Selective antagonist of melanocortin-4 receptor (MC4R)

Novel resveratrol-based multitarget-directed ligand, cellularly activating the NRF2-ARE pathway (CD = 9.83 μM), selectively inhibiting both hMAO-B and QR2 (IC 50 s = 8.05 and 0.57 μM), and promoting hippocampal neurogenesis

Novel minimized theta-defensin, being highly effective against CRE pathogens K. pneumoniae and E. coli in vivo, significantly enhancing survival by promoting rapid host-mediated bacterial clearance and by modulating pathologic cytokine responses, restorin

Novel antituberculosis agent. targeting the respiratory chain of Mycobacterium tuberculosis (Mtb) and being effective against multi drug resistant (MDR) Mtb

Novel BBB permeable potent MT1 and MT2 ligand (MT1, Ki = 0.031 nM; MT2, Ki = 0.070 nM) with good metabolic stability in human hepatic microsomes

Potent TRPV1 agonist

Novel potent and selective PI3Kδ inhibitor

Novel inhibitor of SLC16A3

Novel potent tankyrase (TNKS) inhibitor (EC 50 : 2 nM)

Mitochondrial tRNA-specific modification, regulating efficient mitochondrial translation and energy metabolism in mammals

Novel potent and selective SETD8 inhibitor

Novel inhibitor of Human p53 and CREB Binding Protein (CREBBP) interaction

Novel inhibitor of DNA damage repair

Inhibitor of DNA damage repair

Novel, selective, orally bioavailable, negative allosteric modulator of subtype 5 metabotropic glutamate receptors (mGluR5)

Novel inhibitor of Hedgehog signaling by blocking overlapping binding sites in the transmembrane domain of the Smoothened receptor

Potent inhibitor of TANK-binding kinase-1 (TBK1)/IKKepislon kinases

Novel highly potent A3 adenosine receptor (A3AR) antagonist with Kd values (nM): 0.55 (human), 3.74 (mouse), and 2.80 (rat)

Novel Partial Agonist of Human and Mouse A3 Adenosine Receptors (Ki = 10.9/17.8 nM, at human/mouse A3AR)

Novel highly selective A1 adenosine receptor (A1AR) agonist

Bitopic fluorescent antagonist of the A2A adenosine receptor

Novel potent P2Y14 Receptor Antagonist (IC 50 , 15 nM)

Novel potent antagonist of P2Y 14 receptor (P2Y 14 R) (IC 50 ~20 nM at hP2Y 14 R/mP2Y 14 R)

Novel highly potent human CD73 inhibitor (K i = 0.673 nM)

Potent and selective P2Y6 receptor agonist

Potent P2Y6 agonist

Selective P2Y2 agonist

Selective P2Y6 agonist

Potent P2Y14 receptor agonist

Selective enhancer of the ATP effects at fast desensitizing P2X (P2X1 and P2X3) receptors