BTK

Tolebrutinib (SAR442168) is a potent, selective, orally active and brain-penetrant inhibitor of Bruton tyrosine kinase (BTK), with IC50s of 0.4 and 0.7 nM in Ramos B cells and in HMC microglia cells, respectively.

(S)-Sunvozertinib ((S)-DZD9008), the S-enantiomer of Sunvozertinib, shows inhibitory activity against EGFR exon 20 NPH and ASV insertions, EGFR L858R/T790M mutation and Her2 exon20 YVMA insertion (IC50=51.2 nM, 51.9 nM, 1 nM, and 21.2 nM, respectively). (S)-Sunvozertinib also inhibits BTK.

BIIB091 is a highly selective, reversible and orally active BTK inhibitor for treating autoimmune diseases.

TAK-020 is a covalent Btk inhibitor, which becomes the clinical candidate.

BTK inhibitor 18 is a potent, selective,orally active and covalent Btk inhibitor with a IC50 of 142 nM.

Elsubrutinib (ABBV-105) is an orally active, potent, selective and irreversible Bruton's tyrosine kinase (BTK) inhibitor。The IC50 of Elsubrutinib for BTK catalytic domain is 0.18 μM.

NX-2127 is an orally effective BTK inhibitor that can induce the degradation of mutated BTKC481S in cells. NX-2127 inhibits the proliferation of TMD8 cells with the BTKC481S mutation more effectively than Ibrutinib. NX-2127 catalyzes the degradation of Ikaros (IKZF1) and Aiolos (IKZF3), corresponding to concentrations of 25 nM and 54 nM, respectively. NX-2127 stimulates T cell activation and increases IL-2 production in primary human T cells.

Atuzabrutinib (SAR 444727) is a potent, selective reversible inhibitor of Btk (Bruton's tyrosine kinase) inhibitor.

JS25 is a selective and covalent inhibitor of BTK that inactivates BTK with an IC50 value of 5.8 nM by chelating Tyr551.

RSH-7 is a potent BTK and FLT3 inhibitor with IC50s of 47, 12 nM, respectively.

Larotinib is a potent broad-spectrum and orally active tyrosine kinase inhibitor (TKI) with EGFR as the main target with an IC50 of 0.6 nM.

JNJ-64264681 is a potent, orally active, selective and irreversible covalent BTK inhibitor.

NRX-0492 is an orally active and potent degrader of BTK.

GBD-9 is a double-mechanism degrader that efficiently degrades BTK and GSPT1 by recruiting the E3 ligase cereblon (CRBN).

KIN-8194 is an orally active dual inhibitor of HCK and BTK, with IC50 values of 0.915 and <0.495 nM, respectively.

BTK-IN-29 (compound 14) is an inhibitor of Btk.

UBX-382 is an orally available proteolysis-targeting chimeras (PROTACs) that target BTK to inactivate B-cell receptor signaling.

BIIB129 is a covalent, selective, small molecule inhibitor of Bruton's tyrosine kinase (BTK) capable of penetrating the blood-brain barrier.

(R,R)-Bexobrutideg is the (R,R)-enantiomer of Bexobrutideg.

DFCI-002-06 is an orally active dual-target HCK/BTK PROTAC degrader with DC₅₀ values for HCK and BTK of 1.3 and 4.5 nM respectively.

Btk inhibitor 1 R enantiomer is an impurity of Ibrutinib. Btk inhibitor 1 R enantiomer can be used in synthesis of Btk inhibitor 1 R enantiomer Ibrutinib dimer and Btk inhibitor 1 R enantiomer adduct. Ibrutinib is a selective, irreversible Btk inhibitor with an IC50 of 0.5 nM.