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Assay Detail

CHEMBL5580225

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

Binding
Inhibition of LCK (unknown origin)
9
Total Activities
9
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

Identification of 3,4-dihydropyrimido[4,5-d]pyrimidin-2(1H)-one scaffolds as potent Lck inhibitors as anti-cancer agents.
Ji SH, Kim HB, Song Y, Chung HW, Lee DH, Jung C, Ko Y, Han SJ.
Bioorg Med Chem Lett (2024) 102 : 129645 -129645
PubMed 38316368 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 7.45 8.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL189338 1 8.46
CHEMBL5594600 1 7.97
CHEMBL5583654 1 7.94
CHEMBL5595544 1 7.54
CHEMBL5595581 1 7.41
CHEMBL5595530 1 7.40
CHEMBL5595663 1 7.38
CHEMBL1970879 1 6.83
CHEMBL5593666 1 6.11

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL189338 IC50 = 3.5 nM 8.46
CHEMBL5594600 IC50 = 10.6 nM 7.97
CHEMBL5583654 IC50 = 11.4 nM 7.94
CHEMBL5595544 IC50 = 28.6 nM 7.54
CHEMBL5595581 IC50 = 38.7 nM 7.41
CHEMBL5595530 IC50 = 39.5 nM 7.40
CHEMBL5595663 IC50 = 42.0 nM 7.38
CHEMBL1970879 IC50 = 147.0 nM 6.83
CHEMBL5593666 IC50 = 779.0 nM 6.11