KY-226 是一种有效的，选择性的，口服活性的和变构蛋白酪氨酸磷酸酶 1B (PTP1B) 抑制剂，IC50 为 0.25 μM，且不激活 PPARγ 。KY-226 通过增强胰岛素和瘦素信号传导发挥抗糖尿病和抗肥胖作用。KY-226 还可以保护神经元免受脑缺血损伤。

MLN-4760 是一种有效、选择性的人 ACE2 抑制剂，IC50 值为 0.44 nM，对其选择性是对其他相关蛋白的 5000 多倍，包括人睾丸 ACE (IC50，>100 μM) 和牛 carboxypeptidase A (IC50，27 μM)。

A potent, selective, reversible Cdc25 dual specificity phosphatase inhibitor with Ki of 32/96/40 nM for Cdc25A/B/C, respectively.

UE2343 (UE-2343, Xanamem) is a potent, orally bioavailable, brain penetrant 11β-HSD1 inhibitor with IC50 of 24 nM in cell-free assays, with no activity for isozyme 11β-HSD2.

BI-409306 is a potent and selective PDE9A inhibitor, with an IC50 of 52 nM, and shows weak activity against other PDEs.

DS-1001b is a mutant IDH-1 (Isocitrate Dehydrogenase-1) inhibitor extracted from patent WO2016052697A1, Example 168, and has antitumor activity.

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

PF-04447943 is a brain-permeable phosphodiesterase (PDE) inhibitor that is selective for PDE9A (IC50 = 12 nM) over other PDEs (IC50s = >940 nM) in enzymatic assays of second messenger hydrolysis.

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

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).

TAPI-2 inhibits ADAM8, 10, 12, and TACE with Ki values of 10, 3, 100, and 0.12 µM, respectively.

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

Sivelestat(ONO5046; LY544349; EI546) is a competitive inhibitor of human neutrophil elastase(IC50 = 44 nM; Ki=200 nM); also inhibited leukocyte elastase obtained from rabbit, rat, hamster and mouse.

Benzbromarone is a highly effective and well tolerated non-competitive inhibitor of xanthine oxidase, used as an uricosuric agent, used in the treatment of gout.

Vardenafil is a PDE5 inhibitor used for treating erectile dysfunction.

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

Atorvastatin Calcium

A selective, competitive inhibitor of HMG-CoA reductase, that is also antilipemic.