LPS-123 is a covalently irreversible BTK inhibitor with an IC50 of < 5 nM. LPS-123 simultaneously inhibits the catalytic activity of BTK at Tyr551 and its self-activation at Tyr223. LPS-123 inhibits phosphorylation of the AKT/mTOR and MAPK signaling pathways, activation of PLCγ2, ERK1/2, p38, AKT, and mTOR, and blocks the production of CCL3 and CCL4 chemokines. LPS-123 exhibits significant anti-proliferative activity against various B-cell lymphoma cell lines and effectively induces apoptosis via a caspase-dependent pathway. LPS-123 also demonstrates significant antitumor activity in the OCI-Ly7 xenograft model. LPS-123 can be used for lymphoma research.

CRBN ligand-185 is a CRBN ligand. CRBN ligand-185 can be used as a target protein ligand for the synthesis of PROTACs targeting CRBN (Ligands for Target Protein for PROTAC), such as NX-5948.

TM471-1 is an orally active and covalent Bruton's tyrosine kinase (BTK) inhibitor with IC50 values of 1.3 nM (BTKWT), >40,000 nM (BTKC481S), 7.9 nM (TEC) and 12.4 nM (TXK). TM471-1 inhibits cell growth in vivo and in vitro, arrests cell cycle at G0/G1 phase and induces cell apoptosis.

Midobrutinib (Example 13) is a BTK inhibitor (IC50: 0.813 nM). Midobrutinib can be used for research of diseases involving BTK, particularly cancer.

CFON-026 is a selective, orally active and non-covalent BTK inhibitor with an IC50 of 0.27  nM. CFON-026 has significant antitumor activity against wild-type BTK (TMD8 and REC-1) and all clinically relevant BTK resistance mutations (BTK C481S, T474I, L528W and V416L). CFON-026 induces complete tumor regression in TMD8 xenograft mice model. CFON-026 can be used for research of hematological cancers like chronic lymphocytic leukemia and waldenström macroglobulinemia.

PF-06658607 is an alkynylated irreversible Brutons tyrosine kinase (BTK) inhibitor that covalently reacts with active site cysteines in the ATP-binding pocket. PF-06658607 can be used to detect "off "-targets for covalent kinase inhibitors in cancer cells. The alkyne moiety allows for azide-based detection probe via copper-catalyzed click chemistry.

(Rac)-Ibrutinib alkyne (Compound 8) is a Btk inhibitor with an IC50 of 0.72 nM. (Rac)-Ibrutinib alkyne can effectively inhibit functions related to the B-cell receptor signaling pathway, with an IC50 of 9 nM for inhibiting Ca flux in Ramos cells. (Rac)-Ibrutinib alkyne can be used in the research of diseases such as rheumatoid arthritis.

N-piperidine Ibrutinib hydrochloride (Compound 1) is a reversible Ibrutinib derivative. N-piperidine Ibrutinib hydrochloride is a potent BTK inhibitor with IC50s of 51.0 and 30.7 nM for WT BTK and C481S BTK, respectively. N-piperidine Ibrutinib hydrochloride can be used as a BTK ligand in the synthesis of a series of PROTACs, such as SJF620. SJF620 is a potent PROTAC BTK degrader with a DC50 of 7.9 nM.

Rilzabrutinib (PRN1008) is an orally active Bruton's tyrosine kinase (BTK) inhibitor with anti-inflammatory and immunomodulatory activities. Rilzabrutinib can be used in the research of various inflammatory and immune-related diseases such as acute respiratory distress syndrome and sepsis.

AMX5160 (36) is an orally active BTK inhibitor, with an IC50 of 0.98 nM against mutant BTKC481S. AMX5160 (36) can be used in the research for leukemia, lymphoma, multiple sclerosis, and other autoimmune diseases.

BMS-986195 is a potent, covalent, irreversible inhibitor of Bruton’s tyrosine kinase (BTK).

DZD8586 is an oral, non-covalent, BBB penetrant LYN and BTK dual inhibitor, overcomes resistance mutations to the approved covalent and non-covalent BTK inhibitors.

ACP-5862 is a major metabolite of acalabrutinib and potent and selective covalent BTK inhibitor with IC50 of 5 nM.

GDC-0853 is orally available inhibitor of Bruton's tyrosine kinase (BTK) with potential antineoplastic activity.

BIIB091 is a novel reversible, selective, potent BTK inhibitor with Kd of 0.07 nM.

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

Remibrutinib (LOU064) is a potent, highly selective covalent inhibitor of bruton tyrosine kinase (BTK) with IC50 of 1.3 nM, 2.5 nM and 18 nM for BTK, FcγR-induced IL8 and anti-IgM/IL4-induced CD69, respectively. Remibrutinib (LOU064) exhibits an exquisite kinase selectivity due to binding to an inactive conformation of BTK and has the potential for the treatment of autoimmune diseases.

AS-1763 is an orally available, potent, and selective BTK inhibitor and shows excellent potency against both wild/C481S mutant BTKs with IC50 of 0.85 nM/0.99 nM.

Zanubrutinib is a selective Bruton tyrosine kinase (BTK) inhibitor.

RN-486 is a Bruton's tyrosine kinase (Btk) inhibitor.

PCI-32765 (Ibrutinib) is a potent and highly selective Btk inhibitor with IC50 of 0.5 nM.

PCI 29732 is a selective and irreversible Btk inhibitor with IC50 of 8.2 nM in a FRET based biochemical enzymology assay.

ONO-4059 is a novel Small Molecule Dual Inhibitor Of Bruton’s Tyrosine Kinase (Btk) and Tec Kinase.

FM-A13 is a selective inhibitor of Bruton’s tyrosine kinase (BTK) – IC₅₀’s = 2.5 µM (recombinant BTK) and 17.2 µM (human BTK).

Evobrutinib is an inhibitor of Bruton's tyrosin kinase (Btk) inhibitor extracted from patent US20140162983 example 0174.

AVL-292 is a covalent, highly selective, orally active small molecule inhibitor of Btk currently being evaluated in a Phase 1b clinical trial in relapsed.

ARQ-531 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,

Acalabrutinib (ACP-196) is a second-generation, selective, irreversible inhibitor of BTK.

RSH-7 is a potent Btk and FLT3 inhibitor with IC50s of 47, 12 nM, respectively. RSH-7 induces apoptosis and shows antiproliferative activities. RSH-7 inhibits BTK and FLT3 signaling and shows anti-tumor activity.

(R)-Elsubrutinib ((R)-ABBV-105) is a Btk inhibitor. (R)-Elsubrutinib can be used in studies of immune diseases (such as rheumatoid arthritis, psoriasis, ankylosing spondylitis, asthma, systemic lupus erythematosus) and cancer.