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Assay Detail

CHEMBL2319491

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

Binding
Inhibition of human LCK using poly[Glu:Tyr] (4:1) peptide substrate
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

Tyrosine-protein kinase Lck (CHEMBL258)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and biological evaluation of analogues of the kinase inhibitor nilotinib as Abl and Kit inhibitors.
Duveau DY, Hu X, Walsh MJ, Shukla S, Skoumbourdis AP, Boxer MB, Ambudkar SV, Shen M, Thomas CJ.
Bioorg Med Chem Lett (2013) 23 : 682 -686
PubMed 23273517 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 5.53 6.97

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL255863 NILOTINIB 4.0 1 6.97
CHEMBL2311806 1 5.84
CHEMBL2311807 1 4.96
CHEMBL2311808 1 4.35

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL255863 NILOTINIB IC50 = 108.2 nM 6.97
CHEMBL2311806 IC50 = 1448.0 nM 5.84
CHEMBL2311807 IC50 = 11050.0 nM 4.96
CHEMBL2311808 IC50 = 44620.0 nM 4.35