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..

Cyclooxigenase inhibitor. Anti-inflammatory, analgesic and antipyretic.

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.

NMS-P937 (NMS1286937) is an orally available, selective Polo-like Kinase 1 (PLK1) inhibitor with IC50 of 2 nM, 5000-fold selectivity over PLK2/PLK3. Phase 1.

Ectoine is an inhibitor of protein misfolding. It acts by significantly down-regulating Syp, Mapk3 and Tnfα and up-regulating Vegf in rat's hippocampus, prohibiting insulin amyloid formation in vitro.

Sarsasapogenin is a steroidal sapogenin, that is the aglycosidic portion of a plant saponin.

Bakuchiol is a phytoestrogen isolated from the seeds of Psoralea corylifolia L; has anti-tumor effects.

Naringenin is the predominant flavanone in grapefruit; displays strong anti-inflammatory and antioxidant activities. Naringenin has anti-dengue virus (DENV) activity.

Cytochalasin H is a potent inhibitor of actin incorporation into filaments,a cell-permeable fungal toxin used in actin polymerization studies and cytological research.

D3263 is a novel, orally bioavailable small molecule Trp-p8 agonist.

D-64131 is a novel inhibitor of Tubulin polymerization that competitively binds with [(3)H]colchicine to αβ-Tubulin.

Luteolin (Luteoline), a flavanoid compound, is a potent Nrf2 inhibitor. Luteolin has anti-inflammatory, anti-cancer properties, including the induction of apoptosis and cell cycle arrest, and the inhibition of metastasis and angiogenesis, in several cancer cell lines, including human non-small lung cancer cells.

Ginsenoside Rg1 is one of the major active components of ginseng. Ginsenoside Rg1 displays promising effects by reducing cerebral Aβ levels. Ginsenoside Rg1 also reduces NF-κB nuclear translocation.

BDTX-189 is a potent, orally active and selective inhibitor of allosteric EGFR and HER2 oncogenic mutations, includes EGFR/HER2 exon 20 insertion mutants. BDTX-189 shows KDs of 0.2, 0.76, 13 and 1.2 nM for EGFR, HER2, BLK and RIPK2, reapectively. Anticancer activity.

SYP-5 is a novel HIF-1 inhibitor, suppresses tumor cells invasion and angiogenesis.

Nifurtimox is a 5-nitrofuran and is used to treat diseases caused by trypanosomes including Chagas disease and sleeping sickness. It is given by mouth and not by injection. Nifurtimox is now in a Phase II clinical trial for the treatment of pediatric neuroblastoma and medulloblastoma. Nifurtimox decreased cell viability in a concentration-dependent manner. Nifurtimox also suppressed basal and TrkB-mediated Akt phosphorylation, and the cytotoxicity of nifurtimox was attenuated by a tyrosine hydroxylase inhibitor (alpha-methyl-tyrosine). Nifurtimox killed catecholaminergic, but not cholinergic, autonomic neurons in culture. In vivo xenograft models showed inhibition of tumor growth with a histologic decrease in proliferation and increase in apoptosis. These results suggest that nifurtimox induces cell death in neuroblastoma . Therefore, further studies are warranted to develop nifurtimox as a promising new treatment for neuroblastoma.

DS-6930 (DS 6930, DS6930) is a novel potent, selective PPARγ agonist with EC50 of 41 nM, Emax-68%; significantly recruits several cofactors, such as RIP140 and PGC1, in cofactor recruitment assays; demonstrateshigh PPARγ agonist potency with robust plasma glucose reduction, maintains diminished PPARγ-related adverse effects upon toxicological evaluation in vivo, and demonstrated no hepatotoxicity.

8-Hydroxy-efavirenz is the primary metabolite of the antiretroviral drug Efavirenz, stimulates the glycolytic flux in cultured rat astrocytes.

AZD9977 is a first-in-class, potent, selective, mineralocorticoid receptor (MR) modulator with IC50 of 0.37. 0.08 and 0.08 uM for human, mouse and rat MR, respectively.

AZD 4205 (AZD4205) is a potent, selective JAK1 inhibitor IC50 of 73 nM and Ki of 2.8 nM, shows high selectivity against JAK2 and JAK3 with IC50 of 13,233 nM and >30,000 nM respectively; shows potent inhibition of p-STAT3 in a cell based assay of JAK1 activity with an IC50 of 128 nM and excellent selectivity across the kinome; reduces residual disease and prolongs the benefit of Osimertinib in lung cancer patients with EGFR activating mutations both in vitro and in vivo.

Daidzin is a potent, selective aldehyde dehydrogenase 2 (ALDH2,IC50 = 80 nM) inhibitor, which has antiallergic anti-oxidant, anti-carcinogenic, antithrombotic,and anti-atherosclerotic activities

Cimicoxib, aslo known as UR-8880, is a non-steroidal anti-inflammatory drug (NSAID) used in veterinary medicine to treat dogs for pain and inflammation associated with osteoarthritis and for the management of pain and inflammation associated with surgery. It acts as a COX-2 inhibitor.

BAR501 is a potent and selective agonist of GPBAR1 with an EC50 of 1 μM.

KL201 a circadian clock modulator, is a isoform-selective cryptochrome 1 (CRY1) stabilizer. KL201 has no stabilizing effect on CRY2. KL201 lengthens the period of circadian rhythms in cells and tissues.

Darusentan is a potent inhibitor of endothelin signaling and function in both large and small arteries.

DASA-58 is a highly specific small molecule PKM2 activator. DASA-58 inhibits LPS-induced Hif-1a and IL-1b, as well as the expression of a range of other Hif-1a-dependent genes.