VTP-27999 is an alkyl amine Renin inhibitor; VTP-27999 is useful for Hypertension and End-Organ Diseases.

Vesnarinone is a quinolinone derivative, and its pharmacodynamic effects include inhibition of phosphodiesterase III (PDE3) activity, increases in calcium flux and decreases in potassium flux.

VAS2870 is a selective inhibitor of the NADPH oxidases.

Vardenafil is a PDE5 inhibitor used for treating erectile dysfunction.

U-104 is a potent carbonic anhydrase (CA) inhibitor for CA IX and CA XII with Ki of 45.1 nM and 4.5 nM; low inhibition for CA I and CA II.

TPI-1 is a potent and selective SHP-1 inhibitor effective at low nanomolar levels.

TOK-001 is a multifunctional antiandrogen and CYP17 inhibitor(IC50=47 nM) in castration resistant prostate cancer (CRPC).

TM5275 is an orally available, potent and selective inhibitor of PAI-1 that delivers antithrombotic benefits devoid of bleeding effect in nonhuman primates.

Tipifarnib (IND 58359; R115777) is a potent and specific farnesyltransferase inhibitor with an IC50 of 0.6 nM.

SW033291 is a potent inhibitor of 15-PGDH enzyme with IC50 value of 1.5 nM and dissociation constant Ki app value of 0.1 nM.

SQ 22536 is a inhibitor of adenylyl cyclase (IC50 = 1.4 μM).

SHP099 is a selective, orally bioavailable, and efficacious SHP2 inhibitor with IC50 =0.07 μM and p-ERK modulation in cells IC50 = 0.250 μM.

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.

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

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.

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

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.