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Assay Detail

CHEMBL4701182

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

Functional
In vivo inhibition of BTK in TI-2 antigen/ NP-Ficoll-induced DBA1 mouse immunized model assessed as reduction in BTK phosphorylation administered orally twice daily for 10 days measured post last dose
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Tyrosine-protein kinase BTK (CHEMBL3259478)
Type SINGLE PROTEIN
Organism Mus musculus

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 6.89 6.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4744041 1 6.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4744041 IC50 = 130.0 nM 6.89