Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL4031409

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

Binding
Inhibition of human MV4-11 cells-derived His-tagged FLT3 ITD mutant (564 to 993 residues) expressed in baculovirus infected sf9 cells using poly (4:1 Glu, Tyr) as substrate after 1 hr by ADP-Glo kinase assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Discovery of 1-(4-(4-Amino-3-(4-(2-morpholinoethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)phenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea (CHMFL-FLT3-213) as a Highly Potent Type II FLT3 Kinase Inhibitor Capable of Overcoming a Variety of FLT3 Kinase Mutants in FLT3-ITD Positive AML.
Wang A, Li X, Chen C, Wu H, Qi Z, Hu C, Yu K, Wu J, Liu J, Liu X, Hu Z, Wang W, Wang W, Wang W, Wang L, Wang B, Liu Q, Li L, Ge J, Ren T, Zhang S, Xia R, Liu J, Liu Q.
J Med Chem (2017) 60 : 8407 -8424
PubMed 28956923 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 7.92 8.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4101411 1 8.05
CHEMBL576982 QUIZARTINIB 4.0 1 7.78

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4101411 IC50 = 9.0 nM 8.05
CHEMBL576982 QUIZARTINIB IC50 = 16.8 nM 7.78