Novel selective mTOR inhibitor

Selective 5-HT7 receptor antagonist

Selective 5-HT2C_receptor>5-HT2C inverse agonist

Inhibitor of p38 MAPK

Potent and selective agonist for the human ß3-adrenoceptor

Potent, specific inhibitor of human p38 mitogen-activated protein (MAP) kinase

Dual ETA and ETB receptor antagonist

Selective, active-site-directed 14 kDa PLA2 inhibitor, totally inhibiting LT and PAF formation, while prostanoid formation was not altered

Novel neuroprotective agent, suppressing abnormal tau protein aggregation

Novel reversible covalent inhibitor of the cyclin-dependent kinase 5 (Cdk5)-mediated phosphorylation of PPARγ at Ser245, a key factor in the insulin-sensitizing effect of PPARγ-targeted drugs

PPARγ covalent ligand

Subtype-selective α4β2 nicotinic acetylcholine receptor partial agonist

Inhibitor of H274Y and N294S mutants

Novel inhibitor of salmonella serine acetyltransferase (SAT), the enzyme that catalyzes the rate-limiting step of L-cysteine biosynthesis

Selective non-peptide vasopressin V2 receptor antagonist

Selective non-peptide vasopressin V2 receptor antagonist

Novel potent SARS-CoV-2 MTase Nsp14 and Nsp16 inhibitor

Novel SARS-CoV-2 nsp14 Methyltransferase inhibitor

Novel SARS-CoV-2 Main Protease (Mpro) Inhibitor, inhibiting viral replication with a nanomolar EC 50 value (844 nM) in SARS-CoV-2-infected Vero E6 cells, impairing SARS-CoV-2 replication in human lung epithelial cells and human-induced pluripotent stem ce

Novel potent SARS-CoV-2 3CLpro inhibitor with IC 50 value of 73 nM

Covalent Antineoplastic Agent

Novel Potent Selective Androgen Receptor Degrader (SARD)

Novel Highly Potent Selective Androgen Receptor Degrader (SARD)

Regulator of the sarco-endoplasmic reticulum Ca -ATPase (SERCA1a), significantly slowing down the E2 to Ca2.E1 transition of SERCA1a while it affects neither phosphorylation nor dephosphorylation

Regulator of the sarco-endoplasmic reticulum Ca -ATPase (SERCA1a), significantly slowing down the E2 to Ca2.E1 transition of SERCA1a while it affects neither phosphorylation nor dephosphorylation

Broad spectrum antibiotic

Novel selective and potent dual inhibitor of thrombin and factor Xa

Novel inhibitor of TAFIa (activated thrombin-activatable fibrinolysis inhibitor)

Broad-spectrum antifungal agent, selective inhibiting the cytochrome P-450-dependent ergosterol synthesis in Candida albicans, Aspergillus fumigatus and Trichophyton mentagrophytes, in vitro and in vivo activity against F. pedrosoi

Novel Potent Non-peptidic Inhibitor of Secreted Aspartic Protease 2 (SAP2) for the Treatment of Resistant Fungal Infections