PLpro/RBD-IN-1 (compound 5) is a dual SARS-CoV-2 PLpro and spike protein RBD inhibitor with IC50s of 7.197 μM and 8.673 μM, respectively[1].
Amantadine-d6 is the deuterium labeled Amantadine[1]. Amantadine (1-Adamantanamine) is an orally avtive and potent antiviral agent with activity against influenza A viruses. Amantadine inhibits several ion channels such as NMDA and M2, and also inhibits Coronavirus ion channels. Amantadine also has anti-orthopoxvirus and anticancer activity. Amantadine can be used for Parkinson's disease, postoperative cognitive dysfunction (POCD) and COVID-19 research[2][3][4][5][6][7].
Fluphenazine-d8 is the deuterium labeled Fluphenazine. Fluphenazine is a potent, orally active phenothiazine-based dopamine receptor antagonist. Fluphenazine blocks neuronal voltage-gated sodium channels. Fluphenazine acts primarily through antagonism of postsynaptic dopamine-2 receptors in mesolimbic, nigrostriatal, and tuberoinfundibular neural pathways. Fluphenazine can antagonize Methylphenidate-induced stereotyped gnawing and inhibit climbing behaviour in mice. Fluphenazine can be used for researching psychosis and painful peripheral neuropathy associated with diabetes and has potential to inhibit SARS-CoV-2[1][2][3][4][5][6].
SARS-CoV-2-IN-16 (Compound 12) is a potent SARS-CoV-2 nucleocapsid protein (NPro) inhibitor. SARS-CoV-2-IN-16 exhibits potent anti-viral activity with the EC50 of 3.69 μM. SARS-CoV-2-IN-16 binds to NPro with the low KD value of 7.82 μM, suggesting that SARS-CoV-2-IN-16 is a potent NPro ligand[1].
CMX990 is a SARS-CoV-2 3CL protease inhibitor. The EC90s for inhibiting SARS-CoV-2 were 9.6 nM and 101 nM in human bronchial epithelial cells (HBECs) and HeLa-ACE2 cells, respectively. CMX990 has good ADME and pharmacokinetic properties[1].
Fmoc-leucine-15N is a 15N-labeled and 13C-labled EIDD-1931. EIDD-1931 (Beta-d-N4-hydroxycytidine; NHC) is a novel nucleoside analog and behaves as a potent anti-virus agent. EIDD-1931 effectively inhibits the replication activity of venezuelan equine ence
Adintrevimab (ADG 20) is a human IgG1 monoclonal SARS-CoV (SARS-CoV) antibody. Adintrevimab inhibits SARS-CoV-2 variants and other SARS-like coronaviruses with pandemic potential[1].
CDD-1819 is a non-covalent and non-peptide potent SARS-CoV-2 Mpro inhibitor with a Ki of 5 nM. CDD-1819 also inhibits ΔP168, A173V, and ΔP168/A173V Mpro variants[1].
SARS-CoV-2-IN-15 (compound 11) is a potent inhibitor of SARS-CoV-2 with an IC50 of 0.49 μM. SARS-CoV-2-IN-15 is a niclosamide analogue. SARS-CoV-2-IN-15 contains higher stability in human plasma and liver S9 enzymes assay than niclosamide, which can improve bioavailability and half-life when administered orally[1].
Romlusevimab (BRII-198) is a neutralizing recombinant human IgG1 monoclonal antibody against the spike protein of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2)[1][2].
Chloroquine dihydrochloride is an antimalarial and anti-inflammatory agent widely used to treat malaria and rheumatoid arthritis. Chloroquine dihydrochloride is an autophagy and toll-like receptors (TLRs) inhibitor. Chloroquine dihydrochloride is highly effective in the control of SARS-CoV-2 (COVID-19) infection in vitro (EC50=1.13 μM)[1][2][3][4].
SARS-CoV-2 nsp13-IN-6 (compound C5) is a potent SARS-CoV-2 non-structural protein 13 (nsp13) inhibitor with IC50 values of 27 and 33 μM for ssDNA+ ATPase and ssDNA- ATPase. SARS-CoV-2 nsp13-IN-6 can be used for researching anti-COVID-19[1].
Ivermectin B1b is the minor component of Ivermectin. Ivermectin, a potent anti-parasitic agent, inhibits the replication of SARS-CoV-2 in cell culture[1][2].
Amubarvimab (BRII-196) is a human IgG1 mAb that bind to non-competing epitopes on the receptor binding domain (RBD) of spike protein, with a KD of 5.88 nM. Amubarvimab can effectively neutralize SARS-CoV-2 variants[1][2].
SARS-CoV-2-IN-10 is a potent and nontoxic inhibitor of SARS-CoV-2 3CL protease (3CLpro) with an IC50 and EC50 of 0.13 and 1.03 nM, respectively. SARS-CoV-2 3C-like protease (3CLpro), an enzyme essential for viral replication, is an attractive target for therapeutic intervention. SARS-CoV-2-IN-11 may lead to the emergence of effective SARS-CoV-2-specific antivirals[1].
Direct Violet 1, an azo dye, is a textile dye. Direct Violet 1 is also the protein-protein interaction (PPI) between the SARS-CoV-2 spike protein and ACE2 inhibitor with IC50s of 1.47-2.63 µM[1][2].
Mpro inhibitor N3 is a potent SARS-CoV-2 MPro inhibitor with an EC50 value of 16.77 µM. Mpro inhibitor N3 shows antiviral activities against HCoV-229E, FIPV, IBV and MHV-A59[1][2][3].
1,7-Bis(4-hydroxyphenyl)-1,4,6-heptatrien-3-one is a potent nucleocapsid (N) protein inhibitor can be isolated from Curcuma kwangsiensis. 1,7-Bis(4-hydroxyphenyl)-1,4,6-heptatrien-3-one exhibits excellent antiviral activity against HCoV-OC43 and SARS-CoV-2,with EC50 values of 0.16 μM and 0.17 μM, respectively[1].
Nepuvibart (ZRC3308-B10) is an anti-SARS-CoV-2 monoclonal antibody (IgG1 type). Nepuvibart shows good binding affinity to a non-competing epitope on the RBD of the SARS-CoV-2 spike protein. Nepuvibart can be used in combination with ZRC3308-A7 (HY-145642) at a ratio of 1:1, which is effective for the prevention of COVID-19 and the early stage of COVID-19 before the development of severe disease[1].
Pinokalant is a broad-spectrum and non-selectivecation channel inhibitor. Pinokalant significantly reduces cortical infarct volume. Pinokalant o improves the metabolic and electrophysiologic status of the ischemic penumbra. Pinokalant reduces lesion size on magnetic resonance images in the acute phase following middle cerebral artery occlusion in rats. Pinokalant has the potential for the research of stroke. Pinokalant also shows anti-SARS-CoV-2 activity[1].
F8-S43-S3 is an inhibitor of SARS-CoV-2 main protease, with an IC50 of 9.69 μM[1].
Zevotrelvir (Compound 52) is a coronavirus inhibitor with IC50 ranges of <0.1 μM and <0.1mM for 229E hCoV and SARS-CoV-23C-like (3CL) proteases, respectively. Zevotrelvir has the potential to study viral infections[1].
SARS-CoV-2 3CLpro-IN-7 is a reversible covalent SARS-CoV-2 3CL protease inhibitor with an IC50 value of 1.4 µM[1].
CDD-1845 is a non-covalent and non-peptide potent SARS-CoV-2 Mpro inhibitor with a Ki of 3 nM. CDD-1845 also inhibits ΔP168, A173V, and ΔP168/A173V Mpro variants[1].
Arbemnifosbuvir is a nidovirus DdRp-associated nucleotidyltransferase (NiRAN) domain of non-structural protein 12 (nsp12)-interfering drugs. Arbemnifosbuvir can be used for SARS-CoVs infection research[1].
Z-Arg-Leu-Arg-Gly-Gly-AMC is a peptide substrate of SARS-CoV PLpro[1].
SARS-CoV-2-IN-68 (compound 6C) is a covalent SARS-CoV-2 PLpro/Mpro inhibitor with potent antiviral activities. SARS-CoV-2-IN-68 binds to Zn-finger domain of PLpro[1].
GRL-0496 is a potent chloropyridyl ester-derived SARS-CoV 3CLpro inhibitor, with an IC50 of 30 nM in both enzyme inhibitory and antiviral assays. GRL-0496 shows SARS-CoV antiviral activity, with an EC50 of 6.9 μM[1].
Ivermectin B1a, a derivative of Avermectin B1a (HY-15308), is a main component of Ivermectin (HY-15310)[1]. Ivermectin (MK-933) is a broad-spectrum anti-parasite agent. Ivermectin is a candidate therapeutic against SARS-CoV-2/COVID-19[2].
Bebtelovimab a humanized IgG1-λ2 antibody targeting to SARS-CoV-2, especially COVID-19. Bebtelovimab potently neutralizes SARS-CoV-2 variants, and inhibits COVID-19 with mild-to-moderate efficacy[1][2].