BDM88855 is a novel allosteric efflux-pump inhibitor that potentiate antibiotic activity in E. coli through inhibition of its primary RND transporter, AcrAB-TolC.BDM88855 binds to a unique site on the transmembrane domain of the AcrB L protomer, lined by key catalytic residues involved in proton relay, boost antibiotic activity in E. coli by inhibiting the AcrAB-TolC efflux pump.

BDM88855 Hcl is a novel allosteric efflux-pump inhibitor that potentiate antibiotic activity in E. coli through inhibition of its primary RND transporter, AcrAB-TolC.BDM88855 binds to a unique site on the transmembrane domain of the AcrB L protomer, lined by key catalytic residues involved in proton relay, boost antibiotic activity in E. coli by inhibiting the AcrAB-TolC efflux pump.

Azoffluxin (CMLD012336) is a bis-benzodioxolylindolinone that synergizes with fluconazole against C. auris through the inhibition of efflux pump Cdr1, thus increasing intracellular fluconazole levels.Azoffluxin increases intracellular accumulation of fluconazole (FLC) by inhibiting Cdr1-mediated efflux in C. auris.Azoffluxin potentiates intracellular acting compounds against C. auris, to a similar degree as deletion of CDR1.Azoffluxin is active against diverse C. auris strains, azoffluxin potentiated fluconazole in multiple isolates from three of the four major clades. The clade III isolates from South Africa were the exception.Azoffluxin enhances fluconazole (FLC) activity against azole-resistant C. albicans isolates.Azoffluxin not only enhanced fluconazole activity but also reduced fungal burden by ~1000-fold as a single agent in mice infected with drug-resistant C. auris.

ARN-75041 (ARN75041) is a potent, small molecule fusion inhibitor of arenavirus, inhibits pseudotyped entry of pGTOV and pCHAPV with EC50 of 1.7 and 15.3 nM, respectively. ARN-75041 demonstrated sub-nanomolar against native replicative LASV (LASV EC90<0.3 nM) and JUNV (EC90=6.2 nM).ARN-75041 also potently inhibits mutant T434I pTCRV variant with EC50 of 29 nM.ARN-75041 dramatically improved survival outcome and potently inhibited TCRV replication in serum and various tissues at doses of 10 and 35 mg/kg, provided highly significant post-exposure protection in mice against TCRV infection.

ARN-75039 (ARN75039) is a potent, small molecule fusion inhibitor of arenavirus, inhibits pseudotyped entry of pGTOV and pCHAPV with EC50 of 0.13 and 4.3 nM, respectively.ARN-75039 demonstrated sub-nanomolar EC50 activity against pTCRV that further translated to native wild-and NWAs, including LASV, JUNV and MACV, in pseudotyped virus assays and against native replicative LASV and JUNV.ARN-75039 also potently inhibits mutant T434I pTCRV variant with EC50 of 29 nM.ARN-75039 dramatically improved survival outcome and potently inhibited TCRV replication in serum and various tissues at doses of 10 and 35 mg/kg, provided highly significant post-exposure protection in mice against TCRV infection.

Antimicrobial peptide BING (IRIILRAQGALKI) is a thermostable 13-residue peptide that targets bacterial envelope stress response by suppressing cpxR expression in Gram-negative bacteria.BING downregulates efflux pump components and synergises the effect of antibiotics, and suppresses the development of antibiotic resistance.BING downregulated the expression of efflux pump components mexB, mexY and oprM in P. aeruginosa and significantly synergised the toxicity of antibiotics towards these bacteria.

AN12855 (AN-12855) is potent, cofactor-independent M. tuberculosis InhA inhibitor, binds to and inhibits InhA with IC50 of 0.03 uM, shows potent activity against whole-cell M. tuberculosis H37Rv with IC90 of 0.09 uM; AN12855 demonstrates potent activity against drug-susceptible and drug-resistant strains of M. tuberculosis, exhibits comparable efficacy to the frontline antitubercular drug isoniazid (INH) in both acute and chronic models of TB infection with a lower potential for resistance development and shows in vitro activity against conventional KatG-mediated INH-resistant M. tuberculosis.

Amphihevir is a potent, selective HCV NS4B inhibitor with EC50 of 0.34 and 1.97 nM against the GT1a (H77) and GT1b replicon in luciferase assays.Amphihevir shows weaker acitivity against GT2a (JFH-1) (EC50=186 nM).Amphihevir shows EC50 3.13 nM and 18.16 nM with 100% human serum against GT1a and GT1b replicons using HCV-1b replicon cells test.Amphihevir reduced replicon RNA by nearly 6,300-fold (3.8 log10) at a concentration 25-fold greater than the EC90 (300 nM).Amphihevir was found to be inactive against other viruses, human kinases, and GPCRs, which implies its good selectivity.Amphihevir has good oral bioavailability and appropriate T1/2 in rats and dogs, showed good safety profiles in rats and dogs.Amphihevir is the first reported NS4B inhibitor that has advanced to clinical trials.

ACHN-975 (ACHN975) is a potent bacterial LpxC inhibitor with IC50 of 0.68 nM (P. aeruginosa LpxC); ACHN-975 is potent against the P. aeruginosa isolates with MIC50 of 0.06 ug/mL and MIC90 of 0.25 ug/mL. ACHN-975 demonstrated in a neutropenic mouse thigh model with P. aeruginosa ATCC 27853.

ACAi-028 is a small molecule inhibiting HIV-1 replication (EC50=0.55 uM) that targets a hydrophobic pocket in the N-terminal domain of capsid (CA-NTD).ACAi-028 binds directly and noncovalently to HIV-1 capsid monomer.ACAi-028 inhibits the early stage of the HIV-1 life cycle and does not affect the late stage, also prevents multiple-round HIV-1 infection using HIV-1 strains (HIV-1NL4-3 and HIV-1LAI), except for HIV-2 strain (HIV-2ROD).ACAi-028 inhibits the replication of various types of HIV-1 strains (HIV-1104pre and HIV-1MDR/B) in PBMCs and HIV-1ATVR5μM in MT-4 cells, with negligible cytotoxicity.

AB-506 is a small-molecule inhibitor targeting HBV core protein, inhibits viral replication in vitro (IC50=77 nM).AB-506 binds to HBV core protein, accelerates capsid assembly and inhibits HBV pgRNA encapsidation.AB-506 blocks cccDNA establishment in HBV-infected HepG2-hNTCP-C4 cells and primary human hepatocytes, leading to inhibition of viral RNA, HBsAg, and HBeAg production (EC50=0.64-1.52 uM).AB-506 demonstrated activity across HBV genotypes A-H and maintains antiviral activity against nucleostide analog-resistant variants in vitro.AB-506 showed an 8 to 20-fold increase in EC50 values against L30F, L37Q, and I105T substitutions.AB-506 exhibits good oral bioavailability, systemic exposure, and higher liver to plasma ratios in rodents.

AB-452 (AB452) is a potent, small molecule inhibitor of noncanonical poly(A) polymerases PAPD5 and PAPD7 (PAPD5/7), inhibits PAPD5/7 enzymatic activities, reduces HBsAg in vitro (EC50=1.4/6.8 nM).AB-452 demonstrated specific antiviral activity for HBV, was inactive against a panel of 10 different RNA and DNA viruses with EC50 values of >30 uM.AB-452 reduced HBsAg, HBeAg, and HBV DNA production with EC50 of 0.28-6.8 nM, without cytotoxicity.AB-452 interferes with multiple steps of HBV life cycle by reducing HBV RNA.AB-452 demonstrated antiviral activity in AAV-HBV-transduced mouse model.AB-452 promotes HBV RNA degradation through inhibiting PAPD5 and PAPD7 enzymatic activities and blockage of guanosine incorporation into viral RNA poly(A) tails..

A small molecule CD4-mimetic that binds gp120 and blocks CD4 binding, inhibits HIV-1 entry.

A highly potent, selective HCV NS5B polymerase inhibitor for treatment of HCV infection.

90 (CBR-490) is a potent and selective antiwolbachial activity compound (Anti-Wolbachia wMel In vitro HCI cell-based assay IC50=33 nM, IC90=283 nM).CBR490 demonstrates potent antiwolbachial activity was confirmed in L. sigmodontis, Brugia malayi, and Onchocerca ochengi in vivo preclinical models of filarial disease.CBR490 demonbstrated in vitro selectivity against Loa loa (a safety concern in endemic areas).

2S-alkyne is an irreversible and clickable inhibitor of Streptococcal pyrogenic exotoxin B (SpeB) with IC50 of 1.4 uM; 2S-alkyne showed irreversible enzyme inhibition in biochemical assays and labeled endogenous SpeB in cultured S. pyogenes supernatants. 2S-alkyne decreased S. pyogenes survival in the presence of human neutrophils and supports the role of SpeB-mediated proteolysis as a mechanism to limit complement-mediated host defense.

1-ECBC is a small molecule inhibiting C. albicans filamentation, 1-ABC targets DYRK1-family kinase Yak1, the sole DYRK-family member expressed in C. albicans.1-ECBC blocked C. albicans biofilm formation in several co-culture models and a rat catheter infection model.

MEDS433 is a potent DHODH inhibitor with IC50 of 1.2 nM (hDHODH), inhibits in vitro replication of HSV-1 and HSV-2 in the nanomolar range.

GSK-2485852 (GSK2485852, GSK5852) is a highly potent, selective HCV NS5B polymerase inhibitor with IC50 of 3.0 and 1.6 nM for HCV genotypes 1a and 1b in replicon assay, respectively.

ient S. Tm and hyperpermeable Escherichia coli. The potencies against WT strains of E. coli, Acinetobacter baumannii, and Burkholderia cenocepacia are also improved considerably (up to >128-fold) with the outer-membrane permeabi

Sulfamethoxazole-13C6 is a 13C labeled Sulfamethoxazole. Sulfamethoxazole (Ro 4-2130) is a sulfonamide bacteriostatic antibiotic, used for bacterial infections. Sulfonamides is a competitive antagonist of para-aminobenzoic acid (PABA).

αGalCer-RBD is a self-adjuvanting lipoprotein conjugate. αGalCer-RBD induces potent immunity against SARS-CoV-2 and its variants of concern. αGalCer-RBD conjugate induces RBD-specific, cytokine-producing T cell development. αGalCer-RBD has great potential to be an effective COVID-19 vaccine candidate. α-Galactosylceramide (αGalCer) is a potent invariant natural killer T cell (iNKT) agonist. RBD: receptor-binding domain

Antiviral agent 15 (Compound 15f) is a Clofazimine derivative with antiviral effects. Antiviral agent 15 inhibits both rabies virus and pseudo-typed SARS-CoV-2 with EC50 values of 1.45 μM and 14.6 μM, respectively.

Antimalarial agent 10 (Compound 17b) is an aminoalcohol quinoline compound. Antimalarial agent 10 is an antimalarial agent with IC50 values of 14.9 nM and 11.0 nM against respectively Pf3D7 and PfW2 and a selectivity index higher than 770 whatever the cell line is.

HDAC1-IN-4 (JX34) is a potent Plasmodium falciparum HDAC1 inhibitor shows antimalarial activity (IC50 < 5 nM) and lower cytotoxicity.

CRK12-IN-1 is a potent CRK12 inhibitor. CRK12-IN-1 is extremely potent against T.b. brucei and rapidly cytocidal, as well as equally potent against T. congolense and T. vivax (EC50 of 1.3 and 18 nM, respectively).

Epoxyazadiradione is a limonoid purified from neem (Azadirachta indica) fruits. Epoxyazadiradione inhibits the tautomerase activity of MIF of both human (huMIF) and malaria parasites (Plasmodium falciparum (PfMIF) and Plasmodium yoelii (PyMIF)) non-competitively in a reversible fashion (Ki, 2.11-5.23 μM). Epoxyazadiradione has the potential against proinflammatory reactions induced by MIF of both malaria parasites and human.

Cycloaspeptide A, isolated from the endophytic fungus Penicillium janczewskii, has antiparasitic activity.

Neuraminidase-IN-4 (Compound 4b) is a potent inhibitor of neuraminidase with an EC50 of 1.59 μM. Neuraminidase (NA) is an important target for the treatment of influenza. Neuraminidase-IN-4 exhibits excellent antiviral activity against A/chicken/Hubei/327/2004 (H5N1-DW).

Herquline A (Herqueline A) is a fungal piperazine alkaloid. Herquline A is a fungal metabolite that inhibits platelet aggregation and replication of the influenza virus.