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Assay Detail

CHEMBL5133737

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

Binding
Inhibition of FLT3 (unknown origin)
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

Discovery of a benzimidazole-based dual FLT3/TrKA inhibitor targeting acute myeloid leukemia.
Dokla EME, Abdel-Aziz AK, Milik SN, McPhillie MJ, Minucci S, Abouzid KAM.
Bioorg Med Chem (2022) 56 : 116596 -116596
PubMed 35033885 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 8.03 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1738757 REBASTINIB 2.0 1 8.70
CHEMBL1171837 PONATINIB 4.0 1 7.90
CHEMBL1336 SORAFENIB 4.0 1 7.49

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1738757 REBASTINIB IC50 = 2.0 nM 8.70
CHEMBL1171837 PONATINIB IC50 = 12.6 nM 7.90
CHEMBL1336 SORAFENIB IC50 = 32.6 nM 7.49