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Assay Detail

CHEMBL4222448

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 highly potent orally bioavailable imidazo-[1, 2-a]pyrazine Aurora inhibitor.
Yu T, Zhang Y, Kerekes AD, Tagat JR, Doll RJ, Xiao Y, Esposite S, Hruza A, Belanger DB, Voss M, Rainka MP, Basso A, Liu M, Liang L, Sui N, Prelusky D, Rindgen D, Zhang L.
Bioorg Med Chem Lett (2018) 28 : 1397 -1403
PubMed 29545102 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 8.15 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4228240 1 8.30
CHEMBL4225923 1 8.30
CHEMBL4227082 1 7.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4228240 IC50 = 5.0 nM 8.30
CHEMBL4225923 IC50 = 5.0 nM 8.30
CHEMBL4227082 IC50 = 14.0 nM 7.85