BAY 85-8501 (BAY85-8501) is a potent, selective human neutrophil elastase (HNE) inhibitor with IC50 of 65 pM.

AZD-3988 is a potent and selective diacylglycerol acyltransferase (DGAT-1) inhibitor (IC50 = 0.6 nM).

AZD3293 is a potent and selective orally active, brain-permeable BACE1 inhibitor,currently in development as a potential treatment for early Alzheimer’s disease.

AZD2716(AZD-2716) is a novel potent, selective, orally bioavailable sPLA2 inhibitor with excellent plasma sPLA2 inhibition (IC50=0.1 nM).

AMG-579 is a potent, selective, CNS penetrant, orally bioavailable PDE10A inhibitor with IC50 of 0.1 nM.

AMG 580 (AMG580) is a novel potent, selective phosphodiesterase 10A (PDE10A) inhibitor with IC50 of 0.13 nM.

ALDH3A1 inhibitor EN40 is a potent and selective, covalent, in vivo-active inhibitor of ALDH3A1 with IC50 of 2 uM, demonstrates no activity against ALDH1A3 and ALDH6A1 at 30 uM.

Abiraterone (CB-7598) is a potent CYP17 inhibitor with IC50 of 2 nM.

A selective, reversible inhibitor of MAO-A and serotonin reuptake inhibitor as an antidepressant..

A selective, reversible inhibitor of MAO-A and serotonin reuptake inhibitor as an antidepressant..

A selective protein phosphatase PHLPP inhibitor with IC50 of 4 uM for PP2C domain of PHLPP2.

A potent, selective, competitive, orally active dipeptidyl peptidase-4 (DPP-4) inhibitor with IC50 of 13 nM.

A potent, selective, competitive, orally active dipeptidyl peptidase-4 (DPP-4) inhibitor with IC50 of 13 nM.

A potent, selective, brain penetrant PDE9A inhibitor with IC50 of 1.8 nM.

A potent, selective MMP-2 inhibitor with Ki of 230 nM.

A potent, selective dipeptidyl peptidase-4 (DPP-4) inhibitor for treatment for type 2 diabetes..

A potent, selective and orally active human neutrophil elastase (HNE) inhibitor with Ki of 12 nM.

A potent, selective adenylyl cyclase AC5/6 inhibitor with IC50 of 7.7/17 uM, respectively.

A potent, relatively selective and orally active adenylyl cyclase 1 (AC1) inhibitor with IC50 of 10 uM (cAMP production inhibition).

A potent, orally available hydrophobic aminopeptidase inhibitor that structurally mimics the aminopeptidase inhibitor Tostedostat..

A potent, orally active, centrally acting aminopeptidase inhibitor, the prodrug of the specific and selective aminopeptidase A inhibitor EC33.

A potent, covalent, orally active ALDH1A2 inhibitor with IC50 of 0.3 uM.

A potent, brain penetrant, dual MAO-A and AChE inhibitor that shows neuroprotective effects both in vitro and in vivo.

A potent monoamine oxidase B (MAO-B) inhibitor..

A potent aromatase inhibitor for the treatment of hypogonadism..

A potent and selective, brain penetrant FAAH inhibitor with IC50 of 11 nM.

A novel potent, selective, orally available DPP-4 inhibitor with IC50 of 9 nM.

A novel potent, selective, brain-penetrable and orally active PDE2A inhibitor with IC50 of 1.5 and 4.2 nM for human and rat PDE2A, respectively.

A novel potent, selective PDE9A inhibitor with IC50 of 11 nM, >45-fold selectivity over other PDE isoforms.

A novel potent, selective PDE5 inhibitor with IC50 of 0.056 nM for PDE5A1.