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Assay Detail

CHEMBL4414913

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

Binding
Inhibition of human BTK using poly[Glu:Tyr] (4:1) as substrate preincubated for 60 mins followed by [gamma-33P]-ATP addition and measured after 120 mins by filter binding method
ChEMBL ↗
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

Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase.
Guo Y, Liu Y, Hu N, Yu D, Zhou C, Shi G, Zhang B, Wei M, Liu J, Luo L, Tang Z, Song H, Guo Y, Liu X, Su D, Zhang S, Song X, Zhou X, Hong Y, Chen S, Cheng Z, Young S, Wei Q, Wang H, Wang Q, Lv L, Wang F, Xu H, Sun H, Xing H, Li N, Zhang W, Wang Z, Liu G, Sun Z, Zhou D, Li W, Liu L, Wang L, Wang Z.
J Med Chem (2019) 62 : 7923 -7940
PubMed 31381333 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 9.19 9.34

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1873475 IBRUTINIB 4.0 1 9.34
CHEMBL3936761 ZANUBRUTINIB 4.0 1 9.04

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1873475 IBRUTINIB IC50 = 0.46 nM 9.34
CHEMBL3936761 ZANUBRUTINIB IC50 = 0.92 nM 9.04