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Assay Detail

CHEMBL3583526

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Functional
Cytotoxicity against human MV4-11 cells harboring MLL1 fusion gene assessed as growth inhibition after 4 days by CellTiter-Glo luminescent assay
6
Total Activities
6
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

Structure-Based Design of γ-Carboline Analogues as Potent and Specific BET Bromodomain Inhibitors.
Ran X, Zhao Y, Liu L, Bai L, Yang CY, Zhou B, Meagher JL, Chinnaswamy K, Stuckey JA, Wang S.
J Med Chem (2015) 58 : 4927 -4939
PubMed 26080064 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 7.38 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3581661 1 7.70
CHEMBL3581660 1 7.64
CHEMBL1957266 1 7.62
CHEMBL3581662 1 7.47
CHEMBL1232461 MOLIBRESIB 2.0 1 7.03
CHEMBL2017291 1 6.79

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3581661 IC50 = 20.0 nM 7.70
CHEMBL3581660 IC50 = 23.0 nM 7.64
CHEMBL1957266 IC50 = 24.0 nM 7.62
CHEMBL3581662 IC50 = 34.0 nM 7.47
CHEMBL1232461 MOLIBRESIB IC50 = 93.0 nM 7.03
CHEMBL2017291 IC50 = 162.0 nM 6.79