Enocitabine, a nucleoside analog, is a potent DNA replication inhibitor and a DNA chain terminator. Enocitabine can be used as an effective chemotherapeutic agent for the treatment of acute myelogenous leukaemia and lymphocytic leukaemias[1].
SCH-202676 hydrobromide is an allosteric modulator of G protein-coupled receptors (GPCRs) and adenosine receptor (AR). SCH-202676 hydrobromide has antiviral activity and inhibits 3CLpro in a time-dependent manner with an IC50 value of 0.655 μM[1][2][3][4].
Antibacterial agent 130 is a 1,1-diarylthiogalactoside, used for targeting the Pseudomonas aeruginosa LecA. Antibacterial agent 130 shows high affinity toward LecA (Kd=1 μM). Antibacterial agent 130 has antibiofilm activity, but lacks bactericidal activity. LecA, a lectin and virulence factor from Pseudomonas aeruginosa involved in bacterial adhesion and biofilm formation[1].
BAL-30072, a siderophore sulfactam, is a monocyclic beta-lactam antibiotic, with activity against multiresistant gram-negative bacilli. BAL30072 shows MIC90 values of 4 μg/mL for MDR Acinetobacter spp. and 8 μg/mL for MDR P. aeruginosa, respectively[1][2].
HIV Protease Substrate IV is a substrate of HIV protease. HIV Protease Substrate IV can be used to measure the activity of HIV (human immunodeficiency virus) -1 protease[1].
Vasicine hydrochloride (peganine hydrochloride) is a quinazoline alkaloid isolated from Justicia adhatoda. Vasicine (peganine) possesses anti- tuberculosis activity[1].
Temelimab (GNbAC-1) is an IgG4 monoclonal antibody that targets the human endogenous retroviral envelope protein HERV-W-Env[1][2].
Raxibacumab (ABthrax) is a human IgG1 monoclonal antibody against Bacillus anthracis protective antigen (PA). Raxibacumab blocks the toxin’s deleterious effects by preventing binding of the protective antigen component of the anthrax toxin to its receptors in host cells, thereby blocking the toxin’s deleterious effects. Raxibacumab can be used for anti-anthrax research[1][2].
β-Nor-lapachone is a Candida glabrata antibiofilm agent. β-Nor-lapachone can stimulate ROS production, inhibits efflux activity, adhesion, biofilm formation and the metabolism of mature biofilms of Candida glabrata. β-Nor-lapachone has antifungal activity[1].
MRV03-070 is an inhibitor of colibactin-activating peptidase ClbP with an IC50 value of 69 nM, acts like biosynthetic precursor precolibactin[1].
Voriconazole(UK-109496) is a second-generation triazole antifungal used to treat serious fungal infections.IC50 Value: Target: AntifungalVoriconazole displays potent activity against Candida, Cryptococcus and Aspergillus species. Voriconazole inhibits ergosterol synthesis by inhibiting CYP450-dependent 14-α sterol demethylase resulting in a depletion of ergosterol in fungal cell membranes.
Olendalizumab (ALXN1007) is a mouse-derived and humanized IgG2-G4-κ antibody, targeting to Complement protein C5a (Ki=60 pM). Olendalizumab targets the complement inflammatory pathway. Moreover, Olendalizumab can be used for research of complement mediated disorder caused by corona virus[1][2].
Sotrovimab (VIR 7831) is a human IgG1κ pan-sarbecovirus monoclonal antibody (mAb), neutralizes SARS-CoV-2, SARS-CoV-1, and multiple other sarbecoviruses. Sotrovimab is developed based on S309, exhibits a long half-life and great bioavailability in the respiratory mucosa. Sotrovimab could result in immune-mediated viral clearance and prevent progression of Covid-19 early in the course of disease[1][2].
Propineb (Zinc propylenebis) is a compound widely used in fruit and vegetables cultures, due to its large spectrum of activity against fungal plant diseases[1].
Radicicol is an inhibitor of the ATPase/kinase with IC50 values of 1 μM, 100 μM and 400 μM, respectively for Hsp90, Topo VI and PDK3 [1]. Radicicol inhibits a wide variety of tumor cell lines by targeting Hsp90, binds to the ATPase domain of Hsp90 and prevents maturation of Hsp90 clients, leading to proteasomal degradation [2]. Radicicol is an antifungal antibiotic with antimalarial activity, impairs mitochondrial replication by targeting P. falciparum topoisomerase VIB[2]. Radicicol is an inhibitor of fat mass and obesity-associated protein (FTO), exhibits a dose-dependent inhibition of FTO demethylation activity with an IC50 value of 16.04 µM[3].
Mupirocin calcium hydrate is an orally active antibiotic isolated from Pseudomonas fluorescens. Mupirocin calcium hydrate apparently exerts its antimicrobial activity by reversibly inhibiting isoleucyl-transfer RNA, thereby inhibiting bacterial protein and RNA synthesis[1][2].
DHFR-IN-10 (compound 4c) is a potent DHFR inhibitor, with an IC50 of 4.21 μM for M. tuberculosis DHFR enzyme. DHFR-IN-10 exhibits potent antituberculosis efficiency[1].
Nimbin is a intermediate limonoid isolated from Azadirachta. Nimbin prevents tau aggregation and increases cell viability. Nimbin is effective inhibits the envelope protein of dengue virus. Nimbin has anti-inflammatory, antipyretic, antifungal, antihistamine, antiseptic, antioxidant, anti-cancer and anti-viral properties. Nimbin can across blood-brain barrier[1][2][3].
EFdA-TP is a potent nucleoside reverse transcriptase (RT) inhibitor. EFdA-TP inhibits RT-catalyzed DNA synthesis as an effective immediate or delayed chain terminator (ICT or DCT). EFdA-TP inhibits HIV-1 RT with multiple mechanisms[1].
T-705RTP is a selective and GTP-competitive influenza virus RNA polymerase inhibitor with an IC50 of 0.14 μM and a Ki of 1.52 μM. T-705RTP is the active triphosphate metabolite of T-705 and has potent anti-influenza virus activity[1][2].
HIV-1 inhibitor-43 (compound 12) is a potent HIV-1 inhibitor with an EC50 of 21.3 nM, 6.2 nM, < 0.7 nM and < 0.7 nM for Y188L, K103N-Y181C, K103N and Y181C, respectively. HIV-1 inhibitor-43 can reduce HIV-1 RNA and protein p24[1].
Alamifovir (LY582563; MCC-478), a purine nucleotide analogue prodrug, shows potent activity against wild type and lamivudine resistant hepatitis B virus (HBV). Alamifovir has high activity against HBV replication and sustained antiviral effect[1][2].
Neamine tetrahydrochloride, a degradation product of Neomycin, is a broad-spectrum aminoglycoside antibiotic. Neamine tetrahydrochloride is an anti-angiogenesis agent targeting angiogenin. Neamine tetrahydrochloride has potent antibacterial, antitumor and neuroprotective activities[1][2].
Norchelerythrine is an alkaloid isolated from the roots of Zanthoxylum capense with antibacterial activity against gram-positive and gram-negative bacteria. Norchelerythrine exhibits inhibitory activity against Staphylococcus aureus, Pseudomonas aeruginosa, and Enterococcus faecalis and Escherichia coli with MIC values >50 µg/mL[1].
Oleuropeic acid 8-O-glucoside is a terpenic compound, that can be isolated from twigs with leaves of Juniperus communis var. depressa. Oleuropeic acid 8-O-glucoside shows antibacterial activity against three strains of Helicobacter pylori (NCTC11637, NCTC11916, and OCO1), with MIC of 100 μg/mL all[1].
(+)-JNJ-A07 is a highly potent, orally active pan-serotype dengue virus inhibitor targeting the NS3-NS4B interaction. (+)-JNJ-A07 exerts nanomolar to picomolar activity against a panel of 21 clinical isolates. (+)-JNJ-A07 has a favourable pharmacokinetic profile that results in outstanding efficacy against dengue virus infection in mouse infection models[1].
Decoquinate is a coccidiostat used in veterinary medicine.
Eupatoriopicrin is an antitrypanosomic agent with an IC50 value of 1.2 μM (T. b. rhodesiense). Eupatoriopicrin is cytotoxic to L6 cells with an IC50 value of 1.6 μM[1].
Decamethoxine (Septefril) is a cationic gemini surfactant. Decamethoxine exhibits strong bactericidal and fungicidal effects. Decamethoxine modifies the permeability of the microbial cell membrane, resulting in the destruction and death of diverse microorganisms[1][2].
A2ti-2 is a selective and low-affinity annexin A2/S100A10 heterotetramer (A2t) inhibitor with an IC50 of 230 μM[1]. A2ti-2 specifically disrupts the protein-protein interaction (PPI) between A2 and S100A10. A2ti-2 prevents human papillomavirus type 16 (HPV16) infection[2].