no cytotoxicity

Flibanserin (Girosa) 一种具有口服活性的 5-HT1A 受体激动剂和 5-HT2A 受体拮抗剂，Ki 值分别为 1 和 49 nM。它与多巴胺 D4 受体结合，Ki 值在 4 到 24 nM 之间。它是一种血清素能抗抑郁药，用于治疗性欲减退症。

Polygalasaponin F 是从瓜子金中提取的齐墩果烷型三萜皂苷，可通过调节TLR4-PI3K AKT-NF-kB 信号通路减少神经炎症细胞因子的分泌，能降低炎性细胞因子肿瘤坏死因子 α 的释放。

Tau-aggregation and neuroinflammation-IN-1 是一种有效的 Tau 蛋白聚集体抑制剂， 对 AcPHF6 和全长 tau 蛋白聚集体显示出显著的抑制活性。Tau-aggregation and neuroinflammation-IN-1具有抗炎活性且可减少 NO 释放。Tau-aggregation and neuroinflammation-IN-1 对 LSP 刺激的 BV2 细胞具有低细胞毒性。Tau-aggregation and neuroinflammation-IN-1 可逆转冈田酸诱导的大鼠记忆障碍。

hURAT1 inhibitor 1 (compound 27b)，一种来源于异苦参碱的口服有效hURAT1 GLUT9双重抑制剂，其IC50s为0.16 μM和4.47 μM，适用于治疗高尿酸血症。在高尿酸血症小鼠模型中，10 mg kg的剂量能显著降低尿酸水平。此外，hURAT1 inhibitor 1在体外没有明显的细胞毒性，在体内也未显示出肝脏毒性，且具有良好的药代动力学（PK）特性。

MC1 作为一种NLRP3抑制剂，具有19.3 nM的KD值，显示出高效性与特异性。同时，MC1无细胞毒性，不会引起肝毒性及其他不良反应，能有效改善认知缺陷。因此，MC1在研究阿尔茨海默病方面具备显著潜力。

Antifungalagent 122 (compound 201)，一种高效广谱抗真菌剂。该化合物可阻止真菌相变及生物膜形成，并能抑制CYP3A4-M和CYP3A4-T酶活性，其IC50值分别为2.11 µM和4.53 µM。此外，Antifungalagent 122不具细胞毒性。

Anticanceragent 263 (compound 7) 是一种有效的抗癌剂，与 G-四链体 DNA (G4) 序列 22-mer Pu22 (c-MycDNA 的模拟物) 结合。作为结构调节剂，它显著增强蛋白质 α-螺旋的形成，并具备构建超分子网络的能力，同时不具有细胞毒性。

PB01 是一种 DPP-4 抑制剂，IC50 为 15.66 nM。该化合物能有效抑制高葡萄糖诱导的 ROS 生成和线粒体超氧化物产生，并显著降低 DPP-4 的细胞表达。PB01 还能显著降低糖尿病小鼠的血糖水平。此外，PB01 在 100 μM 浓度下几乎无细胞毒性，显示出良好的安全性，适合用于糖尿病领域的研究。

α-Glucosidase-IN-79 (Compound 4d9) 是一种具有强效非竞争性抑制作用的α-Glucosidase抑制剂，其IC50为2.11 μM，远优于已有的α-Glucosidase抑制剂Acarbose (IC50为327.0 μM) 和HXH8r (IC50为15.32 μM)。该化合物对人类正常肝细胞(LO2)无细胞毒性，并在大鼠血浆中展示出良好的代谢稳定性，因此有潜力应用于2型糖尿病研究。

SLU-10906 (Compound 63) 是一种具备口服活性的Cryptosporidium抑制剂。在基于细胞的感染模型中，该化合物对寄生虫显示出活性 (EC50= 0.19 μM)，并且没有细胞毒性。SLU-10906 有可能被用于隐孢子虫病的研究。

PPARγ-IN-5 (Compound A3) 是一种PPARγ抑制剂，在肝细胞中有效抑制脂质累积，并在 HepG2 细胞（400 µM）条件下无显著细胞毒性。PPARγ-IN-5 可用于研究非酒精性脂肪性肝病。

SJPYT-310 是一种具有选择性拮抗 PXR 的化合物，并且没有明显的细胞毒性。

O6BTG-C8-αGlu 是一种 O6-甲基鸟嘌呤-DNA甲基转移酶 (MGMT) 抑制剂，具有 0.45 μM 的 IC50 值。在 0.1 μM 浓度时，它能够完全抑制 HeLaS3 细胞中的 MGMT，且即使在长时间高剂量 (高达 20 μM) 条件下，也不显示细胞毒性。O6BTG-C8-αGlu 被用于与 MGMT 相关的癌症研究。

The compound effectively and directly inhibits JAK2 tyrosine kinase autophosphorylation and specifically inhibits ligand-dependent JAK2 activation. It has no cytotoxicity at 100 μM. A 16-hour treatment with compound (1 μM) decreases JAK2 tyrosine autophos

A 30312 is a fused indole, which overcomes multidrug resistance in P388 Adr cells in vitro. It potentiates the cytotoxicity of the antitumor drugs Adriamycin, vincristine and vinblastine in multidrug-resistant cells with no effect on drug-sensitive parent P388 cells.

CL385319 is a potent inhibitor of H5N1 avian influenza A virus infection by blocking viral entry. CL-385319 is effective in inhibiting infection of highly pathogenic H5N1 influenza A virus in Madin-Darby Canine Kidney (MDCK) cells with an IC50 of 27.03±2.

I-XW-053 sodium inhibits the replication of a diverse panel of primary HIV-1 isolates in Peripheral blood mononuclear cell with no appreciable cytotoxicity.

rac-1,2-bis-Palmitoyl-3-chloropropanediol is a 3-monochloropropane-1,2-diol (3-MCPD) ester.1It has been found as a contaminant in edible olive oils, with the lowest and highest concentrations in extra virgin and olive pomace oils, respectively.rac-1,2-bis-Palmitoyl-3-chloropropanediol has also been found in cottonseed and palm oils, as well as in shortening.2It induces renal tubular necrosis and a decrease in spermatids, but no gross pathological changes, in mice.3 1.Hung, W.-C., Peng, G.-J., Tsai, W.-J., et al.Identification of 3-MCPD esters to verify the adulteration of extra virgin olive oilFood Addit. Contam. Part B Surveill.10(3)233-239(2017) 2.MacMahon, S., Begley, T.H., and Diachenko, G.W.Occurrence of 3-MCPD and glycidyl esters in edible oils in the United StatesFood Addit. Contam. Part A. Chem. Anal. Control Expo. Risk Assess.30(12)2081-2092(2013) 3.Liu, M., Gao, B.-Y., Qin, F., et al.Acute oral toxicity of 3-MCPD mono- and di-palmitic esters in Swiss mice and their cytotoxicity in NRK-52E rat kidney cellsFood Chem. Toxicol.50(10)3785-3791(2012)

High affinity and selective cell-permeable p300/CBP-associated factor (PCAF) inhibitor (Ki = 47 nM). Exhibits no significant activity against a panel of 48 other bromodomains except GCN5 (Kd = 600 nM). Exhibits >4500-fold selectivity for PCAF over BRD4. Also exhibits metabolic stability in mouse and human liver microsomes and no observable cytotoxicity in peripheral blood mononuclear cells (PBMC). Moustakim et al (2017) Discovery of a PCAF bromodomain chemical probe. Angew.Chem.Int.Ed. 56 827 PMID:27966810

28-Acetylbetulin is a lupane triterpenoid and derivative of the cholesterol biosynthesis inhibitor betulin that has been found inM. chiapensisand has anti-inflammatory and anticancer activities.1,2It inhibits LPS-induced nitric oxide (NO) and prostaglandin E2production by 55.9 and 69.5%, respectively, in RAW 264.7 cells (IC50s = 4.7 and 1.7 μM, respectively).128-Acetylbetulin induces cytotoxicity in a variety of cancer cells, including A549, HT-29, and MCF-7 cells (IC50s = 14.37, 10.96, and 11.38 μM, respectively).2

CCG-203971 是一种Rho MRTF SRF 通路抑制剂，具有潜在的抗转移作用。它有效靶向 RhoA C 激活的 SRE 荧光素酶，IC50为 6.4 μM。它抑制 PC-3 细胞迁移，IC50为 4.2 μM。

YHO-13177 是高活性乳腺癌耐药蛋白多药转运通道（BCRP）抑制剂，可增强SN-38活性。

Aldose reductase-IN-6 (Compound 3) is a competitive inhibitor of aldose reductase (AR), possessing an IC50 of 3.164 μM and a Ki of 0.018 μM. Notably, Aldose reductase-IN-6 demonstrates no cytotoxicity toward normal cells [1].

Tuberculosis inhibitor 5 (Compound 11i) 是一种有效的抗结核剂，无明显细胞毒性。Tuberculosis inhibitor 5 是一种抗分枝杆菌 (antimycobacterial) 联苯类似物。