s 46

Pheneturide (Benuride) is the ureide class, used to treat epilepsy, and is an anticonvulsant.

NR1A/NR2B NMDA receptor antagonist,orally active

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

HRS 4642 is a long-acting, selective KRAS G12D inhibitor with a Kd value of 0.083 nM. It inhibits phosphorylation of downstream MEK and ERK proteins, exhibiting antitumour activity. HRS 4642 reduces target lesions and, when used alone or in combination with Carfilzomib, remodels the tumour microenvironment towards an immunocompetent state.

Doripenem monohydrate (S 4661 monohydrate) is a broad-spectrum injectable antibiotic, used for Gram-positive, Gram-negative and anaerobic pathogens.

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 is a novel and potent antagonist of the P2Y14 receptor.

MRS4654 is an innovative and potent antagonist of the P2Y14 receptor, featuring an IC50 of 15 nM.

LY-364947 (HTS466284) is a potent ATP-competitive inhibitor of TGFβR-I.

WR-S-462 is a STAT3 inhibitor. It effectively blocks the phosphorylation and biological functions of STAT3 in vitro. The IC50 of WR-S-462 for inhibiting MDA-MB-231 cells is 0.03 μM, and it exhibits a strong binding affinity for STAT3 protein with a Kd of 58 nM. WR-S-462 prevents the nuclear translocation of p-STAT3 and selectively inhibits the expression of p-STAT3Tyr705 in MDA-MB-231 cells, as well as the expression of downstream target genes regulated by STAT3, such as Cyclin D1, Bcl-2, and Bcl-xl. This compound inhibits the growth and metastasis of triple-negative breast cancer (TNBC).

Doripenem is a new parenteral carbapenem antibiotic with broad-spectrum activity against gram-negative and gram-positive pathogens.

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)) is a cyclic boronic acid pharmacophore β-lactamase inhibitor with potential antimicrobial activity. (S)-Vamicamide ((S)-Vamicamide (Iso-132373-81-0)) is a novel anticholinergic compound.

E3ligaseLigand-Linker Conjugate 46 is a conjugate consisting of an E3 ligase ligand linked to a linker (E3LigaseLigand-Linker Conjugates), composed of (S,R,S)-AHPC and its corresponding linker. The (S,R,S)-AHPC is a von Hippel-Lindau (VHL) ligand based on VH032, capable of recruiting the VHL protein. E3ligaseLigand-Linker Conjugate 46 serves as a crucial intermediate for synthesizing complete PROTAC molecules.

(S)-Tubercidinylhomocysteine (Page 46) is a potent inhibitor of S-adenosylmethionine-dependent methyltransferases. It is useful in studies of herpes viruses (HSV) and vaccinia virus (VV).

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)