Novel Endogenous Reactive oxygen species (ROS)-activated HDAC inhibitor prodrug, demonstrating selective activity against multiple cancer cell lines such as HeLa, MCF-7, MDA-MB-231 and B16-F10, while remaining benign to non-cancer cells

Novel clickable HDAC inhibitor, selectively labeling HDAC complex proteins

Novel Smoothened receptor agonist

Irreversible and nonselective Monoamine_oxidase_inhibitor>monoamine oxidase inhibitor (MAOI)

Peripherally restricted cannabinoid CB1/CB2 receptor agonist, inhibiting gastrointestinal motility with no effect on experimental colitis in mice

Novel ileal Na /bile acid cotransporter inhibitor

Partial benzodiazepine inverse agonist, showing antidepressant-like pharmacological activity and acting as a cognitive enhancer

Novel Analogue of SUN-B8155, acting as a cell active and functionally-relevant agonist of calcitonin receptor (CTR), inducing different Gs or arrestin activities through CTR

Dual PPARα/γ agonist

Novel glucokinase (GK) activator

Novel glucokinase (GK) activator

Potent inhibitor of glucose-6-phosphate translocase (G6P T1)

Novel modulator of the retrograde signaling including cellular responses to hypoxic and oxidative stress, selectively eliminating superoxide production by complex III without altering oxidative phosphorylation

Potent and selective inhibitor of constitutive Stat3 DNA-binding and transcriptional activities

alpha2-Adrenoceptor Antagonist, Norepinephrine Transporter (NET) Inhibitor, Serotonine Transporter (SERT) Inhibitor

Potent quinone reductase 2 (QR2) inhibitor

Potent activator of the AMP-activated protein kinase (AMPK)

Potent and selective ligand of imidazoline 1 receptor (I1R)

Potent and selective ligand of imidazoline 1 receptor (I1R)

Novel selective sigma 1 receptor (S1R) antagonist, exhibiting potent binding affinity for S1R, high selectivity over S2R and 87 other human targets, acceptable in vitro metabolic stability, slowing clearance in liver microsomes, and excellent blood-brain

Novel potent and selective agonist activity for S1PR4

Selective and highly potent alpha2-adrenoceptor agonist

Novel, Potential Antipsychotic Displaying Marked Antagonist Properties at α1- and α2-Adrenergic Receptors

Potent and selective thrombin inhibitor for the treatment of thromboembolic disorders

Inhibitor of NADPH oxidase, preventing the structural and functional sequelae of diet-induced metabolic heart disease

Potent, orally active, partial 5-HT1A receptor agonist

Potent 5-HT1A receptor agonist, also acting as a 5-HT2A and 5-HT2C receptor antagonist

Novel inhibitor of D-cyclin transactivation via phosphoinositide 3-kinase pathway

Novel HIV-1 integrase inhibitor

FP receptor agonist