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Assay Detail

CHEMBL5135835

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

Binding
Inhibition of BTK in human whole blood
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

The Ascension of Targeted Covalent Inhibitors.
Singh J.
J Med Chem (2022) 65 : 5886 -5901
PubMed 35439421 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 3 8.30 8.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3936761 ZANUBRUTINIB 4.0 1 8.62
CHEMBL1873475 IBRUTINIB 4.0 1 8.24
CHEMBL3707348 ACALABRUTINIB 4.0 1 8.04

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3936761 ZANUBRUTINIB EC50 = 2.4 nM 8.62
CHEMBL1873475 IBRUTINIB EC50 = 5.8 nM 8.24
CHEMBL3707348 ACALABRUTINIB EC50 = 9.2 nM 8.04