Potent and selective agonist of GABAA receptors α5 subunit

Selective agonist of GABA A receptors α5 subunit

Novel inhibitor of the CML mutant Bcr-AblT315I, preempting in vitro resistance when combined with nilotinib or dasatinib.

Novel Potent SGLT1/2 Dual Inhibitor

Novel highly selective SGK1 inhibitor with a highly optimized profile suitable for oral dosing as a potentially disease-modifying agent for osteoarthritis

PKM2 activator, potently inhibiting proliferation of cancer cells in media lacking serine

PKM2 activator, potently inhibiting proliferation of cancer cells in media lacking serine

Novel potent allosteric modulator of N-methyl-D-aspartate receptors (NMDAR)

Negative control for SGC-GAK-1 (GLXC-31266)

Novel probe for CLK1, CLK2, and CLK4

Novel probe for CAMKK2/CAMKK1

Highly Potent and Selective Plasmin Inhibitor, Attenuating Fibrinolysis in Plasma

Cell-permeable antagonist of secreted frizzled related protein-1(sFRP-1), inhibiting Wnt-3/frizzled interaction and restoring cellular response to Wnt-3 stimulation

Novel anticancer agent, arresting cell cycle in S-phase and causes DNA replication stress leading to the phosphorylation of H2AX into gamma-H2AX

Novel dual inhibitor of BRD4 and PI3K, inhibiting BRD4, PI3Kα, PI3Kδ, and PI3Kγ with IC 50 values of 277, 714, 27, and 1170 nM, respectively

Potent, selective, and highly brain-penetrant NPY Y2 receptor antagonist

Potent and selective STAT5 inhibitor

The First potent SecA inhibitor

Novel telomerase inhibitor

Novel potent CYP17 lyase inhibitor, inhibiting androgen production without mineralocorticoid excess or cortisol depletion

Novel inhibitor of Mycobacterium marinum MelF (Rv1936), exhibiting bacteriostatic/bactericidal activity against M. marinum and M. tuberculosis in vitro

The most potent inhibitor of Set7, inhibiting the KMTase G9a

The first-in-class triple-site aaRS inhibitor, targeting Salmonella enterica threonyl-tRNA synthetase (SeThrRS) with IC 50 = 19 nM and K d = 35.4 nM

Highly selective H1 receptor antagonist

Cytochrome P450 14α-demethylase inhibitor, also acting as a BuChE-IDO1 inhibitor

Novel serotonin reuptake inhibitor

Novel mitochondrial KIM-1 receptor modulator to be specifically internalized by renal tubular epithelial cells via KIM-1 receptor-mediated endocytosis and then actively distributed in mitochondria under the effect of TPP, effectively ameliorating injured

Selective inhibitor of the phosphatase regulatory subunit PPP1R15A (R15A) that prolong the benefit of eIF2α phosphorylation, thereby protecting cells from proteostatic defects

Novel selenium-nonsteroidal anti-inflammatory drug (Se-NSAID), inhibiting colorectal cancer (CRC) growth via the inhibition of the cell cycle in G1 and G2/M phases and reduces the cell cycle markers like cyclin E1 and B1 in a dose dependent manner

Sentrin-specific protease 1 (SENP1) inhibitor