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Assay Detail

CHEMBL4008167

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

Binding
Inhibition of EED in human G401 cells assessed as reduction in global H3K27me3 level after 48 hrs by ELISA
5
Total Activities
5
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

Polycomb protein EED (CHEMBL2189117)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of First-in-Class, Potent, and Orally Bioavailable Embryonic Ectoderm Development (EED) Inhibitor with Robust Anticancer Efficacy.
Huang Y, Zhang J, Yu Z, Zhang H, Wang Y, Lingel A, Qi W, Gu J, Zhao K, Shultz MD, Wang L, Fu X, Sun Y, Zhang Q, Jiang X, Zhang J, Zhang C, Li L, Zeng J, Feng L, Zhang C, Liu Y, Zhang M, Zhang L, Zhao M, Gao Z, Liu X, Fang D, Guo H, Mi Y, Gabriel T, Dillon MP, Atadja P, Oyang C.
J Med Chem (2017) 60 : 2215 -2226
PubMed 28092155 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 6.74 7.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4103319 1 7.50
CHEMBL3414621 TAZEMETOSTAT 4.0 1 7.40
CHEMBL4093147 1 6.68
CHEMBL4065484 1 6.66
CHEMBL4096234 1 5.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4103319 IC50 = 32.0 nM 7.50
CHEMBL3414621 TAZEMETOSTAT IC50 = 40.0 nM 7.40
CHEMBL4093147 IC50 = 210.0 nM 6.68
CHEMBL4065484 IC50 = 220.0 nM 6.66
CHEMBL4096234 IC50 = 3280.0 nM 5.48