SB-3CT is an effective and selective gelatinase inhibitor with Ki of 13.9 nM and 600 nM for MMP-2 and MMP-9, respectively.

Saxagliptin is a selective and reversible DPP4 inhibitor with IC50 of 26 nM and Ki of 1.3 nM.

Roflumilast (Daxas) is a selective inhibitor of PDE4 with IC50 of 0.2-4.3 nM.

Ro 61-8048 is a potent and competitive kynurenine 3-hydroxylase inhibitor (Ki = 4.8 nM, IC50 = 37 nM).

Rivaroxaban (Xarelto; BAY 59-7939) is a novel, oral, direct Factor Xa (FXa) inhibitor in late-stage development for the prevention and treatment of thromboembolic disorders.

Raphin1 is an orally available selective phosphatase inhibitor improves proteostasis and diminishes deficits in a mouse model of Huntington’s disease.

Praliciguat (IW-1973, IW1973) is a potent, orally available sGC stimulator that concentration-dependently increases the production of cGMP with EC50 of 267 nM.

Potent phosholipase D (PLD) inhibitor (IC50 values are 20 and 25 nM for PLD2 and PLD1 respectively).

PF-2545920 a highly selective and potent PDE10A inhibitor with an IC50 of 0.37 nM.

PF-05221304 is an orally bioavailable, liver-directed and dual ACC1 (and ACC2) inhibitor with IC50s of 7.5 nM for rat ACC1, 8.2 nM for rat ACC2, 12.4 nM for human ACC1 and 8.7 nM for human ACC2. PF-05221304 is a substrate for organic anion transport polyp

Olprinone Hcl(Loprinone Hcl) is a selective phosphodiesterase 3 (PDE3) inhibitor.

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.

Odanacatib (MK 0822) is a potent, selective, and neutral inhibitor of human and rabbit cathepsin K with IC50 of 0.2 nM and 1 nM , respectively.

NSC 405020 is a noncatalytic inhibitor of MT1-MMP, directly interacts with PEX domain of MT1-MMP, affects PEX homodimerization but not catalytic activity of MT1-MMP.

NLG-8189 is an inhibitor of IDO and INDOL1 (IDO2)

ND-630 is an acetyl-CoA carboxylase (ACC) inhibitor; inhibits human ACC1 and ACC2 with IC50 values of 2.1 and 6.1 nM, respectively.

N6022 is a potent, selective, reversible, and efficacious S-Nitrosoglutathione reductase(GSNOR) inhibitor(IC50=10 nM) which is currently undergoing clinical development.

ML 348(ML348) is a selective and reversible lysophospholipase 1 (LYPLA1) inhibitor (IC50 = 210 nM).

MK-8931 is a BACE1 inhibitor. MK-8931 binds significantly to β-secretase.

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)

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.