Novel potent TRPV4 antagonist (hTRPV4 IC50 4nM; rTRPV4 IC50 27nM)

Novel potent and highly selective leucine rich repeat kinase 2 (LRRK2) inhibitor

Potent and selective inhibitor of diacylglycerol acyltransferase 2 (DGAT2)

Novel non-brain-penetrant long-acting peptide oxytocin (OT) receptor agonist with increased selectivity for the OT receptor and significantly increased pharmacokinetic stability

Novel potent and selective inhibitor of MAP4K4

Novel tyrosine residues probe, rationally targeting active site

Novel potent and selective inhibitor of MAP4K4

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 prdrug of PF-06843195, a potent PI3Kα-selective inhibitor

Novel SAM Competitive PRMT5 Inhibitor, Demonstrating Antitumor Activity in Splicing Dysregulated NSCLC with Decreased Liability of Drug Resistance

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

Potent, selective non-peptidic antagonist of the V1a receptor

Novel dual H3/4 histamine receptor antagonist

Highly selective, extremely potent Mps1 kinase inhibitor

Potent and selective 5-HT2C receptor agonist

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

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

Antimalarial, actively against Plasmodium liver stages

Potent, ATP-competitive, reversible inhibitor of FAK

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

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

Highly selective, extremely potent Mps1 kinase inhibitor