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Assay Detail

CHEMBL3794750

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

Binding
Inhibition of human N-terminal GST-tagged FLT3 cytoplasmic domain (564 to 993 residues) expressed in baculovirus expression system using fluorescence labelled srctide as substrate by mobility shift assay in presence of ATP
3
Total Activities
3
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

Development of a potent and selective FLT3 kinase inhibitor by systematic expansion of a non-selective fragment-screening hit.
Nakano H, Hasegawa T, Imamura R, Saito N, Kojima H, Okabe T, Nagano T.
Bioorg Med Chem Lett (2016) 26 : 2370 -2374
PubMed 26995531 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 7.38 8.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3792850 1 8.05
CHEMBL3793843 1 7.64
CHEMBL508964 1 6.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3792850 IC50 = 9.0 nM 8.05
CHEMBL3793843 IC50 = 23.0 nM 7.64
CHEMBL508964 IC50 = 350.0 nM 6.46