number)
Double-blind Phase: Erlotinib + Placebo24.0
Double-blind Phase: Erlotinib + Entinostat 10 mg20.8

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Identification of Safe-dose for the Phase 2 Double-blind Phase in the Lead-in Phase

Safe recommended Phase 2 dose was determined based on dose-limiting toxicities (DLT) in Cycle 1. A DLT was defined as any of the following occurring in Cycle 1: Grade 3 or greater nonhematologic toxicity that was considered related to either entinostat or erlotinib or a Grade 4 hematologic toxicity lasting more than 7 days and/or resulting in a dose delay. Common Terminology Criteria for Adverse Events (CTCAE) version 3.0 scale was used where Grade 1=mild, Grade 2=Moderate, Grade 3=Severe, medically significant, Grade 4=life-threatening and 5=death. The dose that was found to be safe is reported. (NCT00602030)
Timeframe: Cycle 1 of Lead-in Phase

Interventionmilligrams (mg) (Number)
Lead-in Phase: Erlotinib + Entinostat10

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Objective Response Rate (ORR) in the Double-blind Phase

ORR was defined as the percentage of participants who had confirmed complete response (CR) or partial response (PR) according to Response Evaluation Criteria in Solid Tumors (RECIST) as assessed by the investigator. CR=disappearance of all target lesions; disappearance of non-target lesions and normalization of tumor marker level. PR=At least a 30% decrease in the sum of the longest diameter of target lesions, taking at reference the baseline sum longest diameter. (NCT00602030)
Timeframe: Month 6

Interventionpercentage of participants (Number)
Double-blind Phase: Erlotinib + Placebo9.2
Double-blind Phase: Erlotinib + Entinostat 10 mg3.0

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AUC(0-24): Area Under the Concentration-time Curve From Time 0 to 24 Hours in the Lead-in Phase

(NCT00602030)
Timeframe: Day 1 predose and 0.5, 1, 2, 4 and 6 hours after dose; Days 2 and 8 predose (entinostat alone); Day 15 predose and 0.5, 1, 2, 4, 6 and 24 hours after dose

,
Interventionng*hr/mL (Mean)
Day 1 (entinostat alone)Day 15 (entinostat + erlotinib)
Lead-in Phase: Erlotinib + Entinostat 10 mg133.3110.2
Lead-in Phase: Erlotinib + Entinostat 5 mg46.551.7

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AUC(0-last): Area Under the Concentration-time Curve From Time 0 to Last Quantifiable Concentration in the Lead-in Phase

(NCT00602030)
Timeframe: Day 1 predose and 0.5, 1, 2, 4 and 6 hours after dose; Days 2 and 8 predose (entinostat alone); Day 15 predose and 0.5, 1, 2, 4, 6 and 24 hours after dose

,
Interventionng*hr/mL (Mean)
Day 1 (entinostat alone)Day 15 (entinostat + erlotinib)
Lead-in Phase: Erlotinib + Entinostat 10 mg325.8106.4
Lead-in Phase: Erlotinib + Entinostat 5 mg152.151.7

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Cmax: Maximum Plasma Concentration of Entinostat in the Lead-in Phase

(NCT00602030)
Timeframe: Day 1 predose and 0.5, 1, 2, 4 and 6 hours after dose; Days 2 and 8 predose (entinostat alone); Day 15 predose and 0.5, 1, 2, 4, 6 and 24 hours after dose

,
Interventionng/mL (Mean)
Day 1 (entinostat alone)Day 15 (entinostat + erlotinib)
Lead-in Phase: Erlotinib + Entinostat 10 mg123.199.4
Lead-in Phase: Erlotinib + Entinostat 5 mg19.630.2

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Clinical Benefit Rate (CBR)

CBR is defined as the percentage of participants with overall response (CR + PR) plus stable disease (SD) for 6 months as assessed by the investigator based on RECIST, version 1.0. CR is defined as the disappearance of all target lesions. PR is defined as at least a 30% decrease in the sum of the longest diameter (LD) of target lesions, taking as reference the baseline sum LD. SD is defined as neither sufficient shrinkage to qualify for PR nor sufficient increase to qualify for PD, taking as reference the smallest sum LD since the treatment started. (NCT00676663)
Timeframe: From date of randomization to discontinuation due to disease progression or intolerable AE up to primary completion date (Median follow-up 6 months)

Interventionpercentage of participants (Number)
Exemestane 25 mg + Placebo25.8
Exemestane 25 mg + Entinostat 5 mg26.6

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Objective Response Rate (ORR)

ORR is defined as the percentage of participants with response during treatment classified as complete response (CR) or partial response (PR), as assessed by the investigator based on Response Evaluation Criteria in Solid Tumors (RECIST), version 1.0. CR is defined as the disappearance of all target lesions. PR is defined as at least a 30% decrease in the sum of the longest diameter (LD) of target lesions, taking as reference the baseline sum LD. (NCT00676663)
Timeframe: From date of randomization to discontinuation due to disease progression or intolerable Adverse Event (AE) up to primary completion date (Median follow-up 6 months)

Interventionpercentage of participants (Number)
Exemestane 25 mg + Placebo4.6
Exemestane 25 mg + Entinostat 5 mg4.7

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Overall Survival (OS)

OS was defined as the number of months elapsed between the date of randomization and the date of death (whatever the cause). (NCT00676663)
Timeframe: First dose of study drug to end of study (Median follow-up 24 months in the EE arm and 26.4 months in the EP arm)

Interventionmonths (Median)
Exemestane 25 mg + Placebo (EP)19.84
Exemestane 25 mg + Entinostat 5 mg (EE)28.13

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Progression-free Survival (PFS)

PFS is defined as the number of months from the date of randomization to the earlier of progressive disease (PD) or death due to any cause. (NCT00676663)
Timeframe: From date of randomization to discontinuation due to disease progression or death up to primary completion date (Median follow-up 6 months)

Interventionmonths (Median)
Exemestane 25 mg + Placebo2.27
Exemestane 25 mg + Entinostat 5 mg4.28

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Number of Participants With Treatment-Emergent Adverse Events (TEAEs) and Serious Adverse Events (SAEs)

"An AE is defined as any untoward medical occurrence in a patient or clinical investigation patient administered a pharmaceutical product and that does not necessarily have a causal relationship with this treatment. Worsening of a pre-existing medical condition was considered an AE if there was either an increase in severity, frequency, or duration of the condition or an association with significantly worse outcomes. Abnormal clinical laboratory findings determined by the investigator to be clinically significant were recorded as AEs. A TEAE is an AE that starts after the administration of study drug.~A SAE is any AE that is fatal, life threatening, requires in-patient hospitalization or prolongation of existing hospitalization, results in persistent or significant disability/incapacity, is a congenital anomaly/birth effect or other significant medical hazard." (NCT00676663)
Timeframe: First dose to within 30 days of last dose of study drug (Up to Approximately 2 Years)

,
InterventionParticipants (Count of Participants)
TEAESAE
Exemestane 25 mg + Entinostat 5 mg6010
Exemestane 25 mg + Placebo568

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Objective Response Rate (ORR) During the First 6 Cycles of Study Treatment

ORR is defined as the percentage of participants with response during treatment classified as CR or PR, as assessed by the investigator based on RECIST, version 1.0. CR is defined as the disappearance of all target lesions. PR is defined as at least a 30% decrease in the sum of the LD of target lesions, taking as reference the baseline sum LD. (NCT00828854)
Timeframe: Up to 6, 28-day cycles

Interventionpercentage of participants (Number)
Entinostat 5 mg + AI3.9

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Progression-Free Survival (PFS)

PFS is defined as the number of months from the date of randomization to the earlier of progressive disease (PD) or death due to any cause. (NCT00828854)
Timeframe: Up to 6, 28-day cycles

Interventionmonths (Median)
Entinostat 5 mg + AI3.9

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Number of Participants With Adverse Events (AEs)

An AE is defined as any untoward medical occurrence in a patient or clinical investigation patient administered a pharmaceutical product and that does not necessarily have a causal relationship with this treatment. Worsening of a pre-existing medical condition was considered an AE if there was either an increase in severity, frequency, or duration of the condition or an association with significantly worse outcomes. Abnormal clinical laboratory findings determined by the investigator to be clinically significant were recorded as AEs. (NCT00828854)
Timeframe: Up to 6, 28-day cycles + 30 days

InterventionParticipants (Count of Participants)
Entinostat 5 mg + AI27

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Clinical Benefit Rate (CBR)

CBR is defined as the percentage of participants who achieved complete response (CR) or partial response (PR) or stable disease (SD) for 6 months as assessed by the investigator based on Response Evaluation Criteria in Solid Tumors (RECIST), version 1.0. CR is defined as the disappearance of all target lesions. PR is defined as at least a 30% decrease in the sum of the longest diameter (LD) of target lesions, taking as reference the baseline sum LD. SD is defined as neither sufficient shrinkage to qualify for PR nor sufficient increase to qualify for progressive disease (PD), taking as reference the smallest sum LD since the treatment started. (NCT00828854)
Timeframe: 6 months

Interventionpercentage of participants (Number)
Entinostat 5 mg + AI15.4

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Percentage of Participants With Best Overall Response Based on the Participant's Best Response That is Documented Within the First 6 Cycles of Protocol Therapy

Best Overall Response was defined as Complete Response (CR) or Partial Response (PR). Tumor response was assessed by the Investigators using the International Working Group revised response criteria for malignant lymphoma (Cheson, Pfistner et al. 2007). CR was defined as complete disappearance of all detectable clinical and radiographic evidence of disease and disappearance of all disease-related symptoms if present before therapy, and normalization of those biochemical abnormalities definitely assignable to HL. PR was defined as: At least a 50% decrease in sum of the products of the greatest diameters (SPD) of the six largest dominant nodes or nodal masses, No increase in the size of other nodes, No new sites of disease. (NCT00866333)
Timeframe: Up to 6 months

Interventionpercentage of participants (Number)
Regimen 1: Entinostat 10 mg8.3
Regimen 2: Entinostat 10 mg/15 mg11.8
Regimen 3: Entinostat 15 mg16.7

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Duration of Objective Response for Participants Achieving CR or PR

Duration of objective response was defined as the number of days from the start date of CR or PR (whichever status is recorded first), until the first date that recurrent or progressive disease was objectively documented. (NCT00866333)
Timeframe: Regimen 1 and 2 median follow-up 36.6 months; Regimen 3 median follow-up 18.4 months

Interventionmonths (Median)
Regimen 1: Entinostat 10 mgNA
Regimen 2: Entinostat 10 mg/15 mg28.6
Regimen 3: Entinostat 15 mg8.3

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Percentage of Participants With Best Overall Response Based on the Participant's Best Response Documented Through the Entire Course of Protocol Therapy

Best Overall Response was defined as Complete Response (CR) or Partial Response (PR). Tumor response was assessed by the Investigators using the International Working Group revised response criteria for malignant lymphoma (Cheson, Pfistner et al. 2007). CR was defined as complete disappearance of all detectable clinical and radiographic evidence of disease and disappearance of all disease-related symptoms if present before therapy, and normalization of those biochemical abnormalities definitely assignable to HL. PR was defined as: At least a 50% decrease in sum of the products of the greatest diameters (SPD) of the six largest dominant nodes or nodal masses, No increase in the size of other nodes, No new sites of disease. (NCT00866333)
Timeframe: Regimen 1 and 2 median follow-up 36.6 months; Regimen 3 median follow-up 18.4 months

Interventionpercentage of participants (Number)
Regimen 1: Entinostat 10 mg8.3
Regimen 2: Entinostat 10 mg/15 mg17.6
Regimen 3: Entinostat 15 mg16.7

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Number of Participants With Serious Adverse Events (SAE) and Adverse Events (AEs)

An AE is any untoward medical occurrence in a patient or clinical investigation participant administered a pharmaceutical product and which does not necessarily have a causal relationship with this treatment. A Treatment-Emergent Adverse Event (TEAE) is an AE that occurred after receive study drug. Any changes from baseline in vital signs, electrocardiogram results, and laboratory parameters assessed by the investigator to be clinically significant were reported as AEs. A SAE is defined as an AE that: is fatal, is life threatening, requires in-patient hospitalization or prolongation of existing hospitalization, results in persistent or significant disability/incapacity is a congenital anomaly/birth defect, is another significant medical hazard, such as new malignancy. (NCT00866333)
Timeframe: First dose to within 30 days of the last dose of study drug (Up to 34 months)

,,
InterventionParticipants (Count of Participants)
Any TEAESAE
Regimen 1: Entinostat 10 mg162
Regimen 2: Entinostat 10 mg/15 mg177
Regimen 3: Entinostat 15 mg163

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Incidence of Toxicities

The number of participants with serious adverse events. (NCT01038778)
Timeframe: Up to 30 days

InterventionParticipants (Count of Participants)
Treatment (Entinostat, Aldesleukin)9

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Incidence of Toxicity (Phase I)

Count of participants with grade 4 toxicity. The frequency and grade of toxicities will be tabulated for each dose level. (NCT01038778)
Timeframe: 84 days

InterventionParticipants (Count of Participants)
Dose Level 11
Dose Level 20

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Overall Response Rate (Complete Plus Partial) (Phase II)

"The proportion of patients who have a partial or complete response to treatment evaluated by RECIST V.1.0 criteria.~MEASUREMENT OF EFFECT Patients underwent CT scans at week 11 (+/- 7 days) of each cycle during aldesleukin administration and then every 8-12 weeks (+/- 2 weeks). Response Evaluation Criteria in Solid Tumors (RECIST V.1.0)" (NCT01038778)
Timeframe: Up to 12 months

InterventionProportion of participants (Number)
Treatment (Entinostat, Aldesleukin).39

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Overall Survival

The 3-year overall survival (OS) rate was estimated using standard Kaplan-Meier methods, where estimates of the median were obtained with 95% confidence intervals (CIs). OS was defined as the time from the start of treatment to death due to any cause or last follow-up, patients who did not die were censored. (NCT01038778)
Timeframe: up to 12-months after the last subject enrolls

Interventionpercentage of participants (Number)
Treatment (Entinostat, Aldesleukin)82.1

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Progression-free Survival

"The median progression-free survival (PFS) was estimated using standard Kaplan-Meier methods, where estimates of the median were obtained with 95% confidence intervals (CIs). PFS was defined as the time from the start of treatment to progression or death due to any cause or last follow-up, patients who did not progress or die were censored.~MEASUREMENT OF EFFECT Patients underwent CT scans at week 11 (+/- 7 days) of each cycle during aldesleukin administration and then every 8-12 weeks (+/- 2 weeks). Response Evaluation Criteria in Solid Tumors (RECIST V.1.0)" (NCT01038778)
Timeframe: up to 12-months after the last subject enrolls

Interventionmonths (Median)
Treatment (Entinostat, Aldesleukin)14.0

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Time-to-tumor Progression

The median time to tumor progression (TTP) was estimated using standard Kaplan-Meier methods, where estimates of the median were obtained with 95% confidence intervals (CIs). TTP was defined as the time from the start of treatment to progression or last follow-up. Patients that did not progress were censored. (NCT01038778)
Timeframe: up to 12-months after the last subject enrolls

Interventionmonths (Median)
Treatment (Entinostat, Aldesleukin)14

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Dose-limiting Toxicities of Entinostat When Combined With Aldesleukin Within the Phase I

Number of dose-limiting toxicities of entinostat when combined with aldesleukin within the Phase I MEASUREMENT OF EFFECT Patients underwent CT scans at week 11 (+/- 7 days) of each cycle during aldesleukin administration and then every 8-12 weeks (+/- 2 weeks). Response Evaluation Criteria in Solid Tumors (RECIST V.1.0) (NCT01038778)
Timeframe: 84 days

InterventionParticipants (Count of Participants)
Dose Level 10
Dose Level 20

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Changes in the Level of Specific T Lymphocytes

Mean percent change from baseline of T lymphocytes. (NCT01038778)
Timeframe: Baseline to approximately 4 weeks post-treatment, up to 1 year

Interventionpercentage of cells count (Mean)
Dose Level 126.3
Dose Level 210.5

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Confirmed Tumor Response

Each evaluable patient is classified as having a confirmed tumor response if they have either a complete response (CR) or partial response (PR) lasts at least 4 weeks. Tumor response is measured by using RECIST v1.1 (Response Evaluation Criteria in Solid Tumors). A CR is defined as a disappearance of all target lesions, and each target lymph node must have reduction in short axis to <1.0 cm. A PR is defined as a 30% decrease in the sum of the longest diameter for all target lesions plus the sum of the short axis of all the target lymph nodes at current evaluation, compared to pre-treatment measurements. The confirmed response rate is calculated as the number of confirmed CR+PR, divided by the total number of evaluable patients, with 95% confidence intervals estimated using the approach of Duffy and Santner. (NCT01105377)
Timeframe: At 6 month evaluation

Interventionpercentage of participants (Number)
Cohort II0

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Time to Progression

Time to disease progression (TTP) is defined as the time from the start of treatment to the earliest of the date documenting disease progression or most recent assessment for patients having no progression. The distribution of TTP is estimated using the method of Kaplan-Meier. (NCT01105377)
Timeframe: From the start of treatment to the earliest of the date documenting disease progression, assessed up to 3 years

Interventionmonths (Median)
Cohort I1.8
Cohort II1.9

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Change in HER2

Will be treated as continuous variables. Multivariate analysis of variance may also be used to compare correlated biomarkers' expression. Correlation between biomarkers will be estimated and tested. The repeated measures model approach will be also used. Categorical outcome data (e.g., number of proteins expressed) will be recorded, proportions will be estimated and compared using the Fisher's exact test. (NCT01234532)
Timeframe: Baseline before study treatment and at the time of surgery, up to 30 days

Interventionscore on a scale (Number)
Entinostat & Anastrozole NeoadjuvantNA

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Change in Proliferative Index (Ki67) (Phase II)

The 95% confidence intervals will be constructed for the observed proportions. Exploratory data analysis and appropriate graphs will be used to decide whether data transformation (e.g. log or square-root) is necessary to assure an approximate normality. All descriptive statistics will be reported for ER and Ki67 expression. The general linear model approach and/or its non parametric alternative, the Wilcoxon test, will be used to assess whether there is any evidence of changes due to treatment. (NCT01234532)
Timeframe: Baseline to the time of surgery, within 6 days after the last dose of entinostat, up to 35 days

Interventionpercentage of Ki 67 expression (Number)
Entinostat & Anastrozole NeoadjuvantNA

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Number of Participants With Adverse Events

To address the safety of the regimen, a maximum width 90% confidence interval for any grade 3 or higher toxicity will be approximately 30%. For 5 patients in this study, if the true unknown probability of a rare toxicity is 10%, the probability of observing 1 or more toxicities is 97%, and if the true toxicity rate is 5% then the probability of observing one or more rare toxicities is 83%. (NCT01234532)
Timeframe: Participants were followed during the study and for 30 days post treatment, up to 59 days

InterventionParticipants (Count of Participants)
Entinostat & Anastrozole Neoadjuvant5

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Change in Estrogen-receptor (ER) Expression (Phase II)

The 95% confidence intervals will be constructed for the observed proportions. Exploratory data analysis and appropriate graphs will be used to decide whether data transformation (e.g. log or square-root) is necessary to assure an approximate normality. All descriptive statistics will be reported for ER and Ki67 expression. The general linear model approach and/or its non parametric alternative, the Wilcoxon test, will be used to assess whether there is any evidence of changes due to treatment. (NCT01234532)
Timeframe: Baseline before the study treatment and at the time of surgery, up to 30 days

Interventionpercentage of (ER) expression (Number)
Entinostat & Anastrozole NeoadjuvantNA

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Clinical Benefit Rate

Clinical benefit rate estimated by the number of patients who achieve a confirmed response plus the number of patients who have stable disease for a duration of at least 6 months divided by the total number of evaluable patients. All evaluable patients will be used for this analysis. (NCT01349959)
Timeframe: Up to 3 years

InterventionParticipants (Count of Participants)
TNBCHRBC
Treatment (Entinostat and Azacitidine)01

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Confirmed Response Rate (Percentage of Participants With Complete or Partial Response Noted as the Objective Status on Two Consecutive Evaluations at Least 4 Weeks Apart) Assessed by RECIST

Percentage of participants with complete or partial response will be estimated independently for each cohort by the number of successes divided by the total number of evaluable patients. Confidence intervals for the true success proportion will be calculated according to the approach of Duffy and Santner. (NCT01349959)
Timeframe: Up to 3 years

Interventionpercentage of participants (Number)
Triple-negative Breast Cancer (TNBC)Hormone-resistant Breast Cancer (HRBC)
Treatment (Entinostat and Azacitidine)04

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Confirmed Response Rate to Azacitidine and Entinostat Plus the Addition of Hormone Therapy

Will be estimated in each cohort. All evaluable patients who receive hormonal therapy will be used for this analysis. (NCT01349959)
Timeframe: Up to 3 years

InterventionParticipants (Count of Participants)
TNBCHRBC
Treatment (Entinostat and Azacitidine)01

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Feasibility of the Addition of Hormone Therapy, Evaluated by Calculating the Number of Patients With Disease Progression That go on to Receive Hormonal Therapy

(NCT01349959)
Timeframe: Up to 3 years

InterventionParticipants (Count of Participants)
TNBCHRBC
Treatment (Entinostat and Azacitidine)412

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Number of Participants With Change in Expression of Relevant Genes (e.g., ER Alpha and RAR Beta) Evaluated by Reverse Transcriptase Polymerase Chain Reaction (RT-PCR)

Number of participants with a change in candidate gene re-expression of ER-alpha and RAR beta evaluated by reverse transcriptase polymerase chain reaction (RT-PCR). (NCT01349959)
Timeframe: Baseline to up to 8 weeks

InterventionParticipants (Count of Participants)
TNBCHRBC
Treatment (Entinostat and Azacitidine)014

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Number of Participants With Change in Gene Methylation Evaluated Using Quantitative Multiple Methylation-specific Polymerase Chain Reaction (QM-MSP)

(NCT01349959)
Timeframe: Up to 8 weeks

InterventionParticipants (Count of Participants)
TNBCHRBC
Treatment (Entinostat and Azacitidine)014

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Overall Survival

Median number of months alive, estimated by Kaplan-Meier method. (NCT01349959)
Timeframe: Up to 3 years

Interventionmonths (Median)
TNBCHRBC
Treatment (Entinostat and Azacitidine)6.612.6

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Progression-free Survival (PFS)

Median number of months without progression. Estimated using the method of Kaplan-Meier. (NCT01349959)
Timeframe: 6 months

Interventionmonths (Median)
TNBCHRBC
Treatment (Entinostat and Azacitidine)1.41.8

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Time-to-treatment Deterioration (TTD)

Time-to-treatment deterioration (TTD) was defined as time from randomization to disease progression or death or worsening of symptoms, whichever occurred first. Disease progression was assessed per RECIST v1.1. Symptoms deterioration was measured by 6 items (GP1, GP2, GP4, GF7, B1, P2, scored 0-24) from the 8-item FACT-Breast Symptom Index (FBSI). Symptom deterioration was defined as two consecutive available decreases of at least 3 points from baseline using the 6-item FBSI in this trial, and the second visit time was used as the time of symptom deterioration in this case, unless it was the final score, for which one decrease was sufficient. Kaplan-Meier method was used to estimate the median TTD and TTD rate at a certain time point. Symptoms were assessed every cycle for the first six months after randomization, every two cycles between 6 months and 1 year. It then were assessed based on the same schedule for tumor assessments until disease progression as specified below. (NCT02115282)
Timeframe: Disease assessed at baseline, then every 12 weeks until treatment discontinuation, then every 3 months within 2 years from study entry, every 6 months between 2-5 years and annually between 6-10 years from study entry, until first disease progression

Interventionmonths (Median)
Arm A (Exemestane, Entinostat)2.9
Arm B (Exemestane, Placebo)2.9

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Patient-reported Fatigue

Fatigue was measured by PROMIS Fatigue short form, it had 7 items and all items were rated on a 5-point Likert scale from 1 to 5. The PROMIS Fatigue total score and T score were calculated based on the scoring manual. The total score ranges from 7 to 35, the T score ranges from 29.4 to 83.2, higher scores indicate more fatigue. The PROMIS Fatigue T score was used for arm comparison. The primary comparison of patient-reported fatigue between treatment arms was based on the end of cycle 3 assessment. (NCT02115282)
Timeframe: Assessed at baseline and end of cycle 3

InterventionT-score (Mean)
Arm A (Exemestane, Entinostat)55.5
Arm B (Exemestane, Placebo)54.1

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Lysine Acetylation Change in CD45 Blood Mononuclear Cells Between C1D1 and C1D15 and PFS in Patients on Arm A

Peripheral blood samples (PBMCs) were collected prior to therapy and on Days 8 and 15 of cycle 1, for assessment of lysine acetylation, using an assay developed by the Trepel Laboratory, NCI/NIH. CD45 blood mononuclear cells were measured. Patients with lysine acetylation change of 1.5 folds or higher were compared to patients with lysine acetylation change of less than 1.5 folds. (NCT02115282)
Timeframe: Disease assessed at baseline, then every 12 weeks until treatment discontinuation, then every 3 months within 2 years from study entry, every 6 months between 2-5 years and annually between 6-10 years from study entry, until first disease progression

Interventionmonths (Median)
Arm A (Exemestane, Entinostat)- Lysine Acetylation Change>=1.5 Fold2.8
Arm A (Exemestane, Entinostat)- Lysine Acetylation Change<1.5 Fold2.7

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Objective Response Rate (ORR)

Objective response rate was defined as number of patients with complete response (CR) or partial response (PR) divided by all randomized patients. Responses were evaluated using the revised Response Evaluation Criteria in Solid Tumors (RECIST) guideline. CR was defined as disappearance of all target and non-target lesions. PR was defined as at least a 30% decrease in the sum of the diameters of target lesions (taking as reference the baseline sum diameters), and/or persistence of one or more non-target lesion(s). (NCT02115282)
Timeframe: Assessed at baseline, then every 12 weeks until treatment discontinuation, then every 3 months within 2 years from study entry, every 6 months between 2-5 years and annually between 6-10 years from study entry, until first disease progression

Interventionpercentage of participants (Number)
Arm A (Exemestane, Entinostat)4.6
Arm B (Exemestane, Placebo)4.3

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Overall Survival (OS)

Overall survival (OS) was defined to be time from randomization to death from any cause. Cases who were still alive were censored at the date last known alive. (NCT02115282)
Timeframe: Assessed every 3 months within 2 years from study entry, every 6 months between 2-5 years and annually between 6-10 years from study entry, until death

Interventionmonths (Median)
Arm A (Exemestane, Entinostat)23.4
Arm B (Exemestane, Placebo)21.7

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Patient-reported Diarrhea

Diarrhea was measured by Functional Assessment of Chronic Illness Therapy for Patients With Diarrhea (FACIT-Diarrhea) subscale form, which had 11 items, all items were rated on a 5-point Likert scale from 0 to 4. FACIT-Diarrhea subscale score was calculated based on the scoring manual, subscale score ranges from 0 to 44, and higher score indicates less diarrhea. The primary comparison of patient-reported diarrhea between treatment arms was based on the end of cycle 3 assessment. (NCT02115282)
Timeframe: Assessed at baseline and end of cycle 3

Interventionunits on a scale (Mean)
Arm A (Exemestane, Entinostat)38.8
Arm B (Exemestane, Placebo)41.5

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Patient-reported Nausea and Anorexia

Nausea and anorexia were measured by The Functional Assessment of Anorexia/Cachexia Treatment (FAACT)-additional concerns, which had 12 items, all items were rated on a 5-point Likert scale from 0 to 4. FAACT-additional concerns subscale score was calculated based on scoring manual. Subscale score ranges from 0 to 48, and higher scores indicate less nausea and anorexia. The primary comparison of patient-reported nausea and anorexia between treatment arms was based on the end of cycle 3 assessment. (NCT02115282)
Timeframe: Assessed at baseline and end of cycle 3

Interventionunits on a scale (Mean)
Arm A (Exemestane, Entinostat)35.8
Arm B (Exemestane, Placebo)37.0

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Progression-free Survival (PFS)

Progression-free survival (PFS) was defined to be time from randomization to the earliest documented disease progression as defined by the RECIST criteria, new primary breast cancer, or death without progression. Disease assessment was to continue until disease progression, even after non-protocol anti-cancer therapy was started. Cases with incomplete follow up or without adequate disease evaluations were censored at the date last documented to be free of progression, regardless of whether non-protocol anti-cancer therapy was started or not. Disease progression was based on central review, and defined as at least a 20% increase in the sum of the diameters of target lesions, taking as reference the smallest sum on study. In addition to the relative increase of 20%, the sum must also demonstrate an absolute increase of at least 5 mm. In addition, the appearance of one or more new lesions was also considered progression. Kaplan-Meier method was used to estimate PFS rate. (NCT02115282)
Timeframe: Assessed at baseline, then every 12 weeks until treatment discontinuation, then every 3 months within 2 years from study entry, every 6 months between 2-5 years and annually between 6-10 years from study entry, until first disease progression

Interventionmonths (Median)
Arm A (Exemestane, Entinostat)3.3
Arm B (Exemestane, Placebo)3.1

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Phase 1b: Participants Experiencing DLT

Phase 1b employed a classical 3+3 design, with the determination of DLT based on entinostat in combination with atezolizumab within the first cycle of treatment (that is, between Day 1 to Day 21 of Cycle 1). Six participants were required to be treated in a dose level for it to be considered MTD or the Recommended Phase 2 Dose (RP2D). A DLT was defined as the occurrence of specific events, defined in the protocol, that were considered by the investigator to be at least possibly related to study drug using the National Cancer Institute (NCI) Common Terminology Criteria for Adverse Events version 4.03.The DLT assessment window (Cycle 1) was the time period between Cycle 1 Day 1 until Cycle 2 Day 1 (expected to be 21 days after Cycle 1 Day 1). (NCT02708680)
Timeframe: Up to 21 days after Cycle 1 Day 1

InterventionParticipants (Count of Participants)
Phase 1b Dose Determination: Entinostat Plus Atezolizumab0

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Phase 2 Expansion: Overall Survival (OS)

OS was defined as the number of months from randomization to date of death from any cause. Participants who were alive or lost to follow-up as of a data analysis cutoff date were right-censored. One month was considered 30.4375 days. OS (months) = (Date of Death/Censoring - Date of Randomization + 1)/30.4375 (NCT02708680)
Timeframe: Up to 5 years

Interventionmonths (Median)
Phase 2 Expansion: Entinostat Plus Atezolizumab12.25
Phase 2 Expansion: Placebo Plus Atezolizumab11.20

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Phase 2 Expansion: Duration of Progression-free Survival (PFS) Using Response Evaluation Criteria in Solid Tumors Version 1.1 (RECIST 1.1)

The duration of PFS, assessed using RECIST 1.1, was used to evaluate the efficacy of entinostat at the RP2D in combination with atezolizumab in participants with advanced triple negative breast cancer (aTNBC). It was defined as the number of months from randomization to the earlier of progressive disease or death due to any cause. One month was considered 30.4375 days. PFS (months) = (Date of Progression or Censoring - Date of Randomization + 1)/30.4375. (NCT02708680)
Timeframe: Up to 1 year

Interventionmonths (Median)
Phase 2 Expansion: Entinostat Plus Atezolizumab1.68
Phase 2 Expansion: Placebo Plus Atezolizumab1.51

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Phase 2 Expansion: Duration of PFS Using Immune Response RECIST (irRECIST)

The duration of PFS, assessed using irRECIST, was used to evaluate the efficacy of entinostat at the RP2D in combination with atezolizumab in participants with aTNBC. It was defined as the number of months from randomization to the earlier of progressive disease or death due to any cause. One month was considered 30.4375 days. PFS (months) = (Date of Progression or Censoring - Date of Randomization + 1)/30.4375. (NCT02708680)
Timeframe: Up to 1 year

Interventionmonths (Median)
Phase 2 Expansion: Entinostat Plus Atezolizumab1.68
Phase 2 Expansion: Placebo Plus Atezolizumab1.54

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Phase 2 Expansion: Overall Response Rate (ORR) Using RECIST 1.1 and irRECIST

ORR was defined as the crude percentage of participants achieving a best overall response of complete response (CR) or partial response (PR) assessed using RECIST 1.1 and irRECIST. ORR calculated as: (number of participants with best overall response as CR or PR)/total number of participants. The overall response was determined locally by the investigator at each scheduled assessment. (NCT02708680)
Timeframe: Up to 1 year

,
Interventionpercentage of participants (Number)
ORR per RECIST 1.1ORR per irRECIST 1.1
Phase 2 Expansion: Entinostat Plus Atezolizumab12.512.5
Phase 2 Expansion: Placebo Plus Atezolizumab2.42.4

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Phase 2 Expansion: Clinical Benefit Rate (CBR) Using RECIST 1.1 and irRECIST

CBR was estimated based on the crude percentage of participants in each treatment arm whose best overall response during the course of study treatment was CR, PR, or stable disease (SD) lasting for at least 24 weeks (measured from the date of randomization to the last date where SD was reported). (NCT02708680)
Timeframe: Up to 1 year

,
Interventionpercentage of participants (Number)
CBR per RECIST 1.1CBR per irRECIST 1.1
Phase 2 Entinostat Plus Atezolizumab15.015.0
Placebo Plus Atezolizumab7.37.3

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Phase 1b: Determination of the RP2D

Phase 1b employed a classical 3+3 design, with the determination of the RP2D based on entinostat in combination with atezolizumab within the first cycle of treatment (that is, between Day 1 to Day 21 of Cycle 1). The RP2D was defined as equal to or less than the preliminary maximum tolerated dose (MTD) and was determined in discussion with the sponsor, the study medical monitor, and dose determination phase investigators. The MTD was defined as the highest dose level at which <33% of 6 participants experience DLT. (NCT02708680)
Timeframe: Up to 21 days after Cycle 1 Day 1

Interventionmilligram (Number)
Phase 1b Dose Determination: Entinostat Plus Atezolizumab5

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Total Area Under the Plasma Concentration Curve of Entinostat: AUC

The median (min, max) of the total area under the plasma concentration curve of entinostat stratified by study part, dose level. Time points were assessed at 0, 0.5, 1, 3, 6, 24, and 48-96 hours post-dose during cycle 1, day 1. (NCT02780804)
Timeframe: Up to 96 hours

Interventionhr*ng/mL (Median)
Stratum 1 With 3 mg/m²755
Stratum 1 With 4 mg/m²1111
PK Part With 4 mg/m²1147

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Antitumor Activity of Entinostat

Frequency of response to entinostat per Response Evaluation Criteria In Solid Tumors Criteria (RECIST v1.1) for target lesions and/or assessed by MRI: Complete Response (CR), Disappearance of all target lesions; Partial Response (PR), >=30% decrease in the sum of the longest diameter of target lesions; Overall Response (OR) = CR + PR, stratified by study part and dose (NCT02780804)
Timeframe: Up to 4 years 9 months

InterventionParticipants (Count of Participants)
Stratum 1 With 3 mg/m²0
Stratum 1 With 4 mg/m²0
PK Part With 4 mg/m²0

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Frequency of Adverse Events for Entinostat

The frequency of patients with at least one Grade 3 or greater adverse event that are at least possibly attributable to entinostat during cycle 1 will be summarized by study part, dose level. (NCT02780804)
Timeframe: Up to 28 days

InterventionParticipants (Count of Participants)
Stratum 1 With 3 mg/m²5
Stratum 1 With 4 mg/m²7
PK Part With 4 mg/m²5

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Half-life of Entinostat

The median (min, max) Half-Life of entinostat stratified by study part and dose level. The half-life (t1/2) was calculated using the equation t1/2 = 0.693/λz, where the terminal elimination rate constant (λz) was determined from a least-squares regression of the log-transformed plasma concentration vs. time data for the last 3 - 4 time points. (NCT02780804)
Timeframe: Plasma concentrations were measured at 0, 0.5, 1, 3, 6, 24, and 48-96 hours post-dose during cycle 1, day 1.

InterventionHours (Median)
Stratum 1 With 3 mg/m²50.96
Stratum 1 With 4 mg/m²46.04
PK Part With 4 mg/m²44.23

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Peak Plasma Concentration of Entinostat: C-Max

The median (min, max) of the peak plasma concentration of entinostat stratified by study part, dose level. Time points were assessed at 0, 0.5, 1, 3, 6, 24, and 48-96 hours post-dose during cycle 1, day 1. (NCT02780804)
Timeframe: Up to 96 hours

Interventionng/ml (Median)
Stratum 1 With 3 mg/m²54.4
Stratum 1 With 4 mg/m²61.5
PK Part With 4 mg/m²23.8

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Time to Reach Maximum Plasma Concentration of Entinostat: T-Max

The median (min, max) of the time to reach maximum plasma concentration of entinostat stratified by study part, dose level. Time points were assessed at 0, 0.5, 1, 3, 6, 24, and 48-96 hours post-dose during cycle 1, day 1. (NCT02780804)
Timeframe: Up to 96 hours

InterventionHours (Median)
Stratum 1 With 3 mg/m²1.01
Stratum 1 With 4 mg/m²0.59
PK Part With 4 mg/m²1

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Percent of Participants With a Ki67 Response

A response was defined as a decrease in Ki-67 protein expression in tumor from pre- to post-treatment. (NCT03018249)
Timeframe: Specimens were collected at initial diagnostic biopsy and at hysterectomy on day 21-24 and analyzed in batch.

InterventionParticipants (Count of Participants)
Arm I (Medroxyprogesterone Acetate, Hysterectomy) MPA15
Arm II (Medroxyprogesterone Acetate, Entinostat, Hysterectomy) MPA and Entinostat18

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The Frequency and Severity of CTCAE Version 4.0 Graded Adverse Events (AE)

Maximum grade of physician assessed adverse events reported during treatment and up to 45 days after surgery. Grades start with 1 which is considered mild through grade 5 which is death. Participants on this study had adverse event grades up to grade 3 which is considered moderately severe. (NCT03018249)
Timeframe: Up to 45 days after surgery

,
Interventionparticipants (Number)
Grade 1 AEGrade 2 AEGrade 3 AEGrade 4 AEGrade 5 AE
Arm I (Medroxyprogesterone Acetate, Hysterectomy) MPA114200
Arm II (Medroxyprogesterone Acetate, Entinostat, Hysterectomy) MPA and Entinostat96200

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Percentage of Participants With a Histologic Response

Pre- and post-treatment slides for each patient were evaluated in pairs for complete or partial histologic response by one reviewer. Pre- and post-treatment slides for each patient were evaluated in pairs for complete or partial histologic response by one reviewer. A histologic response was defined as either the absence of identifiable adenocarcinoma in the hysterectomy specimen section (complete) or, subjectively, as the presence of a complex proliferation of glands that retain the architectural characteristics of adenocarcinoma, but with features of secretion, decreased nuclear stratification, or the presence of eosinophilic, squamous or mucinous metaplasia, when this was absent in the initial sample (partial). (NCT03018249)
Timeframe: Specimens were collected at initial diagnostic biopsy and at hysterectomy on day 21-24 and analyzed in batch.

InterventionParticipants (Count of Participants)
Arm I (Medroxyprogesterone Acetate, Hysterectomy) MPA16
Arm II (Medroxyprogesterone Acetate, Entinostat, Hysterectomy) MPA and Entinostat14

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Mean Post-treatment Tumor Progesterone Receptor H-score (Histology Score)

The H-score is defined as the percent cells staining positive (0-100) multiplied by the staining intensity (0, 1, 2 or 3) measured in the tumor by immunohistochemistry and averaged over 3 reviewers. This score can range from 0 to 300. In general, PRs are expected to decrease in response to medroxyprogesterone acetate. It was hypothesized that entinostat would mitigate the decrease in PR relative to the medroxyprogesterone acetate only arm post treatment. Higher PR H-scores post treatment in the arm with entinostat relative to the medroxyprogesterone alone arm would be consistent with this hypothesis. Arm II was thought to result in higher scores which was expected to have a more favorable outcome when treated with MPA therapy. (NCT03018249)
Timeframe: Specimens were collected at hysterectomy on day 21-24 and analyzed in batch.

Interventionunits on a scale (Mean)
Arm I (Medroxyprogesterone Acetate, Hysterectomy) MPA53.6
Arm II (Medroxyprogesterone Acetate, Entinostat, Hysterectomy) MPA and Entinostat42.7

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Maximum Tolerated Dose (MTD) of Hydroxychloroquine and Entinostat in Combination With Regorafenib

Participants were evaluable for toxicity if they have taken one dose of HCQ and one dose of entinostat. To be considered for evaluability in a Phase I cohort in the absence of dose-limiting toxicity, patients should have completed > 85% of HCQ doses, and at least 3 of 4 entinostat doses. The MTD will be defined as a) the dose producing DLT in 1 out of 6 patients, or b) the dose level below the dose which produced DLT in ≥ 2 out of 3 patients, or in ≥ 2 out of 6 patients. DLTs will be defined by toxicity occurring during the first 4 weeks of this study. (NCT03215264)
Timeframe: 18 months

Interventionmg (Number)
Hydroxychloroquine DailyEntinostat weekly
All Participants12005

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Overall Survival (OS) at 24 Months

OS is defined as the proportion of subjects who are alive at 24 months. Estimation based on the Kaplan-Meier curve. (NCT03250273)
Timeframe: 24 months

Interventionproportion of participants (Number)
Arm A - Cholangiocarcinoma0.077
ARM B - Pancreatic Cancer0.035

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Overall Survival (OS) at 36 Months

OS is defined as the proportion of subjects who are alive at 36 months. Estimation based on the Kaplan-Meier curve. (NCT03250273)
Timeframe: 36 months

Interventionproportion of participants (Number)
Arm A - Cholangiocarcinoma0.077
ARM B - Pancreatic Cancer0.035

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Overall Survival (OS) at 6 Months

OS is defined as the proportion of subjects who are alive at 6 months. Estimation based on the Kaplan-Meier curve. (NCT03250273)
Timeframe: 6 months

Interventionproportion of participants (Number)
Arm A - Cholangiocarcinoma0.538
ARM B - Pancreatic Cancer0.311

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Progression Free Survival (PFS) at 12 Months

PFS is defined as the proportion of patients without disease progression (PD or relapse from CR) or death due to any cause at 12 months. Disease progression will be assessed using RECIST (version 1.1). Per RECIST 1.1 criteria, CR = disappearance of all target lesions, Partial Response (PR) is =>30% decrease in sum of diameters of target lesions, Progressive Disease (PD) is >20% increase in sum of diameters of target lesions, Stable Disease (SD) is <30% decrease or <20% increase in sum of diameters of target lesions.Estimation based on the Kaplan-Meier curve. (NCT03250273)
Timeframe: 12 months

Interventionproportion of participants (Number)
Arm A - Cholangiocarcinoma0
ARM B - Pancreatic Cancer0.1

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Progression Free Survival (PFS) at 24 Months

PFS is defined as the proportion of patients without disease progression (PD or relapse from CR) or death due to any cause at 24 months. Disease progression will be assessed using RECIST (version 1.1). Per RECIST 1.1 criteria, CR = disappearance of all target lesions, Partial Response (PR) is =>30% decrease in sum of diameters of target lesions, Progressive Disease (PD) is >20% increase in sum of diameters of target lesions, Stable Disease (SD) is <30% decrease or <20% increase in sum of diameters of target lesions.Estimation based on the Kaplan-Meier curve. (NCT03250273)
Timeframe: 24 months

Interventionproportion of participants (Number)
Arm A - Cholangiocarcinoma0
ARM B - Pancreatic Cancer0

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Progression Free Survival (PFS) at 6 Months

PFS is defined as the proportion of patients without disease progression (PD or relapse from CR) or death due to any cause at 6 months. Disease progression will be assessed using RECIST (version 1.1). Per RECIST 1.1 criteria, CR = disappearance of all target lesions, Partial Response (PR) is =>30% decrease in sum of diameters of target lesions, Progressive Disease (PD) is >20% increase in sum of diameters of target lesions, Stable Disease (SD) is <30% decrease or <20% increase in sum of diameters of target lesions.Estimation based on the Kaplan-Meier curve. (NCT03250273)
Timeframe: 6 months

Interventionproportion of participants (Number)
Arm A - Cholangiocarcinoma0
ARM B - Pancreatic Cancer0.1

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Overall Survival (OS)

OS is defined as the duration of time from start of study treatment to time of death (OS will be censored on the date the subject was last known to be alive for subjects without documentation of death at the time of analysis). Estimation based on the Kaplan-Meier curve. (NCT03250273)
Timeframe: 38 months

Interventionmonths (Median)
Arm A - Cholangiocarcinoma6.378
ARM B - Pancreatic Cancer3.945

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Overall Survival (OS) at 12 Months

OS is defined as the proportion of subjects who are alive at 12 months. Estimation based on the Kaplan-Meier curve. (NCT03250273)
Timeframe: 12 months

Interventionproportion of participants (Number)
Arm A - Cholangiocarcinoma0.308
ARM B - Pancreatic Cancer0.173

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Objective Response Rate (ORR) Using Response Evaluation Criteria for Solid Tumors (RECIST 1.1)

Objective Response Rate (ORR) is defined as the number of patients achieving a complete response (CR) or partial response (PR) based on RECIST 1.1 criteria. CR = disappearance of all target lesions, PR is =>30% decrease in sum of diameters of target lesions. (NCT03250273)
Timeframe: 27 months

InterventionParticipants (Count of Participants)
Arm A - Cholangiocarcinoma0
ARM B - Pancreatic Cancer3

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Duration of Response (DOR)

Duration of response (DOR) will be calculated for subjects who achieve a best overall response of CR or PR. DOR is defined as the number of months from the start date of PR or CR (whichever response is recorded first) and subsequently confirmed to the first date that recurrent or progressive disease or death is documented. Per RECIST 1.1 criteria, CR = disappearance of all target lesions, Partial Response (PR) is =>30% decrease in sum of diameters of target lesions, Progressive Disease (PD) is >20% increase in sum of diameters of target lesions. (NCT03250273)
Timeframe: 27 months

Interventionmonths (Median)
ARM B - Pancreatic Cancer10.2

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Number of Participants With Serious and Non-serious Adverse Events Assessed by the Common Terminology Criteria for Adverse Events (CTCAE v5.0)

Here is the number of participants with serious and non-serious adverse events assessed by the Common Terminology Criteria for Adverse Events (CTCAE v5.0). A non-serious adverse event is any untoward medical occurrence. A serious adverse event is an adverse event or suspected adverse reaction that results in death, a life-threatening adverse drug experience, hospitalization, disruption of the ability to conduct normal life functions, congenital anomaly/birth defect or important medical events that jeopardize the patient or subject and may require medical or surgical intervention to prevent one of the previous outcomes mentioned. (NCT04296942)
Timeframe: Date treatment consent signed to date off study, approximately 5 months and 17 days.

InterventionParticipants (Count of Participants)
1/M7824 (Bintrafusp Alfa) + Bavarian Nordic (BN)-Brachyury1

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Progression-free Survival (PFS) in Triple Negative Breast Cancer (TNBC)

Progression free survival is defined as the duration of time from start of treatment to time of progression or death, whichever occurs first. In the absence of progression or death, PFS is censored at the date of last disease evaluation. Progression was assessed by the Response Evaluation Criteria in Solid Tumors (RECIST)v1.1 and is defined as at least a 20% increase in the sum of diameters of target lesions. appearance of new lesions. Appearance of one or more new lesions. (NCT04296942)
Timeframe: From start of treatment to time of progression or death, whichever occurs first, approximately 5 months and 17 days.

InterventionDays (Number)
1/M7824 (Bintrafusp Alfa) + Bavarian Nordic (BN)-Brachyury63

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Overall Response (Partial Response + Complete Response) for Participants With Triple Negative Breast Cancer (TNBC)

Overall response is defined as the best response (Partial Response + Complete Response) recorded from the start of treatment until disease progression/recurrence assessed by the Response Evaluation Criteria in Solid Tumors (RECIST)v1.1. Complete response is disappearance of all target lesions. Partial response is at least a 30% decrease in the sum of the diameters of target lesions, taking as reference the baseline sum of diameters. Progression is at least a 20% increase in the sum of diameters of target lesions. appearance of new lesions. Appearance of one or more new lesions. (NCT04296942)
Timeframe: From start of treatment until disease progression/recurrence, approximately 5 months and 17 days.

InterventionParticipants (Count of Participants)
Complete ResponsePartial ResponseProgressive Disease
1/M7824 (Bintrafusp Alfa) + Bavarian Nordic (BN)-Brachyury001

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Number of Participants Experiencing at Least One Grade 3 to 5 Adverse Events for Each of the Three Combinations of Agents

Adverse events were recorded using the Common Terminology Criteria for Adverse Events (CTCAE) v5.0. Grade 3 is severe, Grade 4 is life-threatening, and Grade 5 is death related to adverse event. (NCT04296942)
Timeframe: Date treatment consent signed to date off study, approximately 5 months and 17 days.

InterventionParticipants (Count of Participants)
Grade 3Grade 4Grade 5
1/M7824 (Bintrafusp Alfa) + Bavarian Nordic (BN)-Brachyury000

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Number of Participants Experiencing Grade 3 and 4 Adverse Events

Defined by Common Terminology Criteria for Adverse Events version 5.0. Will be summarized by frequency and magnitude. (NCT04631029)
Timeframe: Up to 30 days

InterventionParticipants (Count of Participants)
Grade 3 Adverse EventsGrade 4 Adverse Events
Dose Level 132

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Number of Participants Who Received 3 or More Cycles of the Combination of Entinostat, Atezolizumab, Carboplatin, and Etoposide

The proportion of participants who received 3 or more cycles of the combination, will be calculated with a 90% confidence interval. (NCT04631029)
Timeframe: Up to cycle 4 (1 cycle = 21 days)

InterventionParticipants (Count of Participants)
Received 3 or more cyclesReceived 1 or 2 cycles
Dose Level 103

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Number of Participants With Dose Limiting Toxicities

The Bayesian optimal interval (BOIN) design will be used to find the MTD based on safety as determined by dose limiting toxicities. (NCT04631029)
Timeframe: Up to 21 days

InterventionParticipants (Count of Participants)
Completed Dose Level 1 without a dose-limiting toxicityExperienced a dose limiting toxicity in Dose Level 1
Dose Level 112

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Progression Free Survival (PFS) Rate

Defined as the proportion of patients alive and without disease progression. Progression is defined using Response Evaluation Criteria In Solid Tumors Criteria (RECIST v1.1), as a 20% increase in the sum of the longest diameter of target lesions, or a measurable increase in a non-target lesion, or the appearance of new lesions. Will be estimated with a 90% confidence interval. The Kaplan Meier estimator will be used to estimate survival curves. (NCT04631029)
Timeframe: Up to 2 months

InterventionParticipants (Count of Participants)
Alive without Disease ProgressionDeceased by 2 monthsWithdrew by 2 months
Dose Level 1012

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