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Assay Detail

CHEMBL4814913

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

Binding
Inhibition of recombinant N-terminal GST/His6-tagged human FLT3 ITD mutant (571 to 993 residues) expressed in Sf9 insect cells incubated for 1 hr by LanthaScreen assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Investigation of Selected Flavonoid Derivatives as Potent FLT3 Inhibitors for the Potential Treatment of Acute Myeloid Leukemia.
Yen SC, Chen LC, Huang HL, Ngo ST, Wu YW, Lin TE, Sung TY, Lien ST, Tseng HJ, Pan SL, Huang WJ, Hsu KC.
J Nat Prod (2021) 84 : 1 -10
PubMed 33393294 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 6.35 6.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL243664 ACACETIN 1 6.68
CHEMBL293776 HISPIDULIN 1 6.41
CHEMBL376644 SALVIGENIN 1 6.24
CHEMBL78010 PECTOLINARIGENIN 1 6.06

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL243664 ACACETIN IC50 = 210.0 nM 6.68
CHEMBL293776 HISPIDULIN IC50 = 390.0 nM 6.41
CHEMBL376644 SALVIGENIN IC50 = 580.0 nM 6.24
CHEMBL78010 PECTOLINARIGENIN IC50 = 880.0 nM 6.06