Novel glucocerebrosidase activator; Non-inhibitory chaperones of glucocerebrosidase

Unique F-box/LRR-repeat protein 2 (FBXL2) activator

GABA-A modulator, blocking the sedative effects without lowering the convulsion threshold

Potent and selective blocker for TMEM16A/Anoctamin-1 (ANO1)

Novel dopamine D3 receptor-selective partial agonist

Selective RIP3 kinase inhibitor

Novel selective PAD4 inhibitor

GSK106 is a negative control compound used in binding and functional assays for PAD4 inhibitors.

Novel Potent and Selective Positive Allosteric Modulators of the delta-Opioid Recepto

FIPI (5-Fluoro-2-indolyl des-chlorohalopemide) hydrochloride, a derivative of Halopemide (HY-119093), is a phospholipase D (PLD) inhibitor with IC50s of approximately 25 nM and 20 nM for PLD1 and PLD2, respectively. FIPI hydrochloride inhibits PLD regulation of F-actin cytoskeleton reorganization, cell spreading, and chemotaxis. FIPI hydrochloride has the potential for autoimmunity and cancer metastasis research.

Selective 5-HT1B serotonin receptor antagonist

A potent and selective inhibitor of mitochondrial Na+/Ca2+ exchanger mNCX with neuroprotective activity. It was shown to reduce Ca2+ efflux from the mitochondria to the cytosol with an EC50 value of 690 nM and was shown to protect against Ca2+ overload an

Novel selective inhibitor of collagen prolyl 4-hydroxylase, neither causing general toxicity nor disrupting iron homeostasis

SGC2085 is a Potent and Selective Coactivator Associated Arginine Methyltransferase 1 (CARM1) Inhibitor with an IC50 of 50 nM and more than undred-fold selectivity over other PRMTs. CARM1 is an important positive modulator of Wnt/β-catenin transcription and neoplastic transformation in colorectal cancer as well as a critical factor in estrogen-stimulated breast cancer growth, and its depletion results in decreased proliferation of myeloid leukemia cells in vivo.

Novel proteasome inhibitor, inducing human myeloid tumor-selective apoptosis

Cytokine release inhibitor, inhibiting production of IL-1ß, IL-8, IL-6, IL-10 and TNFalpha

Negative control for GSK'963 (AOB9775). Novel highly potent and selective RIP1 inhibitor

Novel modulator of the UNC119-Cargo Interaction, potently and selectively inhibiting the binding of a myristoylated peptide representing the N-terminus of Src kinase to UNC119A

Selective estrogen receptor modulator (SERM), inhibiting mammalian PLD (PLD1 and PLD2)

Sultopride hydrochloride (LIN-1418 hydrochloride) is a selective antagonist of dopamine D2 receptor.

Neutral retinoic acid receptor (RAR) α-selective antagonist

CID 2745687 is a competitive, reversible antagonist of the orphan receptor GPR35.