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Assay Detail

CHEMBL5333045

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

Binding
Inhibition of G9a (unknown origin) using H3(1-20)-cys as substrate by HPLC analysis
3
Total Activities
3
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 EHMT2 (CHEMBL6032)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of cysteine-targeting covalent histone methyltransferase inhibitors.
Zhao Y, Jiang B, Gu Z, Chen T, Yu W, Liu S, Liu X, Chen D, Li F, Chen W.
Eur J Med Chem (2023) 246 : 115028 -115028
PubMed 36528996 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 6.80 7.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1231795 1 7.82
CHEMBL569864 1 5.77
CHEMBL2441082 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1231795 IC50 = 15.0 nM 7.82
CHEMBL569864 IC50 = 1700.0 nM 5.77
CHEMBL2441082 IC50 < 2.5 nM -