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Assay Detail

CHEMBL3418486

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of human EZH2 Y641S mutant assessed as H3K27me2 level after 30 mins by scintillation counting analysis in presence of [3H]-SAM
1
Total Activities
1
Compounds Tested
1
Activity Types
0
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

Selective inhibitors of protein methyltransferases.
Kaniskan HÜ, Konze KD, Jin J.
J Med Chem (2015) 58 : 1596 -1629
PubMed 25406853 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 1 9.30 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3287735 GSK2816126 1.0 1 9.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3287735 GSK2816126 Ki = 0.5 nM 9.30