GRL-1720 is an irreversible, covalent inhibitor of SARS-CoV-2 main protease (Mpro) with EC50 of 15 µM.

Compound 5i is a novel and brain-penetrant O-GlcNAcase inhibitor with IC50 of 46 nM.

JMX0493 is a potent inhibitor of human adenoviruses (HAdVs) with IC50 of 0.78 μM and displays high selectivity index (SI>100) and 2.5-fold virus yield reduction compared to niclosamide. JMX0493 targets the HAdV entry pathway that prevents viral particle disassembly and subsequent release from the endosome.

CH7233163 is a novel selective inhibitor of various types of EGFR mutants including L858R/T790M/C797S, L858R/T790M, Del19/T790M, Del19, and L858R, showing potent antitumor activities

Reuterin is a broad-spectrum antimicrobial agent active against Gram positive and Gram negative bacteria, as well as yeasts, moulds and protozoa. Reuterin is produced by specific strains of Lactobacillus reuteri during anaerobic metabolism of glycerol. Reuterin also demonstrates potent antimicrobial activity against a broad panel of human and poultry meat campylobacter spp. Isolates.

OSU-03012(AR-12) is a potent inhibitor of recombinant PDK-1 with IC50 of 5 μM and 2-fold increase in potency over OSU-02067.

Aprocitentan (ACT-132577) is the major and pharmacologically active metabolite of macitentan, which is dual ETA/ETB antagonist designed for tissue targeting.

CP-31398 is a small molecule p53 reactivator that protects p53 from thermal denaturation, not only reactivates mutant p53 but also induces stabilization of wild type p53.

Nucleozin targets influenza A nucleoprotein (NP), a multifunctional, RNA-binding protein necessary for virus replication.

IRAK inhibitor 1 is an interleukin-1 receptor associated kinase 4 (IRAK-4) inhibitor.

PF-3450074 (PF74) is a small molecule HIV capsid protein, destabilized the viral capsid in vitro.

SNAP-94847 is a selective, high-affinity, and competitive MCH1 receptor (MCH1-R) antagonist with Ki of 1.69 nM.

PWT143 (ME-401), is an orally bioavailable inhibitor of the delta isoform of phosphatidylinositide 3-kinase (PI3K), with potential antineoplastic activity.

NVP-LCQ195 (AT9311; LCQ195) is a small molecule heterocyclic inhibitor of CDK1, CDK2, CDK3 and CDK5 with IC50 of 1-42 nM.

LS-192629 is a novel OT-R antagonist.

GDC-0623 is a potent, ATP-uncompetitive inhibitors of MEK1(Ki=0.13 nM, +ATP).

A potent and selective antagonist of CXCR4 with IC50 of 13 nM in a CXCR4 125I-SDF inhibition binding assay.

NAB-14 is a potent, selective negative allosteric modulator of GluN2C/2D-containing NMDA receptors with IC50 of 580 nM, >800-fold selective over GluN2A/GluN2 receptors; inhibits triheteromeric (GluN1/GluN2A/GluN2C) NMDARs with modestly reduced potency and efficacy compared to diheteromeric (GluN1/GluN2C/GluN2C) receptors; inhibits GluN2D-mediated synaptic currents in rat subthalamic neurons and mouse hippocampal interneurons, but has no effect on synaptic transmission in hippocampal pyramidal neurons.

PF-915275 is a potent and selective inhibitor of human 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) (Ki ＜ 1 nM) with good preclinical pharmacokinetic properties.IC50 value: ＜ 1 nM (Ki)[2]Target: 11βHSD1in vitro: PF-915275 maintains potency in our cellular assay against human 11βHSD1 (HEK293, EC50 = 5 nM) and is selective against human 11βHSD2 (HEK293, 1.5% inhibition 10 μM). PF-915275 displays only weak affinity for the rodent choline transporter (Ki = 9.6 μM) and the hamster melatonin MT3 receptor (Ki = 9.6 μM) in the Cerep Bioprint screening panel. PF-915275 has good in vitro pharmacokinetic properties. In particular, PF-915275 is categorized as a low clearance compound (liver microsome assays) with high permeability (Caco2 assay). [2]in vivo: As a prelude to in vivo studies with PF-915275, the rat pharmacokinetic properties of this compound were determined. PF-915275 has an excellent pharmacokinetic profile characterized by low clearance, long half-life and good oral bioavailability. [2]

Delafloxacin meglumine (ABT492 meglumine; RX-3341 meglumine; WQ-3034 meglumine) is a broad-spectrum fluoroquinolone antibiotic. Delafloxacin has a broad spectrum of activity that includes drug-resistant Staphylococcus aureus, Streptococcus pneumoniae, and

A potent, noncovalent SARS-CoV papain-like protease (PLpro) inhibitor with IC50 of 2.6 uM.

Pyronaridine tetraphosphate is a Mannich base anti-malarial with demonstrated efficacy against drug resistant Plasmodium falciparum, P. vivax, P. ovale and P. malariae.

Baricitinib phosphate(INCB 028050; LY 3009104) is a selective JAK1 and JAK2 inhibitor with IC50 of 5.9 nM and 5.7 nM, ~70 and ~10-fold selective versus JAK3 and Tyk2, no inhibition to c-Met and Chk2,showed potent activity against COVID-19(SARS-COV-2).

CCG-50014 is the most potent against the regulator of G-protein signaling protein type 4 (RGS4) (IC50 =30 nM) and is >20-fold selective for RGS4 over other RGS proteins. CCG-50014 binds covalently to the RGS, forming an adduct on two cysteine residues located in an allosteric regulatory site. CCG50014, reduces nociceptive responses and enhances opioid-mediated analgesic effects in the mouse formalin test.

Darunavir ethanolate is an HIV protease inhibitor,showed potent activity against COVID-19(SARS-COV-2).

A potent, specific survivin inhibitor that inhibits survivin promoter activity with IC50 of 0.54 nM.

Nelfinavir(AG-1341) is a potent and orally bioavailable human immunodeficiency virus HIV-1 protease inhibitor (Ki=2 nM) and is widely prescribed in combination with HIV reverse transcriptase inhibitors for the treatment of HIV infection.

Rocaglamide (Rocaglamide A) is isolated from the genus Aglaia and can be used for coughs, injuries, asthma and inflammatory skin diseases. Rocaglamide is a potent inhibitor of NF-κB activation in T-cells. Rocaglamide is a potent and selective heat shock factor 1 (HSF1) activation inhibitor with an IC50 of ~50 nM. Rocaglamide inhibits the function of the translation initiation factor eIF4A. Rocaglamide also has anticancer properties in leukemia.

Foxy-5 is a novel Wnt-5A mimicking hexapeptide that inhibits breast cancer metastasis in vivo by targeting cell motility.

FRAX1036 is a novel ATP-competitive small molecule inhibitor of group I p21-activated Kinases (PAKs).