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

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

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

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

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

Inhibitor of DNA damage repair

Novel inhibitor of DNA damage repair

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

Novel potent and selective SETD8 inhibitor

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

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

Novel inhibitor of SLC16A3

Novel potent and selective PI3Kδ inhibitor

Potent TRPV1 agonist

Novel potent broad-spectrum metallo-β-lactamase (MβL) inhibitor, inhibiting the MβLs NDM-1, VIM-2, ImiS, and L1

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

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

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 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

Selective antagonist of melanocortin-4 receptor (MC4R)

Novel Mithramycin A (MTM) 2'-oxime (MTMox) conjugate, displaying an 11-fold increase in plasma exposure and improved efficacy in an Ewing sarcoma xenograft

Novel, potent, and selective brain-penetrant ATP-competitive mTOR inhibitor