GM6001 (galardin, ilomastat) is a broad spectrum MMPs inhibitor for MMP-1, MMP-2, MMP-3, MMP-7, MMP-8, MMP-9, MMP-12, MMP-14, and MMP-26 with Ki of 0.4-27 nM.

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.

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).

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

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.

Betrixaban (PRT-054021) is a highly potent, selective, and orally efficacious factor Xa inhibitor with IC50 of 1.2 nM(inhibition of Factor 10a).

BEC is a boronic acid-based arginine analog that acts as a slow-binding, competitive transition state inhibitor of arginase I and II (Ki = 310 nM for human recombinant type II arginase, pH 7.5).

Batimastat was used to study the role of MMP in proteolytic release of EGF in human follicular thyroid carcinoma cell line FTC-133.

Balicatib(AAE-581) is a potent and selective inhibitor of cathepsin K; 10-100-fold more potent in cell-based enzyme occupancy assays than against cathepsin B, L, and S.

AZD3839 is a potent and selective BACE1 inhibitor with Ki of 26.1 nM, about 14-fold selectivity over BACE2. Phase 1.

APO866 effectively inhibits nicotinamide phosphoribosyltransferase (NMPRTase) with IC50 of 0.09 nM.

Apixaban is a highly selective, reversible inhibitor of Factor Xa with Ki of 0.08 nM and 0.17 nM in human and rabbit, respectively.

AN-2728 is a topically administered, boron-containing, anti-inflammatory compound that inhibits PDE4 activity and thereby suppresses the release of TNFalpha, IL-12, IL-23 and other cytokines.

Aliskiren hemifumarate(CGP 60536) is a direct renin inhibitor with IC50 of 1.5 nM.

Alda-1 is an ALDH2 agonist, cell-permeable activator of both the wild-type ALDH2*1 and the asian E487K mutant ALDH2*2 forms of mitochondrial aldehyde dehydrogenase 2 (mtALDH2).

AGI-6780 is the first highly potent and selective small molecule inhibitor of isocitrate dehydrogenases, which binds in an allosteric manner at the dimer interface of mutant IDH2-R140Q (IC50=23 nM).