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Assay Detail

CHEMBL4701116

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

Binding
Inhibition of BTK in human PBMC assessed as reduction in anti-IgD-induced B cell activation preincubated for 30 mins followed by rabbit F(ab')2 anti-human IgD stimulation and measured after 18 to 22 hrs by CD19-APC and CD69-PE staining based flow cytometry
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Discovery of BIIB068: A Selective, Potent, Reversible Bruton's Tyrosine Kinase Inhibitor as an Orally Efficacious Agent for Autoimmune Diseases.
Ma B,Bohnert T,Otipoby KL,Tien E,Arefayene M,Bai J,Bajrami B,Bame E,Chan TR,Humora M,MacPhee JM,Marcotte D,Mehta D,Metrick CM,Moniz G,Polack E,Poreci U,Prefontaine A,Sheikh S,Schroeder P,Smirnakis K,Zhang L,Zheng F,Hopkins BT
J Med Chem (2020) 63 : 12526 -12541
PubMed 32696648 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 6.96 6.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4744041 1 6.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4744041 IC50 = 110.0 nM 6.96