Assay Detail

CHEMBL5648332

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Binding

Inhibition of human EZH2 using Core Histone and [3H]SAM as substrate incubated for 30 mins to 1 hr by HotSpot kinase assay

ChEMBL ↗

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Target

Histone-lysine N-methyltransferase EZH2 (CHEMBL2189110) ↗

Open DB target context

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Histone-lysine N-methyltransferase EZH2 (CHEMBL2189110) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Histone-lysine N-methyltransferase EZH2

CHEMBL2189110

Anchored from Assay target.

Protein identity Histone-lysine N-methyltransferase EZH2

Disease frame Disease evidence pending

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Review focus Open DB context pending

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Total Activities

Compounds Tested

Activity Types

Assay Parameters

Assay Information

Assay Type	Binding
Organism	Homo sapiens
Confidence	9 — Direct single protein target
Curated By	Autocuration

Target

Histone-lysine N-methyltransferase EZH2 (CHEMBL2189110) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

Novel orally bioavailable EZH1/2 dual inhibitors with greater antitumor efficacy than an EZH2 selective inhibitor.

Honma D, Kanno O, Watanabe J, Kinoshita J, Hirasawa M, Nosaka E, Shiroishi M, Takizawa T, Yasumatsu I, Horiuchi T, Nakao A, Suzuki K, Yamasaki T, Nakajima K, Hayakawa M, Yamazaki T, Yadav AS, Adachi N.
Cancer Sci (2017) 108 : 2069 -2078
PubMed 28741798 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	2	8.29	8.29

Assay Parameters

Parameter	Type	Value	Units	Text
EFO_ID	EFO_ID	-	—	MONDO:0004992
EFO_TERM	EFO_TERM	-	—	cancer

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL5187396	—	—	1	8.29
CHEMBL4597193	VALEMETOSTAT	2.0	1	8.29

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL5187396	—	IC50	=	5.08	nM	8.29
CHEMBL4597193	VALEMETOSTAT	IC50	=	5.08	nM	8.29