Novel RBP4 antagonist with good in vitro potency and selectivity and optimal rodent pharmacokinetic (PK) and pharmacodynamic (PD) characteristics

cyclo-CRVLIR is a cyclic peptide that binds selectively to p110α RAS binding domain (p110α-RBD) with ITC Kd of 3 uM, blocks p110α/RAS interaction in vitro and KRAS cancer cell lines.

Tryptolinamide (TLAM) is a small-molecule compound that activates mitochondrial respiration in cybrids generated from patient-derived mitochondria and fibroblasts from patient-derived iPSCs, inhibits phosphofructokinase-1 (PFK1) with an ATP-uncompetitive

LTGO-33 is a potent, selective inhibitor of voltage-gated sodium channel NaV1.8 with IC50 of 44 nM (hNaV1.8), 600-fold selectivity against NaV1.1-NaV1.7 and NaV1.9.

DS55980254 (DS 55980254) is potent, selective and orally active PTDSS1 (phosphatidylserine synthetase 1) inhibitor, suppresses phosphatidylserine (PS) production activity of PTDSS1 (IC50=100 nM) in cell-free assays, but not that of PTDSS2.

NV-6297 (NV6297) is a potent, selective mTORC1 pathway signaling inhibitor without inhibition on mTORC2, inhibits S6K1 phosphorylation (pS6K1 T389) in MCF7 cells with IC50 of 120 nM, directly and selectively targets GLUT-1.

MS.001 is a small molecule that inhibits both the chaperone binding and ubiquitin ligase activity of C-terminus of Hsc70 interacting protein (CHIP) at low micromolar concentrations (IC50=3.3 uM).

NBCoV2 is a highly potent small molecule viral fusion inhibitor with potential pan-Coronavirus activity (SARS-CoV IC50=13.8 nM, SARS-CoV-2 IC50=22.8 nM, MERS-CoV IC50=77 nM, cell-based single-cycle assays). NBCoV2 also has potent antiviral activity against all mutant pseudoviruses carrying single-, double-, or triple-mutations featured in the B.1.1.7 UK, B.1.351 RSA, and B.1.617.2 Delta variants (IC50=30-80 nM). NBCoV2 completely preventing the induction of any virus-induced CPE (IC100=1.25 uM, SARS-CoV-2 (US_WA-1/2020)). NBCoV2 bind to the S2 subdomain of the SARS-CoV-2 trimer, thus, inhibits the fusion of CoVs with the cell membran, and is specific for the SARS-CoV-2 S protein.

RGT1383 is a novel GLP-1R agonist, an analog of PF-06882961.

R-Sirpiglenastat is the R- isomer of Sirpiglenastat(DRP-104).Sirpiglenastat (DRP104) is a broad acting glutamine antagonist. Sirpiglenastat has anticancer effects by directly targeting tumor metabolism and simultaneously inducing a potent antitumor immune response.