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Assay Detail

CHEMBL3815409

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

Binding
Competitive inhibition of FLT3 ITD mutant (unknown origin) in presence of ATP
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Receptor-type tyrosine-protein kinase FLT3 (CHEMBL1974)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of a Highly Potent and Selective Indenoindolone Type 1 Pan-FLT3 Inhibitor.
Hatcher JM, Weisberg E, Sim T, Stone RM, Liu S, Griffin JD, Gray NS.
ACS Med Chem Lett (2016) 7 : 476 -481
PubMed 27190596 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 8.03 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL576982 QUIZARTINIB 4.0 1 8.70
CHEMBL2105728 CRENOLANIB 3.0 1 8.52
CHEMBL3815054 1 8.00
CHEMBL3813873 PEXIDARTINIB 4.0 1 6.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL576982 QUIZARTINIB IC50 = 2.0 nM 8.70
CHEMBL2105728 CRENOLANIB IC50 = 3.0 nM 8.52
CHEMBL3815054 IC50 = 10.0 nM 8.00
CHEMBL3813873 PEXIDARTINIB IC50 = 130.0 nM 6.89