Novel Foxo1 inhibitor, exerting anti-diabetic and anti-hypertriglyceridemic effects by improving blood glucose and triglyceride metabolism at the gene expression level

Second-generation potent orally-active thrombopoietin (TPO) receptor agonist

Novel GPR119 agonist, potentiating insulin secretion from rat islets and having potent anti-diabetic effects in ICR and diabetic db/db mice

Potent factor Xa inhibitor with significant oral anticoagulant activity

Inhibitor of serotonin (5-HT) and norepinephrine (NE) reuptake, significantly restoring decreased insulin-like growth factor 1 and fibroblast growth factor 2 mRNA levels in dorsal root ganglion and spinal cord, respectively

Inhibitor of D-amino acid oxidase (DAAO)

Novel Potent and Selective Inhibitor of CDC7 Kinase for the Treatment of Solid Cancers

Non-steroidal selective estrogen receptor modulator (SERM)

Inhibitor of the inflammatory responses via NF

The first human arylsulfatase A reversible inhibitor, impairing mouse oocyte fertilization

Selective alpha-7 agonist

Novel potent and selective BRAF inhibitor

Novel selective estrogen receptor degrader (SERD), inducing regression in a tamoxifen-resistant breast cancer xenograft

Novel dual inhibitor of the fatty acid amide hydrolase (FAAH) and the cyclooxygenase (COX) enzymes

Regulator and promotor of immune functions, enhancing the role of macrophages, inhibiting bacteria growth, improving the protein metabolism, and regulating liver function

Natural inhibitor of recombinant purified ClpXP and ClpYQ AAA+ proteases, exhibitung potent antibacterial activity against H. pylori, including multidrug-resistant strains

Selective ecto-ATPase inhibitor, preventing metabolism of P2 purinoceptor agonists

P2T (P2YADP) purinoceptor antagonist

Novel inhibitor of Ark1, the fission yeast member of the conserved Aurora kinase family

Novel selective inhibitor of PREP, displaying great selectivity over FAP, while also not inhibiting the DPPs.

Potent tumor-homing tripeptide, targeting heat shock protein 70 (HSP70)

Long-acting beta-2 adrenergic agonist

Long-acting beta-2 adrenergic agonist

Negative control for ARCC-4, binding androgen receptors (AR) without inducing degradation.

Anticancer agent, inducing apoptosis mediated at least in part by the ERS pathway and inhibiting hepatoma tumor growth

Highly potent and selective fluorescent probe of Rho kinase (ROCK)

Highly potent CK2α inhibitor (K(i) = 0.5 nM), revealing high selectivity for CK2α in a panel of 140 protein kinases

Novel inhibitor of lactate transporters (monocarboxylate transporters; MCTs)

Novel immunosuppressant and monocarboxylate transporter inhibitor, reducing immune responses both in vitro and in vivo, maintaining long-term graft survival, and inducing operational tolerance

Novel 5-hydroxytryptamine 1B (5-HT 1B ) autoreceptor antagonist