s 46

Pheneturide (Benuride) 是Phenobarbita l 脱羧后的产物，可阻止精神运动性癫痫发作。

TCS 46b 是一种具有口服活性的 NR1A/NR2B NMDA 受体拮抗剂。

CS 461 is a cephalosporin antibiotic that has shown effective antimicrobial activity against a variety of bacteria in vitro and in vivo.

HRS 4642是一种长效和选择性的KRAS G12D抑制剂，Kd值为0.083 nM，能够抑制下游MEK和ERK蛋白的磷酸化，具有抗肿瘤作用。HRS 4642能够缩小靶病灶，在单独使用与联用Carfilzomib时都能够将肿瘤微环境重塑为免疫允许型。

Doripenem monohydrate (S 4661 monohydrate) 是广谱β-内酰胺抗生素，它对革兰氏阳性，阴性和厌氧菌有抗菌作用。

cIAP1 Ligand-Linker Conjugates 8 comprises an IAP ligand for the E3 ubiquitin ligase and a PROTAC linker. This compound is specifically utilized for the purpose of SNIPER design[1].

MRS4608是一种新型的P2Y14受体强效拮抗剂。

MRS4654 是一种新型的高效 P2Y14 受体拮抗剂，具有15 nM 的半最大抑制浓度 (IC50)。

LY-364947 (HTS466284) 是有效的、ATP 竞争性的TGFβR-I 抑制剂(IC50:59 nM)，是对 TGFβR-II 选择性的 7 倍。

WR-S-462 是一种STAT3抑制剂，在体外能有效地阻碍STAT3的磷酸化及其生物学功能。该化合物对MDA-MB-231细胞的IC50为0.03 μM，并表现出对STAT3蛋白的强结合亲和力，其Kd为58 nM。WR-S-462 能抑制p-STAT3的核转位，特异性抑制MDA-MB-231细胞中p-STAT3Tyr705的表达，以及由STAT3调控的下游靶基因如Cyclin D1、Bcl-2和Bcl-xl的表达。此外，WR-S-462 有效抑制三阴性乳腺癌 (TNBC) 的生长和转移。

Doripenem 是对革兰氏阳性菌、阴性菌和厌氧菌有效的β-内酰胺广谱抗生素。

BMS-466442 is the first selective amino acid transporter alanine serine cysteine transporter-1 inhibitor.

Cloprednol is a synthetic glucocorticoid. It has an anti-inflammatory potency twice that of prednisone.

GS-462808 is a late sodium current inhibitor of the cardiac Nav1.5 channel. GS-462808 had lower brain penetration and serendipitously lower activity at the brain isoforms.

Nitrosofolic acid is a folic acid derivaive.

PXS-4681A is a powerful, specific, and irreversible inhibitor of semicarbazide-sensitive amine oxidase (SSAO; VAP-1), with an oral activity and a Ki value of 37 nM. It exhibits exceptional selectivity towards related amine oxidases, ion channels, and seven-transmembrane domain receptors. Additionally, PXS-4681A demonstrates potent anti-inflammatory properties.

GTS467 is a EAAT2 Activator.

Chaetomellic acid A is a potent inhibitor of farnesyltransferase in isolated enzyme assays (IC50=55nM) but is inactive in whole cells. Inhibition of farnesyltransferase is selective over geranylgeranyltransferase I and II (IC50=92µM and 34µM respectively).

NPS-467 is a specific CaR agonist.

Doripenem is a broad-spectrum carbapenem antibiotic effective against both Gram-negative and Gram-positive bacteria, such as S. aureus, S. pneumoniae, E. coli, and K. pneumoniae, with minimum inhibitory concentrations (MICs) ranging from less than 0.015 to 0.3 µg/ml. It has been proven to reduce the viable bacteria count in mouse lung models of chronic P. aeruginosa respiratory tract infection at a dosage of 100 mg/kg per day. Doripenem operates by inhibiting bacterial cell wall synthesis through the formation of stable acyl-enzyme complexes with penicillin-binding proteins, leading to their inactivation. This compound has been utilized in various formulations for the treatment of bacterial infections.

(3R,6R)-Vaborbactam ((3R,6R)-Vaborbactam (Iso-1360457-46-0)) 是一种环状硼酸药效团 β-内酰胺酶 (β-lactamase) 抑制剂，具有潜在的抗菌活性。

E3ligaseLigand-Linker Conjugate 46 是一种 E3 连接酶配体-连接子缀合物，由 (S,R,S)-AHPC 和相应的 Linker 组成。(S,R,S)-AHPC 基于 VH032 的 von Hippel-Lindau (VHL) 配体，能够募集 VHL 蛋白。E3ligaseLigand-Linker Conjugate 46 可用作关键中间体，用于合成完整的PROTACs分子。

Xanthoquinodin A1 is a fungal metabolite that has been found inHumicolaand has diverse biological activities.1,2It inhibitsE. tenellaschizont formation in BHK-21 cells with a minimum effective concentration (MEC) value of 0.02 μg/ml.1Xanthoquinodin A1 is active againstB. subtilis,M. luteus,S. aureus,A. laidlawii, andB. fragilisin a disc assay when used at a concentration of 1 mg/ml. It is also active againstB. cereus(MIC = 0.44 μM).2Xanthoquinodin A1 is cytotoxic to KB, MCF-7, and NCI H187 cancer cells. 1.Tabata, N., Suzumura, Y., Tomoda, H., et al.Xanthoquinodins, new anticoccidial agents produced by Humicola sp. Production, isolation and physico-chemical and biological propertiesJ. Antibiot. (Tokyo)46(5)749-755(1993) 2.Tantapakul, C., Promgool, T., Kanokmedhakul, K., et al.Bioactive xanthoquinodins and epipolythiodioxopiperazines from Chaetomium globosum 7s-1, an endophytic fungus isolated from Rhapis cochinchinensis (Lour.) MartNat. Prod. Res.34(4)494-502(2020)

Benastatin C is a polyketide synthase-derived benastatin that has been found inStreptomycesand has diverse biological activities.1,2It inhibits glutathione S-transferase (GST; IC50= 24 μg/ml for the rat liver enzyme).2Benastatin C also inhibits the esterase activity of isolated porcine pancreatic lipase (IC50= 10 μg/ml). It increases LPS- or concanavalin A-induced blastogenesis of isolated mouse spleen lymphocytes in a concentration-dependent manner. 1.Xu, Z., Schenk, A., and Hertweck, C.Molecular analysis of the benastatin biosynthetic pathway and genetic engineering of altered fatty acid-polyketide hybridsJ. Am. Chem. Soc.129(18)6022-6030(2007) 2.Aoyama, T., Kojima, F., Yamazaki, T., et al.Benastatins C and D, new inhibitors of glutathione S-transferase, produced by Streptomyces sp. MI384-DF12. Production, isolation, structure determination and biological activitiesJ. Antibiot. (Tokyo)46(5)712-718(1993)