GAC0003A4 is an LXR inverse agonist that inhibits LXR transcriptional activity. GAC0003A4 also efficiently degrades LXRβ protein. GAC0003A4 has the potential to be used in advanced pancreatic cancer and other refractory malignancies.

Novel LXR inverse agonist, functioning as LXR a degrader, significantly reducing LXR protein levels in PDAC cell lines

Gilteritinib (ASP2215) hemifumarate is a potent and ATP-competitive FLT3/AXL inhibitor with IC50 of 0.29 nM/0.73 nM, respectively.

Novel Inhibitor of the Mycobacterium tuberculosis Demethylmenaquinone Methyltransferase MenG

GSK3-IN-3 is a mitophagy inducer, inducing Parkin-dependent mitophagy. GSK3-IN-3 is also a GSK-3 inhibitor with an IC50 value of 3.01 μM. GSK3-IN-3 is non-ATP nor substrate competitive and is neuroprotective against 6-OHDA.

Novel selective agonist of the human melanocortin 1 receptor (hMC1R) for sunless tanning and prevention of genotoxicity of UV in melanocytes

Peroxisome proliferator-activated receptor-α/γ (PPAR α/γ) dual agonist

M4K2209 is a potent, selective BMP type I receptor ALK2 inhibitor with IC50 of 9 nM, >180-fold selective over ALK5 (IC50=2427 nM).

Neurokinin receptor antagonist with antiemetic activity

Potent and selective inhibitor of NLRP3, reducing interleukin-1β (IL-1β) production in vivo and attenuating the severity of experimental autoimmune encephalomyelitis (EAE)

Novel mc (maleimidocaproyl) linker plus MMAD (Monomethylauristatin D) to be used for prepare antibodies conjugates via cysteine-capped mechanism

Natural antifungal agent, significantly inducing lipid peroxidation, activating the antioxidant enzymes, and exhibiting effective activity against F. solani (EC50 = 10.56 µM)

mG2N001 is a potent negative allosteric modulator (NAM) of metabotropic glutamate receptor 2 (mGluR2) with IC50 of 93 nM.

Nrf2-Activator is a potent Nrf-2 activator.

Dual dopamine D2 and muscarinic M1 receptor ligand with putative antipsychotic and pro-cognitive potential

Novel potent inhibitor of mTOR activity, significantly suppressing macroscopic and histologic abnormalities associated with chemically-induced murine ulcerative colitis.

Potent and selective inhibitor of diacylglycerol acyltransferase 2 (DGAT2)

PF-06835919, also known as MDK1846, is a potent ketohexokinase (KHK) inhibitor. PF-06835919 is reported in patent US 20170183328 A1, example 4. Increased fructose consumption and its subsequent metabolism have been implicated in hepatic steatosis, dyslipidemia, obesity, and insulin resistance in humans. Since ketohexokinase (KHK) is the principal enzyme responsible for fructose metabolism, identification of a selective KHK inhibitor may help to further elucidate the effect of KHK inhibition on these metabolic disorders.

Novel, potent and specific inhibitor of sphingosine kinase-1 (SphK1)

Pradigastat (LCQ-908) is a potent, selective and orally active diacylglycerol acyltransferase 1 (DGAT1) inhibitor. Pradigastat has anti-obesity and anti-diabetic effects.

Novel potent, selective, and cell active protein arginine methyltransferase 5 (PRMT5) inhibitor

Highly potent, selective, competitive, and reversible inhibitor of monoamine oxidase B (MAO-B)