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Assay Detail

CHEMBL1959554

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

Functional
Cytotoxicity against human primary leukemia cells isolated from acute myeloid leukemia patient expressing FLT3-D835Y mutation assessed as cell viability after 72 hrs by luciferase assay
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type Leukemia cell
Confidence 1 — Organism
Curated By Autocuration

Publication

VX-322: a novel dual receptor tyrosine kinase inhibitor for the treatment of acute myelogenous leukemia.
Heidary DK, Huang G, Boucher D, Ma J, Forster C, Grey R, Xu J, Arnost M, Choquette D, Chen G, Zhou JH, Yao YM, Ball ED, Namchuk M, Davies RJ, Henkel G.
J Med Chem (2012) 55 : 725 -734
PubMed 22221201 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 5.93 6.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1835870 1 6.66
CHEMBL1835749 1 6.62
CHEMBL1835867 1 6.52
CHEMBL1835747 1 6.51
CHEMBL941 IMATINIB 4.0 1 6.30
CHEMBL535 SUNITINIB 4.0 1 5.96
CHEMBL124660 TANDUTINIB 2.0 1 5.47
CHEMBL1833992 1 5.23
CHEMBL1835746 1 5.05
CHEMBL1835743 1 4.98

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1835870 IC50 = 220.0 nM 6.66
CHEMBL1835749 IC50 = 240.0 nM 6.62
CHEMBL1835867 IC50 = 300.0 nM 6.52
CHEMBL1835747 IC50 = 310.0 nM 6.51
CHEMBL941 IMATINIB IC50 = 500.0 nM 6.30
CHEMBL535 SUNITINIB IC50 = 1100.0 nM 5.96
CHEMBL124660 TANDUTINIB IC50 = 3400.0 nM 5.47
CHEMBL1833992 IC50 = 5900.0 nM 5.23
CHEMBL1835746 IC50 = 8900.0 nM 5.05
CHEMBL1835743 IC50 = 10500.0 nM 4.98