well-tolerated

Nimodipine (BAY-e 9736) 是一种具有口服活性，耐受性良好的光敏二氢吡啶钙拮抗剂。它可研究脑血管疾病。

Balsalazide sodium hydrate (Balsalazide disodium) 可通过调节IL-6 STAT3通路起抑癌作用，可用于治疗炎症性肠病。

CSRM617 hydrochloride 是转录因子ONECUT2(OC2，雄激素受体 AR 的主要调节剂) 的选择性小分子抑制剂，在 SPR 测定中Kd 为 7.43 uM，直接与 OC2-HOX 结构域结合。CSRM617 hydrochloride 通过裂解 Caspase-3 和 PARP 诱导细胞凋亡 (apoptosis)。CSRM617 hydrochloride 在小鼠的前列腺癌模型中具有良好的耐受性。

Atabecestat (JNJ-54861911) 是一种具有口服活性和脑渗透性的 β-位淀粉样蛋白前体蛋白裂解酶 1 (BACE1) 抑制剂，减缓临床前阿尔茨海默病参与者的认知能力下降。Atabecestat 可用于研究阿尔茨海默氏病。

R1498 is an inhibitor of cyclin-dependent kinase 2. It also acts by targeting angiogenesis and mitosis pathways. It is well-tolerated and orally active for hepatocellular carcinoma and gastric cancer treatment.

Bersiporocin是一种新型的脯氨酸-tRNA合成酶（PRS）抑制剂，通过下调胶原蛋白合成发挥抗纤维化作用, 临床中有良好的耐受性。在特发性肺纤维化（IPF）的细胞和动物模型中，DWN12088显著减少了胶原蛋白的合成并改善了肺功能。

oxepinac 是一种治疗疼痛性骨关节炎的有效且耐受性良好的化合物。oxepinac 在动物实验中对小鼠和家兔胎儿无致畸作用。

Levodropropizine ((S)-(-)-Dropropizine) 是一种组胺受体抑制剂，可用作外周镇咳药。

Propafenone (Propafenonum) 是钠通道阻滞剂，它对 β 受体具有高亲和力 (IC50=32 nM)。它能够阻断瞬时外向钾电流 (Ito) (IC50: 4.9 nM) 和持续延迟整流器K+电流 (Isus) (IC50: 8.6 nM) ，具有抗心律失常的作用。它能够诱导线粒体功能障碍及诱导细胞凋亡，从而抑制食管癌增殖。

Epalrestat (ONO2235) 是醛糖还原酶抑制剂，在长期治疗中具有良好的耐受性。 它可以有效改善糖尿病神经病变的相关症状并延缓疾病的进展，特别是在微血管病变有限且血糖控制良好的患者中。

Cefodizime 是一种新型头孢菌素抗生素，具有广泛的生物活性。Cefodizime 对肾脏没有毒性且具有良好的耐受性和免疫调节活性，具有抗菌活性，可用于研究呼吸系统和泌尿系统的严重感染。

Velpatasvir (GS-5816) 是一种的 HCV NS5A 抑制剂。它也是 SARS-CoV 3CLpro 的抑制剂，IC50为 2.16 μM。

Faldaprevir（法达瑞韦）是一种口服有效的选择性非共价HCV NS3 4A蛋白酶抑制剂，对HCV 1a和1b基因型的抑制活性高（Ki=2.6 nM &2.0 nM）。Faldaprevir通过阻止病毒前体蛋白的分解来抑制病毒复制，具有良好的抗丙型肝炎病毒活性和耐受性。

CP-547632 hydrochloride is a well-tolerated and orally-bioavailable inhibitor of the VEGFR-2 and basic FGF kinases (IC50s: 11 nM and 9 nM) with antitumor efficacy.

OSI-296 is a potent and dual inhibitor of cMET and RON kinases (IC50 value are 42 nM and 200 nM for cMet and sfRon respectively) . OSI-206 shows in vivo efficacy and is well tolerated in tumor xenografts models upon oral dosing. OSI-296 also reduces tumou

JNJ-38158471 (CS-2660) 是一种耐受性好的，有口服活性的、高效的、选择性的 VEGFR-2抑制剂 (IC50:40 nM)，还能抑制 Ret (IC50:180 nM) 和 Kit (IC50:500 nM)。

CSRM617 is a selective small molecule inhibitor of the transcription factor ONECUT2 (OC2, the main regulator of androgen receptor). The Kd in SPR analysis is 7.43 uM, which can directly bind to the OC2-HOX domain. CSRM617 induces apoptosis by cleaving the

Dextrorotation nimorazole phosphate ester is an anti-anaerobic and anti-parasitic agent. D-morpholine ornidazole organic phosphate is a newly developed, highly efficient, well-tolerated fourth-generation nitroimidazole derivative. Objective: Antibacterial

EPI-589, a quinone derivative and oxidoreductase enzyme inhibitor, is considered safe and well tolerated, showing promise for the treatment of amyotrophic lateral sclerosis (ALS).

PF-0463481 is safe and well-tolerated and has the potential for the study of diabetic nephropathy. PF-0463481 is an effective and orally active dual CCR2 CCR5 antagonist. It also has comparable human and rodent CCR2 potency (rat IC50=20.8 nM). PF-0463481

BAY-707, a highly potent and selective substrate-competitive inhibitor of MTH1 (NUDT1) with an IC50 of 2.3 nM, is well-tolerated in mice and exhibits a favorable pharmacokinetic (PK) profile compared to other MTH1 compounds. However, it demonstrates a clear lack of anticancer efficacy both in vitro and in vivo[1].

BMS-962212, a direct, reversible, and selective factor XIa (FXIa) inhibitor, demonstrates fast pharmacodynamic (PD) response onset and rapid elimination with a well-tolerated profile. It dependently increases activated partial thromboplastin time and decreases FXI clotting activity exposure [1].

G-744 is a selective and orally active inhibitor of Btk (IC50: 2 nM). G-744 is well-tolerated, metabolically stable. It also has an efficacious to treat arthritis.

GDC-0339 是可口服的、耐受性良好的泛 Pim 激酶高效抑制剂，具有研究多发性骨髓瘤的潜力，对 Pim1、Pim2 和 Pim3 作用的 Ki 值分别为 0.03、0.1 和 0.02 nM。