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Assay Detail

CHEMBL5129686

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Binding
Binding affinity to human GLP (982 to 1266 residues) assessed as dissociation constant by isothermal titration calorimetry method
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 EHMT1 (CHEMBL6031)
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
Kd 3 6.88 7.34

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5170450 1 7.34
CHEMBL2441082 1 7.21
CHEMBL5191615 1 6.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5170450 Kd = 46.0 nM 7.34
CHEMBL2441082 Kd = 62.0 nM 7.21
CHEMBL5191615 Kd = 790.0 nM 6.10