The first small-molecule substrate identified with high selectivity for BGT1 over the three other GAT subtypes; M1 muscarinic agonist

Novel dual inhibitor of norepinephrine transporter (NET) function and thyrointegrin αvβ3 receptor

Novel Aldose_reductase_inhibitor>aldose reductase (ALR2) inhibitor

Potent inhibitor of centrosomal clustering in malignant cells

Novel potent and selective inhibitor of kynurenine aminotransferase II

Novel probe for neurofibrillary tangles (tau fibrils)

Novel HIF Prolyl Hydrolase Inhibitor, preventing colonic inflammation and fibrosis in murine models of inflammatory bowel disease

Novel BET inhibitor, selectively targeting BRD4-BD1 bromodomain

Novel Dual BET-BRD7/9 Bromodomain Inhibitor, showing a strong antiproliferative effect on various cancer cell lines that could not be observed for BD family selective inhibitors

Selective beta-1 adrenergic receptor antagonist with antihypertensive and anti-glaucoma activities and devoid of intrinsic sympathomimetic activity

Natural antibiofilm agent and adjuvant on the antifungal therapy related to resistant infections caused by C. glabrata

Phytoestrogen, possessing typical curare-like action

Potent ligand of the serotonin (5-HT) and dopamine (DA) transporters used in diagonisis of Parkinson's disease as SPECT imaging precursor

Novel negative allosteric modulator of the ß2-adrenergic receptor (ß2AR), inhibiting cAMP production through the ß2AR, but not that mediated by other Gs-coupled receptors, also inhibiting ß-arrestin recruitment to the activated ß2AR

Novel selective inhibitor of plasma kallikrein, blocking the enzymatic activity of plasma kallikrein in releasing bradykinin, the major biologic peptide that promotes swelling and pain associated with attacks of HAE

Novel inhibitor of plasma kallikrein

Novel antibacterial agent against multidrug-resistant Escherichia coli at low concentrations as 0.007 mM, disintegrating membrane, accelerating ROS accumulation, reducing bacterial metabolism, and intercalating into DNA groove

Novel antibacterial agent against multidrug-resistant Escherichia coli at low concentrations as 0.007 mM, disintegrating membrane, accelerating ROS accumulation, reducing bacterial metabolism, and intercalating into DNA groove

Long-acting calcium-blocking agent with significant anti-anginal activity

Useful pharmaceutical building block

Anorectic, primarily promoting weight loss through reduced appetite

Inhibitor of 4-hydroxyphenylpyruvate dioxygenase (HPPD), acting as a herbicide

anti-HSV agent

Potent D2/D4 dopamine receptor antagonist, neuroleptic and antipsychotic

Antiandrogen, being effective in the treatment of acne, seborrhea, and hirsutism in women

Irreversible and nonselective Monoamine_oxidase_inhibitor>monoamine oxidase inhibitor (MAOI)

Novel inhibitor of HIV-1 Rev function, also acting as a cytostatic agent with substantial antiretroviral activity

Novel potent PI3K inhibitor, suppressing metastasis of non-small cell lung cancer cells by modulating β-catenin/ZEB1 regulatory loop, blocking AKT phosphorylation

Inhibitor of angiotensin-converting enzyme (ACE); Prodrug of benazeprilat

Inhibitor of monoamine oxidase; Anti-serotonin agent