MK-8245 is an liver-targeting inhibitor of stearoyl-CoA desaturase (SCD) with IC50 of 1 nM for human SCD1 and 3 nM for both rat SCD1 and mouse SCD1, with anti-diabetic and anti-dyslipidemic efficacy.

MK-0941 is a novel Glucokinase activator (GKA)

Olinciguat (IW-1701) is an oral guanylate cyclase (sGC) stimulator with concentration-dependent stimulation of sGC in purified rat and human enzyme assays and a whole cell assay.

LY315920 (Varespladib) is a potent and selective human non-pancreatic secretory phospholipase A2 (hnsPLA) inhibitor with IC50 of 7 nM,. Phase 3.

LY2886721 is an BACE inhibitor used for the treatment of Alzheimer's Disease.

LY2811376 is the first orally available non-peptidicβ-secretase(BACE1) inhibitor with IC50 of 239 nM-249 nM.

LSN3154567 is a novel inhibitor of NAMPT with IC50 of 18 nM (NCI-H1155 cell), 49 nM (Calu-6 cell), 333 nM (HCC1937 cell), and 389 nM (MCF-7 cell), respectively.

LCZ696 is a first-in-class dual inhibitor of the angiotensin II receptor(AT II receptor) and neprilysin; a novel single molecule comprising molecular moieties of valsartan and NEP inhibitor prodrug AHU377 (1:1 ratio).

LB-100 is a small-molecular protein phosphatase 2A(PP2A)inhibitor with IC50 of 0.85 μM and 3.87 μM in BxPc-3 and Panc-1 cells.

L 006235 is a reversible and potent cathepsin K inhibitor that displays more than a 4000 fold selectivity over cathepsins B, L and S.

KML29 is an O-hexafluoroisopropyl carbamate analog of JZL 184 that potently and selectively inhibits MAGL (IC50s = 15, 43, and 5.9 nM in mouse, rat, and human brain proteomes, respectively) over FAAH (IC50s >50 μM).

INCB024360 is a potent IDO1 inhibitor(IC50=10 nM) with desirable pharmaceutical properties, which is poised to start clinical trials in cancer patients.

GKT137831 is a novel and specific dual Nox1/Nox4 inhibitor with Ki of 140±40 nM and 110±30 nM; a potent inhibitor of fibrosis and hepatocyte apoptosis.

GI254023X is a potent MMP9 and ADAM10 inhibitor with IC50s of 2.5 and 5.3 nM, respectively.

Galantamine(Narwedin) is a competitive and reversible cholinesterase(AChE) inhibitor.

Fadrozole is a non-steroidal aromatase inhibitor (IC50s = 5 and 1.4 nM for human placental and rat ovarian microsomal aromatase, respectively).

Epacadostat (INCB024360) is a potent and selective indoleamine 2,3-dioxygenase (IDO1) inhibitor with IC50 of 10 nM. Phase 2.

Edoxaban(DU-176) is an oral factor Xa (FXa) inhibitor in clinical development for stroke prevention

Edoxaban(DU-176) is an oral factor Xa (FXa) inhibitor in clinical development for stroke prevention

E-64D is an inhibitor of cathepsins B and L; also thought to inhibit calpain,showed a potent activity for COVID-19(SARS-COV-2)with EC50: MERS-COV(1.275),SARS-COV(0.760)

E6005 potently and selectively inhibited human PDE4 activity with an IC50 of 2.8 nM and suppressed the production of various cytokines from human lymphocytes and monocytes with IC50 values ranging from 0.49 to 3.1 nM.

Donepezil is a specific and potent AChE inhibitor for bAChE and hAChE with IC50 of 8.12 nM and 11.6 nM , respectively.

DO264 is an inhibitor of α/β-hydrolase domain-containing protein 12 (ABHD12; IC50 = 11 nM).It inhibits ABHD12-dependent hydrolysis of lysophosphatidylserine (lyso-PS) in mouse brain membrane lysates (IC50 = 2.8 nM) and human THP-1 cells.

Cenupatide is an urokinase plasminogen activator receptor (uPAR) inhibitor drug candidate. Cenupatide inhibits uPAR binding to the formyl peptide receptors (FPRs) can improve kidney lesions in a rat model of streptozotocin (STZ)-induced diabetes. Cenupati

Darapladib is a selective and orally active inhibitor of Lp-PLA2 (IC50= 270 pM)

CHS-828 is a pyridyl cyanoguanidine anti-tumor agent that has been identified as a competitive inhibitor of Nampt as well as an inhibitor of NF-κB pathway activity.

CHR-2797 is an aminopeptidase inhibitor, with IC50 values of 100 nM for LAP3 (LAP), 150 nM for PSAP (PuSA) and 220 nM for CD13 (Aminopeptidase N).

CA-074 Me is a selective and cell-permeable inhibitor of cathepsin B.

BVT 2733 is a selective 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor,protecting osteoblasts against endogenous glucocorticoid induced dysfunction.

BIBR 953 (Dabigatran, Pradaxa) is a highly selective, reversible, and potent thrombin inhibitor and is orally available as the prodrug, dabigatran etexilate.