Valbenazine 是 四苯喹嗪 α 异构体的前体物质，能够抑制 VMAT2 的功能。

Ezutromid是一个小分子utrophin的调制剂。

Lusutrombopag 是一种可口服的血小板生成素受体 (thrombopoietin receptor) 激动剂，用于治疗慢性肝病。

Acebilustat (CTX-4430) 是一种可口服的白三烯 A4 水解酶抑制剂，用于炎症治疗。

Resmetirom (MGL-3196) 是高度选择性的THR-β激动剂，EC50值为0.21 μM。

Selonsertib是一种选择性的，具有生物口服可利用的凋亡信号调节激酶1 (ASK1) 抑制剂，pIC50 为 8.3。

Deferasirox (ICL 670) 是具有口活性的，用于治疗铁离子过量的螯合剂。

Danicopan (ACH-4471,) is a highly potent, orally active Factor D inhibitor with Kd of 0.54 nM.

A potent, selective, orally availale C5aR (CD88) inhibitor with IC50 of 0.1 nM.

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.

Senicapoc(ICA17043) is a potent and selective Gardos channel blocker; blocked Ca(2+)-induced rubidium flux from human RBCs/ inhibited RBC dehydration with IC50s of 11 nM/30 nM, respectively. IC50 value: 11/30 nM [1] Target: Gardos channel in vitro: I

Desogestrel(Org-2969) is a third-generation 19-nortestosterone derivative progestogen; is contained in many oral contraceptive preparations, both combined (COCs) to ethinyl-estradiol (EE) or alone in a progestin-only pill (POP).

GAL-021 is a new intravenous BKCa-channel blocker.