Inhibitor of NMDA receptors, used as a veterinary anesthetic, and briefly as a general anesthetic for humans

Novel COX-2 inhibitor

Natural nicotinic acetylcholine receptor agonist

Inhibitor of phagocytosis, interacting with and inhibiting the activating Fc receptors on macrophages, inhibiting downstream signaling pathways driving Fc-mediated phagocytosis

Selective ATP competitive ALK inhibitor

Inhibitor of both Bcr-Abl tyrosine kinase and Aurora kinases

Glycolytic enzyme phosphoglycerate mutase 1 (PGAM1) inhibitor

Novel potent matrix metalloproteinase (MMP) inhibitor, targeting MMPs 1, 3, 9, and 13 (24, 18, 1.9, and 1.3 nM, respectively)

Novel allosteric PGAM1 inhibitor, showing efficacious in multiple preclinical models of pancreatic ductal adenocarcinoma (PDAC), especially with high PGAM1 expression

Novel allosteric PGAM1 inhibitor, showing efficacious in multiple preclinical models of pancreatic ductal adenocarcinoma (PDAC), especially with high PGAM1 expression

Potent and selective antagonist of the VIP1 receptor, inhibiting competitively effect of VIP on the VIP1 receptor mediated stimulation of adenylate cyclase activity with Ki values respectively of 15 ± 5 nM and 2 ± 1 nM for the rat and human VIP1 receptor

Novel anti-HIF-1alpha agent

Water soluble derivative pro-drug of PG490 (triptolide)

Novel inhibitor of Profilin1 (Pfn1), reducing the overall level of cellular filamentous (F)-actin, slowing EC migration and proliferation, and inhibiting the angiogenic ability of EC both in vitro and ex vivo

Novel inhibitor of Profilin1 (Pfn1), reducing the overall level of cellular filamentous (F)-actin, slowing EC migration and proliferation, and inhibiting the angiogenic ability of EC both in vitro and ex vivo

Novel selective inhibitor of both Plasmodium and Cryptosporidium lysyl-tRNA synthetase, clearing parasites from mouse models of malaria and cryptosporidiosis infection.

Negative control for PFI-7 (GLXC012596)

Novel dual CBP/p300 and BRD4 bromodomain inhibitor, downregulating IL-6, IL-ß and IFN-ß in macrophages

Novel fluorophosphonate-based probe, specifically and covalently reacts with the tyrosine-111 residue of the Schistosoma japonicum GST (sjGST) tag, rapidly and site-selectively immobilizes sjGST fusion proteins

Highly selective, extremely potent Mps1 kinase inhibitor

Novel Entry Inhibitor of both CCR5- and CXCR4-Tropic Strains of Human Immunodeficiency Virus Type 1 (HIV-1), Targeting a Novel Site on gp41

Novel potent and selective inhibitor of the activation-loop mutant Kit phosphorylation and tumor growth

Potent, ATP-competitive, reversible inhibitor of FAK

Antimalarial, actively against Plasmodium liver stages

Selective and potent PDK1 inhibitor inducing anti-tumor activity in breast cancer cells

Potent and selective 5-HT2C receptor agonist

Highly selective, extremely potent Mps1 kinase inhibitor

Novel dual H3/4 histamine receptor antagonist

Potent, selective non-peptidic antagonist of the V1a receptor

Natural cyclic tetrapeptide HDAC Inhibitor through the inhibition of PfHDAC1 catalytic activity, potently inducing the synthesis of metallothionein