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

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

TM5441 is a novel orrally active TAP-1 antagonist.

TMS is a potent and selective inhibitor of CYP1B1, with an IC50 of 6 nM.

TOFA (RMI14514;MDL14514) is an allosteric inhibitor of acetyl-CoA carboxylase-α (ACCA ).

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

Tolcapone is an orally active catechol-O-methyltransferase (COMT) inhibitor.

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

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.

U-73122 is an inhibitor of phospholipase C, phospholipase A2, and 5-LO (5-lipoxygenase).

Udenafil is a new phosphodiesterase type 5 (PDE5) inhibitor used to treat erectile dysfunction (ED)

UK-371804 is a potent and selective uPA inhibitor with excellent enzyme potency (Ki 10 nM) and selectivity profile (4000-fold versus tPA and 2700-fold versus plasmin).

URB597 is a potent, orally bioavailable FAAH inhibitor with IC50 of 4.6 nM, with no activity on other cannabinoid-related targets.

URB602 is a selective inhibitor of monoglycerol lipase (MGL), exhibiting an IC50 of 28 µM for the rat brain enzyme.

Vardenafil is a PDE5 inhibitor used for treating erectile dysfunction.

VAS2870 is a selective inhibitor of the NADPH oxidases.

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.

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

YC-1(Lificiguat) is a soluble guanylyl cyclase(sGC) activator; binds to the heme-containing domain of the β subunit with Kd value of 0.6-1.1 μM in the presence of CO.

YTX-465 (YTX465) is a specific small molecule that rescues yeast from a-Syn cytotoxicity with EC50 of 15 nM, via inhibiting Ole1, the yeast homolog of human stearoyl-CoA desaturase (SCD).

YW3-56 is a potent peptidylarginine deiminase (PAD) inhibitor with inhibitory activity against PAD2 (IC50=0.5-1 uM) and PAD4 (IC50=1-2 uM), inhibits U2OS cancer cell growth with IC50 of 2.5 uM.

Zifaxaban is a novel, potent, selective, direct and oral factor Xa inhibitor with IC50 of 11.1 nM (human FXa), displays > 10,000-fold selectivity than other serine proteases.