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Assay Detail

CHEMBL3813055

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

Binding
Inhibition of recombinant BTK (unknown origin) preincubated for 1 hr followed by ATP addition by IMAP assay
1
Total Activities
1
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

Structure-based discovery of novel 4,5,6-trisubstituted pyrimidines as potent covalent Bruton's tyrosine kinase inhibitors.
Zou Y, Xiao J, Tu Z, Zhang Y, Yao K, Luo M, Ding K, Zhang Y, Lai Y.
Bioorg Med Chem Lett (2016) 26 : 3052 -3059
PubMed 27210433 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 8.51 8.51

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3707348 ACALABRUTINIB 4.0 1 8.51

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3707348 ACALABRUTINIB IC50 = 3.1 nM 8.51