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Assay Detail

CHEMBL5340359

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

Binding
Inhibition of human recombinant EHMT2 G9a using SAM as substrate incubated for 1 hr by microplate luminescence based HMT assay
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 Dual Lysine Methyltransferase G9a and EZH2 Inhibitors with In Vivo Efficacy against Malignant Rhabdoid Tumor.
Shi Y, Zhang Q, Zhang M, Chen Y, Sun J, Chen L, Liu S, Liu Z, Yang J, Wu C, Zheng Z, Wang L, Chen G.
J Med Chem (2023) 66 : 5685 -5702
PubMed 37021456 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 8.26 8.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5410162 1 8.54
CHEMBL1231795 1 8.43
CHEMBL5406071 1 7.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5410162 IC50 = 2.9 nM 8.54
CHEMBL1231795 IC50 = 3.75 nM 8.43
CHEMBL5406071 IC50 = 15.0 nM 7.82