sars cov-1

SARS-CoV-2-IN-1 is a potent inhibitor of Mpro [SARS-CoV-2 Mpro, SARS-CoV Mpro, and MERS-CoV Mpro] with IC50 values of 0.67, 0.90, and 0.58 μM, respectively.

SARS-CoV-IN-1 is an effective SARS-CoV replication inhibitor with an EC50 of 4.9 μM in Vero cells.

SARS-CoV-2 PLpro-IN-1 (Compound 85) is a non-covalent competitive inhibitor of SARS-CoV-2 PLpro with an IC50 value of 15.06 μM and a Ki value of 22.93 μM. It inhibits the proliferation of Vero cells, exhibiting an IC50 of 7.47 μM.

MProinhibitor 11b is an inhibitor of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) main protease (MPro; IC50= 0.04 μM in a TR-FRET assay).1It reduces viral yield in the culture supernatant of SARS-CoV-2-infected Vero E6 cells (EC50= 0.72 μM). MProinhibitor 11b also reduces viral RNA copy numbers in the same model when used at concentrations ranging from 1.85 to 50 μM. 1.Dai, W., Zhang, B., Jiang, X.-M., et al.Structure-based design of antiviral drug candidates targeting the SARS-CoV-2 main proteaseScience368(6497)1331-1335(2020)

SARS-CoV-2 Mpro-IN-1 (compound 16b-3) is a potent, selective, and irreversible inhibitor of the SARS-CoV-2 main protease (Mpro) with an IC50 value of 116 nM [1].

SARS-CoV-2 nsp3-IN-1 (Compound 15c) exhibits significant selectivity for coronavirus macrodomains, particularly SARS-CoV-2 Mac1, and can inhibit Mac1 ADP-ribosylhydrolase activity with an IC50 of 6.1 μM [1].

SARS-CoV-2 nsp13-IN-1 (compound C1) is a potent inhibitor of nsp13 (non-structural protein 13), selectively inhibiting nsp13 ssDNA+ATPase with an IC50 of 6 μM, but not ssDNA-ATPase, and can be used to study COVID-19.

SARS-CoV-2 nsp14-IN-1 (Compound 3) is a dual-substrate inhibitor of SARS-CoV-2 Nsp14 Mtase with an IC50 of 0.061 μM, targeting substrates such as histone lysine, protein arginine, DNA, and RNA.

SARS-CoV-2 3CLpro-IN-1 (Compound 14c) is a highly potent inhibitor specifically designed to target and inhibit the activity of SARS-CoV-2 3CL pro, a cysteine protease found in the main coronaviruses. This enzyme is a promising target for antiviral drug development, positioning SARS-CoV-2 3CLpro-IN-1 as significant for advancing research in infectious diseases [1].

SARS-CoV-2 MERS Mpro-IN-1 is a potent inhibitor of the main proteases in SARS-CoV-2 and MERS, with IC50 values of 0.10 and 0.06 µM, respectively.

Metformin (1,1-Dimethylbiguanide) is an AMPK activator with blood-brain barrier permeability. Metformin may improve glycemic control by increasing insulin sensitivity and decreasing intestinal glucose uptake, and is commonly used in type 2 diabetes research.

Chloroquine is a Toll-like receptor inhibitor that inhibits autophagy. Chloroquine has anti-malarial and anti-inflammatory activity and is widely used in the treatment of malaria and rheumatoid arthritis. Chloroquine also has anti-SARS-CoV-2 (COVID-19) activity and anti-HIV-1 activity.

CTP Synthetase-IN-1 Ammonium salt is an orally active and potent cytidine 5'-triphosphate synthetase (CTPS) inhibitor with potential antimicrobial, anti-inflammatory and antitumor activity for the study of SARS-CoV-2 viral infections.

PLpro RBD-IN-1 is a dual inhibitor of SARS-CoV-2 PLpro and the spiny protein RBD, with anti-novel coronavirus activity, and is seen for the study of viral infections.

SARS-CoV-2 Mpro-IN-9 (compound c7), a nonpeptidic, noncovalent inhibitor of SARS-CoV-2 main protease (Mpro), exhibits potent inhibitory action (IC50 = 0.085 μM) and improved physicochemical and drug metabolism and pharmacokinetics (DMPK) properties. It effectively suppresses viral replication in SARS-CoV-2-infected Vero E6 cells (EC50 = 1.10 μM) and demonstrates low cytotoxicity (CC50 > 50 μM) [1].

Piperazine,1-(4-fluorophenyl)-4-[(3,4,5-trimethoxyphenyl)methyl]- is a piperazine derivative with anti-SARS-CoV-2 activity.

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.

Mefloquine hydrochloride (Mefloquin hydrochloride) is a quinoline derivative used for the prevention and therapy of P. falciparum malaria.

Mizoribine (NSC-289637) belongs to the family of 1-Ribosyl-imidazolecarboxamides. Mizoribine has been investigated for the treatment of Rheumatoid Arthritis.

Amantadine hydrochloride (CI-719) is an antiviral that is used in the prophylactic or symptomatic treatment of influenza A and Parkinson disease.

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.