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Assay Detail

CHEMBL5539735

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Functional
Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell proliferation incubated for 72 hrs by CellTiterGlo luminescence assay
11
Total Activities
11
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 Novel Phenoxyaryl Pyridones as Bromodomain and Extra-Terminal Domain (BET) Inhibitors with High Selectivity for the Second Bromodomain (BD2) to Potentially Treat Acute Myeloid Leukemia.
Jiang W, Hou Q, Xu H, Yang K, Wang X, Zhang K, Zeng Y, Li W, Wang B, Luo G, Zhao X, Shen H, Xu Y, Wu X.
J Med Chem (2024) 67 : 1513 -1532
PubMed 38175809 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 6.93 7.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5572023 1 7.85
CHEMBL4297454 ABBV-744 1.0 1 7.82
CHEMBL5563490 1 7.47
CHEMBL5568960 1 7.35
CHEMBL5568743 1 7.17
CHEMBL5566025 1 6.92
CHEMBL5566198 1 6.85
CHEMBL5569499 1 6.62
CHEMBL5568810 1 6.34
CHEMBL5567469 1 6.14
CHEMBL5562706 1 5.67

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5572023 IC50 = 14.0 nM 7.85
CHEMBL4297454 ABBV-744 IC50 = 15.0 nM 7.82
CHEMBL5563490 IC50 = 34.0 nM 7.47
CHEMBL5568960 IC50 = 45.0 nM 7.35
CHEMBL5568743 IC50 = 67.0 nM 7.17
CHEMBL5566025 IC50 = 120.0 nM 6.92
CHEMBL5566198 IC50 = 140.0 nM 6.85
CHEMBL5569499 IC50 = 240.0 nM 6.62
CHEMBL5568810 IC50 = 460.0 nM 6.34
CHEMBL5567469 IC50 = 720.0 nM 6.14
CHEMBL5562706 IC50 = 2130.0 nM 5.67