sars cov mpro in 1

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 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.

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].

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-2 Mpro-IN-32 (Compound 1) is a selective inhibitor of SARS-CoV-2 MPro with an IC50 value of 230 nM. In vitro, it also inhibits the replication of various SARS-CoV-2 variants.

SARS-CoV-2 Mpro-IN-37 (compound 8r) is an inhibitor of the SARS-CoV-2 main protease (Mpro), with an IC50 value of 0.0199 μM. It exhibits IC50 values of 0.00945 μM against SARS-CoV-1 Mpro and 0.111 μM against MERS-CoV Mpro. SARS-CoV-2 Mpro-IN-37 demonstrates potent antiviral activity in the nanomolar range without showing cytotoxicity.

Mpro inhibitor N3 hemihydrate is a potent antagonist of the SARS-CoV-2 main protease (Mpro), with an EC50 of 16.77 μM against SARS-CoV-2. It specifically inhibits Mpro in various coronaviruses, including SARS-CoV, MERS-CoV, HCoV-229E (IC50 4.0 μM), FIPV (IC50 8.8 μM), and MHV-A59 (IC50 2.7 μM) [1][2].

Mpro PLpro-IN-1 (Compound 29) is a dual-acting inhibitor of SARS-CoV-2 protease, displaying micromolar inhibition of Mpro (IC50: 1.72 μM) and submicromolar inhibition of PLpro (IC50: 0.67 μM).

SP inhibitor 1 is an inhibitor of SARS-CoV-2 replication at non-toxic concentrations (0.3250<5.98 μM) in vitro. SP inhibitor 1 is a selective inhibitor of SARS-CoV-2 stinger protein (SP), acting on SP protein (IC50: 3.26 μM), Mpro protein (IC50>25 μM) and PLpro protein (IC50>25 μM), and has cellular antiviral effects. and PLpro protein (IC50>25 μM), and has cellular antiviral effects.

(±)-Alliin, the principal active component in garlic, functions as a potential inhibitor of SARS-CoV-2's main protease (Mpro) [1].

TKB245 is a potent inhibitor of the SARS-CoV-2 main protease (Mpro), effectively inhibiting viral replication in VeroE6 cells [1].

SARS-CoV-2-IN-50 (Compound X77C) is a potent inhibitor of the SARS-CoV-2 main protease (M^pro), demonstrating high affinity for the enzyme's catalytic site [1].

SARS-CoV-2 Mpro-IN-7 (compound 6g) effectively inhibits the SARS-CoV-2 main protease (Mpro) with an IC50 value of 8.8 μM and exhibits a cytotoxic concentration (CC50) of 10 μM [1].

SARS-CoV-2 Mpro-IN-8 (compound 6b) is an antiviral agent effective against SARS-CoV-2 [1].

SARS-CoV-2 Mpro-IN-10 (27h) is a potent inhibitor of the Mpro enzyme, with IC50 and EC50 values of 10.9 nM and 43.6 nM, respectively. It is used in research on the SARS-CoV-2 virus [1].

MPI60 is a potent inhibitor of SARS-CoV-2 main protease (M^pro) exhibiting high antiviral efficacy, low cellular cytotoxicity, and considerable in vitro metabolic stability, making it suitable for SARS-CoV-2 research [1].

SARS-CoV-2-IN-58 (Compound 21H) is an antiviral agent targeting SARS-CoV-2, demonstrating an EC50 of 18 μM and specifically inhibiting the SARS-CoV-2 main protease (Mpro) with an IC50 of 0.35 μM [1].

Hydroxyaloin A (10-10-Hydroxyaloin A) is a potent inhibitor of SARS-CoV-2, demonstrating significant efficacy in binding to the active site of the SARS-CoV-2 main protease (M^pro) [1].

SARS-CoV-2-IN-59 (compound E07), an imidazoline derivative, is a non-peptide small molecule that inhibits SARS-CoV-2 by targeting its main protease (Mpro) and exhibits robust binding with Mpro residues (Met 165, Gln 166, Met 165, His 41, Gln 189) [1].

SARS-CoV-2-IN-69 (Compound 7E) is a potent, non-covalent inhibitor of the SARS-CoV-2 main protease (M^pro) with an EC50 of 7.4 μM and also inhibits the papain-like protease (PL^pro) [1].

SARS-CoV-2-IN-68 (compound 6C) is a covalent inhibitor of SARS-CoV-2 PLpro and Mpro, exhibiting potent antiviral properties by targeting the Zn-finger domain of PLpro [1].

SARS-CoV-2 Mpro-IN-12 (compound D026) is an inhibitor of the main protease (Mpro) of SARS-CoV-2, demonstrating antiviral properties [1].

MAT-POS-e194df51-1 is an orally active, non-covalent, non-peptide inhibitor of the SARS-CoV-2 main protease (M^pro) with an IC_50 of 37 nM. It exhibits cytotoxicity, showing EC_50 values of 64 nM in A549-ACE2-TMPRSS2 cells and 126 nM in HeLa-ACE2 cells [1].