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Assay Detail

CHEMBL4201928

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

Binding
Inhibition of anti-IgM-stimulated BTK phosphorylation at Tyr551 in human Ramos cells pre-incubated for 1 hr followed by anti-IgM stimulation for 10 mins by Western blotting
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Tyrosine-protein kinase BTK (CHEMBL5251)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design and Synthesis of Novel Amino-triazine Analogues as Selective Bruton's Tyrosine Kinase Inhibitors for Treatment of Rheumatoid Arthritis.
Kawahata W, Asami T, Kiyoi T, Irie T, Taniguchi H, Asamitsu Y, Inoue T, Miyake T, Sawa M.
J Med Chem (2018) 61 : 8917 -8933
PubMed 30216722 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 7.72 7.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4209441 SOFNOBRUTINIB 2.0 1 7.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4209441 SOFNOBRUTINIB IC50 = 19.0 nM 7.72