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Assay Detail

CHEMBL3265576

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Binding
Inhibition of Syk in alphaIgM-stimulated human B cells assessed as cell proliferation after 1 hr incubation by flow cytometry
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type B
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Discovery of GS-9973, a selective and orally efficacious inhibitor of spleen tyrosine kinase.
Currie KS, Kropf JE, Lee T, Blomgren P, Xu J, Zhao Z, Gallion S, Whitney JA, Maclin D, Lansdon EB, Maciejewski P, Rossi AM, Rong H, Macaluso J, Barbosa J, Di Paolo JA, Mitchell SA.
J Med Chem (2014) 57 : 3856 -3873
PubMed 24779514 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 2 7.11 7.39

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3265032 ENTOSPLETINIB 3.0 1 7.39
CHEMBL475251 R-406 2.0 1 6.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3265032 ENTOSPLETINIB EC50 = 41.0 nM 7.39
CHEMBL475251 R-406 EC50 = 151.0 nM 6.82