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Assay Detail

CHEMBL5637747

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

Binding
Inhibition of recombinant FLT3 D835Y mutant (unknown origin) using peptide substrate incubated for for 30 mins by HTRF assay
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 benzimidazole-indazole derivatives as potent FLT3-tyrosine kinase domain mutant kinase inhibitors for acute myeloid leukemia.
Ko B, Jang Y, Kim MH, Lam TT, Seo HK, Jeong P, Choi M, Kang KW, Lee SD, Park JH, Kim M, Han SY, Kim YC.
Eur J Med Chem (2023) 262 : 115860 -115860
PubMed 37866334 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 9.56 10.21

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5641673 1 10.21
CHEMBL5639279 1 9.70
CHEMBL5647669 1 9.64
CHEMBL3301622 GILTERITINIB 4.0 1 8.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5641673 IC50 = 0.061 nM 10.21
CHEMBL5639279 IC50 = 0.199 nM 9.70
CHEMBL5647669 IC50 = 0.227 nM 9.64
CHEMBL3301622 GILTERITINIB IC50 = 2.02 nM 8.70