sars-cov 3clpro

GRL-0496 is a potent inhibitor with an enzyme inhibitory activity against SARS-CoV 3CLpro with an IC50 of 30 nM and antiviral potency with an EC50 value of 6.9 μM.

Punicalagin is a major ellagitannin found in pomegranates that is reported to produce antioxidant, anti-inflammatory, and anticancer effects. It has been shown to prevent high-fat diet-induced obesity-associated accumulation of cardiac triglyceride and ch

PF-07321332 is a potent and orally active inhibitor of SARS-CoV 3C-like protease (3CLPRO) .

SARS-CoV-2 3CLpro-IN-16 is a covalent inhibitor of SARS-CoV-2 3CLpro activity, exerting its effect by forming a covalent bond with Cys145.

Ensitrelvir (S-217622) is an orally active inhibitor of SARS-CoV-2 3CL protease with IC50 of 13 nM.

Atazanavir sulfate (BMS-232632 sulfate) is an azapeptide and HIV-protease inhibitor used in the treatment of HIV infections and AIDS in combination with other anti-HIV agents.

Atazanavir (BMS-232632)(BMS-232632) is an highly effective HIV-1 protease inhibitor.

Ritonavir (ABT 538) is a peptidomimetic agent that inhibits both HIV-1 and HIV-2 proteases. Ritonavir is highly inhibited by serum proteins but boosts the effect of other HIV proteases by blocking their degradation by cytochrome P450.

Lopinavir (ABT-378) is a peptidomimetic HIV protease inhibitor effective against HIV protease with the Val 82 mutation. It is less affected by serum protein binding compared to the structurally related drug ritonavir.

Velpatasvir (GS-5816), also known as GS-5816, is a potent and selective Hepatitis C virus NS5A inhibitor. GS-5816 has demonstrated pan-genotypic activity and a high barrier to resistance in HCV replicon assays. GS-5816 demonstrated pangenotypic antiviral activity in patients with genotype 1-4 HCV infection. It will be further evaluated in combination with other pangenotypic direct-acting antivirals to achieve the goal of developing a well-tolerated, highly effective treatment for all HCV genotypes.

SARS-CoV-2 3CLpro-IN-25 (compound 56) effectively inhibits the SARS-CoV-2 3CLpro enzyme, exhibiting an IC50 value of 70 nM, and demonstrates cellular antiviral activity with an EC50 of 3.1 μM.

SARS-CoV-2 3CLpro-IN-27 (Compound 9H) is an inhibitor of SARS-CoV-2 3CLpro, demonstrating an IC50 of 21 nM. It also exhibits robust anti-replicase activity against SARS-CoV-2, with an EC50 of 5 nM.

SARS-CoV-2 3CLpro-IN-26 (Compound (S,R)-4y) is a conformational inhibitor of SARS-CoV-2 3CLpro with an IC50 of 0.43 μM. It demonstrates good cellular permeability, being able to effectively cross the cell membrane following co-incubation with Vero-E6 cells.

3CLPro-IN-3 (Compound A36) is an inhibitor of SARS-CoV-2 3CLpro with an IC50 value of 51.3 nM. It exhibits antiviral activity against human coronaviruses 229E, OC43, and the murine coronavirus MHV.

Imidazole-d4 is an isotope-labeled variant of imidazole, which is a heterocyclic aromatic compound. Imidazole molecules serve as inhibitors for acetylcholinesterase (AChEI) and xanthine oxidase (XO) and have been utilized as corrosion inhibitors. They display a range of biological activities, including antifungal, antitubercular, anti-inflammatory, antioxidant, and analgesic properties. Imidazole inhibits platelet microsomes from converting endoperoxides (PGG2 and PGH2) into thromboxane A2. Additionally, imidazole derivatives show inhibitory effects on the SARS-CoV-2 3CLpro enzyme, offering potential for research in Alzheimer’s disease, gout, COVID-19, and thrombotic disorders.

SARS-CoV-2-IN-107 (Compound A7) is an inhibitor of SARS-CoV-2 3CLpro, with an IC50 of 261.3 nM. It inhibits the replication of SARS-CoV-2, exhibiting an EC50 of 11.7 μM. Additionally, SARS-CoV-2-IN-107 demonstrates anti-inflammatory activity in LPS-stimulated RAW264.7 macrophages, with a NO inhibition rate of 68.6%.

SARS-CoV-2 3CLpro-IN-28 (Compound 19) is an inhibitor of SARS-CoV-2 3CLpro, exhibiting an IC50 value of 0.018 μM.

SARS-CoV-2 3CLpro-IN-30 (compound 29) is a potent inhibitor of the SARS-CoV-2 3CL protease (SARS-CoV-2 3CLpro), with an IC50 of 0.04 μM and an EC50 of 0.3 μM.

LU9 is an effective 3CLpro inhibitor with an IC50 of 0.34 µM and potential application in SARS-CoV-2 research.

VK13 (Compound 6) is a potent inhibitor of human cathepsin L (hCatL) and SARS-CoV-2 3CLpro (3CL-PR), with Ki values of 2.6 nM and 0.55 nM, respectively. It also exhibits activity against CoV-2, with an EC50 value of 1.25 μM.

SARS-CoV-2 3CLpro-IN-32 (compound B16) is a potent inhibitor of the SARS-CoV-2 3CLpro enzyme, with an IC50 of 0.109 μM. It also demonstrates antiviral activity against the coronavirus HCoV-OC43, with an EC50 of 1.99 μM.

SARS-CoV-2-IN-71 (compound 8h) is an effective inhibitor of SARS-CoV-2, demonstrating antiviral activity by targeting multiple stages of coronavirus replication. It exhibits its effects by simultaneously acting on 3CLpro and TMPRSS2.

SARS-CoV-2 3CLpro-IN-22 (Compound 17) is an inhibitor of cathepsin L (CTSL) with an IC50 value of 32.5 nM, useful in research related to the SARS-CoV-2 virus.

PROTACKRAS G12D degrader 2 is a peptidomimetic molecule capable of inducing the degradation of SARS-CoV-2 3-chymotrypsin-like protease (3CLPro). Designed as a PROTAC molecule, it combines a dipeptidyl 3CLPro ligand based on GC-376 with a pomalidomide moiety, linked through a piperazine-piperidine linker.