γ-Secretase modulator (GSM) photoaffinity probe, revealing distinct allosteric binding sites on presenilin

Novel OPG/RANKL upregulator, increasing OPG expression without affecting RANKL expression, promoting osteoblast differentiation while inhibiting osteoclast differentiation, regulating OPG expression through canonical Wnt/β-catenin signaling

Novel potent Inhibitor of PI3Kalpha

Novel Selective and Potent EGFR Inhibitor, Overcoming T790M-Mediated Resistance in Non-Small Cell Lung Cancer

Antitumor antibiotic

Novel allosteric inhibitor of the tumor-promoting interaction between the oncogenic factor AIMP2-DX2 and HSP70

Novel Hsp70 agonist, showing no cellular toxicity and induced cellular stress response pathways

Novel and potent leukotriene B(4) receptor antagonist

Novel potent and highly selective inhibitor of VEGFR, exhibiting antitumor activities both in vitro and in vivo.

Potent and selective 5-HT 2A receptor antagonist

Selective 5-HT2A receptor antagonist

Anthracycline antibiotic from Streptomyces

Irreversible DNA minor groove binding alkylating agent, disrupting the nucleic acid architecture and leading to tumor cell death

Antiviral agent against influenza A, parainfluenza Sendai, coxsackie A21, and rhinovirus

Potent and selective degrader of mutant FKBP12F36V fusion proteins

Negative control for DT2216

Novel potent and orally active activator of PP2A

Agonist of S1P receptors

Novel selective mGlu5 receptor negative allosteric modulator (NAM) with potent antidepressant and antimanic activity

Novel potent Dihydroorotate Dehydrogenase (DHODH) inhibitor

Novel Plasmodium falciparum Dihydroorotate Dehydrogenase (PfDHODH) Inhibitor (Pfalcip cells: 0.0018 μM)

Non-toxic human papillomavirus E6 inhibitor

Pathogen motility inhibitor of EcDsbA

Novel Potent, Orally Available G9a/GLP Inhibitor for Treating β-Thalassemia and Sickle Cell Disease

Novel potent orally active hepcidin production inhibitor

Novel non-macrolide GPR38 agonist

Novel and orally bioavailable PTHR1 antagonist

Novel potent orally active hepcidin production inhibitor

Novel selective PPARγ modulator, resulting in robust plasma glucose reductions with excellent DMPK profiles

Novel potent PTHR1 antagonist