Novel Disrupter of Glucokinase−Glucokinase Regulatory Protein (GK−GKRP) Binding

Novel potent and selective inhibitor of c-Kit

Novel potent DPP-IV inhibitor

Potent and selective TRPV1 antagonist

Novel selective IRE1α inhibitor

Novel glucokinase activator, decreasing fasting and postprandial glycaemia

Novel disrupter of glucokinase-glucokinase regulatory protein (GK-GKRP) binding, inducing GK translocation from the nucleus to the cytoplasm in rats and blood glucose reduction in mice

Novel transient receptor potential type V1 (TRPV1) receptor antagonist

Novel PDE10 antagonist

Natural thrombin (E.C. 3.4.21.5) inhibitor, suppressing melanin synthesis, regulating the ATM/ATR signaling pathway and the Skp2-p27 axis in human colon cancer cells

Novel modulator of autophagy activity, triggering autophagy in an Atg5-dependent manner, recruiting Atg16 to the pre-autophagosomal site and causing LC3 lipidation

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Novel inducer of inactivation of eIF2-alpha by phosphorylating serine residue 51 in a dose- and time-dependent manner

Downregulator of genes associated with the translation machinery and fatty acid biosynthesis in Serratia, increasing expression of genes related to the uptake of L-proline after RNA-Seq of S39006 to be treated

Antibiotic against Serratia sp. ATCC 39006 (S39006) strain

Reversible cholinesterase inhibitor used in the management of myasthenia gravis

Novel highly potent inhibitor of human alpha/beta hydrolase domain 6 (hABHD6)

Potent FFA1 (GPR40) agonist, inhibiting insulin secretion from isolated pancreatic islets and reducing blood glucose levels

Potent in vitro and in vivo inhibitor of fatty acid amide hydrolase (FAAH)

Novel GPR40 agonist with minimal CNS penetration, superior pharmacokinetic properties and in vivo efficacy comparable to AMG 837

Novel potent, selective, and orally bioavailable PI3Kdelta inhibitor

The first covalent hCB2 antagonist/inverse agonist

Novel Cannabinoid Receptor CB2 antagonist

Novel potent, selective, and orally bioavailable PI3Kdelta inhibitor

Potent GlyT-2 antagonist

Prodrug of ALX5407, a selective non-transportable inhibitor of the glycine transporter GlyT1

Novel lipoxin A4 receptor/formyl peptide receptor 2 (ALX/FPR2) antagonist

Peripherally acting µ-opioid antagonist

Inhibitor of HSP90, leading to the degradation and depletion of its client proteins such as kinases and transcription factors involved with cell cycle regulation and signal transduction

Novel selective dual inhibitor of Cdk1/cyclin B and GSK-3β