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Assay Detail

CHEMBL5505042

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Functional
Antiproliferative activity against human MV4-11 cells expressing high BCL-2 assessed as cell viability measured after 72 hrs by Cell Counting Kit-8 assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type MV4-11
Confidence 1 — Organism
Curated By Autocuration

Target

MV4-11 (CHEMBL613835)
Type CELL-LINE
Organism Homo sapiens

Publication

Discovery of a Covalent Inhibitor That Overcame Resistance to Venetoclax in AML Cells Overexpressing BFL-1.
Lou J, Zhou Q, Lyu X, Cen X, Liu C, Yan Z, Li Y, Tang H, Liu Q, Ding J, Lu Y, Huang H, Xie H, Zhao Y.
J Med Chem (2024) 67 : 10795 -10830
PubMed 38913996 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 5.22 6.36

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3137309 VENETOCLAX 4.0 1 6.36
CHEMBL5527957 1 5.75
CHEMBL5555333 1 5.63
CHEMBL5542092 1 5.43
CHEMBL5512573 1 5.36
CHEMBL5523629 1 4.90
CHEMBL5558391 1 4.70
CHEMBL5549784 1 4.47
CHEMBL4576854 1 4.34

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3137309 VENETOCLAX IC50 = 440.0 nM 6.36
CHEMBL5527957 IC50 = 1790.0 nM 5.75
CHEMBL5555333 IC50 = 2350.0 nM 5.63
CHEMBL5542092 IC50 = 3690.0 nM 5.43
CHEMBL5512573 IC50 = 4420.0 nM 5.36
CHEMBL5523629 IC50 = 12600.0 nM 4.90
CHEMBL5558391 IC50 = 19860.0 nM 4.70
CHEMBL5549784 IC50 = 33520.0 nM 4.47
CHEMBL4576854 IC50 = 46160.0 nM 4.34