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Assay Detail

CHEMBL4144879

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

Functional
Cytotoxicity against human Pfeiffer cells assessed as decrease in cell viability after 5 days by CellTiter-Glo reagent based luminescence assay
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type Pfeiffer
Confidence 1 — Organism
Curated By Intermediate

Target

Pfeiffer (CHEMBL4296489)
Type CELL-LINE
Organism Homo sapiens

Publication

Discovery of EBI-2511: A Highly Potent and Orally Active EZH2 Inhibitor for the Treatment of Non-Hodgkin's Lymphoma.
Lu B, Shen X, Zhang L, Liu D, Zhang C, Cao J, Shen R, Zhang J, Wang D, Wan H, Xu Z, Ho MH, Zhang M, Zhang L, He F, Tao W.
ACS Med Chem Lett (2018) 9 : 98 -102
PubMed 29456795 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 25 7.42 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4161444 1 8.70
CHEMBL4176554 1 8.52
CHEMBL4162499 1 8.22
CHEMBL4169762 1 8.15
CHEMBL4159112 1 8.10
CHEMBL4165937 1 7.96
CHEMBL4169368 1 7.85
CHEMBL4170327 1 7.85
CHEMBL4162316 1 7.82
CHEMBL4164687 1 7.77
CHEMBL4172576 1 7.77
CHEMBL4170753 1 7.70
CHEMBL4177454 1 7.68
CHEMBL4161265 1 7.68
CHEMBL3414621 TAZEMETOSTAT 4.0 1 7.42
CHEMBL4176373 1 6.82
CHEMBL4169191 1 6.80
CHEMBL4160111 1 6.66
CHEMBL4174176 1 6.62
CHEMBL4169598 1 5.89
CHEMBL4167587 1 5.74
CHEMBL4162406 1 5.48
CHEMBL4165760 1 -
CHEMBL4172992 1 -
CHEMBL3770000 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4161444 IC50 = 2.0 nM 8.70
CHEMBL4176554 IC50 = 3.0 nM 8.52
CHEMBL4162499 IC50 = 6.0 nM 8.22
CHEMBL4169762 IC50 = 7.0 nM 8.15
CHEMBL4159112 IC50 = 8.0 nM 8.10
CHEMBL4165937 IC50 = 11.0 nM 7.96
CHEMBL4169368 IC50 = 14.0 nM 7.85
CHEMBL4170327 IC50 = 14.0 nM 7.85
CHEMBL4162316 IC50 = 15.0 nM 7.82
CHEMBL4164687 IC50 = 17.0 nM 7.77
CHEMBL4172576 IC50 = 17.0 nM 7.77
CHEMBL4170753 IC50 = 20.0 nM 7.70
CHEMBL4177454 IC50 = 21.0 nM 7.68
CHEMBL4161265 IC50 = 21.0 nM 7.68
CHEMBL3414621 TAZEMETOSTAT IC50 = 38.0 nM 7.42
CHEMBL4176373 IC50 = 150.0 nM 6.82
CHEMBL4169191 IC50 = 160.0 nM 6.80
CHEMBL4160111 IC50 = 220.0 nM 6.66
CHEMBL4174176 IC50 = 240.0 nM 6.62
CHEMBL4169598 IC50 = 1300.0 nM 5.89
CHEMBL4167587 IC50 = 1830.0 nM 5.74
CHEMBL4162406 IC50 = 3300.0 nM 5.48
CHEMBL4165760 IC50 - -
CHEMBL4172992 IC50 > 5000.0 nM -
CHEMBL3770000 IC50 - -