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Assay Detail

CHEMBL5380716

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

Binding
Inhibition of c-kit (unknown origin) using peptide substrate incubated for 1 hrs in presence of ATP by fluorescence microplate reader analysis
6
Total Activities
6
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

Mast/stem cell growth factor receptor Kit (CHEMBL1936)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of 5-trifluoromethyl-2-aminopyrimidine derivatives as potent dual inhibitors of FLT3 and CHK1.
Deng M, Gao Y, Wang P, Du W, Xu G, Li J, Zhou Y, Liu T.
RSC Med Chem (2024) 15 : 539 -552
PubMed 38389894 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 5.27 7.08

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL576982 QUIZARTINIB 4.0 1 7.08
CHEMBL5406425 1 5.01
CHEMBL5401267 1 4.98
CHEMBL5428278 1 4.96
CHEMBL5408027 1 4.91
CHEMBL5411672 1 4.67

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL576982 QUIZARTINIB IC50 = 82.63 nM 7.08
CHEMBL5406425 IC50 = 9810.0 nM 5.01
CHEMBL5401267 IC50 = 10497.5 nM 4.98
CHEMBL5428278 IC50 = 10887.5 nM 4.96
CHEMBL5408027 IC50 = 12269.0 nM 4.91
CHEMBL5411672 IC50 = 21348.5 nM 4.67