a-ct

Ponesimod (ACT-128800) 是一种选择性 S1P1可口服激动剂，在放射性配体结合试验中的 IC50值为 6 nM。它可高效激活 S1P1介导的信号转导，EC50为5.7 nM。它可预防淋巴细胞介导的组织炎症，具有潜在的免疫调节活性。

ACT-451840 is a drug of antimalarial activity. It has effective activity against sensitive and resistant Plasmodium falciparum strains.

ACT-209905 is an agonist of S1P1 receptor.

ACT-387042 is a Bacterial Topoisomerase Inhibitor, it has broad-spectrum activity against Gram-positive and Gram-negative bacteria.

2BAct 是一种具有口服活性的高选择性真核起始因子eIF2B 活化剂，EC50为 33 nM。它可防止由慢性综合应激反应引起的神经系统缺陷。

ACT-1004-1239 是一种可口服且具有选择性和高效性的 CXCR7 拮抗剂，具有免疫调节和髓鞘促生作用，用于研究炎性脱髓鞘疾病。

ACT-462206 是一种可口服且可穿过血脑屏障的Orexin 1 Orexin 2 受体拮抗剂。ACT-462206 具有高效性，可用于研究睡眠和焦虑。

ACT-1016-0707 (Compound 49)是一种口服活性及选择性的LPA1受体拮抗剂，主要用于纤维化疾病的研究领域。

ACT-281959, a prodrug of ACT-246475, is a novel potent and selective P2Y12 Receptor Antagonist with a Wider Therapeutic Window in the Rat Than Clopidogrel. ACT-281959 showed antithrombotic efficacy after oral administration in the rat ferric chloride model. ACT-281959 entered clinical studies in healthy volunteers.

ACT-606559，ACT451840的一种代谢物，为新型抗疟活性化合物，可用于研究疟疾。

ACT-660602 是口服具有活力的趋化因子受体 CXCR3 拮抗剂 (IC50: 204 nM)。ACT-660602 能够抑制 T 细胞迁移，并在体内急性肺损伤模型中显示出显著作用。ACT-660602 能够用于研究自身免疫性疾病。

ACT-389949 是一种高效的甲酰肽受体 2 脂蛋白 A4 受体(FPR2) (ALX)选择性激动剂，对 FPR2 ALX 进行内化入单核细胞的EC50值为 3 nM。它对炎性疾病具有潜在的研究价值。

ACT-373898 is a metabolite of the endothelin (ET) receptor type A (ETA) and ETBdual antagonist macitentan .1 1.Dingemanse, J., Sidharta, P.N., Maddrey, W.C., et al.Efficacy, safety and clinical pharmacology of macitentan in comparison to other endothelin receptor antagonists in the treatment of pulmonary arterial hypertensionExpert Opin. Drug Saf.13(3)391-405(2013)

ACT-672125 is a Potent CXCR3 Antagonist with Therapeutic Potential in Autoimmune Diseases. ACT-672125 showed good physicochemical properties and safety profile. In a proof-of-mechanism model of lung inflammation, ACT-672125 inhibited the recruitment of CXCR3 expressing T cells into the inflamed lung in a dose-dependent manner.

ACT-280778 is a potent L T calcium channel blocker.

ACT-451840能够消除敏感和耐药的恶性疟原虫株，具有口服活性、强效、低毒性的优点，在疟原虫的所有无性血液阶段起效迅速，作用机制类似于青蒿素衍生物。在体内实验中，ACT-451840在30 mg kg剂量下表现出极好的抗疟效果，寄生虫减少率达到99.80%。

Setipiprant (ACT-129968) 是一种口服的选择性 CRTH2 拮抗剂，IC50为6.0 nM。

ACT 178882 is a new Renin inhibitor (IC50: 1.4 nM).

ACT-709478 is a potent, selective T-type calcium channel blocker that is orally active and capable of penetrating the brain. It is currently utilized in research focusing on generalized epilepsies[1].

ACT-777991为一种选择性、口服生效的CXCR3拮抗剂，于动物模型中展现出微粒体及肝细胞稳定性，能抑制活化T细胞向CXCL11迁移。

Gallamine is an allosteric antagonist at muscarinic M2 acetylcholine receptors and an inhibitor of acetylcholinesterase.

SLR080811 is a SphK inhibitor. Sphingosine-1-phosphate (S1P) is a ubiquitous, endogenous small molecule that is synthesized by two isoforms of sphingosine kinase (SphK1 and 2). Intervention of the S1P signaling pathway has attracted significant attention because alteration of S1P levels is linked to several disease states including cancer, fibrosis, and sickle cell disease.

GCC-4401C free base is a factor Xa inhibitor similar to rivaroxaban that is currently under development for venous thromboembolic disease (VTE).

CHS-828 nicotinate is a CHS-828 salt with Nicotinic acid.. CHS-828 also known as GMX-1778, is a potent and selective NAMPT inhibitor. CHS-828 inhibits cellular synthesis of NAD. CHS 828 kill tumour cells by inhibiting the nuclear factor-kappaB translocation but unlikely through down-regulation of proteasome. CHS 828 has shown promising anticancer activity in experimental tumor models and primary cultures of cancer cells from patients. CHS 828 showed a synergistic effect with melphalan in 67%, doxorubicin in 47%, etoposide in 38% and Ara-C in 14% of AML samples.