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Assay Detail

CHEMBL4020207

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

Binding
Inhibition of human BTK using KVEKIGEGTYGVVYK as substrate preincubated for 20 mins followed by [gamma-33P]-ATP addition by filter binding method
2
Total Activities
2
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 BTK (CHEMBL5251)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

In Silico Identification of a Novel Hinge-Binding Scaffold for Kinase Inhibitor Discovery.
Wang Y, Sun Y, Cao R, Liu D, Xie Y, Li L, Qi X, Huang N.
J Med Chem (2017) 60 : 8552 -8564
PubMed 28945083 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 9.34 9.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1873475 IBRUTINIB 4.0 1 9.96
CHEMBL4101977 1 8.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1873475 IBRUTINIB IC50 = 0.11 nM 9.96
CHEMBL4101977 IC50 = 1.91 nM 8.72