Aditoprime (Aditoprim), a selective bacterial dihydrofolate reductase (DHFR) inhibitor, inhibits the transformation of dihydrofolic acid to tetrahydrofolic acid. Aditoprime inhibits E.coli and L.casei DHFR with IC50 of 47 and 520 nM, respectively. Aditoprime has a broad antimicrobial spectrum, good antibacterial activity and excellent pharmacokinetics.

Sulfamethomidine is an antibacterial agent.

TP0586352 is a LpxC inhibitor that is effective against carbapenem-resistant Klebsiella pneumoniae and does not pose a cardiovascular risk.

N-3-oxo-dodecanoyl-L-Homoserine lactone (3-oxo-C12-HSL) is a bacterial quorum-sensing signaling molecule produced by P. aeruginosa and strains of the B. cepacia complex.Quorum sensing is a regulatory system used by bacteria for controlling gene expression in response to increasing cell density.N-3-oxo-dodecanoyl-L-Homoserine lactone induces the production of IL-8 in 16HBE human bronchial epithelial cells.

Sirpefenicol is a phenicol antibacterial agent. Sirpefenicol can be used in bacterial infections in animals (extracted from patent WO2020068607A1).

EGCG Octaacetate (AcEGCG) is a prodrug of Green tea epigallocatechin-3-gallate (EGCG). EGCG Octaacetate decreases the proinflammatory mediator levels by down-regulating of PI3K/Akt/NFκB phosphorylation and p65 acetylation. EGCG Octaacetate reduces colitis-driven colon cancer in mice. EGCG octaacetate is the potential antibacterial compound for gram-positive bacteria (GPB) and gram-negative bacteria (GNB).

N-Hexanoyl-DL-homoserine lactone is a bacterial quorum sensing molecule produced in the rhizosphere. N-Hexanoyl-DL-homoserine lactone, a bacterial quorum sensing signal, induces transcriptional changes in Arabidopsis and may contribute to tuning plant growth to the microbial composition of the rhizosphere.

GW-870086 is a glucocorticoid receptor agonist potentially for the treatment of asthma and atopic dermatitis.

RTA-408 is a synthetic triterpenoid that potently activates the antioxidative transcription factor Nrf2 and inhibits the proinflammatory transcription factor NF-κB.

T16Ainh-A01 is an inhibitor of the calcium-activated chloride channel TMEM16A, inhibits Ca2+-activated Cl− channel (CACC) activity in TMEM16A-transfected FRT cells with IC50 of 1 uM; T16Ainh-A01 (1-30 uM) inhibited single calcium (Ca2+)-activated chloride (Cl−) channels and whole cell currents activated by 500 nM free Ca2+; T16Ainh-A01 relaxed mouse thoracic aorta pre-contracted with methoxamine with an IC50 of 1.6 uM and suppressed the methoxamine concentration-effect curve; blocks calcium-activated chloride channels in vascular smooth muscle cells and relaxes murine and human blood vessels.

WAY-213613 (WAY213613) is a potent, non-substrate inhibitor of EAAT2 (GLT-1) with IC50 of 85 nM, displays > 44-fold selectivity over EAAT1 and EAAT3; also exhibits no activity towards ionotropic and metabotropic glutamate receptors.

Mitochondrial fusion promoter M1 is a mitochondrial dynamic modulator. Mitochondrial fusion promoter M1 preserves the mitochondrial function and promotes cellular respiration. Mitochondrial fusion promoter M1 alleviates cardiac and brain damage in rats with cardiac ischemia/reperfusion injury.

AZA1 is a potent dual inhibitor of Rac1 and Cdc42. AZA1 induces prostate cancer cells apoptosis and inhibits prostate cancer cells proliferation, migration and invasion.

FGTI-2734 is a RAS C-terminal mimetic dual farnesyl transferase (FT) and geranylgeranyl transferase-1 (GGT-1) inhibitor. It can prevent membrane localization of KRAS, hence solving KRAS resistance problem and thwarting mutant KRAS patient-derived pancreatic tumors.

Metronidazole acetic acid is a metabolite of Metronidazole with mutagenic activity in bacteria. Metronidazole is a nitroimidazole antibiotic, amebicide, and antiprotozoal agent used particularly for anaerobic bacteria and protozoa.

3-Phenyltoxoflavin, a derivative of Toxoflavin, is an Hsp90 inhibitor, with a Kd of 585 nM for the interaction of Hsp90-TPR2A. 3-Phenyltoxoflavin has anti-cancer activity.

Nor-benzetimide is a major metabolite of Benzetimide. Benzetimide is a mAChR antagonist with anticholinergic activity.

Poloxin is a non-ATP competitive Polo-like Kinase 1 (PLK1) inhibitor that targets the polo-box domain.

Sacubitrilat, also known as LBQ-657, is endopeptidase inhibitor. Sacubitril is a prodrug that is activated to LBQ657 by de-ethylation via esterases. LBQ657 inhibits the enzyme neprilysin, which is responsible for the degradation of atrial and brain natriuretic peptide, two blood pressure lowering peptides that work mainly by reducing blood volume.

S63845 is a potent and selective myeloid cell leukemia 1 (MCL1) inhibitor; binds human MCL1 with a Kd of 0.19 nM.

Semagacestat (LY450139) is a γ-secretase blocker for Aβ42, Aβ40 and Aβ38 with IC50 of 10.9 nM, 12.1 nM and 12.0 nM, also inhibits Notch signaling with IC50 of 14.1 nM.

CSF1R-IN-22 is a potent, cellular active and orally bioavailable CSF1R inhibitor with IC50 of 0.5 nM, displays 120-fold selectivity over c-Kit; has improved metabolic stability and Caco2 permeability.

BTSA1.2 is a rationalized BTSA1 analog with improved binding to BAX, cellular cytotoxicity, and better toleratence in vivo. Combination of BTSA1.2 with Navitoclax demonstrates synergistic efficacy in apoptosis-resistant cancer cells, xenografts, and patient-derived tumors while sparing healthy tissues.

LJ 001 ((LJ-001, LJ001) is a broad-spectrum antiviral agent targeting entry of enveloped viruses, including influenza A, filoviruses, poxviruses, arenaviruses, bunyaviruses, paramyxoviruses, flaviviruses, and HIV-1; specifically intercalates into viral membranes, irreversibly inactivates virions while leaving functionally intact envelope proteins, and inhibits viral entry at a step after virus binding but before virus-cell fusion; specifically inhibits virus-cell but not cell-cell fusion

Sisunatovir, also known as RV521, is a highly potent fusion inhibitor with efficacy against a panel of clinical isolates of RSV-A and RSV-B viruses. RV521 exhibited a mean IC50 of 1.2 nM against a panel of RSV A and B laboratory strains and clinical isolates with antiviral efficacy in the Balb/C mouse model of RSV infection. Oral bioavailability in preclinical species ranged from 42 to >100% with evidence of highly efficient penetration into lung tissue. In healthy adult human volunteers experimentally infected with RSV, a potent antiviral effect was observed with a significant reduction in viral load and symptoms compared to placebo.

A drug-linker conjugate for Antibody-drug conjugates (ADCs) by using the anti-mitotic agent, monomethyl auristatin E (MMAE), linked via the cleavable peptide Val-Cit-PAB..

MC-DM1 is a drug-linker conjugate composed of a potent microtubule-disrupting agent DM1 and a linker MC to make antibody drug conjugate (ADC).

Gefitinib-based PROTAC 3, conjugating an EGFR binding element to a VHL ligand via a linker, induces EGFR degradation with DC50s of 11.7 nM and 22.3 nM in HCC827(exon 19 del) and H3255 (L858R mutantion) cells, respectively.

MMV019313 (MMV 019313, MMV-019313) is a potent, specific malaria bifunctional farnesyl/geranylgeranyl diphosphate synthase (FPPS/GGPPS) inhibitor with IC50 of 330 nM; shows no activity against human FPPS or GGPPS (>200 uM); exhibits distinct modes of inhibition compared with bisphosphonates, inhibits P. falciparum growth with EC50 of 268 nM, overexpression and an S228T variant of PfFPPS/GGPPS confer resistance to MMV 019313.

NEO2734 (EP31670) is a novel, orally active and selective dual inhibitor of p300/CBP and BET bromodomain with IC50 of both <30 nM.