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Assay Detail

CHEMBL5129684

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

Binding
Inhibition of human G9a (913 to 1193 residues) using H3 peptide as substrate measured upto 45 mins in presence of SAM cofactor
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 the First-in-Class G9a/GLP Covalent Inhibitors.
Park KS, Xiong Y, Yim H, Velez J, Babault N, Kumar P, Liu J, Jin J.
J Med Chem (2022) 65 : 10506 -10522
PubMed 35763668 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 6.39 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5170450 1 7.00
CHEMBL2441082 1 6.66
CHEMBL5191615 1 5.51

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5170450 IC50 = 100.0 nM 7.00
CHEMBL2441082 IC50 = 220.0 nM 6.66
CHEMBL5191615 IC50 = 3100.0 nM 5.51