VERU-111 (Sabizabulin) is a novel potent colchicine binding site inhibitor (CBSI) in tubulin with potential anticancer activities. Sabizabulin is a novel oral agent with both anti-viral and anti-inflammatory activities.Sabizabulin is a cytoskeleton disruptor which by causing microtubule depolymerization has both anti-viral and anti-inflammatory activity and could be effective against the SARS-CoV-2 virus by disrupting its intracellular transport along the microtubules. Microtubule trafficking is critical for viruses to be transported, replicated, assembled, and released from the cell. In addition, microtubule depolymerization drugs that target the “colchicine binding site” of microtubules, like sabizabulin, also have strong anti-inflammatory effects, including the potential to treat the cytokine release syndrome (cytokine storm) and septic shock induced by the SARS-CoV-2 viral infection that is associated with high COVID-19 mortality rates.

TRx 0237 (LMTX™) mesylate is a second-generation tau protein aggregation inhibitor for the treatment of Alzheimer's disease (AD) and frontotemporal dementia.

Bay-8040 is a potent, selective human neutrophil elastase (HNE) inhibitor with IC50 of 28 nM; displays no significant inhibition toward 68 other pharmacologically relevant targets (>10 uM), and a panel of related serine proteases; shows in vivo efficacy with regard to decreasing cardiac remodeling and amelioration of cardiac function in monocrotaline-induced rat model for pulmonary arterial hypertension.

CB-103 is a notch signaling pathway inhibitor extracted from patent US9296682B2. CB-103 is developed for the treatment of cancers.

Butabindide is a potent inhibitor of cholecystokinin-inactivating peptidase/tripeptidyl peptidase 2 (CCK-inactivating peptidase/TPP-2; Ki = 7 nM).1 It is selective for CCK-inactivating peptidase/TPP-2 over a panel of serine proteases (Kis = >1 μM) as well as CCK receptors (Kis = >0.1 mM).

FDI-6 is an inhibitor of FOXM1. FDI-6 binds directly to FOXM1 protein, to displace FOXM1 from genomic targets in MCF-7 breast cancer cells, and induce concomitant transcriptional down-regulation.

Omidenepag Isopropyl (DE-117, OMDI) is the prodrug of Omidenepag, which is a potent, selective agonist human EP2 receptor; demonstrates excellent IOP-lowering activities following ocular administration in ocular normotensive monkeys, Omidenepag Isopropyl (OMDI) is a clinical candidate for the treatment of glaucoma.

MsbA inhibitor 1 is a novel small molecule lipopolysaccharide biogenesis inhibitor, inhibits MsbA, an ATP-dependent flippase that translocates LPS across the inner membrane; causes mislocalization of LPS to the cell interior, inhibits Δ5 strain with MIC o

SLMP53-1 is a novel reactivator of wild-type and mutant p53, shows a p53-dependent anti-proliferative activity in human wt and mut p53R280K-expressing tumor cells.

TRIF agonist AV-C is a novel TRIF pathway agonist that activates innate and interferon-associated responses, strongly inhibits replication of ZIKV, CHIKV, and DENV (IC90~5 uM).

Se-Methylselenocysteine, a precursor of Methylselenol, has potent cancer chemopreventive activity and anti-oxidant activity. Se-Methylselenocysteine is orally bioavailable, and induces apoptosis.

A potent, specific, competitive inhibitor of choline kinase-α (Chok-α) by targeting the choline binding site; significantly increases LC3II expression in MCF-7 and MCF-7/TAM cells, increases the size and number of autophagosome, causes MCF-7 and MCF-7/TAM

PF 04878691 (PF 4878691, S 32865, 852A, 3M 001) is a selective TLR7 agonist that potently induces IFN-α and IFN-regulated proteins from human PBMC.

BK-1361(BK1361, cyclo-RLsKDK) is a cyclic peptide with RLsKDK (s=D-serine) that functions as a potent, selective inhibitor of ADAM8 with IC50 of 120 nM.

GPR4 antagonist 3 is a selective, and orally available GPR4 antagonist with an IC50 of 70 nM. Anti-inflammatory activities.

LLY-283 (LLY283) is a potent, selective inhibitor of arginine methyltransferase 5 (PRMT5) with IC50 of 22 nM.

S-99 inhibits LPS-induced TNFa release assay in vivo

RO495 is a very potent TYK2 inhibitor with a IC50 of 1.5nM on TYK2 as tested in cell-based pharmacological assays

NIBR-17 is a pan class I PI3K inhibitor with IC50 values of 1, 9.2, 9 and 20 nM respectively for PI3Kapha - delta.

GNE-490 is a highly selective pan-PI3K inhibitor and demonstrates selectivity over mTOR.

GDC046 is a potent lead analog with good kinase selectivity, physicochemical properties, and pharmacokinetic profile.

The compound (Akt-I-1) inhibits only Akt1 (IC50 4.6 μM) and does not inhibit AKT2, or AKT3.

AMG-1 is a potent inhibitor of human c-Met and RON with IC50 values of 4 and 9 nmol/L respectively.

Rogaratinib (BAY 1163877) is a potent, selective, orally available pan-FGFR with IC50 of 15, <1, 19 and 33 nM for FGFR1, 2, 3 and 4, respectively.

Purfalcamine is a potent, specific inhibitor of Plaasmodium falciparum calcium-dependent protein kinase 1 (PfCDPK1) with IC50 of 17 nM.

NVP-2 is a potent and selective ATP-competitive cyclin dependent kinase 9 (CDK9) probe, inhibits CDK9/CycT activity with an IC50 of 0.514 nM. NVP-2 displays inhibitory effcts on CDK1/CycB, CDK2/CycA and CDK16/CycY kinases with IC50 values of 0.584 µM, 0.7

MN58b is a potent, selective choline kinase α (ChoKα) inhibitor with IC50 of 1.4 uM, >30-fold selectivity over ChoKβ and does not affect MAPKs, PI3Ks, and other enzymes involved in the regulation of phospholipid metabolism.

ML188 is a Potent Noncovalent Small Molecule Inhibitor of the Severe Acute Respiratory Syndrome Coronavirus (SARS-CoV) 3CL Protease. The X-ray structure of SARS-CoV 3CLpro bound with ML188 was instrumental in guiding subsequent rounds of chemistry optimiz

MK2-IN-1 is a potent, selecitve, non-ATP competitive MAPKAPK2(MK2) inhibitor with IC50 of 0.11 uM.

LY-345899 (LY345899) is a novel potent, cytoplasmic and mitochondrial methylenetetrahydrofolate dehydrogenase MTHFD1 and MTHFD2 inhibitor with IC50 of 96 nM and 663 nM, respectively; MTHFD2 is a novel target for drug development.