Nonpeptide partial agonist of oxytocin (OT) and vasopressin V2 receptors

Highly potent NR2B-selective NMDA receptor antagonist

Novel Inhibitor of the malaria parasite protein kinase CLK3, inhibiting the development of liver-stage parasites, killing asexual blood-stage parasites at the trophozoite and schizont stages of the erythrocytic cycle, blocking the development of sexual ga

Antimalarial; Novel inhibitor of HepG2

Potent TRPM8 antagonist, exhibiting antiallodynic properties in pain models

Non-competitive modulator of the proteasome inducing apoptosis a panel of myeloma and leukemia cell lines

Potent and selective antagonist of adenosine A2A receptors

Novel orally bioavailableγ-secretase modulator, reducing Aβ42 levels

Potent CB1 receptor inverse agonist

Aquaporin 1 (AQP1) channel blocker

Novel potent and selective ligand of Brd2(2)

Novel agonist for nicotinic acetylcholine receptors (nAChRs), modestly selectively targeting α6β2 subtype

Novel anti-angiogenesis and vascular disrupting agent, exhibiting moderate inhibitory cell proliferation activity

Novel anti-angiogenesis and vascular disrupting agent, exhibiting moderate inhibitory cell proliferation activity

Novel TBK1/IKKε inhibitor

Highly potent activator of Nrf2; Potent phase 2 cytoprotective pathway inducer and liver carcinogenesis blocker

Novel potent MCT1 inhibitor, exhibiting good single agent anticancer efficacy properties

Novel antibiotic against Mycobacterium tuberculosis (Mtb), potently killing replicating, virulent Mtb H37Rv in a clavulanate-dependent manner

Novel antagonist of IL-6 signaling

Selective mast-cell-stabilizing agent, inhibiting ozone-induced airway hyperresponsiveness

Potential neuroprotective agent, showing effects on cellular models of oxidative stress and neuroinflammation

Novel brain penetrant Cx43 hemichannel blocker

Trans-activator of transcription (TAT) peptide, increasing Hepta-histidine (7H) permeability into cells for treatment of iPS cell-derived neurons carrying Tau or APP mutations suppressed Tau phosphorylation

Novel potent, selective, and orally active CRTH2 antagonist

Potent and selective sphingosine 1-phosphate 1 (S1P1) receptor antagonist (IC50 = 7.8 nM)

Potent and orally active V 1B receptor antagonist with antidepressant and anxiolytic activities in rodents

Tubulin-binding dolastatin-15 analog, demostrating a wide spectrum of In Vivo antitumor activity

Novel selective norepinephrine reuptake inhibitor, displaying significant norepinephrine transporter (NET) inhibitory activity toward the serotonin or dopamine transporters

Potent P-glycoprotein (P-gp) inhibitor

ADAM-17 (TACE) and MMP inhibitor, sensitizing cancer stem cells to the lethal effects of 5-FU and blocking shedding of TNF-α from cell membranes