Zanubrutinib (formerly known as BGB-3111), an S-enantiomer, is a novel, highly selective, second generation BTK inhibitor, currently under clinical investigation in hematological cancers.

BTK inhibitor 17 is a novel and potent irreversible BTK inhibitor (IC50 = 2.1 nM).

Evobrutinib is discontinued due to commercial reason.

CNX-774 (CNX774) is an irreversible/covalent, orally bioavailable, and highly selective inhibitor of BTK (Bruton’s tyrosine kinase) with potential anticancer activity. It inhibits BTK with an IC50 of<1 nM. CNX-774 acts by forming a covalent bond with the Cys-481 residue within the active site of BTK, which is an key enzyme in the B-cell antigen receptor […]

Tirabrutinib HCl (formerly known as ONO-4059; GS4059; ONO-WG-307; Steboronine), the hydrochloride salt of tirabrutinib, is a selective, covalent/irreversible and orally bioavailable BTK inhibitor approved in Japan for cancer treatment. It inhibits BTK with an IC50 of 2.2 nM. Tirabrutinib covalently binds to BTK within B cells, thereby preventing B-cell receptor signaling and impeding B-cell development. […]

RN486 (RN-486) is a novel, potent, reversible and selective BTK (Bruton’s tyrosine kinase) inhibitor with potential anti-inflammatory activity. It inhibits BTK with an IC50 of 4 nM. RN486 exhibits strong in vivo anti-inflammatory and bone-protective effects in mouse CIA and rat adjuvant-induced arthritis (AIA) models. In the AIA model, RN486 inhibits both joint and systemic […]

Ibrutinib (formerly PCI32765; trade name Imbruvica), an approved anticancer drug, is a covalent/irreversible and orally bioavailable Brutons tyrosine kinase (Btk) inhibitor with potential anti-cancer activity. It inhibits BTK with an IC50 of 0.5 nM in cell-free assays, and exhibits modest potency against other kinases such as Bmx, CSK, FGR, BRK, HCK, less potent to EGFR, […]

CGI1746 (CGI-1746) is a reversible/non-covalent and highly selective small-molecule inhibitor of the Bruton’s tyrosine kinase-Btk with potential anti-inflammatory activity. It inhibits BTK with an IC50 of 1.9 nM. CGI-1746 shows high in vivo antiinflammatory efficacy in an anti-collagen II antibody–induced arthritis (CAIA) model in mice.

Remibrutinib (LOU-064) is a potent, highly selective and orally bioavailable covalent inhibitor of bruton tyrosine kinase (BTK) with an IC50 of 0.023μM. It has the potential for Chronic urticaria (CU) treatment. LOU064 exhibits an exquisite kinase selectivity due to binding to an inactive conformation of BTK and has the potential for a best-in-class covalent BTK […]

ONO-4059 analogue, an analogue of ONO-4059, is a novel, covalent, selective and orally bioavailable BTK inhibitor with potential anticancer and anti-inflammatory activity. It inhibits BTK with IC50 of 23.9 nM. ONO-4059 has demonstrated high antitumor activity in several pre-clinical models. It potently and dose-dependently reverse clinical arthritis and prevented bone damage in the CIA model. […]