Tolebrutinib is a potent, selective, orally active and brain-penetrant Bruton tyrosine kinase (BTK) inhibitor(IC50s of 0.4 and 0.7 nM in Ramos B cells and in HMC microglia cells, respectively).

Atuzabrutinib (SAR 444727) is a selective Bruton's tyrosine kinase (Btk) inhibitor that inhibits intra-neutrophilic neutrophilic granulocytes through inhibition of the adhesion receptor signaling pathway, and can be used to study autoimmune disorders such as arthritis in rheumatoid rodents and pemphigus vulgaris.

ARQ-531 (ARQ531) is a potent, reversible, orally available inhibitor of both wild type and C481S-mutant BTK kinase with IC50 of 0.85 and 0.39 nM, respectively.