Pyr01 is a targeted activator of cell kill (TACK) and shows more than 300-fold more potent than doravirine and also retains reverse transcriptase (RT) inhibition activity within about 3-fold of doravirine.

RLY-2608 is an oral allosteric pan-mutant isoform-selective PI3K伪 inhibitor that was discovered using MD modeling and cryo-EM to identify allosteric networks and opportunities for small molecules, followed by DEL screening.

FN1-8 is a novel, synthetic small molecule that efficiently interferes with Gli/TAF9 interaction and downregulate Gli/TAF9-dependent transcriptional activity (at 15 uM); inhibits non-canonical Gli activation and acts downstream of the canonical Hh pathway; suppresses cancer cell proliferation in vitro and inhibits tumor growth in vivo.

TNG260 is a CoREST-selective deacetylase inhibitor and shows 500-fold selectivity for the CoREST complex over the other HDAC1-containing complexes, NuRD and Sin3.

RMC-6291 is a potent covalent inhibitor of KRASG12C(ON) that forms a tri-complex within tumor cells between KRASG12C(ON) and cyclophilin A (CypA). RMC-6291 overcomes limitations of first-generation KRASG12C(OFF) inhibitors in preclinical models by directly targeting the active form of this important oncogenic driver.

LNP023 is a highly potent factor B (FB) inhibitor with an IC50 value of 10 nM. LNP023 shows direct, reversible, and high-affinity binding to human FB (KD=7.9 nM).

UDP-GalNAz disodium (UDP-N-azidoacetylgalactosamine disodium) is the analogue of UDP-GalNAc. UDP-GalNAc is the donor substrate of many N-acetylgalactosaminyltransferases, enzymes which transfer GalNAc from the nucleotide sugar to a saccharide or peptide acceptor.

KAR-5585 (Rodatristat) is the prodrug of the potent TPH1 inhibitor KAR5417, shows robust reduction of intestinal serotonin (5-HT) levels in mice.

MCUF-651 (MCUF651) is a small molecule guanylyl cyclase A receptor (GC-A) positive allosteric modulator (PAM), potentiate ANP-mediated cGMP with EC50 of 0.45 uM (Emax=82%) in HEK293 GC-A cells.MCUF-651 enhanced ANP-mediated cGMP generation in human cardiac, renal, and fat cells and inhibited cardiomyocyte hypertrophy in vitro.MCUF-651 binds to GC-A (Kd=397 nM) and selectively enhances the binding of ANP to GC-A ( MCUF-651+ANP, Kd=0.06 nM).MCUF-651 is orally bioavailable in mice and enhances the ability of endogenous ANP and BNP to generate GC-A-mediated cGMP ex vivo.

WAY-299801 is an antiacterial agent. WAY-299801 showed interesting in vitro antimycobacterial activity against some strains of Mycobacterium and clin. isolates of M. tuberculosis.

GPS167 is a specific small molecule splicing regulator SRSF10 inhibitor, modulates BCLAF1 splicing with IC50 of 2 uM in human colorectal HCT116 cells, directly inhibits CLK1, CLK2 and CLK4, but not SRPK1 and DYRK1A.GPS167 promotes the dephoshorylation of SRSF10 and changes its interaction with partner proteins.GPS167 treatment leads to a partial dephosphorylation of SRSF10 and increases the recovery of CLK1 and CLK4.GPS167 impairs the growth of cancer cell line, elicits p53-dependent cytotoxicity.GPS167 is cytotoxic for human colorectal cancer organoids but not normal organoids.

QC-01-175 is a hetero-bifunctional molecule designed to engage both tau and Cereblon (CRBN) to trigger tau ubiquitination and proteasomal degradation (tau PROTAC).QC-01–175 effected clearance of tau in frontotemporal dementia (FTD) patient-derived neuronal cell models, with minimal effect on tau from neurons of healthy controls.QC-01–175 also rescued stress vulnerability in FTD neurons, phenocopying CRISPR-mediated MAPT-knockout.