SARS-CoV MPro-IN-2 (compound 15) is a potent inhibitor of SARS-CoV-2 Mpro with an IC50 value of 72.07 nM. The main protease (Mpro) of the virus as the major enzyme processing viral polyproteins contributes to the replication and transcription of SARS-CoV-2 in host cells, and has been characterized as an attractive target in drug discovery. SARS-CoV MPro-IN-2 has the potential for the research of COVID-19[1].
Chloramphenicol is a broad-spectrum antibiotic.Target: AntibacterialChloramphenicol is a bacteriostatic drug that stops bacterial growth by inhibiting protein synthesis. Chloramphenicol prevents protein chain elongation by inhibiting the peptidyl transferase activity of the bacterial ribosome. It specifically binds to A2451 and A2452 residues in the 23S rRNA of the 50S ribosomal subunit, preventing peptide bond formation. While chloramphenicol and the macrolide class of antibiotics both interact with ribosomes, chloramphenicol is not a macrolide. It directly interferes with substrate binding, whereas macrolides sterically block the progression of the growing peptide [1, 2].
Cetalkonium chloride is an ammonium antiseptic agent used in many topical drugs for infections of mouth, throat and eye. Cetalkonium chloride acts as anti-inflammatory amphiphilic agent[1].
FNC-TP is the intracellular active form of FNC. FNC is a potent nucleoside reverse transcriptase inhibitor (NRTI), with antiviral activity on HIV, HBV and HCV[1].
G907 is a selective small-molecule antagonist of ATP-binding cassette (ABC) transporter, MsbA. It inhibits purified E. coli MsbA in amphipols with an IC50 of 18 nM. G907 traps MsbA in an inward-facing, lipopolysaccharide-bound conformation by wedging into an architecturally conserved transmembrane pocket. Bactericidal activity[1].
Asunaprevir is a potent hepatitis C virus (HCV) NS3 protease inhibitor, with IC50 of 0.2 nM-3.5 nM.
Antibacterial agent 143 (Compound 5a) is an antibacterial agent with MICs of 25, 25, 50 and 50 μg/mL against B. subtilis ATCC6633, . aureus ATCC6538, P. aeruginosa ATCC13525 and E. coli ATCC35218, respectively[1].
Adefovir (GS-0393) is an adenosine monophosphate analog antiviral agent that after intracellular conversion to Adefovir diphosphate inhibits HBV DNA polymerase. Adefovir has an IC50 of 0.7 μM against HBV in the HepG2.2.15 cell line. Adefovir has good antiviral activity against several viruses, including HBV and herpesviruses[1][2][3].
NIM811 (SDZ NIM811) is a potent mitochondrial permeability transition inhibitor. Sequence: Cyclo[{Aaa}-{Abu}-{Sar}-Ile-Val-Leu-Ala-{D-Ala}-Leu-Leu-Val].
Kakuol is a natural compound isolated from the rhizomes of Asarum sieboldii. Antifungal activity[1].
Faropenem sodium is an orally bioavailable penem antibiotic which can efficiently kill Mycobacterium tuberculosis.
FtsZ-IN-2 (Compound 19) is an inhibitor of the bacterial cell division protein FtsZ with GTPase inhibitory activity. FtsZ-IN-2 exhibits anti-staphylococcal activity with MIC values of 2 µg/ml for MSSA and MRSA[1].
Robenidine hydrochloride is an anticoccidial agent which is also active against MRSA and VRE with MIC50s of 8.1 and 4.7 μM, respectively.
Ethacridine lactate monohydrate is an aromatic organic compound, primarily use as an antiseptic.
Nimorazole (K-1900) is a nitroimidazole anti-infective.
Cefiderocol is a novel siderophore cephalosporin which has a potent activity against a broad range of aerobic Gram-negative bacterial species with MIC50s of 2 μg/mL or less.
DNA Gyrase-IN-4 (compound 8p) is a potent DNA gyrase inhibitor, with an IC50 of 0.13 μM. DNA Gyrase-IN-4 shows excellent antibacterial activity against Staphylococcus aureus, Listeria monocytogenes, Salmonella and Escherichia coli, with MIC values of 0.05, 0.05, 0.05, and 8 μg/mL, respectively[1].
Xanthyletin is a coumarin isolated from Citrus, with anti-tumor and anti-bacterial activities. Xanthyletin also inhibits symbiotic fungus cultivated by leaf-cutting ants[1].
MK-4965 is a nonnucleoside reverse transcriptase inhibitor (NNRTI). MK-4965 displays excellent activities against not only HIV-1 wild-type (WT) virus but also against a broad panel of NNRTI-resistant viruses and can be used for the research of HIV-1 infection[1].
Tilmicosin phosphate is a antibiotic, is used in veterinary medicine for the treatment of bovine respiratory disease and ovine respiratory disease associated with Mannheimia (Pasteurella) haemolytica.
Allopurinol riboside, a metabolite of allopurinol, shows potent activities against parasites.
Fidaxomicin(OPT-80; PAR-101) is a new class of narrow spectrum macrocyclic antibiotic drug; selective eradication of pathogenic Clostridium difficile with minimal disruption to the multiple species of bacteria that make up the normal, healthy intestinal flora.
BRD-6929 (Cpd-60) is a brain-penetrant, selective inhibitor of HDAC1 and HDAC2 (IC50= 1 and 8 nM), extracted from patent US2018360927[1]. BRD-6929 (Cpd-60) shows high-affinity to HDAC1 and HDAC2 with Ki of 0.2 and 1.5 nM, respectively[2]. BRD-6929 (TPB) potentiates the efficacy of gnidimacrin (a PKC Agonist) against latent HIV-1[3].
Griseofulvin(Gris-PEG; Grifulvin) is a spirocyclic fungal natural product used in treatment of fungal dermatophytes; Antifungal drug.
Murrayanol is a natural carbazole alkaloid with a variety of biological activities. Murrayanol shows anti-inflammatory, topoisomerase I and topoisomerase II (Topoisomerase) inhibition activities. Murrayanol also as a mosquitocidal and antimicrobial[1].
Acetyl-CoA Carboxylase-IN-1 is a potent acetyl-CoA carboxylase (ACC) inhibitor with an IC50 value of ＜5 nM. Acetyl-CoA Carboxylase-IN-1 has antibacterial activity[1].
Chrysomycin B is an antibiotic isolated from a strain of Streptomyces. Chrysomycin B causes DNA damage in the human lung adenocarcinoma A549 cell line and inhibits topoisomerase II. Chrysomycin B suppresses the growth of transplantable tumors in mice.
SARS-CoV MPro-IN-1 is a SARS-CoV-2 3CLpro covalent inhibitor, with an IC50 of 40 nM. SARS-CoV MPro-IN-1 shows good anti-SARS-CoV-2-infection activity in cell culture with an EC50 of 0.33 μM. SARS-CoV MPro-IN-1 has the potential for COVID-19 research[1].
Demethoxyencecalin is a chromene isolated from Helianthus annuus, has antifungal activities[1].
Crexavibart (BMS-986413; C-144-LS) is an IgG1λ2 antibody that targets the SARS-CoV2 spike (S) glycoprotein receptor-binding domain[1].