epz-6438 profile

tazemetostat: a histone methyltransferase EZH2 inhibitor with antineoplastic activity [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

ID Source	ID
PubMed CID	66558664
CHEMBL ID	3414621
SCHEMBL ID	19325409
SCHEMBL ID	13276848
SCHEMBL ID	22210809
MeSH ID	M000600254

Synonym
n-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(ethyl(tetrahydro-2h-pyran-4-yl)amino)-4-methyl-4'-(morpholinomethyl)-[1,1'-biphenyl]-3-carboxamide
n-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl) methyl)-5-(ethyl(tetrahydro-2h-pyran-4-yl)amino)-4-methyl-4'-(morpholinomethyl)-[1,1'-biphenyl]-3-carboxamide
NSQSAUGJQHDYNO-UHFFFAOYSA-N
S7128
e-7438
epz 6438
epz6438
tazemetostat
epz-6438
tazverik
gtpl7011
n-[(4,6-dimethyl-2-oxo-1h-pyridin-3-yl)methyl]-3-[ethyl(oxan-4-yl)amino]-2-methyl-5-[4-(morpholin-4-ylmethyl)phenyl]benzamide
CS-1758
HY-13803
1403254-99-8
c34h44n4o4
e7438
tazemetostat [who-dd]
tazemetostat [mi]
e 7438
unii-q40w93wpe1
(1,1'-biphenyl)-3-carboxamide, n-((1,2-dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl)-5-(ethyl(tetrahydro-2h-pyran-4-yl)amino)-4-methyl-4'-(4-morpholinylmethyl)-
n-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(ethyl(oxan-4-yl)amino)-4-methyl-4'-((morpholin-4-yl)methyl)(1,1'-biphenyl)-3-carboxamide
tazemetostat [inn]
tazemetostat [usan:inn]
q40w93wpe1 ,
tazemetostat [usan]
SCHEMBL19325409
SCHEMBL13276848
n-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(ethyl(tetrahydro-2h-pyran-4-yl)amino)-4-methyl-4'-(morpholinomethyl)biphenyl-3-carboxamide
AC-30931
J-690163
J-690164
(r,z)-1-(1-(1-(ethylsulfonyl)piperidin-4-yl)ethyl)-n-((2-hydroxy-4-methoxy-6-methylpyridin-3-yl)methyl)-2-methyl-1h-indole-3-carbimi dic acid
CHEMBL3414621
AKOS026750211
EX-A509
HMS3653O07
mfcd24849415
5-(ethyl(tetrahydro-2h-pyran-4-yl)amino)-n-((2-hydroxy-4,6-dimethylpyridin-3-yl)methyl)-4-methyl-4'-(morpholinomethyl)-[1,1'-biphenyl]-3-carboxamide
NCGC00381562-10
SW220030-1
tazemetostat(epz-6438)
DB12887
FT-0700193
tazemetostat (epz-6438)
NCGC00381562-01
Q27088941
tazemetostat (usan/inn)
D11444
SB22955
HMS3747A09
CCG-264672
BCP07409
epz-6438; epz 6438; e7438; tazemetostat; e-7438; e 7438
AS-55991
nsc791066
nsc-777109
nsc777109
nsc-791066
n-[(4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl]-5-[ethyl(tetrahydropyran-4-yl)amino]-4-methyl-4 inverted exclamation mark -(morpholinomethyl)biphenyl-3-carboxamide
SY040988
SCHEMBL22210809
DTXSID201025831
n-[(4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl]-5-[ethyl(oxan-4-yl)amino]-4-methyl-4'-[(morpholin-4-yl)methyl]-[1,1'-biphenyl]-3-carboxamide
n-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(ethyl(tetrahydro-2h-pyran-4-yl)amino)-4-methyl-4'-(morpholinomethyl)-(1,1'-biphenyl)-3-carboxamide
tazemetostatum

Excerpt	Reference	Relevance
" Primary safety outcomes included risk of grade ≥ 3 treatment-emergent adverse events (TEAEs); primary efficacy outcomes included objective response rate (ORR)."	( A Matching-Adjusted Indirect Comparison of Single-Arm Trials in Patients with Relapsed or Refractory Follicular Lymphoma Who Received at Least Two Prior Systemic Treatments: Tazemetostat was Associated with a Lower Risk for Safety Outcomes Versus the PI3- Adib, D; Gupta, D; Mamlouk, K; Nellesen, D; Proudman, D; Yang, J, 2022)	0.72

Excerpt	Reference	Relevance
" In parallel, regulatory authorities have recommended the application of physiologically based pharmacokinetic (PBPK) modeling, for example, in the recently issued FDA Strategic Plan for Accelerating the Development of Therapies for Pediatric Rare Diseases."	( Physiologically Based Pharmacokinetic Modeling in Pediatric Oncology Drug Development. Rioux, N; Waters, NJ, 2016)	0.43

Excerpt	Reference	Relevance
" We report the discovery of a potent, selective, and orally bioavailable small-molecule inhibitor of EZH2 enzymatic activity, (N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(ethyl(tetrahydro-2H-pyran-4-yl)amino)-4-methyl-4'-(morpholinomethyl)-[1,1'-biphenyl]-3-carboxamide)."	( Durable tumor regression in genetically altered malignant rhabdoid tumors by inhibition of methyltransferase EZH2. Allain, CJ; Chesworth, R; Copeland, RA; Keilhack, H; Klaus, CR; Knutson, SK; Kuntz, KW; Moyer, MP; Pollock, RM; Porter Scott, M; Raimondi, A; Richon, VM; Warholic, NM; Wigle, TJ, 2013)	0.39
" Although both compounds are similar with respect to their mechanism of action and selectivity, EPZ-6438 possesses superior potency and drug-like properties, including good oral bioavailability in animals."	( Selective inhibition of EZH2 by EPZ-6438 leads to potent antitumor activity in EZH2-mutant non-Hodgkin lymphoma. Allain, CJ; Chesworth, R; Copeland, RA; Huang, KC; Kadowaki, T; Kawano, S; Keilhack, H; Klaus, CR; Knutson, SK; Kumar, N; Kuntz, KW; Kuznetsov, G; Minoshima, Y; Moyer, MP; Pollock, RM; Porter-Scott, M; Raimondi, A; Richon, VM; Smith, JJ; Uenaka, T; Uesugi, M; Warholic, NM; Waters, NJ; Wigle, TJ; Xiao, Y; Yokoi, A, 2014)	0.9
" Herein we disclose the discovery of a first-in-class potent, selective, and orally bioavailable EED inhibitor compound 43 (EED226)."	( Discovery of First-in-Class, Potent, and Orally Bioavailable Embryonic Ectoderm Development (EED) Inhibitor with Robust Anticancer Efficacy. Atadja, P; Dillon, MP; Fang, D; Feng, L; Fu, X; Gabriel, T; Gao, Z; Gu, J; Guo, H; Huang, Y; Jiang, X; Li, L; Lingel, A; Liu, X; Liu, Y; Mi, Y; Oyang, C; Qi, W; Shultz, MD; Sun, Y; Wang, L; Wang, Y; Yu, Z; Zeng, J; Zhang, C; Zhang, H; Zhang, J; Zhang, L; Zhang, M; Zhang, Q; Zhao, K; Zhao, M, 2017)	0.46
" Further rational structure-activity relationship exploration and optimization led to the discovery of more potent EZH2 inhibitors with oral bioavailability in mice and rats."	( Discovery of EBI-2511: A Highly Potent and Orally Active EZH2 Inhibitor for the Treatment of Non-Hodgkin's Lymphoma. Cao, J; He, F; Ho, MH; Liu, D; Lu, B; Shen, R; Shen, X; Tao, W; Wan, H; Wang, D; Xu, Z; Zhang, C; Zhang, J; Zhang, L; Zhang, M, 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

Excerpt	Relevance	Reference
" Treatment of xenograft-bearing mice with (N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(ethyl(tetrahydro-2H-pyran-4-yl)amino)-4-methyl-4'-(morpholinomethyl)-[1,1'-biphenyl]-3-carboxamide) leads to dose-dependent regression of MRTs with correlative diminution of intratumoral trimethylation levels of lysine 27 on histone H3, and prevention of tumor regrowth after dosing cessation."	( Durable tumor regression in genetically altered malignant rhabdoid tumors by inhibition of methyltransferase EZH2. Allain, CJ; Chesworth, R; Copeland, RA; Keilhack, H; Klaus, CR; Knutson, SK; Kuntz, KW; Moyer, MP; Pollock, RM; Porter Scott, M; Raimondi, A; Richon, VM; Warholic, NM; Wigle, TJ, 2013)	0.39
" Mice dosed orally with EPZ-6438 for 28 days remained tumor free for up to 63 days after stopping compound treatment in two EZH2-mutant xenograft models."	( Selective inhibition of EZH2 by EPZ-6438 leads to potent antitumor activity in EZH2-mutant non-Hodgkin lymphoma. Allain, CJ; Chesworth, R; Copeland, RA; Huang, KC; Kadowaki, T; Kawano, S; Keilhack, H; Klaus, CR; Knutson, SK; Kumar, N; Kuntz, KW; Kuznetsov, G; Minoshima, Y; Moyer, MP; Pollock, RM; Porter-Scott, M; Raimondi, A; Richon, VM; Smith, JJ; Uenaka, T; Uesugi, M; Warholic, NM; Waters, NJ; Wigle, TJ; Xiao, Y; Yokoi, A, 2014)	0.99
"080 μM), and afforded tumor regression when dosed (200 mpk SC BID) in an EZH2 dependent tumor xenograft model."	( Discovery, design, and synthesis of indole-based EZH2 inhibitors. Albrecht, BK; Audia, JE; Balasubramanian, S; Campbell, R; Cook, AS; Cummings, RT; Dakin, LA; Duplessis, M; Gagnon, A; Gehling, VS; Good, AC; Harmange, JC; Iyer, P; Lee, C; Nasveschuk, CG; Normant, E; Trojer, P; Vaswani, RG; Zhao, F, 2015)	0.42
" Developing drugs for pediatric malignancies also brings with it a number of unique trial design considerations, including flexible enrollment approaches, age-appropriate formulation, acceptable sampling schedules, and balancing the need for age-stratified dosing regimens, given the smaller patient populations."	( Physiologically Based Pharmacokinetic Modeling in Pediatric Oncology Drug Development. Rioux, N; Waters, NJ, 2016)	0.43
" No organ-oriented toxicity increased with tazemetostat dosage escalation (severity and incidence)."	( A LYSA Phase Ib Study of Tazemetostat (EPZ-6438) plus R-CHOP in Patients with Newly Diagnosed Diffuse Large B-Cell Lymphoma (DLBCL) with Poor Prognosis Features. Cullières-Dartigues, P; Dubois, R; Dubois, S; Herbaux, C; Jardin, F; Karlin, L; Le Gouill, S; Michot, JM; Molina, T; Morschhauser, F; Picquenot, JM; Ribrag, V; Salles, G; Sarkozy, C; Suttle, B; Tilly, H, 2020)	0.83
" The recommended dosage regimen is 800 mg twice daily, administered orally with or without food, until disease progression or unacceptable toxicity."	( Tazemetostat: First Approval. Hoy, SM, 2020)	0.56

Protein	Taxonomy	Measurement	Average (µ)	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
cytochrome P450 family 3 subfamily A polypeptide 4	Homo sapiens (human)	Potency	10.6840	0.0123	7.9835	43.2770	AID1645841
G	Vesicular stomatitis virus	Potency	3.3786	0.0123	8.9648	39.8107	AID1645842
cytochrome P450 2D6	Homo sapiens (human)	Potency	23.9185	0.0010	8.3798	61.1304	AID1645840
Interferon beta	Homo sapiens (human)	Potency	3.3786	0.0033	9.1582	39.8107	AID1645842
HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)	Potency	3.3786	0.0123	8.9648	39.8107	AID1645842
Inositol hexakisphosphate kinase 1	Homo sapiens (human)	Potency	3.3786	0.0123	8.9648	39.8107	AID1645842
cytochrome P450 2C9, partial	Homo sapiens (human)	Potency	3.3786	0.0123	8.9648	39.8107	AID1645842
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
[Histone H3]-lysine	Rattus norvegicus (Norway rat)	IC50 (µMol)	0.0040	0.0040	0.0040	0.0040	AID1729424
Polycomb protein EED	Homo sapiens (human)	IC50 (µMol)	0.0153	0.0020	1.2195	8.9000	AID1350244; AID1440571; AID1440572
Histone-binding protein RBBP4	Homo sapiens (human)	IC50 (µMol)	0.0040	0.0040	0.0827	0.2400	AID1350244
Polycomb protein SUZ12	Homo sapiens (human)	IC50 (µMol)	0.0040	0.0040	1.6190	8.9000	AID1350244
Histone-lysine N-methyltransferase EZH2	Homo sapiens (human)	IC50 (µMol)	0.0327	0.0003	0.5047	8.9000	AID1240270; AID1240271; AID1240272; AID1666561; AID1773633; AID1774253; AID1816403; AID1854177; AID1856993; AID1868614; AID1868615; AID1868619; AID1868681; AID1909993
Histone-lysine N-methyltransferase EZH2	Homo sapiens (human)	Ki	0.0025	0.0005	0.0317	0.1940	AID1199158
Zinc finger protein AEBP2	Homo sapiens (human)	IC50 (µMol)	0.0040	0.0040	0.1220	0.2400	AID1350244
Histone-lysine N-methyltransferase EZH1	Homo sapiens (human)	IC50 (µMol)	0.0040	0.0040	2.6165	8.7700	AID1350244
Protein cereblon	Homo sapiens (human)	IC50 (µMol)	0.0100	0.2860	1.7066	3.0000	AID1868614; AID1868681
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Histone-lysine N-methyltransferase EZH2	Homo sapiens (human)	EC50 (µMol)	0.0604	0.0050	0.3204	2.9000	AID1281011; AID1774300; AID1774301; AID1774302; AID1774303; AID1774304; AID1774305; AID1774306; AID1774307
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Process	via Protein(s)	Taxonomy
spinal cord development	Polycomb protein EED	Homo sapiens (human)
negative regulation of DNA-templated transcription	Polycomb protein EED	Homo sapiens (human)
heterochromatin formation	Polycomb protein EED	Homo sapiens (human)
negative regulation of transcription by RNA polymerase II	Polycomb protein EED	Homo sapiens (human)
cell surface receptor signaling pathway via JAK-STAT	Interferon beta	Homo sapiens (human)
response to exogenous dsRNA	Interferon beta	Homo sapiens (human)
B cell activation involved in immune response	Interferon beta	Homo sapiens (human)
cell surface receptor signaling pathway	Interferon beta	Homo sapiens (human)
cell surface receptor signaling pathway via JAK-STAT	Interferon beta	Homo sapiens (human)
response to virus	Interferon beta	Homo sapiens (human)
positive regulation of autophagy	Interferon beta	Homo sapiens (human)
cytokine-mediated signaling pathway	Interferon beta	Homo sapiens (human)
natural killer cell activation	Interferon beta	Homo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT protein	Interferon beta	Homo sapiens (human)
cellular response to interferon-beta	Interferon beta	Homo sapiens (human)
B cell proliferation	Interferon beta	Homo sapiens (human)
negative regulation of viral genome replication	Interferon beta	Homo sapiens (human)
innate immune response	Interferon beta	Homo sapiens (human)
positive regulation of innate immune response	Interferon beta	Homo sapiens (human)
regulation of MHC class I biosynthetic process	Interferon beta	Homo sapiens (human)
negative regulation of T cell differentiation	Interferon beta	Homo sapiens (human)
positive regulation of transcription by RNA polymerase II	Interferon beta	Homo sapiens (human)
defense response to virus	Interferon beta	Homo sapiens (human)
type I interferon-mediated signaling pathway	Interferon beta	Homo sapiens (human)
neuron cellular homeostasis	Interferon beta	Homo sapiens (human)
cellular response to exogenous dsRNA	Interferon beta	Homo sapiens (human)
cellular response to virus	Interferon beta	Homo sapiens (human)
negative regulation of Lewy body formation	Interferon beta	Homo sapiens (human)
negative regulation of T-helper 2 cell cytokine production	Interferon beta	Homo sapiens (human)
positive regulation of apoptotic signaling pathway	Interferon beta	Homo sapiens (human)
response to exogenous dsRNA	Interferon beta	Homo sapiens (human)
B cell differentiation	Interferon beta	Homo sapiens (human)
natural killer cell activation involved in immune response	Interferon beta	Homo sapiens (human)
adaptive immune response	Interferon beta	Homo sapiens (human)
T cell activation involved in immune response	Interferon beta	Homo sapiens (human)
humoral immune response	Interferon beta	Homo sapiens (human)
positive regulation of T cell mediated cytotoxicity	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
adaptive immune response	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class I via ER pathway, TAP-independent	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
regulation of T cell anergy	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
defense response	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
immune response	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
detection of bacterium	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
regulation of interleukin-12 production	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
regulation of interleukin-6 production	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
protection from natural killer cell mediated cytotoxicity	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
innate immune response	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
regulation of dendritic cell differentiation	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class Ib	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
negative regulation of transcription by RNA polymerase II	Histone-binding protein RBBP4	Homo sapiens (human)
DNA replication	Histone-binding protein RBBP4	Homo sapiens (human)
nucleosome assembly	Histone-binding protein RBBP4	Homo sapiens (human)
DNA replication-dependent chromatin assembly	Histone-binding protein RBBP4	Homo sapiens (human)
chromatin remodeling	Histone-binding protein RBBP4	Homo sapiens (human)
regulation of DNA-templated transcription	Histone-binding protein RBBP4	Homo sapiens (human)
brain development	Histone-binding protein RBBP4	Homo sapiens (human)
negative regulation of cell population proliferation	Histone-binding protein RBBP4	Homo sapiens (human)
negative regulation of cell migration	Histone-binding protein RBBP4	Homo sapiens (human)
negative regulation of transforming growth factor beta receptor signaling pathway	Histone-binding protein RBBP4	Homo sapiens (human)
regulation of cell fate specification	Histone-binding protein RBBP4	Homo sapiens (human)
negative regulation of DNA-templated transcription	Histone-binding protein RBBP4	Homo sapiens (human)
positive regulation of DNA-templated transcription	Histone-binding protein RBBP4	Homo sapiens (human)
negative regulation of stem cell population maintenance	Histone-binding protein RBBP4	Homo sapiens (human)
positive regulation of stem cell population maintenance	Histone-binding protein RBBP4	Homo sapiens (human)
regulation of stem cell differentiation	Histone-binding protein RBBP4	Homo sapiens (human)
negative regulation of transcription by RNA polymerase II	Polycomb protein SUZ12	Homo sapiens (human)
cell population proliferation	Polycomb protein SUZ12	Homo sapiens (human)
positive regulation of cell population proliferation	Polycomb protein SUZ12	Homo sapiens (human)
negative regulation of cell differentiation	Polycomb protein SUZ12	Homo sapiens (human)
oligodendrocyte differentiation	Polycomb protein SUZ12	Homo sapiens (human)
random inactivation of X chromosome	Polycomb protein SUZ12	Homo sapiens (human)
facultative heterochromatin formation	Polycomb protein SUZ12	Homo sapiens (human)
G1/S transition of mitotic cell cycle	Histone-lysine N-methyltransferase EZH2	Homo sapiens (human)
negative regulation of transcription by RNA polymerase II	Histone-lysine N-methyltransferase EZH2	Homo sapiens (human)
chromatin organization	Histone-lysine N-methyltransferase EZH2	Homo sapiens (human)
regulation of DNA-templated transcription	Histone-lysine N-methyltransferase EZH2	Homo sapiens (human)
positive regulation of cell population proliferation	Histone-lysine N-methyltransferase EZH2	Homo sapiens (human)
positive regulation of epithelial to mesenchymal transition	Histone-lysine N-methyltransferase EZH2	Homo sapiens (human)
regulation of gliogenesis	Histone-lysine N-methyltransferase EZH2	Homo sapiens (human)
skeletal muscle satellite cell maintenance involved in skeletal muscle regeneration	Histone-lysine N-methyltransferase EZH2	Homo sapiens (human)
cardiac muscle hypertrophy in response to stress	Histone-lysine N-methyltransferase EZH2	Homo sapiens (human)
cerebellar cortex development	Histone-lysine N-methyltransferase EZH2	Homo sapiens (human)
hippocampus development	Histone-lysine N-methyltransferase EZH2	Homo sapiens (human)
B cell differentiation	Histone-lysine N-methyltransferase EZH2	Homo sapiens (human)
keratinocyte differentiation	Histone-lysine N-methyltransferase EZH2	Homo sapiens (human)
positive regulation of cell migration	Histone-lysine N-methyltransferase EZH2	Homo sapiens (human)
regulatory ncRNA-mediated heterochromatin formation	Histone-lysine N-methyltransferase EZH2	Homo sapiens (human)
subtelomeric heterochromatin formation	Histone-lysine N-methyltransferase EZH2	Homo sapiens (human)
methylation	Histone-lysine N-methyltransferase EZH2	Homo sapiens (human)
response to estradiol	Histone-lysine N-methyltransferase EZH2	Homo sapiens (human)
negative regulation of transcription elongation by RNA polymerase II	Histone-lysine N-methyltransferase EZH2	Homo sapiens (human)
cellular response to trichostatin A	Histone-lysine N-methyltransferase EZH2	Homo sapiens (human)
protein modification process	Histone-lysine N-methyltransferase EZH2	Homo sapiens (human)
hepatocyte homeostasis	Histone-lysine N-methyltransferase EZH2	Homo sapiens (human)
regulation of circadian rhythm	Histone-lysine N-methyltransferase EZH2	Homo sapiens (human)
positive regulation of MAP kinase activity	Histone-lysine N-methyltransferase EZH2	Homo sapiens (human)
positive regulation of GTPase activity	Histone-lysine N-methyltransferase EZH2	Homo sapiens (human)
negative regulation of keratinocyte differentiation	Histone-lysine N-methyltransferase EZH2	Homo sapiens (human)
negative regulation of gene expression, epigenetic	Histone-lysine N-methyltransferase EZH2	Homo sapiens (human)
negative regulation of DNA-templated transcription	Histone-lysine N-methyltransferase EZH2	Homo sapiens (human)
negative regulation of retinoic acid receptor signaling pathway	Histone-lysine N-methyltransferase EZH2	Homo sapiens (human)
rhythmic process	Histone-lysine N-methyltransferase EZH2	Homo sapiens (human)
stem cell differentiation	Histone-lysine N-methyltransferase EZH2	Homo sapiens (human)
negative regulation of striated muscle cell differentiation	Histone-lysine N-methyltransferase EZH2	Homo sapiens (human)
synaptic transmission, GABAergic	Histone-lysine N-methyltransferase EZH2	Homo sapiens (human)
cellular response to hydrogen peroxide	Histone-lysine N-methyltransferase EZH2	Homo sapiens (human)
G1 to G0 transition	Histone-lysine N-methyltransferase EZH2	Homo sapiens (human)
protein localization to chromatin	Histone-lysine N-methyltransferase EZH2	Homo sapiens (human)
positive regulation of protein serine/threonine kinase activity	Histone-lysine N-methyltransferase EZH2	Homo sapiens (human)
regulation of kidney development	Histone-lysine N-methyltransferase EZH2	Homo sapiens (human)
liver regeneration	Histone-lysine N-methyltransferase EZH2	Homo sapiens (human)
facultative heterochromatin formation	Histone-lysine N-methyltransferase EZH2	Homo sapiens (human)
positive regulation of dendrite development	Histone-lysine N-methyltransferase EZH2	Homo sapiens (human)
negative regulation of cytokine production involved in inflammatory response	Histone-lysine N-methyltransferase EZH2	Homo sapiens (human)
positive regulation of cell cycle G1/S phase transition	Histone-lysine N-methyltransferase EZH2	Homo sapiens (human)
response to tetrachloromethane	Histone-lysine N-methyltransferase EZH2	Homo sapiens (human)
negative regulation of G1/S transition of mitotic cell cycle	Histone-lysine N-methyltransferase EZH2	Homo sapiens (human)
negative regulation of stem cell differentiation	Histone-lysine N-methyltransferase EZH2	Homo sapiens (human)
heterochromatin formation	Histone-lysine N-methyltransferase EZH2	Homo sapiens (human)
negative regulation of transcription by RNA polymerase II	Zinc finger protein AEBP2	Homo sapiens (human)
chromatin organization	Zinc finger protein AEBP2	Homo sapiens (human)
regulation of transcription by RNA polymerase II	Zinc finger protein AEBP2	Homo sapiens (human)
inositol phosphate metabolic process	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
phosphatidylinositol phosphate biosynthetic process	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
negative regulation of cold-induced thermogenesis	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol phosphate biosynthetic process	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
negative regulation of transcription by RNA polymerase II	Histone-lysine N-methyltransferase EZH1	Homo sapiens (human)
chromatin remodeling	Histone-lysine N-methyltransferase EZH1	Homo sapiens (human)
anatomical structure morphogenesis	Histone-lysine N-methyltransferase EZH1	Homo sapiens (human)
hippocampus development	Histone-lysine N-methyltransferase EZH1	Homo sapiens (human)
heterochromatin formation	Histone-lysine N-methyltransferase EZH1	Homo sapiens (human)
subtelomeric heterochromatin formation	Histone-lysine N-methyltransferase EZH1	Homo sapiens (human)
methylation	Histone-lysine N-methyltransferase EZH1	Homo sapiens (human)
positive regulation of transcription by RNA polymerase II	Histone-lysine N-methyltransferase EZH1	Homo sapiens (human)
protein ubiquitination	Protein cereblon	Homo sapiens (human)
positive regulation of Wnt signaling pathway	Protein cereblon	Homo sapiens (human)
negative regulation of protein-containing complex assembly	Protein cereblon	Homo sapiens (human)
positive regulation of protein-containing complex assembly	Protein cereblon	Homo sapiens (human)
negative regulation of monoatomic ion transmembrane transport	Protein cereblon	Homo sapiens (human)
locomotory exploration behavior	Protein cereblon	Homo sapiens (human)
proteasome-mediated ubiquitin-dependent protein catabolic process	Protein cereblon	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
transcription corepressor binding	Polycomb protein EED	Homo sapiens (human)
protein binding	Polycomb protein EED	Homo sapiens (human)
enzyme activator activity	Polycomb protein EED	Homo sapiens (human)
histone methyltransferase activity	Polycomb protein EED	Homo sapiens (human)
identical protein binding	Polycomb protein EED	Homo sapiens (human)
nucleosome binding	Polycomb protein EED	Homo sapiens (human)
cytokine activity	Interferon beta	Homo sapiens (human)
cytokine receptor binding	Interferon beta	Homo sapiens (human)
type I interferon receptor binding	Interferon beta	Homo sapiens (human)
protein binding	Interferon beta	Homo sapiens (human)
chloramphenicol O-acetyltransferase activity	Interferon beta	Homo sapiens (human)
TAP binding	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
signaling receptor binding	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
protein binding	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
peptide antigen binding	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
TAP binding	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
protein-folding chaperone binding	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
ATP-dependent activity, acting on DNA	Histone-binding protein RBBP4	Homo sapiens (human)
nucleosomal DNA binding	Histone-binding protein RBBP4	Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA binding	Histone-binding protein RBBP4	Homo sapiens (human)
protein binding	Histone-binding protein RBBP4	Homo sapiens (human)
histone binding	Histone-binding protein RBBP4	Homo sapiens (human)
histone deacetylase binding	Histone-binding protein RBBP4	Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA binding	Polycomb protein SUZ12	Homo sapiens (human)
transcription corepressor binding	Polycomb protein SUZ12	Homo sapiens (human)
protein binding	Polycomb protein SUZ12	Homo sapiens (human)
enzyme activator activity	Polycomb protein SUZ12	Homo sapiens (human)
methylated histone binding	Polycomb protein SUZ12	Homo sapiens (human)
histone methyltransferase activity	Polycomb protein SUZ12	Homo sapiens (human)
metal ion binding	Polycomb protein SUZ12	Homo sapiens (human)
lncRNA binding	Polycomb protein SUZ12	Homo sapiens (human)
promoter-specific chromatin binding	Polycomb protein SUZ12	Homo sapiens (human)
chromatin DNA binding	Polycomb protein SUZ12	Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA binding	Histone-lysine N-methyltransferase EZH2	Homo sapiens (human)
RNA polymerase II core promoter sequence-specific DNA binding	Histone-lysine N-methyltransferase EZH2	Homo sapiens (human)
transcription corepressor binding	Histone-lysine N-methyltransferase EZH2	Homo sapiens (human)
chromatin binding	Histone-lysine N-methyltransferase EZH2	Homo sapiens (human)
transcription corepressor activity	Histone-lysine N-methyltransferase EZH2	Homo sapiens (human)
protein binding	Histone-lysine N-methyltransferase EZH2	Homo sapiens (human)
protein-lysine N-methyltransferase activity	Histone-lysine N-methyltransferase EZH2	Homo sapiens (human)
chromatin DNA binding	Histone-lysine N-methyltransferase EZH2	Homo sapiens (human)
histone methyltransferase activity	Histone-lysine N-methyltransferase EZH2	Homo sapiens (human)
ribonucleoprotein complex binding	Histone-lysine N-methyltransferase EZH2	Homo sapiens (human)
histone H3K27 methyltransferase activity	Histone-lysine N-methyltransferase EZH2	Homo sapiens (human)
primary miRNA binding	Histone-lysine N-methyltransferase EZH2	Homo sapiens (human)
lncRNA binding	Histone-lysine N-methyltransferase EZH2	Homo sapiens (human)
histone H3 methyltransferase activity	Histone-lysine N-methyltransferase EZH2	Homo sapiens (human)
histone H3K27 trimethyltransferase activity	Histone-lysine N-methyltransferase EZH2	Homo sapiens (human)
promoter-specific chromatin binding	Histone-lysine N-methyltransferase EZH2	Homo sapiens (human)
DNA binding	Zinc finger protein AEBP2	Homo sapiens (human)
transcription coregulator activity	Zinc finger protein AEBP2	Homo sapiens (human)
metal ion binding	Zinc finger protein AEBP2	Homo sapiens (human)
inositol-1,3,4,5,6-pentakisphosphate kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol hexakisphosphate kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol heptakisphosphate kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol hexakisphosphate 5-kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
protein binding	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
ATP binding	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol hexakisphosphate 1-kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol hexakisphosphate 3-kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol 5-diphosphate pentakisphosphate 5-kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol diphosphate tetrakisphosphate kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
DNA binding	Histone-lysine N-methyltransferase EZH1	Homo sapiens (human)
histone binding	Histone-lysine N-methyltransferase EZH1	Homo sapiens (human)
transcription corepressor activity	Histone-lysine N-methyltransferase EZH1	Homo sapiens (human)
protein binding	Histone-lysine N-methyltransferase EZH1	Homo sapiens (human)
nucleosome binding	Histone-lysine N-methyltransferase EZH1	Homo sapiens (human)
histone H3K27 methyltransferase activity	Histone-lysine N-methyltransferase EZH1	Homo sapiens (human)
molecular condensate scaffold activity	Histone-lysine N-methyltransferase EZH1	Homo sapiens (human)
histone H3K27 trimethyltransferase activity	Histone-lysine N-methyltransferase EZH1	Homo sapiens (human)
chromatin binding	Histone-lysine N-methyltransferase EZH1	Homo sapiens (human)
protein binding	Protein cereblon	Homo sapiens (human)
transmembrane transporter binding	Protein cereblon	Homo sapiens (human)
metal ion binding	Protein cereblon	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
nucleus	Polycomb protein EED	Homo sapiens (human)
nucleoplasm	Polycomb protein EED	Homo sapiens (human)
chromosome	Polycomb protein EED	Homo sapiens (human)
cytosol	Polycomb protein EED	Homo sapiens (human)
ESC/E(Z) complex	Polycomb protein EED	Homo sapiens (human)
extracellular space	Interferon beta	Homo sapiens (human)
extracellular region	Interferon beta	Homo sapiens (human)
Golgi membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
endoplasmic reticulum	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
Golgi apparatus	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
plasma membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
cell surface	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
ER to Golgi transport vesicle membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
secretory granule membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
phagocytic vesicle membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
early endosome membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
recycling endosome membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
extracellular exosome	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
lumenal side of endoplasmic reticulum membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
MHC class I protein complex	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
extracellular space	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
external side of plasma membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
chromosome, telomeric region	Histone-binding protein RBBP4	Homo sapiens (human)
chromatin	Histone-binding protein RBBP4	Homo sapiens (human)
nucleus	Histone-binding protein RBBP4	Homo sapiens (human)
nucleoplasm	Histone-binding protein RBBP4	Homo sapiens (human)
cytosol	Histone-binding protein RBBP4	Homo sapiens (human)
NuRD complex	Histone-binding protein RBBP4	Homo sapiens (human)
NURF complex	Histone-binding protein RBBP4	Homo sapiens (human)
CAF-1 complex	Histone-binding protein RBBP4	Homo sapiens (human)
Sin3-type complex	Histone-binding protein RBBP4	Homo sapiens (human)
ATPase complex	Histone-binding protein RBBP4	Homo sapiens (human)
histone deacetylase complex	Histone-binding protein RBBP4	Homo sapiens (human)
protein-containing complex	Histone-binding protein RBBP4	Homo sapiens (human)
ESC/E(Z) complex	Histone-binding protein RBBP4	Homo sapiens (human)
nucleus	Histone-binding protein RBBP4	Homo sapiens (human)
nucleus	Polycomb protein SUZ12	Homo sapiens (human)
nucleoplasm	Polycomb protein SUZ12	Homo sapiens (human)
nucleolus	Polycomb protein SUZ12	Homo sapiens (human)
nuclear body	Polycomb protein SUZ12	Homo sapiens (human)
sex chromatin	Polycomb protein SUZ12	Homo sapiens (human)
chromatin silencing complex	Polycomb protein SUZ12	Homo sapiens (human)
ESC/E(Z) complex	Polycomb protein SUZ12	Homo sapiens (human)
ribonucleoprotein complex	Polycomb protein SUZ12	Homo sapiens (human)
RSC-type complex	Polycomb protein SUZ12	Homo sapiens (human)
nucleus	Polycomb protein SUZ12	Homo sapiens (human)
chromosome	Histone-lysine N-methyltransferase EZH2	Homo sapiens (human)
chromosome, telomeric region	Histone-lysine N-methyltransferase EZH2	Homo sapiens (human)
nucleus	Histone-lysine N-methyltransferase EZH2	Homo sapiens (human)
nucleoplasm	Histone-lysine N-methyltransferase EZH2	Homo sapiens (human)
pronucleus	Histone-lysine N-methyltransferase EZH2	Homo sapiens (human)
synapse	Histone-lysine N-methyltransferase EZH2	Homo sapiens (human)
chromatin	Histone-lysine N-methyltransferase EZH2	Homo sapiens (human)
chromatin silencing complex	Histone-lysine N-methyltransferase EZH2	Homo sapiens (human)
pericentric heterochromatin	Histone-lysine N-methyltransferase EZH2	Homo sapiens (human)
ESC/E(Z) complex	Histone-lysine N-methyltransferase EZH2	Homo sapiens (human)
nucleus	Histone-lysine N-methyltransferase EZH2	Homo sapiens (human)
nucleoplasm	Zinc finger protein AEBP2	Homo sapiens (human)
chromatin	Zinc finger protein AEBP2	Homo sapiens (human)
ESC/E(Z) complex	Zinc finger protein AEBP2	Homo sapiens (human)
fibrillar center	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
nucleoplasm	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
cytosol	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
nucleus	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
cytoplasm	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
chromosome, telomeric region	Histone-lysine N-methyltransferase EZH1	Homo sapiens (human)
nucleoplasm	Histone-lysine N-methyltransferase EZH1	Homo sapiens (human)
heterochromatin	Histone-lysine N-methyltransferase EZH1	Homo sapiens (human)
ESC/E(Z) complex	Histone-lysine N-methyltransferase EZH1	Homo sapiens (human)
nucleus	Histone-lysine N-methyltransferase EZH1	Homo sapiens (human)
nucleus	Protein cereblon	Homo sapiens (human)
cytoplasm	Protein cereblon	Homo sapiens (human)
cytosol	Protein cereblon	Homo sapiens (human)
membrane	Protein cereblon	Homo sapiens (human)
perinuclear region of cytoplasm	Protein cereblon	Homo sapiens (human)
Cul4A-RING E3 ubiquitin ligase complex	Protein cereblon	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (180)

Assay ID	Title	Year	Journal	Article
AID1350245	Cytotoxicity against human Pfeiffer cells assessed as decrease in cell viability after 5 days by CellTiter-Glo reagent based luminescence assay	2018	ACS medicinal chemistry letters, Feb-08, Volume: 9, Issue:2	Discovery of EBI-2511: A Highly Potent and Orally Active EZH2 Inhibitor for the Treatment of Non-Hodgkin's Lymphoma.
AID1773627	Antiproliferative activity against human MCF7 cells assessed as cell viability after 72 hrs by MTT assay
AID1774333	Toxicity in NCG mouse xenografted with human KARPAS-422 cells harboring EZH2 Y641N mutant assessed as effect on body weight at 200 mg/kg, po BID via gavage measured after 28 days	2021	Journal of medicinal chemistry, 10-28, Volume: 64, Issue:20	Discovery of IHMT-EZH2-115 as a Potent and Selective Enhancer of Zeste Homolog 2 (EZH2) Inhibitor for the Treatment of B-Cell Lymphomas.
AID1854177	Inhibition of EZH2 (unknown origin)	2022	European journal of medicinal chemistry, Aug-05, Volume: 238	Targeting EZH2 for cancer therapy: From current progress to novel strategies.
AID1909972	Induction of apoptosis in human HCT116 cells assessed as early apoptotic cells at 10 uM measured after 72 hrs by flow cytometry (Rvb = 2.8 %)	2022	Journal of medicinal chemistry, 05-12, Volume: 65, Issue:9	Design and Synthesis of Dual EZH2/BRD4 Inhibitors to Target Solid Tumors.
AID1440573	Antiproliferative activity against human KARPAS422 cells harboring monoallelic Y641N EZH2 mutation assessed as reduction in cell viability measured every 3 to 4 days up to 14 days by Beckman Coulter-based method	2017	Journal of medicinal chemistry, 03-23, Volume: 60, Issue:6	Discovery of First-in-Class, Potent, and Orally Bioavailable Embryonic Ectoderm Development (EED) Inhibitor with Robust Anticancer Efficacy.
AID1860970	Antiproliferative activity against human MCF-10A cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	2022	European journal of medicinal chemistry, Aug-05, Volume: 238	Discovery of precision targeting EZH2 degraders for triple-negative breast cancer.
AID1199171	Selectivity ratio of IC50 for PRMT8 (unknown origin) to IC50 for wild-type human EZH2	2015	Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4	Selective inhibitors of protein methyltransferases.
AID1816501	Downregulation of CENPK mRNA expression in human A549 cells at 10 uM incubated for 48 hrs by qRT-PCR analysis
AID1199161	Selectivity ratio of IC50 for GLP (unknown origin) to IC50 for wild-type human EZH2	2015	Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4	Selective inhibitors of protein methyltransferases.
AID1816499	Downregulation of ARL6IP mRNA expression in human A549 cells at 10 uM incubated for 48 hrs by qRT-PCR analysis
AID1199202	Selectivity ratio of IC50 for PRMT4 (unknown origin) to IC50 for wild-type human EZH2	2015	Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4	Selective inhibitors of protein methyltransferases.
AID1860973	Antiproliferative activity against human HK-2 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	2022	European journal of medicinal chemistry, Aug-05, Volume: 238	Discovery of precision targeting EZH2 degraders for triple-negative breast cancer.
AID1820282	Antitumor activity against human SU-DHL-6 cells xenografted in nude Balb/c mouse assessed as reduction in H3K27me3 level in tumor tissue at 42.5 mg/kg, ip administered for 6 times weekly for 3 weeks by Western blot analysis	2021	Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14	Design, Synthesis, and Evaluation of VHL-Based EZH2 Degraders to Enhance Therapeutic Activity against Lymphoma.
AID1857043	Synergistic antiproliferative activity against human HCT-116 cells assessed as combination index in presence of SAHA incubated for 72 hrs by CCK-8 assay	2022	Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19	Histone Deacetylase and Enhancer of Zeste Homologue 2 Dual Inhibitors Presenting a Synergistic Effect for the Treatment of Hematological Malignancies.
AID1666564	Antiproliferative activity against over expressing E2H2 human SUDHL4 cells	2020	Bioorganic & medicinal chemistry letters, 03-01, Volume: 30, Issue:5	Design and synthesis of (E)-1,2-diphenylethene-based EZH2 inhibitors.
AID1857039	Synergistic antiproliferative activity against human HL-60 cells assessed as combination index in presence of SAHA incubated for 72 hrs by CCK-8 assay	2022	Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19	Histone Deacetylase and Enhancer of Zeste Homologue 2 Dual Inhibitors Presenting a Synergistic Effect for the Treatment of Hematological Malignancies.
AID1440582	Oral bioavailability in CD-1 mouse at 2 mg/kg by LC-MS/MS analysis	2017	Journal of medicinal chemistry, 03-23, Volume: 60, Issue:6	Discovery of First-in-Class, Potent, and Orally Bioavailable Embryonic Ectoderm Development (EED) Inhibitor with Robust Anticancer Efficacy.
AID1774314	Antiproliferative activity against human Raji cells expressing wild type EZH2 assessed as inhibition of cell growth measured after 6 days by CellTiter-Glo luminescent assay	2021	Journal of medicinal chemistry, 10-28, Volume: 64, Issue:20	Discovery of IHMT-EZH2-115 as a Potent and Selective Enhancer of Zeste Homolog 2 (EZH2) Inhibitor for the Treatment of B-Cell Lymphomas.
AID1816505	Downregulation of ARL6IP mRNA expression in human NCI-H1299 cells at 10 uM incubated for 48 hrs by qRT-PCR analysis
AID1868629	Antiproliferative activity against human MCF7 cells	2022	Journal of medicinal chemistry, 05-26, Volume: 65, Issue:10	Targeting Enhancer of Zeste Homolog 2 for the Treatment of Hematological Malignancies and Solid Tumors: Candidate Structure-Activity Relationships Insights and Evolution Prospects.
AID1860966	Antiproliferative activity against human MDA-MB-468 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	2022	European journal of medicinal chemistry, Aug-05, Volume: 238	Discovery of precision targeting EZH2 degraders for triple-negative breast cancer.
AID1240271	Inhibition of EZH2 Y641N mutant (unknown origin) using biotinylated nucleosome, H3K27me3 activator and [3H]-SAM incubated for 60 mins by top-count based method	2015	Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17	Discovery, design, and synthesis of indole-based EZH2 inhibitors.
AID1816403	Inhibition of N-terminal His-tagged EZH2 in human PRC2 complex (2 to end residues) expressed in Sf9 cells using [3H]-SAM as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins by AlphaLISA immunodetection assay
AID1350281	Antitumor activity against human Pfeiffer cells xenografted in athymic nude mouse assessed as tumor growth inhibition at 100 mg/kg, po qd administered for 20 days measured twice per week	2018	ACS medicinal chemistry letters, Feb-08, Volume: 9, Issue:2	Discovery of EBI-2511: A Highly Potent and Orally Active EZH2 Inhibitor for the Treatment of Non-Hodgkin's Lymphoma.
AID1199160	Selectivity ratio of IC50 for G9a (unknown origin) to IC50 for wild-type human EZH2	2015	Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4	Selective inhibitors of protein methyltransferases.
AID1773628	Antiproliferative activity against human MCF-10A cells assessed as cell viability after 72 hrs by MTT assay
AID1240275	Intrinsic clearance in dog liver microsomes	2015	Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17	Discovery, design, and synthesis of indole-based EZH2 inhibitors.
AID1774307	Inhibition of EZH2 Y641S mutant in human SU-DHL-4 cells assessed as suppression H3K27 trimethylation measured after 72 hrs by immunoblot analysis	2021	Journal of medicinal chemistry, 10-28, Volume: 64, Issue:20	Discovery of IHMT-EZH2-115 as a Potent and Selective Enhancer of Zeste Homolog 2 (EZH2) Inhibitor for the Treatment of B-Cell Lymphomas.
AID1773632	Inhibition of recombinant PRC2 complex (unknown origin) assessed as kd/ka using H3K27me0 peptide substrate incubated for 3 hrs by HMT assay
AID1816407	Antiproliferative activity against human WSUDLCL2 cells harboring EZH2-Y641F mutant assessed as inhibition of cell growth at 10 uM incubated for 9 days by optical microscopic analysis
AID1860974	Binding affinity to recombinant PRC2 complex (unknown origin) assessed as association rate constant by surface plasmon resonance assay	2022	European journal of medicinal chemistry, Aug-05, Volume: 238	Discovery of precision targeting EZH2 degraders for triple-negative breast cancer.
AID1816480	PROTAC activity at CRBN E3 ligase/EZH2 in PRC2 complex in human WSUDLCL2 cells assessed as reduction in EED level at 10 uM measured after 48 hrs by Western blot analysis
AID1868628	Antiproliferative activity against human MDA-MB-468 cells	2022	Journal of medicinal chemistry, 05-26, Volume: 65, Issue:10	Targeting Enhancer of Zeste Homolog 2 for the Treatment of Hematological Malignancies and Solid Tumors: Candidate Structure-Activity Relationships Insights and Evolution Prospects.
AID1666565	Antiproliferative activity against human MV4-11 cells	2020	Bioorganic & medicinal chemistry letters, 03-01, Volume: 30, Issue:5	Design and synthesis of (E)-1,2-diphenylethene-based EZH2 inhibitors.
AID1774351	Antitumor activity against human KARPAS-422 cells harboring EZH2 Y641N mutant xenografted in NCG mouse assessed as change in tumor weight at 200 mg/kg, po BID via gavage measured after 28 days (Rvb = 2.14 g)	2021	Journal of medicinal chemistry, 10-28, Volume: 64, Issue:20	Discovery of IHMT-EZH2-115 as a Potent and Selective Enhancer of Zeste Homolog 2 (EZH2) Inhibitor for the Treatment of B-Cell Lymphomas.
AID1857042	Synergistic antiproliferative activity against human MDA-MB-231 cells assessed as combination index in presence of SAHA incubated for 72 hrs by CCK-8 assay	2022	Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19	Histone Deacetylase and Enhancer of Zeste Homologue 2 Dual Inhibitors Presenting a Synergistic Effect for the Treatment of Hematological Malignancies.
AID1909993	Inhibition of EZH2 (unknown origin) using H3-derivede peptide (21 to 44) as substrate incubated for 60 min in presence of SAM by MTase-Glo assay	2022	Journal of medicinal chemistry, 05-12, Volume: 65, Issue:9	Design and Synthesis of Dual EZH2/BRD4 Inhibitors to Target Solid Tumors.
AID1816478	PROTAC activity at CRBN E3 ligase/EZH2 in PRC2 complex in human WSUDLCL2 cells assessed as reduction in SUZ12 level at 10 uM measured after 48 hrs by Western blot analysis
AID1820258	Induction of cell cycle arrest in human SU-DHL-6 cells assessed as accumulation of cells at G0/G1 phase at 1 to 5 uM after 24 hrs by flow cytometry	2021	Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14	Design, Synthesis, and Evaluation of VHL-Based EZH2 Degraders to Enhance Therapeutic Activity against Lymphoma.
AID1666563	Antiproliferative activity against over expressing E2H2 human WSU-DLCL2 cells	2020	Bioorganic & medicinal chemistry letters, 03-01, Volume: 30, Issue:5	Design and synthesis of (E)-1,2-diphenylethene-based EZH2 inhibitors.
AID1199163	Selectivity ratio of IC50 for SMYD2 (unknown origin) to IC50 for wild-type human EZH2	2015	Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4	Selective inhibitors of protein methyltransferases.
AID1856995	Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	2022	Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19	Histone Deacetylase and Enhancer of Zeste Homologue 2 Dual Inhibitors Presenting a Synergistic Effect for the Treatment of Hematological Malignancies.
AID1199162	Selectivity ratio of IC50 for SETD7 (unknown origin) to IC50 for wild-type human EZH2	2015	Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4	Selective inhibitors of protein methyltransferases.
AID1860968	Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	2022	European journal of medicinal chemistry, Aug-05, Volume: 238	Discovery of precision targeting EZH2 degraders for triple-negative breast cancer.
AID1440571	Inhibition of recombinant N-terminal GST-tagged EED (76 to 441 residues) (unknown origin) expressed in Escherichia coli BL21-CodonPlus(DE3)-RIL assessed as reduction in SAH production using H3[21-44,K27Me0) peptide as substrate measured after 20 mins by L	2017	Journal of medicinal chemistry, 03-23, Volume: 60, Issue:6	Discovery of First-in-Class, Potent, and Orally Bioavailable Embryonic Ectoderm Development (EED) Inhibitor with Robust Anticancer Efficacy.
AID1868614	Protac activity at CRBN E3 ligase/EZH2 in human DOHH-2 cells assessed as induction of EZH2 degradation	2022	Journal of medicinal chemistry, 05-26, Volume: 65, Issue:10	Targeting Enhancer of Zeste Homolog 2 for the Treatment of Hematological Malignancies and Solid Tumors: Candidate Structure-Activity Relationships Insights and Evolution Prospects.
AID1281013	AUC in mouse at 2 mg/kg, iv and 10 mg/kg, po by LC-MS/MS analysis	2016	Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4	The Importance of Being Me: Magic Methyls, Methyltransferase Inhibitors, and the Discovery of Tazemetostat.
AID1868640	Aqueous solubility of the compound	2022	Journal of medicinal chemistry, 05-26, Volume: 65, Issue:10	Targeting Enhancer of Zeste Homolog 2 for the Treatment of Hematological Malignancies and Solid Tumors: Candidate Structure-Activity Relationships Insights and Evolution Prospects.
AID1860969	Antiproliferative activity against human HL-60 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	2022	European journal of medicinal chemistry, Aug-05, Volume: 238	Discovery of precision targeting EZH2 degraders for triple-negative breast cancer.
AID1860972	Antiproliferative activity against human L02 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	2022	European journal of medicinal chemistry, Aug-05, Volume: 238	Discovery of precision targeting EZH2 degraders for triple-negative breast cancer.
AID1281012	Clearance in mouse at 2 mg/kg, iv and 10 mg/kg, po by LC-MS/MS analysis	2016	Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4	The Importance of Being Me: Magic Methyls, Methyltransferase Inhibitors, and the Discovery of Tazemetostat.
AID1816512	Downregulation of CHEK1 mRNA expression in human MDA-MB-468 cells at 10 uM incubated for 48 hrs by qRT-PCR analysis
AID1816391	PROTAC activity at CRBN E3 ligase/EZH2 in PRC2 complex in human WSUDLCL2 cells assessed as induction of SUZ12 degradation at 1 uM incubated for 48 hrs by Western blot analysis
AID1666561	Inhibition of wild type EZH2 (unknown origin) by AlphaLISA assay	2020	Bioorganic & medicinal chemistry letters, 03-01, Volume: 30, Issue:5	Design and synthesis of (E)-1,2-diphenylethene-based EZH2 inhibitors.
AID1440580	Volume of distribution at steady state in CD-1 mouse at 1 mg/kg, iv or 2 mg/kg, po by LC-MS/MS analysis	2017	Journal of medicinal chemistry, 03-23, Volume: 60, Issue:6	Discovery of First-in-Class, Potent, and Orally Bioavailable Embryonic Ectoderm Development (EED) Inhibitor with Robust Anticancer Efficacy.
AID1331315	Oxidative metabolic stability in human liver microsomes assessed as amount of parent compound remaining at 1 uM after 30 mins by LC-MS/MS	2017	Bioorganic & medicinal chemistry letters, 01-15, Volume: 27, Issue:2	Novel 3-methylindoline inhibitors of EZH2: Design, synthesis and SAR.
AID1860976	Binding affinity to recombinant PRC2 complex (unknown origin) assessed as Equilibrium dissociation constant by surface plasmon resonance assay	2022	European journal of medicinal chemistry, Aug-05, Volume: 238	Discovery of precision targeting EZH2 degraders for triple-negative breast cancer.
AID1856998	Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	2022	Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19	Histone Deacetylase and Enhancer of Zeste Homologue 2 Dual Inhibitors Presenting a Synergistic Effect for the Treatment of Hematological Malignancies.
AID1199169	Selectivity ratio of IC50 for PRMT5 (unknown origin) to IC50 for wild-type human EZH2	2015	Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4	Selective inhibitors of protein methyltransferases.
AID1816517	Antiproliferative activity against human NCI-H1299 cells harboring SWI/SNF mutant assessed as inhibition of cell growth at 10 uM treated for 9 days by optical microscopic analysis
AID1240278	Protein binding in rat plasma	2015	Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17	Discovery, design, and synthesis of indole-based EZH2 inhibitors.
AID1816511	Downregulation of CEP76 mRNA expression in human MDA-MB-468 cells at 10 uM incubated for 48 hrs by qRT-PCR analysis
AID1816390	PROTAC activity at CRBN E3 ligase/EZH2 in PRC2 complex in human WSUDLCL2 cells assessed as induction of RbAp48 degradation at 1 uM incubated for 48 hrs by Western blot analysis
AID1854182	Solubility of the compound in water	2022	European journal of medicinal chemistry, Aug-05, Volume: 238	Targeting EZH2 for cancer therapy: From current progress to novel strategies.
AID1868627	Antiproliferative activity against human MDA-MB-23 cells	2022	Journal of medicinal chemistry, 05-26, Volume: 65, Issue:10	Targeting Enhancer of Zeste Homolog 2 for the Treatment of Hematological Malignancies and Solid Tumors: Candidate Structure-Activity Relationships Insights and Evolution Prospects.
AID1281011	Inhibition of methyltransferase activity of EZH2 in human G401 cells assessed as H3K27 trimethylation after 4 hrs by ELISA	2016	Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4	The Importance of Being Me: Magic Methyls, Methyltransferase Inhibitors, and the Discovery of Tazemetostat.
AID1729424	Inhibition of rat EZH2 using H3K27 peptides as substrate	2020	Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24	Small Molecule Approaches for Targeting the Polycomb Repressive Complex 2 (PRC2) in Cancer.
AID1240272	Inhibition of EZH2 in human HeLa cells assessed as reduction in H3K27me3 levels incubated for 72 hrs by ELISA method	2015	Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17	Discovery, design, and synthesis of indole-based EZH2 inhibitors.
AID1199170	Selectivity ratio of IC50 for PRMT6 (unknown origin) to IC50 for wild-type human EZH2	2015	Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4	Selective inhibitors of protein methyltransferases.
AID1868618	Inhibition of human PRC2 assessed as inhibition constant	2022	Journal of medicinal chemistry, 05-26, Volume: 65, Issue:10	Targeting Enhancer of Zeste Homolog 2 for the Treatment of Hematological Malignancies and Solid Tumors: Candidate Structure-Activity Relationships Insights and Evolution Prospects.
AID1816504	Downregulation of BRIC5 mRNA expression in human NCI-H1299 cells at 10 uM incubated for 48 hrs by qRT-PCR analysis
AID1240279	Protein binding in dog plasma	2015	Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17	Discovery, design, and synthesis of indole-based EZH2 inhibitors.
AID1331311	Kinetic solubility of compound in PBS buffer at pH 7.4 after 1 hr by micro-plate nephelometric analysis	2017	Bioorganic & medicinal chemistry letters, 01-15, Volume: 27, Issue:2	Novel 3-methylindoline inhibitors of EZH2: Design, synthesis and SAR.
AID1774311	Antiproliferative activity against human SU-DHL-6 cells harboring EZH2 Y641N mutant assessed as inhibition of cell growth measured after 6 days by CellTiter-Glo luminescent assay	2021	Journal of medicinal chemistry, 10-28, Volume: 64, Issue:20	Discovery of IHMT-EZH2-115 as a Potent and Selective Enhancer of Zeste Homolog 2 (EZH2) Inhibitor for the Treatment of B-Cell Lymphomas.
AID1199165	Selectivity ratio of IC50 for MMSET (unknown origin) to IC50 for wild-type human EZH2	2015	Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4	Selective inhibitors of protein methyltransferases.
AID1440581	Terminal half-life in CD-1 mouse at 1 mg/kg, iv or 2 mg/kg, po by LC-MS/MS analysis	2017	Journal of medicinal chemistry, 03-23, Volume: 60, Issue:6	Discovery of First-in-Class, Potent, and Orally Bioavailable Embryonic Ectoderm Development (EED) Inhibitor with Robust Anticancer Efficacy.
AID1240280	Protein binding in human plasma	2015	Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17	Discovery, design, and synthesis of indole-based EZH2 inhibitors.
AID1845919	Reactivation of HIV-1 latency infected in human Th17 cells assessed as increase in HIV production by measuring phosphorylated S175 CDK9 levels at 10 nM incubated for 96 hrs by flow cytometry	2021	European journal of medicinal chemistry, Mar-05, Volume: 213	HIV latency reversal agents: A potential path for functional cure?
AID1816392	PROTAC activity at CRBN E3 ligase/EZH2 in PRC2 complex in human WSUDLCL2 cells assessed as induction of EED degradation at 1 uM incubated for 48 hrs by Western blot analysis
AID1816503	Downregulation of TACC3 mRNA expression in human A549 cells at 10 uM incubated for 48 hrs by qRT-PCR analysis
AID1820236	Antiproliferative activity against human SUDHL2 cells assessed as viable cells at 10 uM by cello meter auto T4 cell counter relative to control	2021	Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14	Design, Synthesis, and Evaluation of VHL-Based EZH2 Degraders to Enhance Therapeutic Activity against Lymphoma.
AID1820281	Toxicity in nude BALB/c mouse xenografted with SU-DHL-6 cells assessed as weight loss at 42.5 mg/kg, ip administered for 6 times weekly for 3 weeks	2021	Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14	Design, Synthesis, and Evaluation of VHL-Based EZH2 Degraders to Enhance Therapeutic Activity against Lymphoma.
AID1774302	Inhibition of EZH2 in human Daudi cells assessed as suppression H3K27 trimethylation measured after 72 hrs by immunoblot analysis	2021	Journal of medicinal chemistry, 10-28, Volume: 64, Issue:20	Discovery of IHMT-EZH2-115 as a Potent and Selective Enhancer of Zeste Homolog 2 (EZH2) Inhibitor for the Treatment of B-Cell Lymphomas.
AID1774312	Antiproliferative activity against human SU-DHL-4 cells harboring EZH2 Y641S mutant assessed as inhibition of cell growth measured after 6 days by CellTiter-Glo luminescent assay	2021	Journal of medicinal chemistry, 10-28, Volume: 64, Issue:20	Discovery of IHMT-EZH2-115 as a Potent and Selective Enhancer of Zeste Homolog 2 (EZH2) Inhibitor for the Treatment of B-Cell Lymphomas.
AID1774301	Inhibition of EZH2 in human Raji cells assessed as suppression H3K27 trimethylation measured after 72 hrs by immunoblot analysis	2021	Journal of medicinal chemistry, 10-28, Volume: 64, Issue:20	Discovery of IHMT-EZH2-115 as a Potent and Selective Enhancer of Zeste Homolog 2 (EZH2) Inhibitor for the Treatment of B-Cell Lymphomas.
AID1199167	Selectivity ratio of IC50 for PRMT1 (unknown origin) to IC50 for wild-type human EZH2	2015	Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4	Selective inhibitors of protein methyltransferases.
AID1774309	Antiproliferative activity against human WSUDLCL2 cells harboring EZH2 Y641F mutant assessed as inhibition of cell growth measured after 6 days by CellTiter-Glo luminescent assay	2021	Journal of medicinal chemistry, 10-28, Volume: 64, Issue:20	Discovery of IHMT-EZH2-115 as a Potent and Selective Enhancer of Zeste Homolog 2 (EZH2) Inhibitor for the Treatment of B-Cell Lymphomas.
AID1868631	Inhibition of PRC2 (unknown origin) assessed as dissociation constant	2022	Journal of medicinal chemistry, 05-26, Volume: 65, Issue:10	Targeting Enhancer of Zeste Homolog 2 for the Treatment of Hematological Malignancies and Solid Tumors: Candidate Structure-Activity Relationships Insights and Evolution Prospects.
AID1440578	Dose normalized unbound AUC in CD-1 mouse at 2 mg/kg, po by LC-MS/MS analysis	2017	Journal of medicinal chemistry, 03-23, Volume: 60, Issue:6	Discovery of First-in-Class, Potent, and Orally Bioavailable Embryonic Ectoderm Development (EED) Inhibitor with Robust Anticancer Efficacy.
AID1240276	Intrinsic clearance in human liver microsomes	2015	Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17	Discovery, design, and synthesis of indole-based EZH2 inhibitors.
AID1816516	Antiproliferative activity against human A549 cells harboring SWI/SNF mutant assessed as inhibition of cell growth at 10 uM treated for 9 days by optical microscopic analysis
AID1816482	PROTAC activity at CRBN E3 ligase/EZH2 in PRC2 complex in human WSUDLCL2 cells assessed as reduction in RbAp48 level at 10 uM measured after 48 hrs by Western blot analysis
AID1774313	Antiproliferative activity against human U2932 cells expressing wild type EZH2 assessed as inhibition of cell growth measured after 6 days by CellTiter-Glo luminescent assay	2021	Journal of medicinal chemistry, 10-28, Volume: 64, Issue:20	Discovery of IHMT-EZH2-115 as a Potent and Selective Enhancer of Zeste Homolog 2 (EZH2) Inhibitor for the Treatment of B-Cell Lymphomas.
AID1774304	Inhibition of EZH2 Y641F mutant in human WSUDLCL2 cells assessed as suppression H3K27 trimethylation measured after 72 hrs by immunoblot analysis	2021	Journal of medicinal chemistry, 10-28, Volume: 64, Issue:20	Discovery of IHMT-EZH2-115 as a Potent and Selective Enhancer of Zeste Homolog 2 (EZH2) Inhibitor for the Treatment of B-Cell Lymphomas.
AID1773630	Inhibition of recombinant PRC2 complex (unknown origin) assessed as association rate constant using H3K27me0 peptide substrate incubated for 3 hrs by HMT assay
AID1860975	Binding affinity to recombinant PRC2 complex (unknown origin) assessed as dissociation rate constant by surface plasmon resonance assay	2022	European journal of medicinal chemistry, Aug-05, Volume: 238	Discovery of precision targeting EZH2 degraders for triple-negative breast cancer.
AID1816498	Downregulation of BRIC5 mRNA expression in human A549 cells at 10 uM incubated for 48 hrs by qRT-PCR analysis
AID1773631	Inhibition of recombinant PRC2 complex (unknown origin) assessed as dissociation rate constant using H3K27me0 peptide substrate incubated for 3 hrs by HMT assay
AID1774308	Antiproliferative activity against human Pfeiffer cells harboring EZH2 A677G mutant assessed as inhibition of cell growth measured after 6 days by CellTiter-Glo luminescent assay	2021	Journal of medicinal chemistry, 10-28, Volume: 64, Issue:20	Discovery of IHMT-EZH2-115 as a Potent and Selective Enhancer of Zeste Homolog 2 (EZH2) Inhibitor for the Treatment of B-Cell Lymphomas.
AID1774306	Inhibition of EZH2 Y641N mutant in human SU-DHL-6 cells assessed as suppression H3K27 trimethylation measured after 72 hrs by immunoblot analysis	2021	Journal of medicinal chemistry, 10-28, Volume: 64, Issue:20	Discovery of IHMT-EZH2-115 as a Potent and Selective Enhancer of Zeste Homolog 2 (EZH2) Inhibitor for the Treatment of B-Cell Lymphomas.
AID1820277	Induction of EZH2 degradation in human SUDHL2 cells assessed as reduction in H3K27me3 level at 0.02 to 1 uM after 24 hrs by Western blot analysis	2021	Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14	Design, Synthesis, and Evaluation of VHL-Based EZH2 Degraders to Enhance Therapeutic Activity against Lymphoma.
AID1816508	Downregulation of TACC3 mRNA expression in human NCI-H1299 cells at 10 uM incubated for 48 hrs by qRT-PCR analysis
AID1860971	Antiproliferative activity against human MV4-11 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	2022	European journal of medicinal chemistry, Aug-05, Volume: 238	Discovery of precision targeting EZH2 degraders for triple-negative breast cancer.
AID1909992	Antiproliferative activity against human ASPC1 cells assessed as cell growth inhibition incubated for 6 days by MTS assay	2022	Journal of medicinal chemistry, 05-12, Volume: 65, Issue:9	Design and Synthesis of Dual EZH2/BRD4 Inhibitors to Target Solid Tumors.
AID1440572	Inhibition of EED in human G401 cells assessed as reduction in global H3K27me3 level after 48 hrs by ELISA	2017	Journal of medicinal chemistry, 03-23, Volume: 60, Issue:6	Discovery of First-in-Class, Potent, and Orally Bioavailable Embryonic Ectoderm Development (EED) Inhibitor with Robust Anticancer Efficacy.
AID1816500	Downregulation of CEP76 mRNA expression in human A549 cells at 10 uM incubated for 48 hrs by qRT-PCR analysis
AID1820238	Antiproliferative activity against human SU-DHL-6 cells assessed as viable cells at 10 uM by cello meter auto T4 cell counter relative to control	2021	Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14	Design, Synthesis, and Evaluation of VHL-Based EZH2 Degraders to Enhance Therapeutic Activity against Lymphoma.
AID1281014	Volume of distribution at steady state in mouse at 2 mg/kg, iv and 10 mg/kg, po by LC-MS/MS analysis	2016	Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4	The Importance of Being Me: Magic Methyls, Methyltransferase Inhibitors, and the Discovery of Tazemetostat.
AID1774305	Inhibition of EZH2 Y641N mutant in human KARPAS-422 cells assessed as suppression H3K27 trimethylation measured after 72 hrs by immunoblot analysis	2021	Journal of medicinal chemistry, 10-28, Volume: 64, Issue:20	Discovery of IHMT-EZH2-115 as a Potent and Selective Enhancer of Zeste Homolog 2 (EZH2) Inhibitor for the Treatment of B-Cell Lymphomas.
AID1868619	Inhibition of EZH2 (unknown origin) assessed as reduction in H3K27me3 level treated for 4 days by cellular assay based Western blot analysis	2022	Journal of medicinal chemistry, 05-26, Volume: 65, Issue:10	Targeting Enhancer of Zeste Homolog 2 for the Treatment of Hematological Malignancies and Solid Tumors: Candidate Structure-Activity Relationships Insights and Evolution Prospects.
AID1816476	PROTAC activity at CRBN E3 ligase/EZH2 in PRC2 complex in human WSUDLCL2 cells assessed as reduction in EZH2 level at 10 uM measured after 48 hrs by Western blot analysis
AID1816510	Downregulation of ARL6IP mRNA expression in human MDA-MB-468 cells at 10 uM incubated for 48 hrs by qRT-PCR analysis
AID1868681	Protac activity at CRBN E3 ligase/EZH2 in human OCILY7 cells assessed as induction of EZH2 degradation	2022	Journal of medicinal chemistry, 05-26, Volume: 65, Issue:10	Targeting Enhancer of Zeste Homolog 2 for the Treatment of Hematological Malignancies and Solid Tumors: Candidate Structure-Activity Relationships Insights and Evolution Prospects.
AID1856993	Inhibition of EZH2 (unknown origin)	2022	Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19	Histone Deacetylase and Enhancer of Zeste Homologue 2 Dual Inhibitors Presenting a Synergistic Effect for the Treatment of Hematological Malignancies.
AID1331316	Oxidative metabolic stability in mouse liver microsomes assessed as amount of parent compound remaining at 1 uM after 30 mins by LC-MS/MS	2017	Bioorganic & medicinal chemistry letters, 01-15, Volume: 27, Issue:2	Novel 3-methylindoline inhibitors of EZH2: Design, synthesis and SAR.
AID1856994	Antiproliferative activity against human HL-60 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	2022	Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19	Histone Deacetylase and Enhancer of Zeste Homologue 2 Dual Inhibitors Presenting a Synergistic Effect for the Treatment of Hematological Malignancies.
AID1816404	Downregulation of CENPK mRNA expression in human NCI-H1299 cells at 10 uM incubated for 48 hrs by qRT-PCR analysis
AID1440575	Protein binding in mouse plasma assessed as unbound fraction	2017	Journal of medicinal chemistry, 03-23, Volume: 60, Issue:6	Discovery of First-in-Class, Potent, and Orally Bioavailable Embryonic Ectoderm Development (EED) Inhibitor with Robust Anticancer Efficacy.
AID1909960	Inhibition of EZH2/BRD4 in human A549 cell lysate assessed as ternary complex formation at 1 uM preincubated for 24 hrs for 30 mins followed by DSP treatment by co-immunoprecipitation method	2022	Journal of medicinal chemistry, 05-12, Volume: 65, Issue:9	Design and Synthesis of Dual EZH2/BRD4 Inhibitors to Target Solid Tumors.
AID1856991	Binding affinity to recombinant PRC2 complex (unknown origin) assessed as association rate constant incubated for 90 seconds by surface plasmon resonance assay	2022	Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19	Histone Deacetylase and Enhancer of Zeste Homologue 2 Dual Inhibitors Presenting a Synergistic Effect for the Treatment of Hematological Malignancies.
AID1856997	Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	2022	Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19	Histone Deacetylase and Enhancer of Zeste Homologue 2 Dual Inhibitors Presenting a Synergistic Effect for the Treatment of Hematological Malignancies.
AID1820262	Induction of apoptosis in human SU-DHL-6 cells at 1 to 5 uM incubated for 48 hrs by Annexin V/propidium iodide staining based flow cytometry	2021	Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14	Design, Synthesis, and Evaluation of VHL-Based EZH2 Degraders to Enhance Therapeutic Activity against Lymphoma.
AID1860965	Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	2022	European journal of medicinal chemistry, Aug-05, Volume: 238	Discovery of precision targeting EZH2 degraders for triple-negative breast cancer.
AID1658430	Antitumor activity against human KARPAS422 cells xenografted in CB-17 SCID mouse assessed as tumor regression at 160 mg/kg, po bid for 23 days and measured three times per week by caliper method	2020	ACS medicinal chemistry letters, Jun-11, Volume: 11, Issue:6	Design, Synthesis, and Pharmacological Evaluation of Second Generation EZH2 Inhibitors with Long Residence Time.
AID1820239	Antiproliferative activity against EZH2 knockdown human SUDHL2 cells assessed as cell growth inhibition measured upto 6 days	2021	Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14	Design, Synthesis, and Evaluation of VHL-Based EZH2 Degraders to Enhance Therapeutic Activity against Lymphoma.
AID1860967	Antiproliferative activity against human BT-549 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	2022	European journal of medicinal chemistry, Aug-05, Volume: 238	Discovery of precision targeting EZH2 degraders for triple-negative breast cancer.
AID1240270	Inhibition of EZH2 (unknown origin) using biotinylated nucleosome, H3K27me3 activator and [3H]-SAM incubated for 60 mins by top-count based method	2015	Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17	Discovery, design, and synthesis of indole-based EZH2 inhibitors.
AID1774300	Inhibition of EZH2 in human U2932 cells assessed as suppression H3K27 trimethylation measured after 72 hrs by immunoblot analysis	2021	Journal of medicinal chemistry, 10-28, Volume: 64, Issue:20	Discovery of IHMT-EZH2-115 as a Potent and Selective Enhancer of Zeste Homolog 2 (EZH2) Inhibitor for the Treatment of B-Cell Lymphomas.
AID1774253	Inhibition of EZH2 (unknown origin) using SAM as substrate incubated for 60 mins by luminescence microplate reader assay	2021	Journal of medicinal chemistry, 10-28, Volume: 64, Issue:20	Discovery of IHMT-EZH2-115 as a Potent and Selective Enhancer of Zeste Homolog 2 (EZH2) Inhibitor for the Treatment of B-Cell Lymphomas.
AID1199168	Selectivity ratio of IC50 for PRMT3 (unknown origin) to IC50 for wild-type human EZH2	2015	Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4	Selective inhibitors of protein methyltransferases.
AID1350282	Toxicity in athymic nude mouse xenografted with human Pfeiffer cells assessed as body weight loss at 10 to 100 mg/kg, po qd administered for 20 days measured twice per week	2018	ACS medicinal chemistry letters, Feb-08, Volume: 9, Issue:2	Discovery of EBI-2511: A Highly Potent and Orally Active EZH2 Inhibitor for the Treatment of Non-Hodgkin's Lymphoma.
AID1816393	PROTAC activity at CRBN E3 ligase/EZH2 in PRC2 complex in human WSUDLCL2 cells assessed as induction of EZH2 degradation at 1 uM incubated for 48 hrs by Western blot analysis
AID1199159	Selectivity ratio of IC50 for EZH1 (unknown origin) to IC50 for wild-type human EZH2	2015	Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4	Selective inhibitors of protein methyltransferases.
AID1816509	Downregulation of BRIC5 mRNA expression in human MDA-MB-468 cells at 10 uM incubated for 48 hrs by qRT-PCR analysis
AID1350244	Inhibition of human N-terminal His-tagged EZH2/flag-tagged EED/SUZ12/AEBP2/RBAP48 A677G mutant (2 to end residues) expressed in baculovirus infected Sf9 insect cells using histone H3 (1 to 50 residues)-GGK as substrate after 2 hrs in presence of SAM by fl	2018	ACS medicinal chemistry letters, Feb-08, Volume: 9, Issue:2	Discovery of EBI-2511: A Highly Potent and Orally Active EZH2 Inhibitor for the Treatment of Non-Hodgkin's Lymphoma.
AID1774310	Antiproliferative activity against human KARPAS-422 cells harboring EZH2 Y641N mutant assessed as inhibition of cell growth measured after 6 days by CellTiter-Glo luminescent assay	2021	Journal of medicinal chemistry, 10-28, Volume: 64, Issue:20	Discovery of IHMT-EZH2-115 as a Potent and Selective Enhancer of Zeste Homolog 2 (EZH2) Inhibitor for the Treatment of B-Cell Lymphomas.
AID1773633	Inhibition of EZH2 (unknown origin) using H3K27me0 peptide substrate incubated for 3 hrs by HMT assay
AID1856996	Antiproliferative activity against human SU-DHL-10 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	2022	Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19	Histone Deacetylase and Enhancer of Zeste Homologue 2 Dual Inhibitors Presenting a Synergistic Effect for the Treatment of Hematological Malignancies.
AID1773625	Antiproliferative activity against human MDA-MB-231 cells assessed as cell viability after 72 hrs by MTT assay
AID1820234	Induction of cell cycle arrest in human SU-DHL-6 cells assessed as accumulation of cells at sub G1 phase at 1 to 5 uM after 24 hrs by flow cytometry	2021	Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14	Design, Synthesis, and Evaluation of VHL-Based EZH2 Degraders to Enhance Therapeutic Activity against Lymphoma.
AID1281015	Oral bioavailability in mouse at 10 mg/kg by LC-MS/MS analysis	2016	Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4	The Importance of Being Me: Magic Methyls, Methyltransferase Inhibitors, and the Discovery of Tazemetostat.
AID1774331	Toxicity in NCG mouse xenografted with human Pfeiffer cells harboring EZH2 A677G mutant assessed as effect on body weight at 200 mg/kg, po BID via gavage measured after 28 days	2021	Journal of medicinal chemistry, 10-28, Volume: 64, Issue:20	Discovery of IHMT-EZH2-115 as a Potent and Selective Enhancer of Zeste Homolog 2 (EZH2) Inhibitor for the Treatment of B-Cell Lymphomas.
AID1816530	Downregulation of CENPK mRNA expression in human MDA-MB-468 cells at 10 uM incubated for 48 hrs by qRT-PCR analysis
AID1774255	Antiproliferative activity against human WSUDLCL2 cells assessed as inhibition of cell growth measured after 6 days by CellTiter-Glo luminescent assay	2021	Journal of medicinal chemistry, 10-28, Volume: 64, Issue:20	Discovery of IHMT-EZH2-115 as a Potent and Selective Enhancer of Zeste Homolog 2 (EZH2) Inhibitor for the Treatment of B-Cell Lymphomas.
AID1240277	Protein binding in mouse plasma	2015	Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17	Discovery, design, and synthesis of indole-based EZH2 inhibitors.
AID1773626	Antiproliferative activity against human MDA-MB-468 cells assessed as cell viability after 72 hrs by MTT assay
AID1199172	Selectivity ratio of IC50 for DOT1L (unknown origin) to IC50 for wild-type human EZH2	2015	Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4	Selective inhibitors of protein methyltransferases.
AID1774303	Inhibition of EZH2 A677G mutant in human Pfeiffer cells assessed as suppression H3K27 trimethylation measured after 72 hrs by immunoblot analysis	2021	Journal of medicinal chemistry, 10-28, Volume: 64, Issue:20	Discovery of IHMT-EZH2-115 as a Potent and Selective Enhancer of Zeste Homolog 2 (EZH2) Inhibitor for the Treatment of B-Cell Lymphomas.
AID1240274	Intrinsic clearance in rat liver microsomes	2015	Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17	Discovery, design, and synthesis of indole-based EZH2 inhibitors.
AID1440579	Plasma clearance in CD-1 mouse at 1 mg/kg, iv or 2 mg/kg, po by LC-MS/MS analysis	2017	Journal of medicinal chemistry, 03-23, Volume: 60, Issue:6	Discovery of First-in-Class, Potent, and Orally Bioavailable Embryonic Ectoderm Development (EED) Inhibitor with Robust Anticancer Efficacy.
AID1856990	Binding affinity to recombinant PRC2 complex (unknown origin) assessed as dissociation rate constant incubated for 90 seconds by surface plasmon resonance assay	2022	Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19	Histone Deacetylase and Enhancer of Zeste Homologue 2 Dual Inhibitors Presenting a Synergistic Effect for the Treatment of Hematological Malignancies.
AID1868615	Inhibition of EZH2 (unknown origin)	2022	Journal of medicinal chemistry, 05-26, Volume: 65, Issue:10	Targeting Enhancer of Zeste Homolog 2 for the Treatment of Hematological Malignancies and Solid Tumors: Candidate Structure-Activity Relationships Insights and Evolution Prospects.
AID1816507	Downregulation of CHEK1 mRNA expression in human NCI-H1299 cells at 10 uM incubated for 48 hrs by qRT-PCR analysis
AID1774326	Antitumor activity against human Pfeiffer cells harboring EZH2 A677G mutant xenografted in NCG mouse assessed as tumor growth inhibition at 200 mg/kg, po BID via gavage measured after 28 days relative to control	2021	Journal of medicinal chemistry, 10-28, Volume: 64, Issue:20	Discovery of IHMT-EZH2-115 as a Potent and Selective Enhancer of Zeste Homolog 2 (EZH2) Inhibitor for the Treatment of B-Cell Lymphomas.
AID1854195	Antiproliferative activity against human K562 cells assessed as inhibition of cell proliferation incubated for 48 hrs by MTT assay	2022	European journal of medicinal chemistry, Aug-05, Volume: 238	Targeting EZH2 for cancer therapy: From current progress to novel strategies.
AID1199158	Inhibition of wild-type human EZH2 by flash plate assay	2015	Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4	Selective inhibitors of protein methyltransferases.
AID1774329	Antitumor activity against human KARPAS-422 cells harboring EZH2 Y641N mutant xenografted in NCG mouse assessed as tumor growth inhibition at 200 mg/kg, po BID via gavage measured after 28 days relative to control	2021	Journal of medicinal chemistry, 10-28, Volume: 64, Issue:20	Discovery of IHMT-EZH2-115 as a Potent and Selective Enhancer of Zeste Homolog 2 (EZH2) Inhibitor for the Treatment of B-Cell Lymphomas.
AID1199164	Selectivity ratio of IC50 for SMYD3 (unknown origin) to IC50 for wild-type human EZH2	2015	Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4	Selective inhibitors of protein methyltransferases.
AID1816502	Downregulation of CHEK1 mRNA expression in human A549 cells at 10 uM incubated for 48 hrs by qRT-PCR analysis
AID1857040	Synergistic antiproliferative activity against human MV4-11 cells assessed as combination index in presence of SAHA incubated for 72 hrs by CCK-8 assay	2022	Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19	Histone Deacetylase and Enhancer of Zeste Homologue 2 Dual Inhibitors Presenting a Synergistic Effect for the Treatment of Hematological Malignancies.
AID1440576	Dose normalized AUC in CD-1 mouse at 1 mg/kg, iv by LC-MS/MS analysis	2017	Journal of medicinal chemistry, 03-23, Volume: 60, Issue:6	Discovery of First-in-Class, Potent, and Orally Bioavailable Embryonic Ectoderm Development (EED) Inhibitor with Robust Anticancer Efficacy.
AID1856992	Binding affinity to recombinant PRC2 complex (unknown origin) incubated for 90 seconds by surface plasmon resonance assay	2022	Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19	Histone Deacetylase and Enhancer of Zeste Homologue 2 Dual Inhibitors Presenting a Synergistic Effect for the Treatment of Hematological Malignancies.
AID1816513	Downregulation of TACC3 mRNA expression in human MDA-MB-468 cells at 10 uM incubated for 48 hrs by qRT-PCR analysis
AID1774315	Antiproliferative activity against human Daudi cells expressing wild type EZH2 assessed as inhibition of cell growth measured after 6 days by CellTiter-Glo luminescent assay	2021	Journal of medicinal chemistry, 10-28, Volume: 64, Issue:20	Discovery of IHMT-EZH2-115 as a Potent and Selective Enhancer of Zeste Homolog 2 (EZH2) Inhibitor for the Treatment of B-Cell Lymphomas.
AID1857041	Synergistic antiproliferative activity against human SU-DHL-10 cells assessed as combination index in presence of SAHA incubated for 72 hrs by CCK-8 assay	2022	Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19	Histone Deacetylase and Enhancer of Zeste Homologue 2 Dual Inhibitors Presenting a Synergistic Effect for the Treatment of Hematological Malignancies.
AID1440577	Dose normalized AUC in CD-1 mouse at 2 mg/kg, po by LC-MS/MS analysis	2017	Journal of medicinal chemistry, 03-23, Volume: 60, Issue:6	Discovery of First-in-Class, Potent, and Orally Bioavailable Embryonic Ectoderm Development (EED) Inhibitor with Robust Anticancer Efficacy.
AID1440574	Hepatic extraction ratio in mouse liver microsomes	2017	Journal of medicinal chemistry, 03-23, Volume: 60, Issue:6	Discovery of First-in-Class, Potent, and Orally Bioavailable Embryonic Ectoderm Development (EED) Inhibitor with Robust Anticancer Efficacy.
AID1845920	Reactivation of HIV-1 latency infected in human Th17 cells assessed as increase in HIV production by measuring phosphorylated S175 CDK9 levels at 1 uM incubated for 96 hrs by flow cytometry	2021	European journal of medicinal chemistry, Mar-05, Volume: 213	HIV latency reversal agents: A potential path for functional cure?
AID1816506	Downregulation of CEP76 mRNA expression in human NCI-H1299 cells at 10 uM incubated for 48 hrs by qRT-PCR analysis
AID1199166	Selectivity ratio of IC50 for WHSC1L1 (unknown origin) to IC50 for wild-type human EZH2	2015	Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4	Selective inhibitors of protein methyltransferases.
AID1820237	Antiproliferative activity against human SU-DHL-4 cells assessed as viable cells at 10 uM by cello meter auto T4 cell counter relative to control	2021	Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14	Design, Synthesis, and Evaluation of VHL-Based EZH2 Degraders to Enhance Therapeutic Activity against Lymphoma.
AID1240273	Intrinsic clearance in mouse liver microsomes	2015	Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17	Discovery, design, and synthesis of indole-based EZH2 inhibitors.
AID1296008	Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening	2020	SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1	Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347159	Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay	2020	Proceedings 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.
AID1346986	P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen	2019	Molecular pharmacology, 11, Volume: 96, Issue:5	A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346987	P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen	2019	Molecular pharmacology, 11, Volume: 96, Issue:5	A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347160	Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors	2020	Proceedings 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.
AID1347411	qHTS 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) Libary	2020	ACS 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.
AID1346024	Human enhancer of zeste 2 polycomb repressive complex 2 subunit (2.1.1.43 Histone methyltransferases (HMTs))	2013	Proceedings of the National Academy of Sciences of the United States of America, May-07, Volume: 110, Issue:19	Durable tumor regression in genetically altered malignant rhabdoid tumors by inhibition of methyltransferase EZH2.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	0 (0.00)	18.2507
2000's	0 (0.00)	29.6817
2010's	35 (31.25)	24.3611
2020's	77 (68.75)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Publication Type	This drug (%)	All Drugs (%)
Trials	8 (7.08%)	5.53%
Reviews	16 (14.16%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	89 (78.76%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Trials	Classes	Roles
valproic acid Valproic Acid: A fatty acid with anticonvulsant and anti-manic properties that is used in the treatment of EPILEPSY and BIPOLAR DISORDER. The mechanisms of its therapeutic actions are not well understood. It may act by increasing GAMMA-AMINOBUTYRIC ACID levels in the brain or by altering the properties of VOLTAGE-GATED SODIUM CHANNELS.. valproic acid : A branched-chain saturated fatty acid that comprises of a propyl substituent on a pentanoic acid stem.	2.31	1	0	branched-chain fatty acid; branched-chain saturated fatty acid	anticonvulsant; antimanic drug; EC 3.5.1.98 (histone deacetylase) inhibitor; GABA agent; neuroprotective agent; psychotropic drug; teratogenic agent
fluorouracil Fluorouracil: A pyrimidine analog that is an antineoplastic antimetabolite. It interferes with DNA synthesis by blocking the THYMIDYLATE SYNTHETASE conversion of deoxyuridylic acid to thymidylic acid.. 5-fluorouracil : A nucleobase analogue that is uracil in which the hydrogen at position 5 is replaced by fluorine. It is an antineoplastic agent which acts as an antimetabolite - following conversion to the active deoxynucleotide, it inhibits DNA synthesis (by blocking the conversion of deoxyuridylic acid to thymidylic acid by the cellular enzyme thymidylate synthetase) and so slows tumour growth.	2.25	1	0	nucleobase analogue; organofluorine compound	antimetabolite; antineoplastic agent; environmental contaminant; immunosuppressive agent; radiosensitizing agent; xenobiotic
4-(dimethylamino)-n-(7-(hydroxyamino)-7-oxoheptyl)benzamide 4-(dimethylamino)-N-(7-(hydroxyamino)-7-oxoheptyl)benzamide: structure in first source. 4-(dimethylamino)-N-[7-(hydroxyamino)-7-oxoheptyl]benzamide : A benzamide resulting from the formal condensation of the carboxy group of 4-(dimethylamino)benzoic acid with the amino group of 7-amino-N-hydroxyheptanamide. It is a potent inhibitor of histone deacetylases and induces cell cycle arrest and apoptosis in several human cancer cell lines.	3.41	1	0	benzamides; hydroxamic acid; secondary carboxamide; tertiary amino compound	antineoplastic agent; apoptosis inducer; EC 3.5.1.98 (histone deacetylase) inhibitor
pyrimethamine Maloprim: contains above 2 cpds	2.25	1	0	aminopyrimidine; monochlorobenzenes	antimalarial; antiprotozoal drug; EC 1.5.1.3 (dihydrofolate reductase) inhibitor
vorinostat Vorinostat: A hydroxamic acid and anilide derivative that acts as a HISTONE DEACETYLASE inhibitor. It is used in the treatment of CUTANEOUS T-CELL LYMPHOMA and SEZARY SYNDROME.. vorinostat : A dicarboxylic acid diamide comprising suberic (octanedioic) acid coupled to aniline and hydroxylamine. A histone deacetylase inhibitor, it is marketed under the name Zolinza for the treatment of cutaneous T cell lymphoma (CTCL).	9.13	3	0	dicarboxylic acid diamide; hydroxamic acid	antineoplastic agent; apoptosis inducer; EC 3.5.1.98 (histone deacetylase) inhibitor
thalidomide Thalidomide: A piperidinyl isoindole originally introduced as a non-barbiturate hypnotic, but withdrawn from the market due to teratogenic effects. It has been reintroduced and used for a number of immunological and inflammatory disorders. Thalidomide displays immunosuppressive and anti-angiogenic activity. It inhibits release of TUMOR NECROSIS FACTOR-ALPHA from monocytes, and modulates other cytokine action.. thalidomide : A racemate comprising equimolar amounts of R- and S-thalidomide.. 2-(2,6-dioxopiperidin-3-yl)-1H-isoindole-1,3(2H)-dione : A dicarboximide that is isoindole-1,3(2H)-dione in which the hydrogen attached to the nitrogen is substituted by a 2,6-dioxopiperidin-3-yl group.	2.17	1	0	phthalimides; piperidones
prednisolone Prednisolone: A glucocorticoid with the general properties of the corticosteroids. It is the drug of choice for all conditions in which routine systemic corticosteroid therapy is indicated, except adrenal deficiency states.. prednisolone : A glucocorticoid that is prednisone in which the oxo group at position 11 has been reduced to the corresponding beta-hydroxy group. It is a drug metabolite of prednisone.	2.1	1	0	11beta-hydroxy steroid; 17alpha-hydroxy steroid; 20-oxo steroid; 21-hydroxy steroid; 3-oxo-Delta(1),Delta(4)-steroid; C21-steroid; glucocorticoid; primary alpha-hydroxy ketone; tertiary alpha-hydroxy ketone	adrenergic agent; anti-inflammatory drug; antineoplastic agent; drug metabolite; environmental contaminant; immunosuppressive agent; xenobiotic
prednisone Prednisone: A synthetic anti-inflammatory glucocorticoid derived from CORTISONE. It is biologically inert and converted to PREDNISOLONE in the liver.. prednisone : A synthetic glucocorticoid drug that is particularly effective as an immunosuppressant, and affects virtually all of the immune system. Prednisone is a prodrug that is converted by the liver into prednisolone (a beta-hydroxy group instead of the oxo group at position 11), which is the active drug and also a steroid.	7.03	4	1	11-oxo steroid; 17alpha-hydroxy steroid; 20-oxo steroid; 21-hydroxy steroid; 3-oxo-Delta(1),Delta(4)-steroid; C21-steroid; glucocorticoid; primary alpha-hydroxy ketone; tertiary alpha-hydroxy ketone	adrenergic agent; anti-inflammatory drug; antineoplastic agent; immunosuppressive agent; prodrug
lysine Lysine: An essential amino acid. It is often added to animal feed.. lysine : A diamino acid that is caproic (hexanoic) acid bearing two amino substituents at positions 2 and 6.. L-lysine : An L-alpha-amino acid; the L-isomer of lysine.	2.6	1	0	aspartate family amino acid; L-alpha-amino acid zwitterion; L-alpha-amino acid; lysine; organic molecular entity; proteinogenic amino acid	algal metabolite; anticonvulsant; Escherichia coli metabolite; human metabolite; micronutrient; mouse metabolite; nutraceutical; plant metabolite; Saccharomyces cerevisiae metabolite
quinazolines Quinazolines: A group of aromatic heterocyclic compounds that contain a bicyclic structure with two fused six-membered aromatic rings, a benzene ring and a pyrimidine ring.. quinazoline : A mancude organic heterobicyclic parent that is naphthalene in which the carbon atoms at positions 1 and 3 have been replaced by nitrogen atoms.. quinazolines : Any organic heterobicyclic compound based on a quinazoline skeleton and its substituted derivatives.	3.92	2	0	azaarene; mancude organic heterobicyclic parent; ortho-fused heteroarene; quinazolines
acridines Acridines: Compounds that include the structure of acridine.. acridine : A polycyclic heteroarene that is anthracene in which one of the central CH groups is replaced by a nitrogen atom.	2.25	1	0	acridines; mancude organic heterotricyclic parent; polycyclic heteroarene	genotoxin
indazoles Indazoles: A group of heterocyclic aromatic organic compounds consisting of the fusion of BENZENE and PYRAZOLES.	3.92	3	0	indazole
hydrazine diamine : Any polyamine that contains two amino groups.	2.17	1	0	azane; hydrazines	EC 4.3.1.10 (serine-sulfate ammonia-lyase) inhibitor
azacitidine Azacitidine: A pyrimidine analogue that inhibits DNA methyltransferase, impairing DNA methylation. It is also an antimetabolite of cytidine, incorporated primarily into RNA. Azacytidine has been used as an antineoplastic agent.. 5-azacytidine : An N-glycosyl-1,3,5-triazine that is 4-amino-1,3,5-triazin-2(1H)-one substituted by a beta-D-ribofuranosyl residue via an N-glycosidic linkage. An antineoplastic agent, it is used in the treatment of myeloid leukaemia.	3.73	2	0	N-glycosyl-1,3,5-triazine; nucleoside analogue	antineoplastic agent
plumbagin plumbagin: a superoxide anion generator. plumbagin : A hydroxy-1,4-naphthoquinone that is 1,4-naphthoquinone in which the hydrogens at positions 2 and 5 are substituted by methyl and hydroxy groups, respectively.	2.41	1	0	hydroxy-1,4-naphthoquinone; phenols	anticoagulant; antineoplastic agent; immunological adjuvant; metabolite
platinum Platinum: A heavy, soft, whitish metal, resembling tin, with atomic number 78, atomic weight 195.084, symbol Pt. It is used in manufacturing equipment for laboratory and industrial use. It occurs as a black powder (platinum black) and as a spongy substance (spongy platinum) and may have been known in Pliny's time as alutiae.	2.25	1	0	elemental platinum; nickel group element atom; platinum group metal atom
etoposide [no description available]	3.31	1	0	beta-D-glucoside; furonaphthodioxole; organic heterotetracyclic compound	antineoplastic agent; DNA synthesis inhibitor
irinotecan [no description available]	2.31	1	0	carbamate ester; delta-lactone; N-acylpiperidine; pyranoindolizinoquinoline; ring assembly; tertiary alcohol; tertiary amino compound	antineoplastic agent; apoptosis inducer; EC 5.99.1.2 (DNA topoisomerase) inhibitor; prodrug
adenosine quinquefolan B: isolated from roots of Panax quinquefolium L.; RN not in Chemline 10/87; RN from Toxlit	4.03	3	0	adenosines; purines D-ribonucleoside	analgesic; anti-arrhythmia drug; fundamental metabolite; human metabolite; vasodilator agent
triazoles Triazoles: Heterocyclic compounds containing a five-membered ring with two carbon atoms and three nitrogen atoms with the molecular formula C2H3N3.. triazoles : An azole in which the five-membered heterocyclic aromatic skeleton contains three N atoms and two C atoms.	2.25	1	0	1,2,3-triazole
3-deazaneplanocin 3-deazaneplanocin: S-adenosylhomocysteine hydrolase antagonist	4.79	4	0
bendamustine hydrochloride [no description available]	3.51	1	0
indolactam v indolactam V: only the (-)-isomer of indolactam V showed carcinogenic activity; structure given in first source	3.41	1	0	indoles
pterosin b pterosin B: structure in first source	2.25	1	0
pomalidomide 3-aminophthalimidoglutarimide: structure in first source	2.17	1	0	aromatic amine; dicarboximide; isoindoles; piperidones	angiogenesis inhibitor; antineoplastic agent; immunomodulator
lenalidomide [no description available]	4.76	4	0	aromatic amine; dicarboximide; isoindoles; piperidones	angiogenesis inhibitor; antineoplastic agent; immunomodulator
nsc 663284 NSC 663284: structure in first source	2.11	1	0	quinolone
s-adenosylhomocysteine S-Adenosylhomocysteine: 5'-S-(3-Amino-3-carboxypropyl)-5'-thioadenosine. Formed from S-adenosylmethionine after transmethylation reactions.. S-adenosyl-L-homocysteine : An organic sulfide that is the S-adenosyl derivative of L-homocysteine.	2.13	1	0	adenosines; amino acid zwitterion; homocysteine derivative; homocysteines; organic sulfide	cofactor; EC 2.1.1.72 [site-specific DNA-methyltransferase (adenine-specific)] inhibitor; EC 2.1.1.79 (cyclopropane-fatty-acyl-phospholipid synthase) inhibitor; epitope; fundamental metabolite
trichostatin a trichostatin A: chelates zinc ion in the active site of histone deacetylases, resulting in preventing histone unpacking so DNA is less available for transcription; do not confuse with TRICHOSANTHIN which is a protein; found in STREPTOMYCES	3.41	1	0	antibiotic antifungal agent; hydroxamic acid; trichostatin	bacterial metabolite; EC 3.5.1.98 (histone deacetylase) inhibitor; geroprotector
decitabine [no description available]	7.21	1	0	2'-deoxyribonucleoside
12-deoxyphorbol 13-acetate [no description available]	3.41	1	0	phorbol ester	metabolite
thioacetamide Thioacetamide: A crystalline compound used as a laboratory reagent in place of HYDROGEN SULFIDE. It is a potent hepatocarcinogen.. thioacetamide : A thiocarboxamide consiting of acetamide having the oxygen replaced by sulfur.	2.31	1	0	thiocarboxamide	hepatotoxic agent
oxalylglycine oxalylglycine: structure given in first source. N-oxalylglycine : An amino dicarboxylic acid that is iminodiacetic acid with an oxo substituent. It is used as an inhibitor of alpha-ketoglutarate dependent (EC 1.14.11.*) enzymes.	2.25	1	0	amino dicarboxylic acid; N-acylglycine	EC 1.14.11.* (oxidoreductase acting on paired donors, 2-oxoglutarate as one donor, incorporating 1 atom each of oxygen into both donors) inhibitor
naphthoquinones Naphthoquinones: Naphthalene rings which contain two ketone moieties in any position. They can be substituted in any position except at the ketone groups.	2.41	1	0
wedelolactone wedelolactone: antihepatotoxic coumestan from Eclipta prostrata and Wedelia calendulacea (both Asteraceae); structure given in first source. wedelolactone : A member of the class of coumestans that is coumestan with hydroxy substituents as positions 1, 8 and 9 and a methoxy substituent at position 3.	4.33	2	0	aromatic ether; coumestans; delta-lactone; polyphenol	antineoplastic agent; apoptosis inducer; EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor; hepatoprotective agent; metabolite
ellagic acid [no description available]	2.11	1	0	catechols; cyclic ketone; lactone; organic heterotetracyclic compound; polyphenol	antioxidant; EC 1.14.18.1 (tyrosinase) inhibitor; EC 2.3.1.5 (arylamine N-acetyltransferase) inhibitor; EC 2.4.1.1 (glycogen phosphorylase) inhibitor; EC 2.5.1.18 (glutathione transferase) inhibitor; EC 2.7.1.127 (inositol-trisphosphate 3-kinase) inhibitor; EC 2.7.1.151 (inositol-polyphosphate multikinase) inhibitor; EC 2.7.4.6 (nucleoside-diphosphate kinase) inhibitor; EC 2.7.7.7 (DNA-directed DNA polymerase) inhibitor; EC 5.99.1.2 (DNA topoisomerase) inhibitor; EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor; food additive; fungal metabolite; geroprotector; plant metabolite; skin lightening agent
brefeldin a [no description available]	2.31	1	0	macrolide antibiotic	Penicillium metabolite
su 11248 [no description available]	2.6	1	0	monocarboxylic acid amide; pyrroles	angiogenesis inhibitor; antineoplastic agent; EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor; immunomodulator; neuroprotective agent; vascular endothelial growth factor receptor antagonist
ganglioside, gd2 [no description available]	2.66	2	0
bvt.948 [no description available]	2.11	1	0
belinostat [no description available]	3.41	1	0	hydroxamic acid; olefinic compound; sulfonamide	antineoplastic agent; EC 3.5.1.98 (histone deacetylase) inhibitor
panobinostat Panobinostat: An indole and hydroxamic acid derivative that acts as a HISTONE DEACETYLASE inhibitor. It is used as an antineoplastic agent in combination with BORTEZOMIB and DEXAMETHASONE for the treatment of MULTIPLE MYELOMA.. panobinostat : A hydroxamic acid obtained by formal condensation of the carboxy group of (2E)-3-[4-({[2-(2-methylindol-3-yl)ethyl]amino}methyl)phenyl]prop-2-enoic acid with the amino group of hydroxylamine. A histone deacetylase inhibitor used (as its lactate salt) in combination with bortezomib and dexamethasone for the treatment of multiple myeloma.	3.41	1	0	cinnamamides; hydroxamic acid; methylindole; secondary amino compound	angiogenesis modulating agent; antineoplastic agent; EC 3.5.1.98 (histone deacetylase) inhibitor
n-(2-amino-5-fluorobenzyl)-4-(n-(pyridine-3-acrylyl)aminomethyl)benzamide [no description available]	3.41	1	0
azd 6244 AZD 6244: a MEK inhibitor	2.25	1	0	benzimidazoles; bromobenzenes; hydroxamic acid ester; monochlorobenzenes; organofluorine compound; secondary amino compound	anticoronaviral agent; antineoplastic agent; EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor
cl 075 [no description available]	3.41	1	0
regorafenib [no description available]	2.25	1	0	(trifluoromethyl)benzenes; aromatic ether; monochlorobenzenes; monofluorobenzenes; phenylureas; pyridinecarboxamide	antineoplastic agent; hepatotoxic agent; tyrosine kinase inhibitor
bi 2536 [no description available]	3.41	1	0
danusertib [no description available]	2.15	1	0	piperazines
idelalisib idelalisib: an antineoplastic agent and p110delta inhibitor; structure in first source. idelalisib : A member of the class of quinazolines that is 5-fluoro-3-phenylquinazolin-4-one in which the hydrogen at position 2 is replaced by a (1S)-1-(3H-purin-6-ylamino)propyl group. used for for the treatment of refractory indolent non-Hodgkin's lymphoma and relapsed chronic lymphocytic leukemia.	3.51	1	0	aromatic amine; organofluorine compound; purines; quinazolines; secondary amino compound	antineoplastic agent; apoptosis inducer; EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor
olaparib [no description available]	3.51	1	0	cyclopropanes; monofluorobenzenes; N-acylpiperazine; phthalazines	antineoplastic agent; apoptosis inducer; EC 2.4.2.30 (NAD(+) ADP-ribosyltransferase) inhibitor
az 505 AZ 505: an SMYD2 inhibitor; structure in first source	3.68	2	0
bix 01294 [no description available]	4.52	3	0	piperidines
dabrafenib [no description available]	2.25	1	0	1,3-thiazoles; aminopyrimidine; organofluorine compound; sulfonamide	anticoronaviral agent; antineoplastic agent; B-Raf inhibitor
unc 0638 UNC 0638: inhibits lysine methyltransferases G9a and GLP; structure in first source	3.41	1	0	quinazolines
jq1 compound [no description available]	3.86	2	0	carboxylic ester; organochlorine compound; tert-butyl ester; thienotriazolodiazepine	angiogenesis inhibitor; anti-inflammatory agent; antineoplastic agent; apoptosis inducer; bromodomain-containing protein 4 inhibitor; cardioprotective agent; ferroptosis inducer
dinaciclib [no description available]	2.21	1	0	pyrazolopyrimidine
abt-199 venetoclax: A BCL-2 inhibitor with antineoplastic activity that is used in the treatment of CHRONIC LYMPHOCYTIC LEUKEMIA associated with chromosome 17p deletion; structure in first source.. venetoclax : A member of the class of pyrrolopyridines that is a potent inhibitor of the antiapoptotic protein B-cell lymphoma 2. It is used for treamtment of chronic lymphocytic leukemia with 17p deletion.	3.51	1	0	aromatic ether; C-nitro compound; monochlorobenzenes; N-alkylpiperazine; N-arylpiperazine; N-sulfonylcarboxamide; oxanes; pyrrolopyridine	antineoplastic agent; apoptosis inducer; B-cell lymphoma 2 inhibitor
ipi-145 [no description available]	3.51	1	0	isoquinolines
epz004777 [no description available]	2.11	1	0	N-glycosyl compound
epz-5676 [no description available]	3.62	2	0	5'-deoxyribonucleoside
epz005687 EPZ005687: inhibits EZH2 protein; structure in first source	5.76	7	0	indazoles
gsk-2816126 GSK-2816126: inhibits EZH2 methyltransferase; structure in first source	6.58	17	0	piperazines; pyridines
gsk343 GSK343: an EZH2 methyltransferase inhibitor. GSK343 : A member of the class of indazoles that is 1-isopropyl-1H-indazole-4-carboxamide in which the nitrogen of the carboxamide group is substituted by a (6-methyl-2-oxo-4-propyl-1,2-dihydropyridin-3-yl)methyl group and in which the indazole ring is substituted at position 6 by a 2-(4-methylpiperazin-1-yl)pyridin-4-yl group. A highly potent and selective EZH2 inhibitor (IC50 = 4 nM).	4.68	4	0	aminopyridine; indazoles; N-alkylpiperazine; N-arylpiperazine; pyridone; secondary carboxamide	antineoplastic agent; apoptosis inducer; EC 2.1.1.43 (enhancer of zeste homolog 2) inhibitor
2-methoxy-n-(3-methyl-2-oxo-1,2,3,4-tetrahydroquinazolin-6-yl)benzenesulfonamide 2-methoxy-N-(3-methyl-2-oxo-1,2,3,4-tetrahydroquinazolin-6-yl)benzenesulfonamide: a probe for bromo and extra C-terminal domain proteins; structure in first source	3.41	1	0	quinazolines
(r)-pfi-2 (R)-PFI-2: a potent and selective inhibitor of SETD7 methyltransferase; structure in first source	2.11	1	0
1-[(1R)-1-(1-ethylsulfonyl-4-piperidinyl)ethyl]-N-[(4-methoxy-6-methyl-2-oxo-1H-pyridin-3-yl)methyl]-2-methyl-3-indolecarboxamide (R)-1-(1-(1-(ethylsulfonyl)piperidin-4-yl)ethyl)-N-((4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1H-indole-3-carboxamide: EZH2 inhibitor	2.11	1	0	indolecarboxamide
gsk-j4 GSK-J4: a JMJD3 inhibitor; structure in first source	2.25	1	0	organonitrogen heterocyclic compound
onc201 TIC10 compound: a TRAIL-dependent antitumor agent; structure in first source	7.31	1	0
lly-507 LLY-507: inhibits methyltransferase SMYD2; structure in first source. LLY-507 : A secondary carboxamide resulting from the formal condensation of the carboxy group of 5-cyano-2'-{4-[2-(3-methyl-1H-indol-1-yl)ethyl]piperazin-1-yl}[biphenyl]-3-carboxylic acid with the amino group of 3-(pyrrolidin-1-yl)propan-1-amine. It is a potent and selective inhibitor of SMYD2 and inhibits the ability of SMYD2 to methylate p53. It serves as a valuable chemical probe to aid in the dissection of SMYD2 function in cancer and other biological processes.	2.11	1	0
orabase Orabase: used in therapy of oral mucosal ulcers	2.41	1	0
rvx 208 apabetalone: a bromodomain and extra-terminal domain protein (BET) inhibitor; prevents interactions between BET proteins and acetyl-lysine residues on histone tails to modify epigenetic regulation	3.41	1	0
bay 80-6946 copanlisib: an antineoplastic agent with PI3K inhibitory activity; structure in first source. copanlisib : An imidazoquinazoline that is 2,3-dihydroimidazo[1,2-c]quinazoline substituted by (2-aminopyrimidine-5-carbonyl)amino, methoxy, and 3-(morpholin-4-yl)propoxy groups at positions 5, 7 and 8, respectively. It is a intravenous pan-class I PI3K inhibitor used for the treatment of relapsed follicular lymphoma in patients who have received at least 2 prior systemic therapies.	3.92	2	0
sp2509 SP2509: inhibits histone demethylase LSD1; SP2513 is the pharmacologically inactive enantiomer; structure in first source	2.17	1	0

Condition	Indicated	Relationship Strength	Studies	Trials
Benign Neoplasms [description not available]	0	6.76	15	0
Neoplasms New abnormal growth of tissue. Malignant neoplasms show a greater degree of anaplasia and have the properties of invasion and metastasis, compared to benign neoplasms.	1	8.76	15	0
Rhabdoid Tumor A rare but highly lethal childhood tumor found almost exclusively in infants. Histopathologically, it resembles RHABDOMYOSARCOMA but the tumor cells are not of myogenic origin. Although it arises primarily in the kidney, it may be found in other parts of the body. The rhabdoid cytomorphology is believed to be the expression of a very primitive malignant cell. (From Holland et al., Cancer Medicine, 3d ed, p2210)	0	2.58	2	0
Diffuse Large B-Cell Lymphoma [description not available]	0	13.84	8	3
Lymphoma, Large B-Cell, Diffuse Malignant lymphoma composed of large B lymphoid cells whose nuclear size can exceed normal macrophage nuclei, or more than twice the size of a normal lymphocyte. The pattern is predominantly diffuse. Most of these lymphomas represent the malignant counterpart of B-lymphocytes at midstage in the process of differentiation.	1	10.84	8	3
Congenital Zika Syndrome [description not available]	0	2.25	1	0
Disease Models, Animal Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.	0	3.94	10	0
Zika Virus Infection A viral disease transmitted by the bite of AEDES mosquitoes infected with ZIKA VIRUS. Its mild DENGUE-like symptoms include fever, rash, headaches and ARTHRALGIA. The viral infection during pregnancy, in rare cases, is associated with congenital brain and ocular abnormalities, called Congenital Zika Syndrome, including MICROCEPHALY and may also lead to GUILLAIN-BARRE SYNDROME.	0	2.25	1	0
HIV Coinfection [description not available]	0	3.23	1	0
HIV Infections Includes the spectrum of human immunodeficiency virus infections that range from asymptomatic seropositivity, thru AIDS-related complex (ARC), to acquired immunodeficiency syndrome (AIDS).	0	3.23	1	0
Germinoblastoma [description not available]	0	2.31	1	0
Lymphoma A general term for various neoplastic diseases of the lymphoid tissue.	1	4.31	1	0
Experimental Neoplasms [description not available]	0	2.61	2	0
B-Cell Lymphoma [description not available]	0	6.25	5	2
Lymphoma, B-Cell A group of heterogeneous lymphoid tumors generally expressing one or more B-cell antigens or representing malignant transformations of B-lymphocytes.	0	6.25	5	2
Hematologic Malignancies [description not available]	0	3.95	3	0
Hematologic Neoplasms Neoplasms located in the blood and blood-forming tissue (the bone marrow and lymphatic tissue). The commonest forms are the various types of LEUKEMIA, of LYMPHOMA, and of the progressive, life-threatening forms of the MYELODYSPLASTIC SYNDROMES.	0	3.95	3	0
ER-Negative PR-Negative HER2-Negative Breast Cancer [description not available]	0	2.69	2	0
Triple Negative Breast Neoplasms Breast neoplasms that do not express ESTROGEN RECEPTORS; PROGESTERONE RECEPTORS; and do not overexpress the NEU RECEPTOR/HER-2 PROTO-ONCOGENE PROTEIN.	0	2.69	2	0
Cancer of Lung [description not available]	0	3.07	3	0
Lung Neoplasms Tumors or cancer of the LUNG.	0	3.07	3	0
Benign Neoplasms, Brain [description not available]	0	3.11	4	0
Brain Neoplasms Neoplasms of the intracranial components of the central nervous system, including the cerebral hemispheres, basal ganglia, hypothalamus, thalamus, brain stem, and cerebellum. Brain neoplasms are subdivided into primary (originating from brain tissue) and secondary (i.e., metastatic) forms. Primary neoplasms are subdivided into benign and malignant forms. In general, brain tumors may also be classified by age of onset, histologic type, or presenting location in the brain.	0	3.11	4	0
Brill-Symmers Disease [description not available]	0	9.33	12	3
Lymphoma, Follicular Malignant lymphoma in which the lymphomatous cells are clustered into identifiable nodules within the LYMPH NODES. The nodules resemble to some extent the GERMINAL CENTER of lymph node follicles and most likely represent neoplastic proliferation of lymph node-derived follicular center B-LYMPHOCYTES.	1	13.72	24	6
Diffuse Mixed Small and Large Cell Lymphoma [description not available]	0	5.14	3	1
Lymphoma, Non-Hodgkin Any of a group of malignant tumors of lymphoid tissue that differ from HODGKIN DISEASE, being more heterogeneous with respect to malignant cell lineage, clinical course, prognosis, and therapy. The only common feature among these tumors is the absence of giant REED-STERNBERG CELLS, a characteristic of Hodgkin's disease.	1	7.14	3	1
Local Neoplasm Recurrence [description not available]	0	8.23	9	2
Malignant Mesothelioma [description not available]	0	2.41	1	0
Neoplasms, Pleural [description not available]	0	2.41	1	0
Mesothelioma A tumor derived from mesothelial tissue (peritoneum, pleura, pericardium). It appears as broad sheets of cells, with some regions containing spindle-shaped, sarcoma-like cells and other regions showing adenomatous patterns. Pleural mesotheliomas have been linked to exposure to asbestos. (Dorland, 27th ed)	1	4.76	2	0
Cancer of Paranasal Sinus [description not available]	0	2.41	1	0
Paranasal Sinus Neoplasms Tumors or cancer of the PARANASAL SINUSES.	0	2.41	1	0
Cancer of Ovary [description not available]	0	2.66	2	0
Ovarian Neoplasms Tumors or cancer of the OVARY. These neoplasms can be benign or malignant. They are classified according to the tissue of origin, such as the surface EPITHELIUM, the stromal endocrine cells, and the totipotent GERM CELLS.	0	2.66	2	0
Adenocarcinoma Of Kidney [description not available]	0	2.6	1	0
Cancer of Kidney [description not available]	0	2.6	1	0
Carcinoma, Renal Cell A heterogeneous group of sporadic or hereditary carcinoma derived from cells of the KIDNEYS. There are several subtypes including the clear cells, the papillary, the chromophobe, the collecting duct, the spindle cells (sarcomatoid), or mixed cell-type carcinoma.	0	2.6	1	0
Kidney Neoplasms Tumors or cancers of the KIDNEY.	0	2.6	1	0
Carcinoma, Squamous Cell of Head and Neck [description not available]	0	2.6	1	0
Cancer of Head [description not available]	0	2.76	2	0
Squamous Cell Carcinoma of Head and Neck The most common type of head and neck carcinoma that originates from cells on the surface of the NASAL CAVITY; MOUTH; PARANASAL SINUSES, SALIVARY GLANDS, and LARYNX. Mutations in TNFRSF10B, PTEN, and ING1 genes are associated with this cancer.	0	2.6	1	0
Head and Neck Neoplasms Soft tissue tumors or cancer arising from the mucosal surfaces of the LIP; oral cavity; PHARYNX; LARYNX; and cervical esophagus. Other sites included are the NOSE and PARANASAL SINUSES; SALIVARY GLANDS; THYROID GLAND and PARATHYROID GLANDS; and MELANOMA and non-melanoma skin cancers of the head and neck. (from Holland et al., Cancer Medicine, 4th ed, p1651)	0	2.76	2	0
Acute Brain Injuries [description not available]	0	2.6	1	0
Infarct [description not available]	0	2.6	1	0
Brain Injuries Acute and chronic (see also BRAIN INJURIES, CHRONIC) injuries to the brain, including the cerebral hemispheres, CEREBELLUM, and BRAIN STEM. Clinical manifestations depend on the nature of injury. Diffuse trauma to the brain is frequently associated with DIFFUSE AXONAL INJURY or COMA, POST-TRAUMATIC. Localized injuries may be associated with NEUROBEHAVIORAL MANIFESTATIONS; HEMIPARESIS, or other focal neurologic deficits.	0	2.6	1	0
Cancer of Esophagus [description not available]	0	2.6	1	0
Esophageal Neoplasms Tumors or cancer of the ESOPHAGUS.	0	2.6	1	0
Carcinoma, Anaplastic [description not available]	0	3.01	2	0
Carcinoma A malignant neoplasm made up of epithelial cells tending to infiltrate the surrounding tissues and give rise to metastases. It is a histological type of neoplasm and not a synonym for cancer.	0	3.01	2	0
Cancer of Endometrium [description not available]	0	2.6	1	0
Endometrial Neoplasms Tumors or cancer of ENDOMETRIUM, the mucous lining of the UTERUS. These neoplasms can be benign or malignant. Their classification and grading are based on the various cell types and the percent of undifferentiated cells.	0	2.6	1	0
Hepatocellular Carcinoma [description not available]	0	2.6	1	0
Cancer of Liver [description not available]	0	2.6	1	0
Carcinoma, Hepatocellular A primary malignant neoplasm of epithelial liver cells. It ranges from a well-differentiated tumor with EPITHELIAL CELLS indistinguishable from normal HEPATOCYTES to a poorly differentiated neoplasm. The cells may be uniform or markedly pleomorphic, or form GIANT CELLS. Several classification schemes have been suggested.	0	2.6	1	0
Liver Neoplasms Tumors or cancer of the LIVER.	0	2.6	1	0
Arthritis, Degenerative [description not available]	0	2.66	2	0
Hypertrophy General increase in bulk of a part or organ due to CELL ENLARGEMENT and accumulation of FLUIDS AND SECRETIONS, not due to tumor formation, nor to an increase in the number of cells (HYPERPLASIA).	0	2.25	1	0
Osteoarthritis A progressive, degenerative joint disease, the most common form of arthritis, especially in older persons. The disease is thought to result not from the aging process but from biochemical changes and biomechanical stresses affecting articular cartilage. In the foreign literature it is often called osteoarthrosis deformans.	0	2.66	2	0
Experimental Mammary Neoplasms [description not available]	0	2.58	2	0
Familial Nonmedullary Thyroid Cancer [description not available]	0	2.25	1	0
Carcinogenesis The origin, production or development of cancer through genotypic and phenotypic changes which upset the normal balance between cell proliferation and cell death. Carcinogenesis generally requires a constellation of steps, which may occur quickly or over a period of many years.	0	2.25	1	0
Benign Cerebellar Neoplasms [description not available]	0	2.25	1	0
Arachnoidal Cerebellar Sarcoma, Circumscribed [description not available]	0	2.25	1	0
Medulloblastoma A malignant neoplasm that may be classified either as a glioma or as a primitive neuroectodermal tumor of childhood (see NEUROECTODERMAL TUMOR, PRIMITIVE). The tumor occurs most frequently in the first decade of life with the most typical location being the cerebellar vermis. Histologic features include a high degree of cellularity, frequent mitotic figures, and a tendency for the cells to organize into sheets or form rosettes. Medulloblastoma have a high propensity to spread throughout the craniospinal intradural axis. (From DeVita et al., Cancer: Principles and Practice of Oncology, 5th ed, pp2060-1)	0	2.25	1	0
Sarcoma, Epithelioid [description not available]	0	9.86	10	4
Cancer of Skin [description not available]	0	3.48	2	0
Sarcoma A connective tissue neoplasm formed by proliferation of mesodermal cells; it is usually highly malignant.	1	11.86	10	4
Skin Neoplasms Tumors or cancer of the SKIN.	0	3.48	2	0
Cell Transformation, Neoplastic Cell changes manifested by escape from control mechanisms, increased growth potential, alterations in the cell surface, karyotypic abnormalities, morphological and biochemical deviations from the norm, and other attributes conferring the ability to invade, metastasize, and kill.	0	3.17	1	0
Metastase [description not available]	0	3.17	1	0
Neoplasm Metastasis The transfer of a neoplasm from one organ or part of the body to another remote from the primary site.	0	3.17	1	0
Innate Inflammatory Response [description not available]	0	2.59	2	0
Hemorrhage, Subarachnoid [description not available]	0	2.25	1	0
Inflammation A pathological process characterized by injury or destruction of tissues caused by a variety of cytologic and chemical reactions. It is usually manifested by typical signs of pain, heat, redness, swelling, and loss of function.	0	2.59	2	0
Subarachnoid Hemorrhage Bleeding into the intracranial or spinal SUBARACHNOID SPACE, most resulting from INTRACRANIAL ANEURYSM rupture. It can occur after traumatic injuries (SUBARACHNOID HEMORRHAGE, TRAUMATIC). Clinical features include HEADACHE; NAUSEA; VOMITING, nuchal rigidity, variable neurological deficits and reduced mental status.	0	2.25	1	0
Rhabdomyosarcoma A malignant solid tumor arising from mesenchymal tissues which normally differentiate to form striated muscle. It can occur in a wide variety of sites. It is divided into four distinct types: pleomorphic, predominantly in male adults; alveolar (RHABDOMYOSARCOMA, ALVEOLAR), mainly in adolescents and young adults; embryonal (RHABDOMYOSARCOMA, EMBRYONAL), predominantly in infants and children; and botryoidal, also in young children. It is one of the most frequently occurring soft tissue sarcomas and the most common in children under 15. (From Dorland, 27th ed; Holland et al., Cancer Medicine, 3d ed, p2186; DeVita Jr et al., Cancer: Principles & Practice of Oncology, 3d ed, pp1647-9)	0	2.31	1	0
Soft Tissue Neoplasms Neoplasms of whatever cell type or origin, occurring in the extraskeletal connective tissue framework of the body including the organs of locomotion and their various component structures, such as nerves, blood vessels, lymphatics, etc.	0	3.23	1	0
Colorectal Cancer [description not available]	0	2.66	2	0
Colorectal Neoplasms Tumors or cancer of the COLON or the RECTUM or both. Risk factors for colorectal cancer include chronic ULCERATIVE COLITIS; FAMILIAL POLYPOSIS COLI; exposure to ASBESTOS; and irradiation of the CERVIX UTERI.	0	2.66	2	0
Injuries, Radiation [description not available]	0	2.31	1	0
Colitis Inflammation of the COLON section of the large intestine (INTESTINE, LARGE), usually with symptoms such as DIARRHEA (often with blood and mucus), ABDOMINAL PAIN, and FEVER.	0	2.31	1	0
Bone Cancer [description not available]	0	2.61	2	0
Osteogenic Sarcoma [description not available]	0	2.31	1	0
Bone Neoplasms Tumors or cancer located in bone tissue or specific BONES.	0	2.61	2	0
Osteosarcoma A sarcoma originating in bone-forming cells, affecting the ends of long bones. It is the most common and most malignant of sarcomas of the bones, and occurs chiefly among 10- to 25-year-old youths. (From Stedman, 25th ed)	0	2.31	1	0
Cirrhosis, Liver [description not available]	0	2.31	1	0
Liver Cirrhosis Liver disease in which the normal microcirculation, the gross vascular anatomy, and the hepatic architecture have been variably destroyed and altered with fibrous septa surrounding regenerated or regenerating parenchymal nodules.	0	2.31	1	0
Recrudescence [description not available]	0	3.7	1	1
Acute Myelogenous Leukemia [description not available]	0	2.17	1	0
Leukemia, Myeloid, Acute Clonal expansion of myeloid blasts in bone marrow, blood, and other tissue. Myeloid leukemias develop from changes in cells that normally produce NEUTROPHILS; BASOPHILS; EOSINOPHILS; and MONOCYTES.	0	2.17	1	0
Kahler Disease [description not available]	0	2.58	2	0
Multiple Myeloma A malignancy of mature PLASMA CELLS engaging in monoclonal immunoglobulin production. It is characterized by hyperglobulinemia, excess Bence-Jones proteins (free monoclonal IMMUNOGLOBULIN LIGHT CHAINS) in the urine, skeletal destruction, bone pain, and fractures. Other features include ANEMIA; HYPERCALCEMIA; and RENAL INSUFFICIENCY.	1	4.58	2	0
Graft-Versus-Host Disease [description not available]	0	2.17	1	0
Graft vs Host Disease The clinical entity characterized by anorexia, diarrhea, loss of hair, leukopenia, thrombocytopenia, growth retardation, and eventual death brought about by the GRAFT VS HOST REACTION.	0	2.17	1	0
Ewing Sarcoma [description not available]	0	2.21	1	0
Sarcoma, Ewing A malignant tumor of the bone which always arises in the medullary tissue, occurring more often in cylindrical bones. The tumor occurs usually before the age of 20, about twice as frequently in males as in females.	0	2.21	1	0
Cancer of Mediastinum [description not available]	0	3.12	1	0
Chromosomal Translocation [description not available]	0	3.12	1	0
Mediastinal Neoplasms Tumors or cancer of the MEDIASTINUM.	0	3.12	1	0
Astrocytoma, Grade IV [description not available]	0	2.54	2	0
Glial Cell Tumors [description not available]	0	2.54	2	0
Glioblastoma A malignant form of astrocytoma histologically characterized by pleomorphism of cells, nuclear atypia, microhemorrhage, and necrosis. They may arise in any region of the central nervous system, with a predilection for the cerebral hemispheres, basal ganglia, and commissural pathways. Clinical presentation most frequently occurs in the fifth or sixth decade of life with focal neurologic signs or seizures.	0	2.54	2	0
Glioma Benign and malignant central nervous system neoplasms derived from glial cells (i.e., astrocytes, oligodendrocytes, and ependymocytes). Astrocytes may give rise to astrocytomas (ASTROCYTOMA) or glioblastoma multiforme (see GLIOBLASTOMA). Oligodendrocytes give rise to oligodendrogliomas (OLIGODENDROGLIOMA) and ependymocytes may undergo transformation to become EPENDYMOMA; CHOROID PLEXUS NEOPLASMS; or colloid cysts of the third ventricle. (From Escourolle et al., Manual of Basic Neuropathology, 2nd ed, p21)	0	7.54	2	0
Abnormalities, Autosome [description not available]	0	2.15	1	0
Neuroblastoma A common neoplasm of early childhood arising from neural crest cells in the sympathetic nervous system, and characterized by diverse clinical behavior, ranging from spontaneous remission to rapid metastatic progression and death. This tumor is the most common intraabdominal malignancy of childhood, but it may also arise from thorax, neck, or rarely occur in the central nervous system. Histologic features include uniform round cells with hyperchromatic nuclei arranged in nests and separated by fibrovascular septa. Neuroblastomas may be associated with the opsoclonus-myoclonus syndrome. (From DeVita et al., Cancer: Principles and Practice of Oncology, 5th ed, pp2099-2101; Curr Opin Oncol 1998 Jan;10(1):43-51)	0	2.15	1	0
Brain Stem Neoplasms, Primary [description not available]	0	2.15	1	0
Brain Stem Neoplasms Benign and malignant intra-axial tumors of the MESENCEPHALON; PONS; or MEDULLA OBLONGATA of the BRAIN STEM. Primary and metastatic neoplasms may occur in this location. Clinical features include ATAXIA, cranial neuropathies (see CRANIAL NERVE DISEASES), NAUSEA, hemiparesis (see HEMIPLEGIA), and quadriparesis. Primary brain stem neoplasms are more frequent in children. Histologic subtypes include GLIOMA; HEMANGIOBLASTOMA; GANGLIOGLIOMA; and EPENDYMOMA.	0	2.15	1	0

epz-6438

Description

Cross-References

Synonyms (67)

Research Excerpts

Toxicity

Pharmacokinetics

Bioavailability

Dosage Studied

Protein Targets (15)

Potency Measurements

Inhibition Measurements

Activation Measurements

Biological Processes (118)

Molecular Functions (46)

Ceullar Components (45)

Bioassays (180)

Research

Studies (112)

Market Indicators

Research Demand Index: 32.86

Study Types

epz-6438

Description

Cross-References

Synonyms (67)

Research Excerpts

Toxicity

Pharmacokinetics

Bioavailability

Dosage Studied

Protein Targets (15)

Potency Measurements

Inhibition Measurements

Activation Measurements

Biological Processes (118)

Molecular Functions (46)

Ceullar Components (45)

Bioassays (180)

Research

Studies (112)

Market Indicators

Research Demand Index: 32.86

Study Types

Related Drugs (73)

Related Conditions (108)