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Assay Detail

CHEMBL4828527

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

ADMET
Inhibition of CYP2D6 (unknown origin)
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Cytochrome P450 2D6 (CHEMBL289)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of EEDi-5273 as an Exceptionally Potent and Orally Efficacious EED Inhibitor Capable of Achieving Complete and Persistent Tumor Regression.
Rej RK, Wang C, Lu J, Wang M, Petrunak E, Zawacki KP, McEachern D, Yang CY, Wang L, Li R, Chinnaswamy K, Wen B, Sun D, Stuckey JA, Zhou Y, Chen J, Tang G, Wang S.
J Med Chem (2021) 64 : 14540 -14556
PubMed 34613724 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 4.76 4.84

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4870920 1 4.84
CHEMBL4854800 1 4.72
CHEMBL4861394 1 4.71

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4870920 IC50 = 14300.0 nM 4.84
CHEMBL4854800 IC50 = 18900.0 nM 4.72
CHEMBL4861394 IC50 = 19700.0 nM 4.71