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

Novel selective and reproducible inhibitor of DNA synthesis in E. coli JL553

Novel potent and selective RORγT inhibitor, showing no appreciable activity against a panel of related nuclear hormone receptors

Novel potent RORγT inhibitor

Novel potent and selective RORγT inhibitor, showing no appreciable activity against a panel of related nuclear hormone receptors

Novel peripheral CB1R antagonist, being highly biased toward inhibiting CB1R-induced β-arrestin-2 (βArr2) recruitment over G-protein activation

Activator of MrgX1 receptor signaling

Novel positive allosteric modulator (PAM) of mas-related G protein-coupled receptor X1 (MRGPRX1), reducing behavioral heat hypersensitivity in humanized MRGPRX1 mice, demonstrating the therapeutic potential in treating neuropathic pain

Novel inhibitor of the main protease (Mpro) of SARS-CoV-2