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Assay Detail

CHEMBL2173409

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

Binding
Inhibition of SYK in human mast cell cultures assessed as reduction in Anti-IgG-stimulated FcgammaR-mediated leukotriene LTC4 production by fluorescence polarization assay
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

Tyrosine-protein kinase SYK (CHEMBL2599)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery and development of spleen tyrosine kinase (SYK) inhibitors.
Singh R, Masuda ES, Payan DG.
J Med Chem (2012) 55 : 3614 -3643
PubMed 22257213 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 7.31 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1235110 1 8.30
CHEMBL475251 R-406 2.0 1 7.39
CHEMBL1229525 1 6.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1235110 IC50 = 5.0 nM 8.30
CHEMBL475251 R-406 IC50 = 41.0 nM 7.39
CHEMBL1229525 IC50 = 570.0 nM 6.24