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Assay Detail

CHEMBL5329056

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

Binding
Inhibition of FLT3 in human MOLM-13 cells
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type MOLM-13
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 <i>N</i>-(4-(Aminomethyl)phenyl)-5-methylpyrimidin-2-amine Derivatives as Potent and Selective JAK2 Inhibitors.
Tian Y, Qin S, Zhang F, Luo J, He X, Sun Y, Yang T.
ACS Med Chem Lett (2023) 14 : 1113 -1121
PubMed 37583815 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 5.85 6.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5422938 1 6.24
CHEMBL5403283 1 6.12
CHEMBL5436902 1 6.08
CHEMBL5408539 1 6.05
CHEMBL5437784 1 6.05
CHEMBL5440964 1 6.02
CHEMBL5419978 1 5.90
CHEMBL5408994 1 5.89
CHEMBL5424098 1 5.82
CHEMBL5429688 1 5.78
CHEMBL5418281 1 5.78
CHEMBL5432626 1 5.75
CHEMBL5404973 1 5.75
CHEMBL5416914 1 5.25
CHEMBL5415635 1 5.23
CHEMBL5398984 1 -
CHEMBL5416946 1 -
CHEMBL5429799 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5422938 IC50 = 582.6 nM 6.24
CHEMBL5403283 IC50 = 755.7 nM 6.12
CHEMBL5436902 IC50 = 825.6 nM 6.08
CHEMBL5408539 IC50 = 885.4 nM 6.05
CHEMBL5437784 IC50 = 882.4 nM 6.05
CHEMBL5440964 IC50 = 961.2 nM 6.02
CHEMBL5419978 IC50 = 1254.1 nM 5.90
CHEMBL5408994 IC50 = 1276.5 nM 5.89
CHEMBL5424098 IC50 = 1505.7 nM 5.82
CHEMBL5429688 IC50 = 1665.4 nM 5.78
CHEMBL5418281 IC50 = 1676.2 nM 5.78
CHEMBL5432626 IC50 = 1760.2 nM 5.75
CHEMBL5404973 IC50 = 1796.7 nM 5.75
CHEMBL5416914 IC50 = 5560.4 nM 5.25
CHEMBL5415635 IC50 = 5843.6 nM 5.23
CHEMBL5398984 IC50 > 10.0 nM -
CHEMBL5416946 IC50 > 10.0 nM -
CHEMBL5429799 IC50 > 10.0 nM -