Highly potent and selective tankyrase inhibitor

Novel highly potent and selective TNKS2 inhibitor with antiproliferative effects in a colorectal cancer cell line (DLD-1) where the Wnt pathway is constitutively activated

Novel selective inhibitor of TNKS-USP25 interaction, effectively reducing prostate cancer cell proliferation and tumor growth

Novel non-nucleoside reverse transcriptase inhibitor of HIV-1

Emivirine analog with improved activity against drug-resistant HIV mutants

Novel inhibitor of tumor necrosis factor-α (TNF-α)

Novel potent inhibitor of TNF-α

Novel activator of necrostatin-1 sensitive necroptotic cell death, triggering apoptosis, autophagy and necroptosis crosstalk in chronic myeloid leukemia

Allosteric agonist and positive allosteric modulator (PAM) of 5-HT3 receptor

Novel caged protein labeling agent

Novel degrader of E. coli DHFR (eDHFR), as well as eDHFR-EGFP fusion proteins, demonstrating that degradation does not require covalent attachment of the tag to the target protein

Dual Inhibitor of SIRT2 Deacetylase and Defatty-Acylase Activities

Novel protease inhibitor (PI) against a variety of HIV-1 strains, including multi-PI-resistant strains, and may be less likely to generate resistance, also showing antiviral avtivity as a potential treatment for COVID-19 caused by SARS-CoV-2

Penem beta-lactam antibiotic

Novel inhibitor of plasminogen activator inhibitor-1 (PAI-1)

Novel inhibitor of both JAK/STAT and proteasome activities, inducing cell death in myeloma cells

Potent histone methyltransferase inhibitor with rapid antimalarial activity against all blood stage forms in Plasmodium falciparum

The first small molecule inhibitor of translesion synthesis (TLS) that target Rev1-CT

Novel toll-like receptor 8 (TLR8) inhibitor, potently and selectively reducing TLR8-mediated signaling

Novel potent and selective dual TLR7/8 inhibitor

Novel Toll-Like Receptor 4 (TLR4) Inhibitor

Novel Insulin Receptor Modulator

The first small molecule degrader, inducing anaplastic lymphoma kinase (ALK) degradation, including in non-small-cell lung cancer (NSCLC), anaplastic large-cell lymphoma (ALCL), and neuroblastoma (NB) cell lines

The first small molecule degrader, inducing anaplastic lymphoma kinase (ALK) degradation, including in non-small-cell lung cancer (NSCLC), anaplastic large-cell lymphoma (ALCL), and neuroblastoma (NB) cell lines

Novel AC220-based FLT3 degrader

Novel AC220-based FLT3 degrader

Anti-arrhythmia agent

hPPAR-pan agonist

Dual PPA

hPPAR