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Assay Detail

CHEMBL5323882

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

Toxicity
Inhibition of c-KIT (unknown origin) using peptide substrate TK-S and ATP as substrate incubated for 1 hr by HTRF assay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Toxicity
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 2-Aminopyrimidine Derivatives as Potent Dual FLT3/CHK1 Inhibitors with Significantly Reduced hERG Inhibitory Activities.
Li X, Wang P, Wang C, Jin T, Xu R, Tong L, Hu X, Shen L, Li J, Zhou Y, Liu T.
J Med Chem (2023) 66 : 11792 -11814
PubMed 37584545 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 5.60 6.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5428756 1 6.15
CHEMBL5431016 1 6.04
CHEMBL5409504 1 5.96
CHEMBL5411251 1 5.75
CHEMBL5403690 1 5.73
CHEMBL5426241 1 5.70
CHEMBL5410841 1 5.69
CHEMBL5439250 1 5.65
CHEMBL5433322 1 5.61
CHEMBL5408927 1 5.51
CHEMBL5427417 1 5.42
CHEMBL5421825 1 5.34
CHEMBL5409206 1 5.32
CHEMBL5413462 1 5.32
CHEMBL5419654 1 5.30
CHEMBL5427282 1 5.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5428756 IC50 = 704.5 nM 6.15
CHEMBL5431016 IC50 = 901.85 nM 6.04
CHEMBL5409504 IC50 = 1083.5 nM 5.96
CHEMBL5411251 IC50 = 1795.5 nM 5.75
CHEMBL5403690 IC50 = 1874.0 nM 5.73
CHEMBL5426241 IC50 = 1985.0 nM 5.70
CHEMBL5410841 IC50 = 2031.0 nM 5.69
CHEMBL5439250 IC50 = 2238.0 nM 5.65
CHEMBL5433322 IC50 = 2464.5 nM 5.61
CHEMBL5408927 IC50 = 3094.5 nM 5.51
CHEMBL5427417 IC50 = 3840.5 nM 5.42
CHEMBL5421825 IC50 = 4616.5 nM 5.34
CHEMBL5409206 IC50 = 4774.5 nM 5.32
CHEMBL5413462 IC50 = 4776.5 nM 5.32
CHEMBL5419654 IC50 = 5057.5 nM 5.30
CHEMBL5427282 IC50 = 8914.0 nM 5.05