First-in-class activin antagonist, specifically binding to ALK4, which opens a completely new approach to inhibiting the activity of TGF-beta receptor superfamily members

Novel potent activin antagonist

Novel highly potent and selective MEK4 inhibitor

Novel DNA methytransferase inhibitor, be significantly safer and more effective than decitabine in xenograft models of human leukemia and colon cancer

Novel potent CDK2 inhibitor

Novel potent and selective non-thiazolidinedione partial Peroxisome_proliferator-activated_receptor>PPARγ agonist, acting as an antibiotic effectively against bacterial persisters

Novel potent STAT3 inhibitor

Novel potent STAT3 inhibitor, exhibiting much improved in vivo pharmacokinetic parameters in rats and efficacies against proliferations in multiple cancer cell lines

The first NTR-responsive PROTAC, incorporating the caging group on the Von Hippel-Lindau (VHL) E3 ubiquitin ligase ligand, efficiently degrading the EGFR protein and subsequently exert antitumor efficacy

Novel Allosteric Modulator of RNA Binding Targeting the N-Terminal Domain of TDP-43

Novel nonpeptide potent and selective partial agonist of the Neurotensin receptor type 2 (NTS2)

Novel nonpeptide selective ligand for NTS2

Potent anti-HBV agent, targeting the NTCP-APOA1-HBx-Beclin1-mediated autophagic pathway

Novel free radical scavenger, against light-induced photoreceptor cell damage

Novel inhibitor of neutral sphingomyelinase 2 (nSMase2) for the treatment of neurodegenerative diseases

Novel stimulator of neurogenesis of human hippocampus-derived neural stem cells in vitro and in vivo.

Novel B-Raf(V600E) inhibitor

First-in-class probe of Rad6 function, inhibiting Rad6 function and Rad6-Rad18 interaction in the PCNA ubiquitination cascade

Tyrosyl-DNA phosphodiesterase (Tdp1) inhibitor

Potent inhibitor of endopeptidase activity of botulinum neurotoxin type A light chain (rBoNT/A-LC)

Selective inhibitor of HsEg5

Novel inhibitor of nucleoside hydrolase (NH)

The first reported BoNT/E small molecule inhibitor

Novel inhibitor of lipid metabolism, disrupting tubulin polymerization,suppressing monoglycerol metabolism depleting lipids and inhibiting the growth of both lymphoma and RCC both in vitro and in vivo

Novel inhibitor of poly (ADP-ribose) polymerase-1 (PARP-1)

Telomerase inhibitor, anticancer agent

Telomerase inhibitor, stabilizing G-quadruplex and suppressing cell growth of A549 human lung cancer cells through activation of the ATR/Chk1-dependent pathway

Novel down-regulator of EZH2, inducing G2/M cell-cycle arrest of cancer cells and degradating p53 via proteasome-dependent and -independent pathways

Novel anticancer agent, suppressing the growth of several cell lines derived from lung, colon, breast, ovarian, and kidney cancers

Cytotoxic MDR-selective ligand